Search results for: herbal formulation
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 1438

Search results for: herbal formulation

1108 Formulation and in Vitro Evaluation of Cubosomes Containing CeO₂ Nanoparticles Loaded with Glatiramer Acetate Drug

Authors: Akbar Esmaeili, Zahra Salarieh

Abstract:

Cerium oxide nanoparticles (nano-series) are used as catalysts in industrial applications due to their free radical scavenging properties. Given that free radicals play an essential role in the pathology of many neurological diseases, we investigated the use of nanocrystals as a potential therapeutic agent for oxidative damage. This project synthesized nano-series from a new and environmentally friendly bio-pathway. Investigation of cerium nitrate in culture medium containing inoculated Lactobacillus acidophilus strain before incubation produces nano-series. Loaded with glatiramer acetate (GA) was formed by coating carboxymethylcellulose (CMC) and CeO2. FE-SEM analysis showed nano-series in the 9-11 nm range, spherical shape, and uniform particle size distribution. Cubic nanoparticles containing anti-multiple sclerosis (anti-Ms) treatment called GA were used. Glycerol monostearate (GMS) was used as a fat base, and evening primrose extract was used as an anti-inflammatory in cubosomes. Design-Expert® software was used to study the effects of different formulation factors on the properties of GAloaded cubic dispersions. Thirty GA-labeled cubic dispersions were prepared with GA-labeled carboxymethylcellulose and evaluated in vitro. The results showed an average nano-series size of 89.02 and a zeta potential of -49.9. Cubosomes containing GA-CMC/CeO2 showed a stable release profile for 180 min. The results showed that cubosomes containing GA-CMC/CeO2 could be a promising drug carrier with normal release behavior.

Keywords: ciochemistry, biotechnology, molecular, biology

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1107 Stability-Indicating High-Performance Thin-Layer Chromatography Method for Estimation of Naftopidil

Authors: P. S. Jain, K. D. Bobade, S. J. Surana

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A simple, selective, precise and Stability-indicating High-performance thin-layer chromatographic method for analysis of Naftopidil both in a bulk and in pharmaceutical formulation has been developed and validated. The method employed, HPTLC aluminium plates precoated with silica gel as the stationary phase. The solvent system consisted of hexane: ethyl acetate: glacial acetic acid (4:4:2 v/v). The system was found to give compact spot for Naftopidil (Rf value of 0.43±0.02). Densitometric analysis of Naftopidil was carried out in the absorbance mode at 253 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r2=0.999±0.0001 with respect to peak area in the concentration range 200-1200 ng per spot. The method was validated for precision, recovery and robustness. The limits of detection and quantification were 20.35 and 61.68 ng per spot, respectively. Naftopidil was subjected to acid and alkali hydrolysis, oxidation and thermal degradation. The drug undergoes degradation under acidic, basic, oxidation and thermal conditions. This indicates that the drug is susceptible to acid, base, oxidation and thermal conditions. The degraded product was well resolved from the pure drug with significantly different Rf value. Statistical analysis proves that the method is repeatable, selective and accurate for the estimation of investigated drug. The proposed developed HPTLC method can be applied for identification and quantitative determination of Naftopidil in bulk drug and pharmaceutical formulation.

Keywords: naftopidil, HPTLC, validation, stability, degradation

Procedia PDF Downloads 388
1106 Finite Difference Modelling of Temperature Distribution around Fire Generated Heat Source in an Enclosure

Authors: A. A. Dare, E. U. Iniegbedion

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Industrial furnaces generally involve enclosures of fire typically initiated by the combustion of gases. The fire leads to temperature distribution inside the enclosure. A proper understanding of the temperature and velocity distribution within the enclosure is often required for optimal design and use of the furnace. This study was therefore directed at numerical modeling of temperature distribution inside an enclosure as typical in a furnace. A mathematical model was developed from the conservation of mass, momentum and energy. The stream function-vorticity formulation of the governing equations was solved by an alternating direction implicit (ADI) finite difference technique. The finite difference formulation obtained were then developed into a computer code. This was used to determine the temperature, velocities, stream function and vorticity. The effect of the wall heat conduction was also considered, by assuming a one-dimensional heat flow through the wall. The computer code (MATLAB program) developed was used for the determination of the aforementioned variables. The results obtained showed that the transient temperature distribution assumed a uniform profile which becomes more chaotic with increasing time. The vertical velocity showed increasing turbulent behavior with time, while the horizontal velocity assumed decreasing laminar behavior with time. All of these behaviours were equally reported in the literature. The developed model has provided understanding of heat transfer process in an industrial furnace.

Keywords: heat source, modelling, enclosure, furnace

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1105 Effect of Additives on Post-hydrogen Decompression Microstructure and Mechanical Behaviour of PA11 Involved in Type-IV Hydrogen Tank Liners

Authors: Mitia Ramarosaona, Sylvie Castagnet, Damien Halm, Henri-Alexandre Cayzac, Nicolas Dufaure, Philippe Papin

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In light of the ongoing energy transition, 'Infrastructure developments' for hydrogen transportation and storage raise studies on the materials employed for hyperbaric vessels. Type IV tanks represent the most mature choice for gaseous hydrogen storage at high pressure – 70MPa. These tanks are made of a composite shell and an internal hydrogen-exposed polymer liner. High pressure conditions lead to severe mechanical loading requiring high resistance. Liner is in contact with hydrogen and undergoes compression – decompression cycles during system filling and emptying. Stresses induced by this loading, coupled with hydrogen diffusion, were found to cause microstructural changes and degradation of mechanical behaviour after decompression phase in some studies on HDPE. These phenomena are similar to those observed in elastomeric components like sealing rings, which can affect permeability and lead to their failure. They may lead to a hydrogen leak, compromising security and tightness of the tank. While these phenomena have been identified in elastomers, they remain less addressed in thermoplastics and consequences post-decompression damages on mechanical behaviour and to the best of author's knowledge was not studied either. Different additives are also included in liner formulation to improve its behaviour. This study aimed to better understand damage micro-mechanisms in PA11s exposed to hydrogen compression-decompression cycles and understand if additives influence their resistance. Samples of pure, plasticized and impact-modified PA11s are exposed to 1, 3 and 8 pressure cycles including hydrogen saturation at 70MPa followed by severe 15-second decompression. After hydrogen exposure and significantly later than full desorption, the residual mechanical behaviour is characterized through impact and monotonic tensile tests, on plain and notched samples. Several techniques of microstructure and micro-nano damage characterization are carried out to assess whether changes in macroscopic properties are driven by microstructural changes in the crystalline structure (SAXS-WAXS acquisitions and SEM micrographs). Thanks to WAXS acquisition and microscopic observation, the effects due to additives and pressure consequences can be decorrelated. Pure PA11 and PA11 with a low percentage of additives show an increase in stress level at the first yielding point after hydrogen cycles. The amplitude of the stress increase is more important in formulation with additives because of changes in PA11 matrix behavior and environment created by additives actions. Plasticizer modifies chain mobility leading to microstructure changes while other additives, more ductile than PA11, is able to cavitate inside PA11 matrix when undergoing decompression. On plasticized formulation, plasticizer migration are suspected to enhance impact of hydrogen cycling on mechanical behaviour. Compared to the literature on HDPE and elastomers, no damages like cavitation or cracking could be evidenced from SAXS experiments on every PA11 formulation tested. In perspectives, on all formulation, experimental work is underway to confirm influence of residual pressure level after decompression on post-decompression damages level, the aim is to better understand the factors affecting the mechanical behavior of thermoplastics subject to mechanical solicitation from decompression in hydrogen tank liners, not mechanical behaviour of liner in hydrogen tanks directly.

Keywords: additives, hydrogen tank liner, microstructural analysis, PA11

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1104 Pharmacokinetic and Tissue Distribution of Etoposide Loaded Modified Glycol Chitosan Nanoparticles

Authors: Akhtar Aman, Abida Raza, Shumaila Bashir, Mehboob Alam

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The development of efficient delivery systems remains a major concern in cancer chemotherapy as many efficacious anticancer drugs are hydrophobic and difficult to formulate. Nanomedicines based on drug-loaded amphiphilic glycol chitosan micelles offer potential advantages for the formulation of drugs such as etoposide that may improve the pharmacokinetics and reduce the formulation-related adverse effects observed with current formulations. Amphiphilic derivatives of glycol chitosan were synthesized by chemical grafting of palmitic acid N-hydroxysuccinimide and quaternization to glycol chitosan backbone. To this end, a 7.9 kDa glycol chitosan was modified by palmitoylation and quaternization, yielding a 13 kDa amphiphilic polymer. Micelles prepared from this amphiphilic polymer had a size of 162nm and were able to encapsulate up to 3 mg/ml etoposide. Pharmacokinetic results indicated that the GCPQ micelles transformed the biodistribution pattern and increased etoposide concentration in the brain significantly compared to free drugs after intravenous administration. AUC 0.5-24h showed statistically significant difference in ETP-GCPQ vs. Commercial preparation in liver (25 vs.70, p<0.001), spleen (27 vs.36, p<0.05), lungs (42 vs.136,p<0.001),kidneys(25 vs.70,p< 0.05),and brain(19 vs.9,p<0.001). ETP-GCPQ crossed the blood-brain barrier, and 4, 3.5, 2.6, 1.8, 1.7, 1.5, and 2.5 fold higher levels of etoposide were observed at 0.5, 1, 2, 4, 6, 12, and 24hrs; respectively suggesting these systems could deliver hydrophobic anticancer drugs such as etoposide to tumors but also increased their transport through the biological barriers, thus making it a good delivery system

Keywords: glycol chitosan, micelles, pharmacokinetics, tissue distribution

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1103 Nitrogen, Phosphorus, Potassium (NPK) Hydroxyapatite Nano-Hybrid Slow Release Fertilizer

Authors: Tinomuvonga Manenji Zhou, Eubert Mahofa, Tatenda Crispen Madzokere

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The nanostructured formulation can increase fertilizer efficacy and uptake ratio of the soil nutrients in agriculture production and save fertilizer resources. Controlled release modes have properties of both release rate and release pattern of nutrients, for fertilizers that are soluble in water might be correctly controlled. Nanoparticles can reduce the rate at which fertilizer nutrients are in the soil by leaching. A slow release NPK-hydroxyapatite nano hybrid fertilizer was synthesized using exfoliated bentonite as filler material. A simple, scalable method was used to synthesize the nitrogen-phosphorus hydroxyapatite nano fertilizer, where calcium hydroxide, phosphoric acid, and urea were used as precursor material, followed by the incorporation of potassium through a liquid grinding method. The product obtained was an NPK-hydroxyapatite nano hybrid fertilizer. A quantitative analysis was done to determine the percentage of nitrogen, phosphorus, and potassium in the hybrid fertilizer. AAS was used to determine the percentage of potassium in the fertilizer. An accelerated water test was conducted to compare the nutrient release behavior of nutrients between the synthesized NPK-hydroxyapatite nano hybrid fertilizer and commercial NPK fertilizer. The rate of release of Nitrogen, phosphorus, and potassium was significantly lower in the synthesized NPK hydroxyapatite nano hybrid fertilizer than in the convectional NPK fertilizer. The synthesized fertilizer was characterized using XRD. NPK hydroxyapatite nano hybrid fertilizer encapsulated in exfoliated bentonite thus prepared can be used as an environmentally friendly fertilizer formulation which could be extended to solve one of the major problems faced in the global fertilization of low nitrogen, phosphorus, and potassium use efficiency in agriculture.

Keywords: NPK hydroxyapatite nano hybrid fertilizer, bentonite, encapsulation, low release

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1102 Pressure-Controlled Dynamic Equations of the PFC Model: A Mathematical Formulation

Authors: Jatupon Em-Udom, Nirand Pisutha-Arnond

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The phase-field-crystal, PFC, approach is a density-functional-type material model with an atomic resolution on a diffusive timescale. Spatially, the model incorporates periodic nature of crystal lattices and can naturally exhibit elasticity, plasticity and crystal defects such as grain boundaries and dislocations. Temporally, the model operates on a diffusive timescale which bypasses the need to resolve prohibitively small atomic-vibration time steps. The PFC model has been used to study many material phenomena such as grain growth, elastic and plastic deformations and solid-solid phase transformations. In this study, the pressure-controlled dynamic equation for the PFC model was developed to simulate a single-component system under externally applied pressure; these coupled equations are important for studies of deformable systems such as those under constant pressure. The formulation is based on the non-equilibrium thermodynamics and the thermodynamics of crystalline solids. To obtain the equations, the entropy variation around the equilibrium point was derived. Then the resulting driving forces and flux around the equilibrium were obtained and rewritten as conventional thermodynamic quantities. These dynamics equations are different from the recently-proposed equations; the equations in this study should provide more rigorous descriptions of the system dynamics under externally applied pressure.

Keywords: driving forces and flux, evolution equation, non equilibrium thermodynamics, Onsager’s reciprocal relation, phase field crystal model, thermodynamics of single-component solid

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1101 Surfactant-Assisted Aqueous Extraction of Residual Oil from Palm-Pressed Mesocarp Fibre

Authors: Rabitah Zakaria, Chan M. Luan, Nor Hakimah Ramly

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The extraction of vegetable oil using aqueous extraction process assisted by ionic extended surfactant has been investigated as an alternative to hexane extraction. However, the ionic extended surfactant has not been commercialised and its safety with respect to food processing is uncertain. Hence, food-grade non-ionic surfactants (Tween 20, Span 20, and Span 80) were proposed for the extraction of residual oil from palm-pressed mesocarp fibre. Palm-pressed mesocarp fibre contains a significant amount of residual oil ( 5-10 wt %) and its recovery is beneficial as the oil contains much higher content of vitamin E, carotenoids, and sterols compared to crude palm oil. In this study, the formulation of food-grade surfactants using a combination of high hydrophilic-lipophilic balance (HLB) surfactants and low HLB surfactants to produce micro-emulsion with very low interfacial tension (IFT) was investigated. The suitable surfactant formulation was used in the oil extraction process and the efficiency of the extraction was correlated with the IFT, droplet size and viscosity. It was found that a ternary surfactant mixture with a HLB value of 15 (82% Tween 20, 12% Span 20 and 6% Span 80) was able to produce micro-emulsion with very low IFT compared to other HLB combinations. Results suggested that the IFT and droplet size highly affect the oil recovery efficiency. Finally, optimization of the operating parameters shows that the highest extraction efficiency of 78% was achieved at 1:31 solid to liquid ratio, 2 wt % surfactant solution, temperature of 50˚C, and 50 minutes contact time.

Keywords: food-grade surfactants, aqueous extraction of residual oil, palm-pressed mesocarp fibre, interfacial tension

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1100 Chemical, Physical and Microbiological Characteristics of a Texture-Modified Beef- Based 3D Printed Functional Product

Authors: Elvan G. Bulut, Betul Goksun, Tugba G. Gun, Ozge Sakiyan Demirkol, Kamuran Ayhan, Kezban Candogan

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Dysphagia, difficulty in swallowing solid foods and thin liquids, is one of the common health threats among the elderly who require foods with modified texture in their diet. Although there are some commercial food formulations or hydrocolloids to thicken the liquid foods for dysphagic individuals, there is still a need for developing and offering new food products with enriched nutritional, textural and sensory characteristics to safely nourish these patients. 3D food printing is an appealing alternative in creating personalized foods for this purpose with attractive shape, soft and homogenous texture. In order to modify texture and prevent phase separation, hydrocolloids are generally used. In our laboratory, an optimized 3D printed beef-based formulation specifically for people with swallowing difficulties was developed based on the research project supported by the Scientific and Technological Research Council of Turkey (TÜBİTAK Project # 218O017). The optimized formulation obtained from response surface methodology was 60% beef powder, 5.88% gelatin, and 0.74% kappa-carrageenan (all in a dry basis). This product was enriched with powders of freeze-dried beet, celery, and red capia pepper, butter, and whole milk. Proximate composition (moisture, fat, protein, and ash contents), pH value, CIE lightness (L*), redness (a*) and yellowness (b*), and color difference (ΔE*) values were determined. Counts of total mesophilic aerobic bacteria (TMAB), lactic acid bacteria (LAB), mold and yeast, total coliforms were conducted, and detection of coagulase positive S. aureus, E. coli, and Salmonella spp. were performed. The 3D printed products had 60.11% moisture, 16.51% fat, 13.68% protein, and 1.65% ash, and the pH value was 6.19, whereas the ΔE* value was 3.04. Counts of TMAB, LAB, mold and yeast and total coliforms before and after 3D printing were 5.23-5.41 log cfu/g, < 1 log cfu/g, < 1 log cfu/g, 2.39-2.15 log EMS/g, respectively. Coagulase positive S. aureus, E. coli, and Salmonella spp. were not detected in the products. The data obtained from this study based on determining some important product characteristics of functional beef-based formulation provides an encouraging basis for future research on the subject and should be useful in designing mass production of 3D printed products of similar composition.

Keywords: beef, dysphagia, product characteristics, texture-modified foods, 3D food printing

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1099 Quantifying Meaning in Biological Systems

Authors: Richard L. Summers

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The advanced computational analysis of biological systems is becoming increasingly dependent upon an understanding of the information-theoretic structure of the materials, energy and interactive processes that comprise those systems. The stability and survival of these living systems are fundamentally contingent upon their ability to acquire and process the meaning of information concerning the physical state of its biological continuum (biocontinuum). The drive for adaptive system reconciliation of a divergence from steady-state within this biocontinuum can be described by an information metric-based formulation of the process for actionable knowledge acquisition that incorporates the axiomatic inference of Kullback-Leibler information minimization driven by survival replicator dynamics. If the mathematical expression of this process is the Lagrangian integrand for any change within the biocontinuum then it can also be considered as an action functional for the living system. In the direct method of Lyapunov, such a summarizing mathematical formulation of global system behavior based on the driving forces of energy currents and constraints within the system can serve as a platform for the analysis of stability. As the system evolves in time in response to biocontinuum perturbations, the summarizing function then conveys information about its overall stability. This stability information portends survival and therefore has absolute existential meaning for the living system. The first derivative of the Lyapunov energy information function will have a negative trajectory toward a system's steady state if the driving force is dissipating. By contrast, system instability leading to system dissolution will have a positive trajectory. The direction and magnitude of the vector for the trajectory then serves as a quantifiable signature of the meaning associated with the living system’s stability information, homeostasis and survival potential.

Keywords: meaning, information, Lyapunov, living systems

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1098 The Influence of Viscosifier Concentration on Rheological Properties of Invert Emulsion Mud

Authors: Suzan Ibrahim

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Oil-based muds are the most regularly used rotary drilling methods in the oil and gas industry. However, they have a negative impact on the environment, which leads to restrictions of their application in many countries of the world. Consequently, looking for new eco-friendly alternative formulations of oil-based drilling fluids for the exploration of troublesome formations. As one of the developments of Novel formulation of environmentally friendly drilling fluids and investigation of the formulation for jatropha oil-based drilling fluid samples at different concentrations of viscosifiers such as low viscosity polyanionic cellulose (PAC- LV), high viscosity polyanionic cellulose (PAC-V) and local Egyptian bentonite. The oil-water ratio was taken as 70:30, which is beneficial in producing a low fluid loss. 15 drilling fluid samples were formulated different concentrations of bentonite, PAC- LV and PAC-V individually and their mud density, rheological properties, electrical stability and filtration loss properties were determined. The rheological performance showed at higher concentrations of viscosifier, the trend of viscosity increment of PAC performed in a similar way to bentonite. The best result of electrical stability by using the lowest concentration of viscosifier was achieved with PAC-V. The lowest fluid loss volumes were obtained by using the highest concentrations (4 g) of viscosifiers. Mud cake thickness of samples increased by using viscosifiers; however, a lower range was achieved compared to API specification. From the overall experiment, it can be concluded that as the concentrations of viscosifier increase, the viscosity trend increase in a similar way to both PAC-V and bentonite. But we must note that the PAC-V is a more environmentally friendly additive and a renewable resource, cheaper than bentonite and improves properties of eco-friendly OBMs well. It is a preferable choice for oil-based drilling fluids.

Keywords: invert emulsion mud, oil-based mud, rheological properties, viscosifier

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1097 Cross-Sectional Analysis of the Health Product E-Commerce Market in Singapore

Authors: Andrew Green, Jiaming Liu, Kellathur Srinivasan, Raymond Chua

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Introduction: The size of Singapore’s online health product (HP) market (e-commerce) is largely unknown. However, it is recognized that a large majority comes from overseas and thus, unregulated. As buying HP from unauthorized sources significantly compromises public health safety, understanding e-commerce users’ demographics and their perceptions on online HP purchasing becomes a pivotal first step to form a basis for recommendations in Singapore’s pharmacovigilance efforts. Objective: To assess the prevalence of online HP purchasing behaviour among Singaporean e-commerce users. Methodology: This is a cross-sectional study targeting Singaporean e-commerce users recruited from various local websites and online forums. Participants were not randomized into study arms but instead stratified by random sampling method based on participants’ age. A self-administered anonymous questionnaire was used to explore participants' demographics, online HP purchasing behaviour, knowledge and attitude. The association of different variables with online HP purchasing behaviour was analysed using logistic regression statistics. Main outcome measures: Prevalence of HP e-commerce users in Singapore (%) and variables that contribute to the prevalence (adjusted prevalent ratio). Results: The study recruited 372 complete and valid responses. The prevalence of online HP consumers among e-commerce users in Singapore is estimated to be 55.9% (1.7 million consumers). Online purchasing of complementary HP (46.9%) was the most prevalent, followed by medical devices (21.6%) and Western medicine (20.5%). Multivariate analysis showed that age is an independent variable that correlates with the likelihood of buying HP online. The prevalence of HP e-commerce users is highest in the 35-44 age group (64.1%) and lowest among the 16-24 age group (36.4%). The most bought HP through the internet are vitamins and minerals (21.5%), non-herbal (15.9%), herbal (13.9%), weight loss (8.7%) and sports (8.4%) supplements. While the top 3 products are distributed equally between the genders, there is a skew towards female respondents (12.4% in females vs. 4.9% in males) for weight loss supplements and towards males (13.2% in males vs. 3.7% in females) for sports supplements. Even though online consumers are in the younger age brackets, our study found that up to 72.0% of HP bought online are bought for others (buyer’s family and/or friends). Multivariate analysis showed a statistically significant association between purchasing HP through online means and the perceptions that 'internet is safe' (adjusted Prevalence Ratio=1.15, CI 1.03-1.28), 'buying HP online is time saving' (PR=1.17, CI 1.01-1.36), and 'recognition of HP brand' (PR=1.21 CI 1.06-1.40). Conclusions: This study has provided prevalence data for online HP market in Singapore, and has allowed the country’s regulatory body to formulate a targeted pharmacovigilance approach to this growing problem.

Keywords: e-commerce, pharmaceuticals, pharmacovigilance, Singapore

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1096 A Mixed 3D Finite Element for Highly Deformable Thermoviscoplastic Materials Under Ductile Damage

Authors: João Paulo Pascon

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In this work, a mixed 3D finite element formulation is proposed in order to analyze thermoviscoplastic materials under large strain levels and ductile damage. To this end, a tetrahedral element of linear order is employed, considering a thermoviscoplastic constitutive law together with the neo-Hookean hyperelastic relationship and a nonlocal Gurson`s porous plasticity theory The material model is capable of reproducing finite deformations, elastoplastic behavior, void growth, nucleation and coalescence, thermal effects such as plastic work heating and conductivity, strain hardening and strain-rate dependence. The nonlocal character is introduced by means of a nonlocal parameter applied to the Laplacian of the porosity field. The element degrees of freedom are the nodal values of the deformed position, the temperature and the nonlocal porosity field. The internal variables are updated at the Gauss points according to the yield criterion and the evolution laws, including the yield stress of matrix, the equivalent plastic strain, the local porosity and the plastic components of the Cauchy-Green stretch tensor. Two problems involving 3D specimens and ductile damage are numerically analyzed with the developed computational code: the necking problem and a notched sample. The effect of the nonlocal parameter and the mesh refinement is investigated in detail. Results indicate the need of a proper nonlocal parameter. In addition, the numerical formulation can predict ductile fracture, based on the evolution of the fully damaged zone.

Keywords: mixed finite element, large strains, ductile damage, thermoviscoplasticity

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1095 Hybrid-Nanoengineering™: A New Platform for Nanomedicine

Authors: Mewa Singh

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Nanomedicine, a fusion of nanotechnology and medicine, is an emerging technology ideally suited to the targeted therapies. Nanoparticles overcome the low selectivity of anti-cancer drugs toward the tumor as compared to normal tissue and hence result-in less severe side-effects. Our new technology, HYBRID-NANOENGINEERING™, uses a new molecule (MR007) in the creation of nanoparticles that not only helps in nanonizing the medicine but also provides synergy to the medicine. The simplified manufacturing process will result in reduced manufacturing costs. Treatment is made more convenient because hybrid nanomedicines can be produced in oral, injectable or transdermal formulations. The manufacturing process uses no protein, oil or detergents. The particle size is below 180 nm with a narrow distribution of size. Importantly, these properties confer great stability of the structure. The formulation does not aggregate in plasma and is stable over a wide range of pH. The final hybrid formulation is stable for at least 18 months as a powder. More than 97 drugs, including paclitaxel, docetaxel, tamoxifen, doxorubicinm prednisone, and artemisinin have been nanonized in water soluble formulations. Preclinical studies on cell cultures of tumors show promising results. Our HYBRID-NANOENGINEERING™ platform enables the design and development of hybrid nano-pharmaceuticals that combine efficacy with tolerability, giving patients hope for both extended overall survival and improved quality of life. This study would discuss or present this new discovery of HYBRID-NANOENGINEERING™ which targets drug delivery, synergistic, and potentiating effects, and barriers of drug delivery and advanced drug delivery systems.

Keywords: nano-medicine, nano-particles, drug delivery system, pharmaceuticals

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1094 Model Predictive Control Applied to Thermal Regulation of Thermoforming Process Based on the Armax Linear Model and a Quadratic Criterion Formulation

Authors: Moaine Jebara, Lionel Boillereaux, Sofiane Belhabib, Michel Havet, Alain Sarda, Pierre Mousseau, Rémi Deterre

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Energy consumption efficiency is a major concern for the material processing industry such as thermoforming process and molding. Indeed, these systems should deliver the right amount of energy at the right time to the processed material. Recent technical development, as well as the particularities of the heating system dynamics, made the Model Predictive Control (MPC) one of the best candidates for thermal control of several production processes like molding and composite thermoforming to name a few. The main principle of this technique is to use a dynamic model of the process inside the controller in real time in order to anticipate the future behavior of the process which allows the current timeslot to be optimized while taking future timeslots into account. This study presents a procedure based on a predictive control that brings balance between optimality, simplicity, and flexibility of its implementation. The development of this approach is progressive starting from the case of a single zone before its extension to the multizone and/or multisource case, taking thus into account the thermal couplings between the adjacent zones. After a quadratic formulation of the MPC criterion to ensure the thermal control, the linear expression is retained in order to reduce calculation time thanks to the use of the ARMAX linear decomposition methods. The effectiveness of this approach is illustrated by experiment and simulation.

Keywords: energy efficiency, linear decomposition methods, model predictive control, mold heating systems

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1093 Development of an Ecological Binder by Geopolymerization of Untreated Dredged Sediments

Authors: Lisa Monteiro, Jacqueline Saliba, Nadia Saiyouri, Humberto Y. Godoy

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Theevolution of the global environmental context incites companies to reduce their impact by reusing local materials and promoting circular economy. Dredged sediments represent a potential source of materials due to their large volume. Indeed, the dredging operations carried out in Gironde alone generated an annual volume of sediment of approximately 9 million m³. Moreover, on the eve of the evolution of laws concerning dredging practices, the recovery of sediments is necessary to create a viable economy for their management. This thesis work is oriented towards the development of an ecological binder from the fine fraction of untreated dredged sediments. In fact, their physico-chemical properties make them favorable for the synthesis of geopolymer, current competitor of cement, thanks to its lower carbon footprint and environmental impact. However, several obstacles must be overcome before implementing this new family of materials: the use of sediments without thermal or chemical treatment, the absence of a formulation approach, ignorance of the reactions produced, etc. During the first year of the thesis, a physico-chemical characterization of the sediments made it possible to validate their use as precursors forgeopolymerization according to three criteria: their fineness, their mineralogical composition, and the percentage of amorphous phase. Following these results, several formulations have been defined, taking into account the environmental impact. The sediments were activated with an alkaline solution of sodium hydroxide and sodium silicate. Two other formulations with cement and blast furnace slag have been defined for comparison. The results highlighted the possibility of forming geopolymers from untreated and still wet dredged sediments. The development of structural bonds through the formation of hydrated sodium aluminosilicate thus leads to higher strengths at 90 days (4.78 MPa) than a mixture with cement (0.75 MPa). A 30% gain in CO₂ emissions has also been obtained compared to cement. In order to reduce the uncertainties linked to the absence of a formulation approach, to optimize the number of experiments to be carried out in the laboratory, and to obtain an optimal formulation, an analysis by mixing plan was conducted in order to frame the responses according to the proportions of the constituents. Following the obtaining of an optimal binder, the work will focus on the study of the durability and the interspecific variability of the sediments on the mechanical properties by testing the binder developed with different sediments dredged from the Bordeaux estuary. , the Grand Port Maritime of Bayonne, La Rochelle, and the Bassinsd'Arcachon.

Keywords: compressive strength, dredged sediments, ecological binder, geopolymers

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1092 Nude Cosmetic Water-Rich Compositions for Skin Care and Consumer Emotions

Authors: Emmanuelle Merat, Arnaud Aubert, Sophie Cambos, Francis Vial, Patrick Beau

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Basically, consumers are sensitive to many stimuli when applying a cream: brand, packaging and indeed formulation compositions. Many studies demonstrated the influence of some stimuli such as brand, packaging, formula color and odor (e.g. in make-up applications). Those parameters influence perceived quality of the product. The objective of this work is to further investigate the relationship between nude skincare basic compositions with different textures and consumer experience. A tentative final step will be to connect the consumer feelings with key ingredients in the compositions. A new approach was developed to better understand touch-related subjective experience in consumers based on a combination of methods: sensory analysis with ten experts, preference mapping on one hundred female consumers and emotional assessments on thirty consumers (verbal and non-verbal through prosody and gesture monitoring). Finally, a methodology based on ‘sensorial trip’ (after olfactory, haptic and musical stimuli) has been experimented on the most interesting textures with 10 consumers. The results showed more or less impact depending on compositions and also on key ingredients. Three types of formulation particularly attracted the consumer: an aqueous gel, an oil-in-water emulsion, and a patented gel-in-oil formulation type. Regarding these three formulas, the preferences were both revealed through sensory and emotion tests. One was recognized as the most innovative in consumer sensory test whereas the two other formulas were discriminated in emotions evaluation. The positive emotions were highlighted especially in prosody criteria. The non-verbal analysis, which corresponds to the physical parameters of the voice, showed high pitch and amplitude values; linked to positive emotions. Verbatim, verbal content of responses (i.e., ideas, concepts, mental images), confirmed the first conclusion. On the formulas selected for their positive emotions generation, the ‘sensorial trip’ provided complementary information to characterize each emotional profile. In the second step, dedicated to better understand ingredients power, two types of ingredients demonstrated an obvious input on consumer preference: rheology modifiers and emollients. As a conclusion, nude cosmetic compositions with well-chosen textures and ingredients can positively stimulate consumer emotions contributing to capture their preference. For a complete achievement of the study, a global approach (Asia, America territories...) should be developed.

Keywords: sensory, emotion, cosmetic formulations, ingredients' influence

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1091 Increasing Solubility and Bioavailability of Fluvastatin through Transdermal Nanoemulsion Gel Delivery System for the Treatment of Osteoporosis

Authors: Ramandeep Kaur, Makula Ajitha

Abstract:

Fluvastatin has been reported for increasing bone mineral density in osteoporosis since last decade. Systemically administered drug undergoes extensive hepatic first-pass metabolism, thus very small amount of drug reaches the bone tissue which is highly insignificant. The present study aims to deliver fluvastatin in the form of nanoemulsion (NE) gel directly to the bone tissue through transdermal route thereby bypassing hepatic first pass metabolism. The NE formulation consisted of isopropyl myristate as oil, tween 80 as surfactant, transcutol as co-surfactant and water as the aqueous phase. Pseudoternary phase diagrams were constructed using aqueous titration method and NE’s obtained were subjected to thermodynamic-kinetic stability studies. The stable NE formulations were evaluated for their droplet size, zeta potential, and transmission electron microscopy (TEM). The nano-sized formulations were incorporated into 0.5% carbopol 934 gel matrix. Ex-vivo permeation behaviour of selected formulations through rat skin was investigated and compared with the conventional formulations (suspension and emulsion). Further, in-vivo pharmacokinetic study was carried using male Wistar rats. The optimized NE formulations mean droplet size was 11.66±3.2 nm with polydispersity index of 0.117. Permeation flux of NE gel formulations was found significantly higher than the conventional formulations i.e. suspension and emulsion. In vivo pharmacokinetic study showed significant increase in bioavailability (1.25 fold) of fluvastatin than oral formulation. Thus, it can be concluded that NE gel was successfully developed for transdermal delivery of fluvastatin for the treatment of osteoporosis.

Keywords: fluvastatin, nanoemulsion gel, osteoporosis, transdermal

Procedia PDF Downloads 178
1090 Screening for Larvicidal Activity of Aqueous and Ethanolic Extracts of Fourteen Selected Plants and Formulation of a Larvicide against Aedes aegypti (Linn.) and Aedes albopictus (Skuse) Larvae

Authors: Michael Russelle S. Alvarez, Noel S. Quiming, Francisco M. Heralde

Abstract:

This study aims to: a) obtain ethanolic (95% EtOH) and aqueous extracts of Selaginella elmeri, Christella dentata, Elatostema sinnatum, Curculigo capitulata, Euphorbia hirta, Murraya koenigii, Alpinia speciosa, Cymbopogon citratus, Eucalyptus globulus, Jatropha curcas, Psidium guajava, Gliricidia sepium, Ixora coccinea and Capsicum frutescens and screen them for larvicidal activities against Aedes aegypti (Linn.) and Aedes albopictus (Skuse) larvae; b) to fractionate the most active extract and determine the most active fraction; c) to determine the larvicidal properties of the most active extract and fraction against by computing their percentage mortality, LC50, and LC90 after 24 and 48 hours of exposure; and d) to determine the nature of the components of the active extracts and fractions using phytochemical screening. Ethanolic (95% EtOH) and aqueous extracts of the selected plants will be screened for potential larvicidal activity against Ae. aegypti and Ae. albopictus using standard procedures and 1% malathion and a Piper nigrum based ovicide-larvicide by the Department of Science and Technology as positive controls. The results were analyzed using One-Way ANOVA with Tukey’s and Dunnett’s test. The most active extract will be subjected to partial fractionation using normal-phase column chromatography, and the fractions subsequently screened to determine the most active fraction. The most active extract and fraction were subjected to dose-response assay and probit analysis to determine the LC50 and LC90 after 24 and 48 hours of exposure. The active extracts and fractions will be screened for phytochemical content. The ethanolic extracts of C. citratus, E. hirta, I. coccinea, G. sepium, M. koenigii, E globulus, J. curcas and C. frutescens exhibited significant larvicidal activity, with C. frutescens being the most active. After fractionation, the ethyl acetate fraction was found to be the most active. Phytochemical screening of the extracts revealed the presence of alkaloids, tannins, indoles and steroids. A formulation using talcum powder–300 mg fraction per 1 g talcum powder–was made and again tested for larvicidal activity. At 2 g/L, the formulation proved effective in killing all of the test larvae after 24 hours.

Keywords: larvicidal activity screening, partial purification, dose-response assay, capsicum frutescens

Procedia PDF Downloads 320
1089 The Role of Privatization on the Formulation of Productive Supply Chain: The Case of Ethiopian Firms

Authors: Merhawit Fisseha Gebremariam, Yohannes Yebabe Tesfay

Abstract:

This study focuses on the formulation of a sustainable, effective, and efficient supply chain strategy framework that will enable Ethiopian privatized firms. The study examined the role of privatization in productive sourcing, production, and delivery to Ethiopian firm’s performances. To analyze our hypothesis, the authors applied the concepts of Key Performance Indicator (KPI), strategic outsourcing, purchasing portfolio analysis, and Porter's marketing analysis. The authors selected ten privatized companies and compared their financial, market expansion, and sustainability performances. The Chi-Square Test showed that at the 5% level of significance, privatization and outsourcing activities can assist the business performances of Ethiopian firms in terms of product promotion and new market expansion. At the 5% level of significance, the independent t-test result showed that firms that were privatized by Ethiopian investors showed stronger financial performance than those that were privatized by foreign investors. Furthermore, it is better if Ethiopian firms apply both cost leadership and differentiated strategy to enhance thriving in their business area. Ethiopian firms need to implement the supply chain operations reference (SCOR) model for an exclusive framework that supports communication links the supply chain partners, and enhances productivity. The government of Ethiopia should be aware that the privatization of firms by Ethiopian investors will strengthen the economy. Otherwise, the privatization process will be risky for the country, and therefore, the government of Ethiopia should stop doing those activities.

Keywords: correlation analysis, market strategies, KPIs, privatization, risk and Ethiopia

Procedia PDF Downloads 49
1088 Preparation and In vitro Characterization of Nanoparticle Hydrogel for Wound Healing

Authors: Rajni Kant Panik

Abstract:

The aim of the present study was to develop and evaluate mupirocin loaded nanoparticle incorporated into hydrogel as an infected wound healer. Incorporated Nanoparticle in hydrogel provides a barrier that effectively prevents the contamination of the wound and further progression of infection to deeper tissues. Hydrogel creates moist healing environment on wound space with good fluid absorbance. Nanoparticles were prepared by double emulsion solvent evaporation method using different ratios of PLGA polymer and the hydrogels was developed using sodium alginate and gelatin. Further prepared nanoparticles were then incorporated into the hydrogels. The formulations were characterized by FT-IR and DSC for drug and polymer compatibility and surface morphology was studied by TEM. Nanoparticle hydrogel were evaluated for their size, shape, encapsulation efficiency and for in vitro studies. The FT-IR and DSC confirmed the absence of any drug polymer interaction. The average size of Nanoparticle was found to be in range of 208.21-412.33 nm and shape was found to be spherical. The maximum encapsulation efficiency was found to be 69.03%. The in vitro release profile of Nanoparticle incorporated hydrogel formulation was found to give sustained release of drug. Antimicrobial activity testing confirmed that encapsulated drug preserve its effectiveness. The stability study confirmed that the formulation prepared were stable. Present study complements our finding that mupirocin loaded Nanoparticle incorporated into hydrogel has the potential to be an effective and safe novel addition for the release of mupirocin in sustained manner, which may be a better option for the management of wound. These finding also supports the progression of antibiotic via hydrogel delivery system is a novel topical dosage form for the management of wound.

Keywords: hydrogel, nanoparticle, PLGA, wound healing

Procedia PDF Downloads 301
1087 3D Printing of Dual Tablets: Modified Multiple Release Profiles for Personalized Medicine

Authors: Veronika Lesáková, Silvia Slezáková, František Štěpánek

Abstract:

Additive manufacturing technologies producing drug dosage forms aimed at personalized medicine applications are promising strategies with several advantages over the conventional production methods. One of the emerging technologies is 3D printing which reduces manufacturing steps and thus allows a significant drop in expenses. A decrease in material consumption is also a highly impactful benefit as the tested drugs are frequently expensive substances. In addition, 3D printed dosage forms enable increased patient compliance and prevent misdosing as the dosage forms are carefully designed according to the patient’s needs. The incorporation of multiple drugs into a single dosage form further increases the degree of personalization. Our research focuses on the development of 3D printed tablets incorporating multiple drugs (candesartan, losartan) and thermoplastic polymers (e.g., KlucelTM HPC EF). The filaments, an essential feed material for 3D printing,wereproduced via hot-melt extrusion. Subsequently, the extruded filaments of various formulations were 3D printed into tablets using an FDM 3D printer. Then, we have assessed the influence of the internal structure of 3D printed tablets and formulation on dissolution behaviour by obtaining the dissolution profiles of drugs present in the 3D printed tablets. In conclusion, we have developed tablets containing multiple drugs providing modified release profiles. The 3D printing experiments demonstrate the high tunability of 3D printing as each tablet compartment is constructed with a different formulation. Overall, the results suggest that the 3D printing technology is a promising manufacturing approach to dual tablet preparation for personalized medicine.

Keywords: 3D printing, drug delivery, hot-melt extrusion, dissolution kinetics

Procedia PDF Downloads 160
1086 Chemical and Bioactive Constituents Isolated from the Formosa Zamia furfureace L.

Authors: Chien-Liang Chao, Yun-Sheng Lin

Abstract:

Secondary metabolites are applied in the human life of the Chinese herbal medicine. Many drugs are originally extracted from natural products with combination of pharmaceutical and chemical studies. Crude extract of the leaves from Zamia furfureace L. has been shown to exhibit anticancer activities. The first chemical investigation of this plant was carried out by our group. In this study, four known compounds were isolated from Zamia furfureace L. with three lignins (Sesamin (1), Wodeshiol (2) and Paulownin (3)), and one dipeptide (Aurantiamide acetate (4)). The structures of these compounds were analyzed through the 1D-NMR(1H-NMR,13C-NMR)、2D-NMR(COSY、HMQC、HMBC、NOESY) spectroscopic analysis, and by comparison of variety of physical data (IR, mass spectrometry, ultraviolet, optical rotation). Among them, Aurantiamide acetate (4) exhibited weak cytotoxic activity against human gastric cancer cells.

Keywords: Zamia furfureace L., AGS, sesamin, Aurantiamide acetate, secondary metabolites

Procedia PDF Downloads 473
1085 The Effect of Hydroxyl Ethyl Cellulose (HEC) and Hydrophobically-Modified Alkali Soluble Emulsions (HASE) on the Properties and Quality of Water Based Paints

Authors: Haleden Chiririwa, Sandile S. Gwebu

Abstract:

The coatings industry is a million dollar business, and it is easy and inexpensive to set-up but it is growing very slowly in developing countries, and this study developed a paint formulation which gives better quality and good application properties. The effect of rheology modifiers, i.e. non-ionic polymers hydrophobically-modified ethoxylated urethanes (HEUR), anionic polymers hydrophobically-modified alkali soluble emulsions (HASE) and hydroxyl ethyl cellulose (HEC) on the quality and properties of water-based paints have been investigated. HEC provides the in-can viscosity and increases open working time while HASE improves application properties like spatter resistance and brush loading and HEUR provides excellent scrub resistance. Four paint recipes were prepared using four different thickeners HEC, HASE (carbopol) and Cellulose nitrate. The fourth formulation was thickened with a combination of HASE and HEC, this aimed at improving quality and at the same time reducing cost. The four samples were tested for quality tests such viscosity, sag resistance, volatile matter, tinter effect, drying times, hiding power, scrub resistance and stability on storage. Environmental factors were incorporated in the attempt to formulate an economic and green product. Hydroxyl ethyl cellulose and cellulose nitrate gave high quality and good properties of the paint. HEC and Cellulose nitrate showed stability on storage whereas carbopol thickener was very unstable.

Keywords: properties, thickeners, rheology modifiers, water based paints

Procedia PDF Downloads 255
1084 Formulation and Optimization of Topical 5-Fluorouracil Microemulsions Using Central Compisite Design

Authors: Sudhir Kumar, V. R. Sinha

Abstract:

Water in oil topical microemulsions of 5-FU were developed and optimized using face centered central composite design. Topical w/o microemulsion of 5-FU were prepared using sorbitan monooleate (Span 80), polysorbate 80 (Tween 80), with different oils such as oleic acid (OA), triacetin (TA), and isopropyl myristate (IPM). The ternary phase diagrams designated the microemulsion region and face centered central composite design helped in determining the effects of selected variables viz. type of oil, smix ratio and water concentration on responses like drug content, globule size and viscosity of microemulsions. The CCD design exhibited that the factors have statistically significant effects (p<0.01) on the selected responses. The actual responses showed excellent agreement with the predicted values as suggested by the CCD with lower residual standard error. Similarly, the optimized values were found within the range as predicted by the model. Furthermore, other characteristics of microemulsions like pH, conductivity were investigated. For the optimized microemulsion batch, ex-vivo skin flux, skin irritation and retention studies were performed and compared with marketed 5-FU formulation. In ex vivo skin permeation studies, higher skin retention of drug and minimal flux was achieved for optimized microemulsion batch then the marketed cream. Results confirmed the actual responses to be in agreement with predicted ones with least residual standard errors. Controlled release of drug was achieved for the optimized batch with higher skin retention of 5-FU, which can further be utilized for the treatment of many dermatological disorders.

Keywords: 5-FU, central composite design, microemulsion, ternanry phase diagram

Procedia PDF Downloads 467
1083 Novel Liposomal Nanocarriers For Long-term Tumor Imaging

Authors: Mohamad Ahrari, Kayvan Sadri, Mahmoud Reza Jafari

Abstract:

PEGylated liposomes have a smaller volume of distribution and decreased clearance, consequently, due to their more prolonged presence in bloodstream and maintaining their stability during this period, these liposomes can be applied for imaging tumoral sites. The purpose of this study is to develop an appropriate radiopharmaceutical agent in long-term imaging for improved diagnosis and evaluation of tumors. In this study, liposomal formulations encapsulating albumin is synthesized by solvent evaporation method along with homogenization, and their characteristics were assessed. Then these liposomes labeled by Philips method and the rate of stability of labeled liposomes in serum, and ultimately the rate of biodistribution and gamma scintigraphy in C26-colon carcinoma tumor-bearing mice, were studied. The result of the study of liposomal characteristics displayed that capable of accumulating in tumor sites based of EPR phenomenon. these liposomes also have high stability for maintaining encapsulated albumin in a long time. In the study of biodistribution of these liposomes in mice, they accumulated more in the kidney, liver, spleen, and tumor sites, which, even after clearing formulations in the bloodstream, they existed in high levels in these organs up to 96 hours. In gamma scintigraphy also, organs with high activity accumulation from early hours up to 96 hours were visible in the form of hot spots. concluded that PEGylated liposomal formulation encapsulating albumin can be labeled with In-Oxine, and obtained stabilized formulation for long-term imaging, that have more favorable conditions for the evaluation of tumors and it will cause early diagnosis of tumors.

Keywords: nano liposome, 111In-oxine, imaging, biodistribution, tumor

Procedia PDF Downloads 98
1082 Screening of Potential Sources of Tannin and Its Therapeutic Application

Authors: Mamta Kumari, Shashi Jain

Abstract:

Tannins are a unique category of plant phytochemicals especially in terms of their vast potential health-benefiting properties. Researchers have described the capacity of tannins to enhance glucose uptake and inhibit adipogenesis, thus being potential drugs for the treatment of non-insulin dependent diabetes mellitus. Thus, the present research was conducted to find out tannin content of food products. The percentage of tannin in various analyzed sources ranged from 0.0 to 108.53%; highest in kathaa and lowest in ker and mango bark. The percentage of tannins present in the plants, however, varies. Numerous studies have confirmed that the naturally occurring polyphenols are key factor for the beneficial effects of the herbal medicines. Isolation and identification of active constituents from plants, preparation of standardized dose & dosage regimen can play a significant role in improving the hypoglycaemic action.

Keywords: tannins, diabetes, polyphenols, antioxidant, hypoglycemia

Procedia PDF Downloads 371
1081 Development of 4-Allylpyrocatechol Loaded Self-Nanoemulsifying Drug Delivery System for Enhancing Water Solubility and Antibacterial Activity against Oral Pathogenic Bacteria

Authors: Pimpak Phumat, Sakornrat Khongkhunthian, Thomas Rades, Anette Müllertz, Siriporn Okonogi

Abstract:

Self-nanoemulsifying drug delivery systems (SNEDDS) containing 4-allylpyrocatechol (AP) extracted from Piper betle were developed to enhance water solubility of AP by using modeling and design (MODDE) program. The amount of AP in each SNEDDS formulation was determined by using high-performance liquid chromatography. The formulation consisted of 20% Miglyol®812N, 40 % Kolliphor®RH40, 30 % Maisine®35-1 and 10 % ethanol was found to be the best SNEDDS that provided the highest loading capacity of AP. (141.48±15.64 mg/g SNEDDS). The system also showed miscibility with water. The particle shape and size of the AP-SNEDDS after dispersing in water was investigated by using a transmission electron microscope and photon correlation spectrophotometer, respectively. The results showed that they were a spherical shape, having a particle size of 34.27 ± 1.14 nm with a narrow size distribution of 0.17 ± 0.04. The particles showed negative zeta potential with a value of -21.66 ± 2.09 mV. Antibacterial activity of AP-SNEDDS containing 1.5 mg/mL of AP was investigated against Streptococcus intermedius. The effect of this system on S. intermedius cells was observed by a scanning electron microscope (SEM). The results from SEM revealed that the bacterial cells were obviously destroyed. Killing kinetic study of AP-SNEDDS was carried out. It was found that the killing rate of AP-SNEDDS against S. intermedius was dose-dependent and the bacterial reduction was 79.86 ± 0.45 % within 30 min. In comparison with chlorhexidine (CHX), AP-SNEDDS showed similar antibacterial effects against S. intermedius. It is concluded that SNEDDS is a potential system for enhancing water solubility of AP. The antibacterial study reveals that AP-SNEDDS can be a promising system to treat bacterial infection caused by S. intermedius.

Keywords: SNEDDS, 4-allylpyrocathecol, solubility, antibacterial activity, Streptococcus intermedius

Procedia PDF Downloads 105
1080 Development and Characterization of Novel Topical Formulation Containing Niacinamide

Authors: Sevdenur Onger, Ali Asram Sagiroglu

Abstract:

Hyperpigmentation is a cosmetically unappealing skin problem caused by an overabundance of melanin in the skin. Its pathophysiology is caused by melanocytes being exposed to paracrine melanogenic stimuli, which can upregulate melanogenesis-related enzymes (such as tyrosinase) and cause melanosome formation. Tyrosinase is linked to the development of melanosomes biochemically, and it is the main target of hyperpigmentation treatment. therefore, decreasing tyrosinase activity to reduce melanosomes has become the main target of hyperpigmentation treatment. Niacinamide (NA) is a natural chemical found in a variety of plants that is used as a skin-whitening ingredient in cosmetic formulations. NA decreases melanogenesis in the skin by inhibiting melanosome transfer from melanocytes to covering keratinocytes. Furthermore, NA protects the skin from reactive oxygen species and acts as a main barrier with the skin, reducing moisture loss by increasing ceramide and fatty acid synthesis. However, it is very difficult for hydrophilic compounds such as NA to penetrate deep into the skin. Furthermore, because of the nicotinic acid in NA, it is an irritant. As a result, we've concentrated on strategies to increase NA skin permeability while avoiding its irritating impacts. Since nanotechnology can affect drug penetration behavior by controlling the release and increasing the period of permanence on the skin, it can be a useful technique in the development of whitening formulations. Liposomes have become increasingly popular in the cosmetics industry in recent years due to benefits such as their lack of toxicity, high penetration ability in living skin layers, ability to increase skin moisture by forming a thin layer on the skin surface, and suitability for large-scale production. Therefore, liposomes containing NA were developed for this study. Different formulations were prepared by varying the amount of phospholipid and cholesterol and examined in terms of particle sizes, polydispersity index (PDI) and pH values. The pH values of the produced formulations were determined to be suitable with the pH value of the skin. Particle sizes were determined to be smaller than 250 nm and the particles were found to be of homogeneous size in the formulation (pdi<0.30). Despite the important advantages of liposomal systems, they have low viscosity and stability for topical use. For these reasons, in this study, liposomal cream formulations have been prepared for easy topical application of liposomal systems. As a result, liposomal cream formulations containing NA have been successfully prepared and characterized. Following the in-vitro release and ex-vivo diffusion studies to be conducted in the continuation of the study, it is planned to test the formulation that gives the most appropriate result on the volunteers after obtaining the approval of the ethics committee.

Keywords: delivery systems, hyperpigmentation, liposome, niacinamide

Procedia PDF Downloads 102
1079 Physicochemical and Biological Characterization of 1,2-Dialkoylamidopropane-Based Lipoplexes for Gene Delivery

Authors: Suhair Saleh, Ahmad Aljaberi

Abstract:

Cationic lipid-mediated delivery of nucleic acids represents an exciting approach for developing therapeutically realistic gene medicines. Elucidation of the molecular and formulation requirements for efficient lipofection is a prerequisite to enhance the biological activity of such delivery systems. To this end, the in vitro lipofection activity of the ionizable asymmetric 1,2-dialkoylamidopropane-based derivatives bearing single primary amine group as the cationic head group was evaluated. The electrostatic interactions of these cationic lipids with plasmid DNA in physiologically relevant medium were investigated by means of gel electrophoresis retardation and Eth-Br quenching assays. The effect of the presence of the helper lipid on these interactions was evaluated. The physicochemical properties of these lipids in terms of bilayer fluidity and extent of ionization were investigated using fluorescence anisotropy and surface potential techniques, respectively. The results showed that only the active lipid, 1,2lmp[5], existed in a liquid crystalline state at physiological temperature. Moreover, the extent of ionization of this lipid in assemblies was significantly higher that it's saturated analogues. Inclusion of the helper lipid DOPE improved the encapsulation and association between 1,2lmp[5] and plasmid DNA, which was reflected by the significant boost of lipofection activity of the 1,2lmp[5]/DOPE formulation as compared to the lipid alone. In conclusion, membrane fluidity and sufficient protonation of ionizable cationic lipid are required for efficient association and encapsulation of plasmid DNA and promoting improved in vitro lipofection activity.

Keywords: cationic lipids, gene delivery, lipofection, membrane fluidity, helper lipids, surface potential

Procedia PDF Downloads 229