Search results for: dissolution

Authors: Tim Dunne, Jiaxiang Ren, Lei Zhao, Peng Cheng, Yi Song, Yu Liu, Wenhan Yue, Xiongwen Yang

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Two decades of the Shale Revolution has transforming transformed the global energy market, in part by the adaption of multi-stage dissolvable frac plugs. Magnesium has been favored for the bulk of plugs, requiring development of materials to suit specific field requirements. Herein, the mechanical and dissolution results from equal channel angular pressing (ECAP) of two cast dissolvable magnesium alloy are described. ECAP was selected as a route to increase the mechanical properties of two formulations of dissolvable magnesium, as solutionizing failed. In this study, 1” square cross section samples cast Mg alloys formulations containing rare earth were processed at temperatures ranging from 200 to 350 °C, at a rate of 0.005”/s, with a backpressure from 0 to 70 MPa, in a brass, or brass + graphite sheet. Generally, the yield and ultimate tensile strength (UTS) doubled for all. For formulation DM-2, the yield increased from 100 MPa to 250 MPa; UTS from 175 MPa to 325 MPa, but the strain fell from 2 to 1%. Formulation DM-3 yield increased from 75 MPa to 200 MPa, UTS from 150 MPa to 275 MPa, with strain increasing from 1 to 3%. Meanwhile, ECAP has also been found to reduce the dissolution rate significantly. A microstructural analysis showed grain refinement of the alloy and the movement of secondary phases away from the grain boundary. It is believed that reconfiguration of the grain boundary phases increased the mechanical properties and decreased the dissolution rate. ECAP processing of dissolvable high rare earth content magnesium is possible despite the brittleness of the material. ECAP is a possible processing route to increase mechanical properties for dissolvable aluminum alloys that do not extrude.

Keywords: equal channel angular processing, dissolvable magnesium, frac plug, mechanical properties

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Authors: Nawel Ouennoughi, Kamel Daoud

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During recent years, new pharmaceutical dosage forms were developed in the research laboratories and which consists of encapsulating one or more active molecules in a polymeric envelope. Several techniques of encapsulation allow obtaining the microparticles or the nanoparticles containing one or several polymers. In the industry, microencapsulation is implemented to fill the following objectives: to ensure protection, the compatibility and the stabilization of an active matter in a formulation, to carry out an adapted working, to improve the presentation of a product, to mask a taste or an odor, to modify and control the profile of release of an active matter to obtain, for example, prolonged or started effect. To this end, we focus ourselves on the encapsulation of the antidiabetic. It is an oral hypoglycemic agent belonging to the second generation of sulfonylurea’s commonly employed in the treatment of type II non-insulin-dependent diabetes in order to improve profile them dissolution. Our choice was made on the technique of encapsulation by complex coacervation with two types of polymers (gelatin and the gum Arabic) which is a physicochemical process. Several parameters were studied at the time of the formulation of the microparticles and the nanoparticles: temperature, pH, ratio of polymers etc. The microparticles and the nanoparticles obtained were characterized by microscopy, laser granulometry, FTIR and UV-visible spectrophotometry. The profile of dissolution obtained for the microparticles showed an improvement of the kinetics of dissolution compared to that obtained for the active ingredient.

Keywords: coacervation, gum Arabic, microencapsulation, gelatin

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Authors: Namdeo Jadhav, Nitin Salunkhe

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Currently, sericin is being treated as waste of sericulture industry, especially at reeling process. Looking at prospective physicochemical properties, an attempt has been made to explore pharmaceutical applications of sericin waste in fabrication of medicated solid dispersions. Solid dispersions (SDs) of poorly soluble drugs (Lornoxicam, Meloxicam & Felodipine) were prepared by spray drying, solvent evaporation, ball milling and physical kneading in mass ratio of drug: sericin (1:0.5, 1:1, 1:1.5, 1:2, 1:2.5 and 1:3 w/w) and were investigated by solubility, ATR-FTIR, XRD and DSC, micromeritics and tablettability, surface morphology and in-vitro dissolution. It has been observed that sericin improves solubility of drugs by 8 to 10 times compared to pure drugs. The presence of hydrogen bonding between drugs and sericin was confirmed from the ATR-FTIR spectra. Amongst these methods, spray dried (1:2 w/w) SDs showed fully amorphous state representing molecularly distributed drug as confirmed from XRD and DSC study. Spray dried meloxicam SDs showed better compressibility and compactibility. The microphotograph of spray dried batches of lornoxicam (SDLX) and meloxicam SDs (SDMX) showed bowl shaped, and bowl plus spherical particles respectively, while spray dried felodipine SDs (SDFL) showed spherical shape. The SDLX, SDMX and SDFL (1:2 w/w) displayed better dissolution performance than other methods. Conclusively, hydrophilic matrix of sericin can be used to deliver poor water soluble drugs and its aerodynamic shape may show a great potential for various drug deliveries. If established as pharmaceutical excipient, sericin holds a potential to revolutionise economics of pharmaceutical industry, and sericulture farming, especially of Asian countries.

Keywords: biosericin, poorly soluble drugs, solid dispersion, solubility and dissolution improvement

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Authors: Priyanka Agrawal, Janou Koskamp, Amir Raoof, Mariette Wolthers

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Calcite is the main mineral found in carbonate rocks, which form significant hydrocarbon reservoirs and subsurface repositories for CO2 sequestration. The injected CO2 mixes with the reservoir fluid and disturbs the geochemical equilibrium, triggering calcite dissolution. Different combinations of fluid chemistry and injection rate may therefore result in different evolution of porosity, permeability and dissolution patterns. To model the changes in porosity and permeability Kozeny-Carman equation K∝〖(∅)〗^n is used, where K is permeability and ∅ is porosity. The value of n is mostly based on experimental data or pore network models. In pore network models, this derivation is based on accuracy of relation used for conductivity and pore volume change. In fact, at a single pore scale, this relationship is the result of the pore shape development due to dissolution. We have prepared a new reactive transport model for a single pore which simulates the complex chemical reaction of carbonic-acid induced calcite dissolution and subsequent pore-geometry evolution at a single pore scale. We use COMSOL Multiphysics package 5.3 for the simulation. COMSOL utilizes the arbitary-Lagrangian Eulerian (ALE) method for the free-moving domain boundary. We examined the effect of flow rate on the evolution of single pore shape profiles due to calcite dissolution. We used three flow rates to cover diffusion dominated and advection-dominated transport regimes. The fluid in diffusion dominated flow (Pe number 0.037 and 0.37) becomes less reactive along the pore length and thus produced non-uniform pore shapes. However, for the advection-dominated flow (Pe number 3.75), the fast velocity of the fluid keeps the fluid relatively more reactive towards the end of the pore length, thus yielding uniform pore shape. Different pore shapes in terms of inlet opening vs overall pore opening will have an impact on the relation between changing volumes and conductivity. We have related the shape of pore with the Pe number which controls the transport regimes. For every Pe number, we have derived the relation between conductivity and porosity. These relations will be used in the pore network model to get the porosity and permeability variation.

Keywords: single pore, reactive transport, calcite system, moving boundary

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Authors: Alireza Bahramian

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High-purity TiO₂ nanoparticles (NPs) with size ranging between 50 nm and 100 nm are synthesized from titanium slag through sulphate route under sonochemical procedure. The effect of dissolution parameters such as the sulfuric acid/slag weight ratio, caustic soda concentration, digestion temperature and time, and initial particle size of the dried slag on the extraction efficiency of TiO₂ and removal of iron are examined. By optimizing the digestion conditions, a rutile TiO₂ powder with surface area of 42 m²/g and mean pore diameter of 22.4 nm were prepared. A thermo-kinetic analysis showed that the digestion temperature has an important effect, while the acid/slag weight ratio and initial size of the slag has a moderate effect on the dissolution rate. The shrinking-core model including both chemical surface reaction and surface diffusion is used to describe the leaching process. A low value of activation energy, 38.12 kJ/mol, indicates the surface chemical reaction model is a rate-controlling step. The kinetic analysis suggested a first order reaction mechanism with respect to the acid concentrations.

Keywords: TiO₂ nanoparticles, titanium slag, dissolution rate, sonochemical method, thermo-kinetic study

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Authors: B. S. Muddukrishna, Karthik Aithal, Aravind Pai

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Introduction: Preparation of binary cocrystals of Etraverine (ETR) by using Tartaric Acid (TAR) as a conformer was the main focus of this study. Etravirine is a Class IV drug, as per the BCS classification system. Methods: Cocrystals were prepared by slow evaporation technique. A mixture of total 500mg of ETR: TAR was weighed in molar ratios of 1:1 (371.72mg of ETR and 128.27mg of TAR). Saturated solution of Etravirine was prepared in Acetone: Methanol (50:50) mixture in which tartaric acid is dissolved by sonication and then this solution was stirred using a magnetic stirrer until the solvent got evaporated. Shimadzu FTIR – 8300 system was used to acquire the FTIR spectra of the cocrystals prepared. Shimadzu thermal analyzer was used to achieve DSC measurements. X-ray diffractometer was used to obtain the X-ray powder diffraction pattern. Shake flask method was used to determine the equilibrium dynamic solubility of pure, physical mixture and cocrystals of ETR. USP buffer (pH 6.8) containing 1% of Tween 80 was used as the medium. The pure, physical mixture and the optimized cocrystal of ETR were accurately weighed sufficient to maintain the sink condition and were filled in hard gelatine capsules (size 4). Electrolab-Tablet Dissolution tester using basket apparatus at a rotational speed of 50 rpm and USP phosphate buffer (900 mL, pH = 6.8, 37 ˚C) + 1% Tween80 as a media, was used to carry out dissolution. Shimadzu LC-10 series chromatographic system was used to perform the analysis with PDA detector. An Hypersil BDS C18 (150mm ×4.6 mm ×5 µm) column was used for separation with mobile phase comprising of a mixture of ace¬tonitrile and phosphate buffer 20mM, pH 3.2 in the ratio 60:40 v/v. The flow rate was 1.0mL/min and column temperature was set to 30°C. The detection was carried out at 304 nm for ETR. Results and discussions: The cocrystals were subjected to various solid state characterization and the results confirmed the formation of cocrystals. The C=O stretching vibration (1741cm-1) in tartaric acid was disappeared in the cocrystal and the peak broadening of primary amine indicates hydrogen bond formation. The difference in the melting point of cocrystals when compared to pure Etravirine (265 °C) indicates interaction between the drug and the coformer which proves that first ordered transformation i.e. melting endotherm has disappeared. The difference in 2θ values of pure drug and cocrystals indicates the interaction between the drug and the coformer. Dynamic solubility and dissolution studies were also conducted by shake flask method and USP apparatus one respectively and 3.6 fold increase in the dynamic solubility were observed and in-vitro dissolution study shows four fold increase in the solubility for the ETR: TAR (1:1) cocrystals. The ETR: TAR (1:1) cocrystals shows improved solubility and dissolution as compared to the pure drug which was clearly showed by solid state characterization and dissolution studies.

Keywords: dynamic solubility, Etraverine, in vitro dissolution, slurry method

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Authors: C. Rattanakawin, S. Vasailor

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Acid leaching of flotation concentrate of oxide copper ore containing mainly of malachite was performed in a standard agitation tank with various parameters. The effects of solid to liquid ratio, sulfuric acid concentration, agitation speed, leaching temperature and time were examined to get proper conditions. The best conditions are 1:8 solid to liquid ratio, 10% concentration by weight, 250 rev/min, 30 ^oC and 5-min leaching time in respect. About 20% Cu grade assayed by atomic absorption technique with 98% copper recovery was obtained from these combined optimum conditions. Dissolution kinetics of the concentrate was approximated as a logarithmic function. As a result, the first-order reaction rate is suggested from this leaching study.

Keywords: agitation leaching, dissolution kinetics, flotation concentrate, oxide copper ore, sulfuric acid

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Authors: Rui Sousa, Aurora Futuro, António Fiúza

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The exploitation of gold ore deposits is highly dependent on efficient mineral processing methods, although actual perspectives based on life-cycle assessment introduce difficulties that were unforeseen in a very recent past. Cyanidation is the most applied gold processing method, but the potential environmental problems derived from the usage of cyanide as leaching reagent led to a demand for alternative methods. Ammoniacal thiosulfate leaching is one of the most important alternatives to cyanidation. In this article, some experimental studies carried out in order to assess the feasibility of thiosulfate as a leaching agent for the ore from the unexploited Portuguese gold mine of Castromil. It became clear that the process depends on the concentrations of ammonia, thiosulfate and copper. Based on this fact, a few leaching tests were performed in order to assess the best reagent prescription, and also the effects of different combination of these concentrations. Higher thiosulfate concentrations cause the decrease of gold dissolution. Lower concentrations of ammonia require higher thiosulfate concentrations, and higher ammonia concentrations require lower thiosulfate concentrations. The addition of copper increases the gold dissolution ratio. Subsequently, some alternative operatory conditions were tested such as variations in temperature and in the solid/liquid ratio as well as the application of a pre-treatment before the leaching stage. Finally, thiosulfate leaching was compared to cyanidation. Thiosulfate leaching showed to be an important alternative, although a pre-treatment is required to increase the yield of the gold dissolution.

Keywords: gold, leaching, pre-treatment, thiosulfate

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Authors: Joseph Lillington, Tom Gout, Mike Harrison, Ian Farnan

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The vitrification of high-level nuclear waste within borosilicate glass and its incorporation within a multi-barrier repository deep underground is widely accepted as the preferred disposal method. However, for this to happen, any safety case will require validation that the initially localized radionuclides will not be considerably released into the near/far-field. Therefore, accurate mechanistic models are necessary to predict glass dissolution, and these should be robust to a variety of incorporated waste species and leaching test conditions, particularly given substantial variations across international waste-streams. Here, machine learning is used to predict glass material properties (viscosity, density) and glass leaching model parameters from large-scale industrial data. A variety of different machine learning algorithms have been compared to assess performance. Density was predicted solely from composition, whereas viscosity additionally considered temperature. To predict suitable glass leaching model parameters, a large simulated dataset was created by coupling MATLAB and the chemical reactive-transport code HYTEC, considering the state-of-the-art GRAAL model (glass reactivity in allowance of the alteration layer). The trained models were then subsequently applied to the large-scale industrial, experimental data to identify potentially appropriate model parameters. Results indicate that ensemble methods can accurately predict viscosity as a function of temperature and composition across all three industrial datasets. Glass density prediction shows reliable learning performance with predictions primarily being within the experimental uncertainty of the test data. Furthermore, machine learning can predict glass dissolution model parameters behavior, demonstrating potential value in GRAAL model development and in assessing suitable model parameters for large-scale industrial glass dissolution data.

Keywords: machine learning, predictive modelling, pattern recognition, radioactive waste glass

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Authors: Esther Mafunda, Simbarashe Muparangi

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The present paper tests the applicability of the Regression Hypothesis on the pathological language dissolution of a Shona male adult with Broca’s aphasia. It particularly assesses the prediction of the Regression Hypothesis, which states that the process according to which language is forgotten will be the reversal of the process according to which it will be acquired. The main aim of the paper is to find out whether mirror symmetries between L1 acquisition and L1 dissolution of tense in Shona and, if so, what might cause these regression patterns. The paper also sought to highlight the practical contributions that Linguistic theory can make to solving language-related problems. Data was collected from a 46-year-old male adult with Broca’s aphasia who was receiving speech therapy at St Giles Rehabilitation Centre in Harare, Zimbabwe. The primary data elicitation method was experimental, using the probe technique. The TART (Test for Assessing Reference Time) Shona version in the form of sequencing pictures was used to access tense by Broca’s aphasic and 3.5-year-old child. Using the SPSS (Statistical Package for Social Studies) and Excel analysis, it was established that the use of the future tense was impaired in Shona Broca’s aphasic whilst the present and past tense was intact. However, though the past tense was intact in the male adult with Broca’s aphasic, a reference to the remote past was made. The use of the future tense was also found to be difficult for the 3,5-year-old speaking child. No difficulties were encountered in using the present and past tenses. This means that mirror symmetries were found between L1 acquisition and L1 dissolution of tense in Shona. On the basis of the results of this research, it can be concluded that the use of tense in a Shona adult with Broca’s aphasia supports the Regression Hypothesis. The findings of this study are important in terms of speech therapy in the context of Zimbabwe. The study also contributes to Bantu linguistics in general and to Shona linguistics in particular. Further studies could also be done focusing on the rest of the Bantu language varieties in terms of aphasia.

Keywords: Broca’s Aphasia, regression hypothesis, Shona, language dissolution

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Authors: M. Kumpugdee-Vollrath, M. Tabatabaeifar, M. Helmis

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Shellac is a natural polyester resin secreted by insects. Pectins are natural, non-toxic and water-soluble polysaccharides extracted from the peels of citrus fruits or the leftovers of apples. Both polymers are allowed for the use in the pharmaceutical industry and as a food additive. SSB Aquagold® is the aqueous solution of shellac and can be used for a coating process as an enteric or controlled drug release polymer. In this study, tablets containing 10 mg methylene blue as a model drug were prepared with a rotary press. Those tablets were coated with mixtures of shellac and one of the pectin different types (i.e. CU 201, CU 501, CU 701 and CU 020) mostly in a 2:1 ratio or with pure shellac in a small scale fluidized bed apparatus. A stable, simple and reproducible three-stage coating process was successfully developed. The drug contents of the coated tablets were determined using UV-VIS spectrophotometer. The characterization of the surface and the film thickness were performed with the scanning electron microscopy (SEM) and the light microscopy. Release studies were performed in a dissolution apparatus with a basket. Most of the formulations were enteric coated. The dissolution profiles showed a delayed or sustained release with a lagtime of at least 4 h. Dissolution profiles of coated tablets with pure shellac had a very long lagtime ranging from 13 to 17.5 h and the slopes were quite high. The duration of the lagtime and the slope of the dissolution profiles could be adjusted by adding the proper type of pectin to the shellac formulation and by variation of the coating amount. In order to apply a coating formulation as a colon delivery system, the prepared film should be resistant against gastric fluid for at least 2 h and against intestinal fluid for 4-6 h. The required delay time was gained with most of the shellac-pectin polymer mixtures. The release profiles were fitted with the modified model of the Korsmeyer-Peppas equation and the Hixson-Crowell model. A correlation coefficient (R²) > 0.99 was obtained by Korsmeyer-Peppas equation.

Keywords: shellac, pectin, coating, fluidized bed, release, colon delivery system, kinetic, SEM, methylene blue

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Authors: Md. Shadab, Mariyam N. Nashid, Venkata Srikanth Meka, Thiagarajan Madheswaran

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Naringenin (NAR), is a naturally occurring plant flavonoid, found predominantly in citrus fruits, that possesses a wide range of pharmacological properties including anti-oxidant, anti-inflammatory behaviour, cholesterol-lowering and anticarcinogenic activities. However, despite the therapeutic potential of naringenin shown in a number of animal models, its clinical development has been hindered due to its low aqueous solubility, slow dissolution rate and inefficient transport across biological membranes resulting in low bioavailability. Naringenin nanosuspension were produced using stabilizers Tween® 80 by high pressure homogenization techniques. The nanosuspensions were characterized with regard to size (photon correlation spectroscopy (PCS), size distribution, charge (zeta potential measurements), morphology, short term physical stability, dissolution profile and antioxidant potential. A nanocrystal PCS size of about 500 nm was obtained after 20 homogenization cycles at 1500 bar. The short-term stability was assessed by storage of the nanosuspensions at 4 ◦C, room temperature and 40 ◦C. Result showed that naringenin nanosuspension was physically unstable due to large fluctuations in the particle size and zeta potential after 30 days. Naringenin nanosuspension demonstrated higher drug dissolution (97.90%) compared to naringenin powder (62.76%) after 120 minutes of testing. Naringenin nanosuspension showed increased antioxidant activity compared to naringenin powder with a percentage DPPH radical scavenging activity of 49.17% and 31.45% respectively at the lowest DPPH concentration.

Keywords: bioavailability, naringenin, nanosuspension, oral delivery

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Authors: Lin Zhang

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The fear of leprosy has been longstanding throughout the human history. In an era where isolation is practiced as a means of epidemic prevention, the leprosy rehabilitation group has itself become an isolated community with an entrenched metaphor. In the process of new mediatization of the leprosy isolation community, what are the relations among media literacy, the leprosy internalized stigma and social support? To address the question, the “portrait” of leprosy rehabilitation group is re-delineated through two field studies in the “post-leprosy age” in 2012 and 2020, respectively. Taking an isolation community on Si’an Leprosy Island in Dongguan City, Guangdong Province, China as the study object, it is found that new media promotes the dissolution of segregation effect of the leprosy isolation community and the cultivation of opinion leaders by breaking spatial, psychological and social segregation and by building a community of village affairs and public space in the following way: the cured patients with high new media literacy, especially those who use WeChat and other applications and largely rely on new media for information, have a low level of leprosy internalized stigma and a high level of social support, and they are often the opinion leaders inside their community; on the contrary, the cured patients with low new media literacy, a high level of leprosy internalized stigma and a low level of social support are often the followers inside their community. Such effects of dissolution and construction are reflected not only in the vertical differentiation of the same individual at different times, but also in the horizontal differentiation between different individuals at the same time.

Keywords: segregation, the leprosy rehabilitation group, new mediatization, digital empowerment, opinion leaders

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Authors: Sami Meddeb, M. L Giorgi, J. L. Courouau

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This work presents the progress of studies aiming to guarantee the lifetime of 316L(N) steel in a sodium-cooled fast reactor by determining the elementary corrosion mechanism, which is akin to an accelerated dissolution by dissolved oxygen. The mechanism involving iron, the main element of steel, is particularly studied in detail, from the viewpoint of the data available in the literature, the modeling of the various mechanisms hypothesized. Experiments performed in the CORRONa facility at controlled temperature and dissolved oxygen content are used to test both literature data and hypotheses. Current tests, performed at various temperatures and oxygen content, focus on specifying the chemical reaction at play, determining its free enthalpy, as well as kinetics rate constants. Specific test configuration allows measuring the reaction kinetics and the chemical equilibrium state in the same test. In the current state of progress of these tests, the dissolution of iron accelerated by dissolved oxygen appears as directly related to a chemical complexation reaction of mixed iron-sodium oxide (Na-Fe-O), a compound that is soluble in the liquid sodium solution. Results obtained demonstrate the presence in the solution of this corrosion product, whose kinetics is the limiting step under the conditions of the test. This compound, the object of hypotheses dating back more than 50 years, is predominant in solution compared to atomic iron, presumably even for the low oxygen concentration, and cannot be neglected for the long-term corrosion modeling of any heat transfer system.

Keywords: corrosion, sodium fast reactors, iron, oxygen

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Authors: Veronika Lesáková, Silvia Slezáková, František Štěpánek

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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

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Authors: Nitin Jadhav, Pradeep R. Vavia

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Poor water soluble drugs are difficult to promote for oral drug delivery as they demonstrate poor and variable bioavailability because of its poor solubility and dissolution in GIT fluid. Nowadays lipid based formulations especially self microemulsifying drug delivery system (SMEDDS) is found as the most effective technique. With all the impressive advantages, the need of high amount of surfactant (50% - 80%) is the major drawback of SMEDDS. High concentration of synthetic surfactant is known for irritation in GIT and also interference with the function of intestinal transporters causes changes in drug absorption. Surfactant may also reduce drug activity and subsequently bioavailability due to the enhanced entrapment of drug in micelles. In chronic treatment these issues are very conspicuous due to the long exposure. In addition the liquid self microemulsifying system also suffers from stability issues. Recently one novel approach of solid stabilized micro and nano emulsion (Pickering emulsion) has very admirable properties such as high stability, absence or very less concentration of surfactant and easily converts into the dry form. So here we are exploring pickering dry emulsion system for dissolution enhancement of anti-lipemic, extremely poorly water soluble drug (Fenofibrate). Oil moiety for emulsion preparation was selected mainly on the basis of higher solubility of drug. Captex 300 was showed higher solubility for fenofibrate, hence selected as oil for emulsion. With Silica (solid stabilizer); Span 20 was selected to improve the wetting property of it. Emulsion formed by Silica and Span20 as stabilizer at the ratio 2.5:1 (silica: span 20) was found very stable at the particle size 410 nm. The prepared emulsion was further preceded for spray drying and formed microcapsule evaluated for in-vitro dissolution study, in-vivo pharmacodynamic study and characterized for DSC, XRD, FTIR, SEM, optical microscopy etc. The in vitro study exhibits significant dissolution enhancement of formulation (85 % in 45 minutes) as compared to plain drug (14 % in 45 minutes). In-vivo study (Triton based hyperlipidaemia model) exhibits significant reduction in triglyceride and cholesterol with formulation as compared to plain drug indicating increasing in fenofibrate bioavailability. DSC and XRD study exhibit loss of crystallinity of drug in microcapsule form. FTIR study exhibit chemical stability of fenofibrate. SEM and optical microscopy study exhibit spherical structure of globule coated with solid particles.

Keywords: captex 300, fenofibrate, pickering dry emulsion, silica, span20, stability, surfactant

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Authors: Nikhil John Kollannur, Dali Naidu Arnepalli

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Most of the surface related phenomena in the case of fine-grained soil are attributed to their unique surface charge properties and specific surface area. The temporal variations in soil behavior, to some extent, can be credited to the changes in these properties. Among the multitude of factors that affect the charge and surface area of clay minerals, the inherent system chemistry occupies the cardinal position. The impact is more profound when the chemistry change is manifested in terms of the system pH. pH plays a significant role by modifying the edge charges of clay minerals and facilitating mineral dissolution. Hence there is a need to address the variations in physical and charge properties of fine-grained soils treated over a range of acidic as well as alkaline conditions. In the present study, three soils (two soils commercially procured and one natural soil) exhibiting distinct mineralogical compositions are subjected to different pH environment over a range of 2 to 13. The soil-solutions prepared at a definite liquid to solid ratio are adjusted to the required pH value by adding measured quantities of 0.1M HCl/0.1M NaOH. The studies are conducted over a range of interaction time, varying from 1 to 96 hours. The treated soils are then analyzed for their physical properties in terms of specific surface area and particle size characteristics. Further, modifications in surface morphology are evaluated from scanning electron microscope (SEM) imaging. Changes in the surface charge properties are assessed in terms of zeta potential measurements. Studies show significant variations in total surface area, probably because of the dissolution of clay minerals. This observation is further substantiated by the morphological analysis with SEM imaging. The zeta potential measurements on soils indicate noticeable variation upon pH treatment, which is partially ascribed to the modifications in the pH-dependant edge charges and partially due to the clay mineral dissolution. The results provide valuable insight into the role of pH in a clay-electrolyte system upon surface related phenomena such as species adsorption, fabric modification etc.

Keywords: acid and alkali treatment, mineral dissolution , specific surface area, zeta potential

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Authors: Mohammad Hossein Karimi Darvanjooghi, Sara Magdouli, Satinder Kaur Brar

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It has been reported that the microorganism’s attachment to the surfaces of ore samples is a key factor that influences the biooxidation in pretreatment for recovery of gold in sulfide-bearing ores. In this research, the implementation of D-(+)-Sucrose on the biooxidation of ore samples were studied in a semi-pilot experiment. The experiments were carried out in five separate jacketed columns (1 m height and 6 cm diameter) at a constant temperature of 37.5 ̊C and saturated humidity. The airflow rate and recycling solution flow rate were studied in the research and the optimum operating condition were reported. The ore sample (0.49 ppm gold grade) was obtained from the Hammond Reef mine site containing 15 wt.% of pyrite which included 98% of gold according to the results of micrograph images. The experiments were continued up to 100 days while air flow rates were chosen to be 0.5, 1, 1.5, 2, and 3 lit/min and the recycling solution (Containing 9K media and 0.4 wt.% D-(+)-Sucrose) flow rates were kept 5, 8, 15 ml/hr. The results indicated that the addition of D-(+)-Sucrose increased the bacterial activity due to the overproduction of extracellular polymeric substance (EPS) up to 95% and for the condition that the recycling solution and air flow rate were chosen to be 8 ml/hr and 2 lit/min, respectively, the maximum pyrite dissolution of 76% was obtained after 60 days. The results indicated that for the air flow rates of 0.5, 1, 1.5, 2, and 3 lit/min the ratio of daily pyrite dissolution per daily solution lost were found to be 0.025, 0.033, 0.031, 0.043, and 0.009 %-pyrite dissolution/ml-lost. The implementation of this microorganisms and the addition of D-(+)-Sucrose will enhance the efficiency of gold recovery through faster biooxidation process and leads to decrease in the time and energy of operation toward desired target; however, still other parameters including particle size distribution, agglomeration, aeration design, chemistry of recycling solution need to be controlled and monitored for reaching the optimum condition.

Keywords: column tests, biooxidation, gold recovery, Ferroplasma acidophilum, optimization

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Authors: Farzad Khajavi, Farzaneh Jalilfar, Faranak Jafari, Leila Shokrani

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Formulation of gliclazide in the form of extended-release tablet in 30 and 60 mg dosage forms was performed using hypromellose (HPMC K4M) as a retarding agent. Drug-release profiles were investigated in comparison with references Diamicron MR 30 and 60 mg tablets. The effect of size of powder particles, the amount of hypromellose in formulation, hardness of tablets, and also the effect of halving the tablets were investigated on drug release profile. A mathematical model which describes hypromellose behavior in initial times of drug release was proposed for the estimation of hypromellose content in modified-release gliclazide 60 mg tablet. This model is based on erosion of hypromellose in dissolution media. The model is applicable to describe release profiles of insoluble drugs. Therefore, by using dissolved amount of drug in initial times of dissolution and the model, the amount of hypromellose in formulation can be predictable. The model was used to predict the HPMC K4M content in modified-release gliclazide 30 mg and extended-release quetiapine 200 mg tablets.

Keywords: Gliclazide, hypromellose, drug release, modified-release tablet, mathematical model

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Authors: Grmay Kassa Brhane, Hailemariam Siyum Mekonen

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This study was designed to identify the hydrogeochemical and anthropogenic processes controlling the evaluation of groundwater chemistry in the Ellala catchment which covers about 296.5 km2 areal extent. The chemical analysis revealed that the major ions in the groundwater are Ca2+, Mg2+, Na+, and K+ (cations) and HCO3-, PO43-, Cl-, NO3-, and SO42-(anions). Most of the groundwater samples (68.42%) revealed that the groundwater in the catchment is non-alkaline. In addition to the contribution of aquifer material, the solid materials and liquid wastes discharged from different sources can be the main sources of pH and EC in the groundwater. It is observed that the EC of the groundwater is fairly correlated with the DTS. This indicates that high mineralized water is more conductor than water with low concentration. The degree of salinity of the groundwater increases along the groundwater flow path from East to West; then, areas surrounding Mekelle City are highly saline due to the liquid and solid wastes discharged from the city and the industries. The groundwater facies in the catchment are predominated with calcium, magnesium, and bicarbonate which are labeled as Ca-Mg-HCO3 and Mg-Ca-HCO3. The main geochemical process controlling the evolution of the groundwater chemistry in the catchment is rock-water interaction, particularly carbonate dissolution. Due to the clay layer in the aquifer, the reverse is ion exchange. Non-significant silicate weathering and halite dissolution also contribute to the evolution of groundwater chemistry in the catchment. The groundwater in the catchment is dominated by the meteoritic origin although it needs further groundwater chemistry study with isotope dating analysis. The groundwater is under-saturated with calcite, dolomite, and aragonite minerals; hence, the more these minerals encounter the groundwater, the more the minerals dissolve. The main source of calcium and magnesium in groundwater is the dissolution of carbonate minerals (calcite and dolomite) since carbonate rocks are the dominant aquifer materials in the catchment. In addition to this, the weathering of dolerite rock is a possible source of magnesium ions. The relatively higher concentration of sodium over chloride indicates that the source of sodium-ion is reverse ion exchange and/or weathering of sodium-bearing materials, such as shale and dolerite rather than halite dissolution. High concentration of phosphate, nitrate, and chloride in the groundwater is the main anthropogenic source that needs treatment, quality control, and management in the catchment. From the Base Exchange Index Analysis, it is possible to understand that, in the catchment, the groundwater is dominated by the meteoritic origin, although it needs further groundwater chemistry study with isotope dating analysis.

Keywords: Ellala catchment, factor, chemistry, geochemical, groundwater

Procedia PDF Downloads 44

Authors: Madhav Khadilkar

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Construction of a large standby reservoir was required to provide secure water supply. The new reservoir was required to be constructed at the same location of an abandoned old open pond due to space constraints. Some investigations were carried out earlier to improvise and re-commission the existing pond. But due to a lack of quantified risk of settlement from voids in the underlying limestone, the shallow foundations were not found feasible. Since the reservoir was resting on hard strata for about three-quarter of plan area and one quarter was resting on soil underlying with limestone and considerably low subgrade modulus. Further investigations were carried out to ascertain the locations and extent of voids within the limestone. It was concluded that the risk due to lime dissolution was acceptably low, and the site was found geotechnically feasible. The hazard posed by limestone dissolution was addressed through the integrated structural and geotechnical analysis and design approach. Finite Element Analysis was carried out to quantify the stresses and differential settlement due to various probable loads and soil-structure interaction. Walls behaving as cantilever under operational loads were found undergoing in-plane bending and tensile forces due to soil-structure interaction. Sensitivity analysis for varying soil subgrade modulus was carried out to check the variation in the response of the structure and magnitude of stresses developed. The base slab was additionally checked for the loss of soil contact due to lime pocket formations at random locations. The expansion and contraction joints were planned to receive minimal additional forces due to differential settlement. The reservoir was designed to sustain the actions corresponding to allowable deformation limits per code, and geotechnical measures were proposed to achieve the soil parameters set in structural analysis.

Keywords: differential settlement, limestone dissolution, reservoir, soil structure interaction

Procedia PDF Downloads 129

Authors: Matej Buzgo, Erico Himawan, Ksenija JašIna, Aiva Simaite

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Electrospinning is a versatile and efficient technology for producing nanofibers for biomedical applications. One of the most common polymers used for the preparation of nanofibers for regenerative medicine and drug delivery applications is polycaprolactone (PCL). PCL is a biocompatible and bioabsorbable material that can be used to stimulate the regeneration of various tissues. It is also a common material used for the development of drug delivery systems by blending the polymer with small active molecules. However, for many drug delivery applications, e.g. cancer immunotherapy, PCL biodegradation rate that may exceed 9 months is too long, and faster nanofiber dissolution is needed. In this paper, we investigate the dissolution and small molecule release rates of PCL blends with two hydrophilic polymers: polyethylene oxide (PEO) or polyvinylpyrrolidone (PVP). We show that adding hydrophilic polymer to the PCL reduces the water contact angle, increases the dissolution rate, and strengthens the interactions between the hydrophilic drug and polymer matrix that further sustain its release. Finally using this method, we were also able to increase the nanofiber degradation rate when PCL-PEO and PCL-PVP were used as a shell in the electrospun core-shell nanofibers and spread up the release of active proteins from their core. Electrospinning can be used for the preparation of the core-shell nanofibers, where active ingredients are encapsulated in the core and their release rate is regulated by the shell. However, such fibers are usually prepared by coaxial electrospinning that is an extremely low-throughput technique. An alternative is emulsion electrospinning that could be upscaled using needleless blades. In this work, we investigate the possibility of using emulsion electrospinning for encapsulation and sustained release of the growth factors for the development of the organotypic skin models. The core-shell nanofibers were prepared using the optimized formulation and the release rate of proteins from the fibers was investigated for 2 weeks – typical cell culture conditions.

Keywords: electrospinning, polycaprolactone (PCL), polyethylene oxide (PEO), polyvinylpyrrolidone (PVP)

Procedia PDF Downloads 251

Authors: Adam Fheed

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Carbonate porosity can be deceptive in the aspect of hydrocarbon exploration due to pore geometry variations, which are to some extent controlled by fossils. Therefore, the main aim of this paper was to assess the dependence of pore geometry and reservoir quality on fossils. The Permian Zechstein Limestone (Ca1) carbonates from the Brońsko Reef, located on the Wolsztyn Ridge in West Poland, were examined. Seventy meters of drill cores were described along with well log examination and transmitted-light microscope research. The archival porosity-permeability data was utilized to calibrate the well logs and look for the potential petrophysical trends. Several organism assemblages were recognized in the reef. Its bottom was colonized by the branched bryozoans which were fragmented and dissolved leaving poorly connected molds. Subsequently, numerous bivalves and gastropods appeared and their shells were heavily dissolved to form huge, albeit poorly communicated caverns. Such pores were also typical for local brachiopod occurrences. Although the caverns were widespread, and probably linked to the meteoric dissolution or freshwater flushing, severe anhydrite cementation has destroyed the majority of pores. Close to the top of Ca1, near the center of the reef, the fossil-rich zone comprising fenestrate bryozoans, extremely abundant encrusting foraminifers, bivalves, brachiopods, gastropods and ostracods, was identified. The zone contained extremely frequent dissolution channels formed within former shells of foraminifers, which had previously encrusted the bryozoans. The deposition of Ca1 strata has ultimately terminated with a poorly porous and generally impermeable stromatolitic layer containing scarce fossils. In general, the permeability of the reef rocks studied turned out to be the highest under the presence of foraminifer-related channels. In such cases, it frequently approached 100 mD. The presence of channels and other pores gave the average effective porosity derived from shallow resistivity and helium porosimetry of around 16 and 18 %, respectively. The highest porosity (over 18 %), often co-occurring with relatively low permeability (chiefly below 20 mD) was noted for the bottommost zone of the reef, represented by branched bryozoans. This is probably owing to a large amount of unconnected bryozoan-related molds. It was concluded that fossils played a major role in porosity formation and controlled the pore geometry significantly. While the dissolution of bivalves and brachiopods resulted in cavernous porosity formation, numerous molds were typically related with the alteration of branched bryozoans, gastropods and ostracods. Importantly, the bendy dissolution channels after the encrusting foraminifers appeared to be decisive in improving reservoir quality – specifically when permeability is considered. Acknowledgment: The research was financed by the Polish National Science Centre’s project No. UMO-2016/23/N/ST10/00350.

Keywords: dissolution channels, fossils, Permian, porosity

Procedia PDF Downloads 62

Authors: Leslie Raphael de M. Ferraz, Salvana Priscylla M. Costa, Tarcyla de A. Gomes, Giovanna Christinne R. M. Schver, Cristóvão R. da Silva, Magaly Andreza M. de Lyra, Danilo Augusto F. Fontes, Larissa A. Rolim, Amanda Carla Q. M. Vieira, Miracy M. de Albuquerque, Pedro J. Rolim-Neto

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Efavirenz (EFV) is a drug used as first-line treatment of AIDS. However, it has poor aqueous solubility and wettability, presenting problems in the gastrointestinal tract absorption and bioavailability. One of the most promising strategies to improve the solubility is the use of solid dispersions (SD). Therefore, this study aimed to characterize SD EFZ with the polymers: PVP-K30, PVPVA 64 and SOLUPLUS in order to find an optimal formulation to compose a future pharmaceutical product for AIDS therapy. Initially, Physical Mixtures (PM) and SD with the polymers were obtained containing 10, 20, 50 and 80% of drug (w/w) by the solvent method. The best formulation obtained between the SD was selected by in vitro dissolution test. Finally, the drug-carrier system chosen, in all ratios obtained, were analyzed by the following techniques: Differential Scanning Calorimetry (DSC), polarization microscopy, Scanning Electron Microscopy (SEM) and spectrophotometry of absorption in the region of infrared (IR). From the dissolution profiles of EFV, PM and SD, the values of area Under The Curve (AUC) were calculated. The data showed that the AUC of all PM is greater than the isolated EFV, this result is derived from the hydrophilic properties of the polymers thus favoring a decrease in surface tension between the drug and the dissolution medium. In adittion, this ensures an increasing of wettability of the drug. In parallel, it was found that SD whom had higher AUC values, were those who have the greatest amount of polymer (with only 10% drug). As the amount of drug increases, it was noticed that these results either decrease or are statistically similar. The AUC values of the SD using the three different polymers, followed this decreasing order: SD PVPVA 64-EFV 10% > SD PVP-K30-EFV 10% > SD Soluplus®-EFV 10%. The DSC curves of SD’s did not show the characteristic endothermic event of drug melt process, suggesting that the EFV was converted to its amorphous state. The analysis of polarized light microscopy showed significant birefringence of the PM’s, but this was not observed in films of SD’s, thus suggesting the conversion of the drug from the crystalline to the amorphous state. In electron micrographs of all PM, independently of the percentage of the drug, the crystal structure of EFV was clearly detectable. Moreover, electron micrographs of the SD with the two polymers in different ratios investigated, we observed the presence of particles with irregular size and morphology, also occurring an extensive change in the appearance of the polymer, not being possible to differentiate the two components. IR spectra of PM corresponds to the overlapping of polymer and EFV bands indicating thereby that there is no interaction between them, unlike the spectra of all SD that showed complete disappearance of the band related to the axial deformation of the NH group of EFV. Therefore, this study was able to obtain a suitable formulation to overcome the solubility limitations of the EFV, since SD PVPVA 64-EFZ 10% was chosen as the best system in delay crystallization of the prototype, reaching higher levels of super saturation.

Keywords: characterization, dissolution, Efavirenz, solid dispersions

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Authors: Rajasekhar Reddy Poonuru, Anusha Parnem

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Purpose: To formulate proliposome powder of agomelatine, an antipsychotic drug, and to evaluate physicochemical, in vitro characters and effect of surface charge on ex vivo intestinal permeation. Methods: Film deposition technique was employed to develop proliposomal powders of agomelatin with varying molar ratios of lipid Hydro Soy PC L-α-phosphatidylcholine (HSPC) and cholesterol with fixed sum of drug. With the aim to derive free flowing and stable proliposome powder, fluid retention potential of various carriers was examined. Liposome formation and number of vesicles formed for per mm3 up on hydration, vesicle size, and entrapment efficiency was assessed to deduce an optimized formulation. Sodium cholate added to optimized formulation to induce surface charge on formed vesicles. Solid-state characterization (FTIR, DSC, and XRD) was performed with the intention to assess native crystalline and chemical behavior of drug. The in vitro dissolution test of optimized formulation along with pure drug was evaluated to estimate dissolution efficiency (DE) and relative dissolution rate (RDR). Effective permeability co-efficient (Peff(rat)) in rat and enhancement ratio (ER) of drug from formulation and pure drug dispersion were calculated from ex vivo permeation studies in rat ileum. Results: Proliposomal powder formulated with equimolar ratio of HSPC and cholesterol ensued in higher no. of vesicles (3.95) with 90% drug entrapment up on hydration. Neusilin UFL2 was elected as carrier because of its high fluid retention potential (4.5) and good flow properties. Proliposome powder exhibited augmentation in DE (60.3 ±3.34) and RDR (21.2±01.02) of agomelation over pure drug. Solid state characterization studies demonstrated the transformation of native crystalline form of drug to amorphous and/or molecular state, which was in correlation with results obtained from in vitro dissolution test. The elevated Peff(rat) of 46.5×10-4 cm/sec and ER of 2.65 of drug from charge induced proliposome formulation with respect to pure drug dispersion was assessed from ex vivo intestinal permeation studies executed in ileum of wistar rats. Conclusion: Improved physicochemical characters and ex vivo intestinal permeation of drug from charge induced proliposome powder with Neusilin UFL2 unravels the potentiality of this system in enhancing oral delivery of agomelatin.

Keywords: agomelatin, proliposome, sodium cholate, neusilin

Procedia PDF Downloads 104

Authors: Mojtaba Heydarizad

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Khorasan Razavi is the second most important province in north-east of Iran, which faces a water shortage crisis due to recent droughts and huge water consummation. Kardeh and Torogh dam reservoirs in this province provide a notable part of Mashhad metropolitan (with more than 4.5 million inhabitants) potable water needs. Hydrochemical analyses on these dam reservoirs samples demonstrate that MgHCO₃ in Kardeh and CaHCO₃ and to lower extent MgHCO₃ water types in Torogh dam reservoir are dominant. On the other hand, Gibbs binary diagram demonstrates that rock weathering is the main factor controlling water quality in dam reservoirs. Plotting dam reservoir samples on Mg²⁺/Na⁺ and HCO₃^-/Na⁺ vs. Ca²⁺/ Na⁺ diagrams demonstrate evaporative and carbonate mineral dissolution is the dominant rock weathering ion sources in these dam reservoirs. Cluster Analyses (CA) also demonstrate intense role of rock weathering mainly (carbonate and evaporative minerals dissolution) in water quality of these dam reservoirs. Studying water quality by the U.S. National Sanitation Foundation (NSF) WQI index NSF-WQI, Oregon Water Quality Index (OWQI) and Canadian Water Quality Index DWQI index show moderate and good quality.

Keywords: hydrochemistry, water quality classification, water quality indexes, Torogh and Kardeh dam reservoir

Procedia PDF Downloads 227

Authors: Hend Ben Tkhayat , Khaled Al Zahabi, Husam Younes

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Introduction: Vildagliptin (VG), a dipeptidyl peptidase-4 inhibitor (DPP-4), was proven to be an active agent for the treatment of type 2 diabetes. VG works by enhancing and prolonging the activity of incretins which improves insulin secretion and decreases glucagon release, therefore lowering blood glucose level. It is usually used with various classes, such as insulin sensitizers or metformin. VG is currently only marketed as an immediate-release tablet that is administered twice daily. In this project, we aim to formulate an extended-release with a zero-order profile tableted lipid microparticles of VG that could be administered once daily ensuring the patient’s convenience. Method: The spray-congealing technique was used to prepare VG microparticles. Compritol® was heated at 10 oC above its melting point and VG was dispersed in the molten carrier using a homogenizer (IKA T25- USA) set at 13000 rpm. VG dispersed in the molten Compritol® was added dropwise to the molten Gelucire® 50/13 and PEG® (400, 6000, and 35000) in different ratios under manual stirring. The molten mixture was homogenized and Carbomer® amount was added. The melt was pumped through the two-fluid nozzle of the Buchi® Spray-Congealer (Buchi B-290, Switzerland) using a Pump drive (Master flex, USA) connected to a silicone tubing wrapped with silicone heating tape heated at the same temperature of the pumped mix. The physicochemical properties of the produced VG-loaded microparticles were characterized using Mastersizer, Scanning Electron Microscope (SEM), Differential Scanning Calorimeter (DSC) and X‐Ray Diffractometer (XRD). VG microparticles were then pressed into tablets using a single punch tablet machine (YDP-12, Minhua pharmaceutical Co. China) and in vitro dissolution study was investigated using Agilent Dissolution Tester (Agilent, USA). The dissolution test was carried out at 37±0.5 °C for 24 hours in three different dissolution media and time phases. The quantitative analysis of VG in samples was realized using a validated High-Pressure Liquid Chromatography (HPLC-UV) method. Results: The microparticles were spherical in shape with narrow distribution and smooth surface. DSC and XRD analyses confirmed the crystallinity of VG that was lost after being incorporated into the amorphous polymers. The total yields of the different formulas were between 70% and 80%. The VG content in the microparticles was found to be between 99% and 106%. The in vitro dissolution study showed that VG was released from the tableted particles in a controlled fashion. The adjustment of the hydrophilic/hydrophobic ratio of excipients, their concentration and the molecular weight of the used carriers resulted in tablets with zero-order kinetics. The Gelucire 50/13®, a hydrophilic polymer was characterized by a time-dependent profile with an important burst effect that was decreased by adding Compritol® as a lipophilic carrier to retard the release of VG which is highly soluble in water. PEG® (400,6000 and 35 000) were used for their gelling effect that led to a constant rate delivery and achieving a zero-order profile. Conclusion: Tableted spray-congealed lipid microparticles for extended-release of VG were successfully prepared and a zero-order profile was achieved.

Keywords: vildagliptin, spray congealing, microparticles, controlled release

Procedia PDF Downloads 100

Authors: H. R. Kelidari, M. Saeedi, J. Akbari, K. Morteza-Semnani, H. Valizadeh

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Spironolactoe (SP) a synthetic steroid diuretic is a poorly water-soluble drug with a low and variable oral bioavailability. Regarding to the good solubility of SP in lipid materials, SP loaded Solid lipid nanoparticles (SP-SLNs) and nanostructured lipid carrier (SP-SLNs) were thus prepared in this work for accelerating dissolution of this drug. The SP loaded NLC with stearic acid (SA) as solid lipid and different Oleic Acid (OA) as liquid lipid content and SLN without OA were prepared by probe ultrasonication method. With increasing the percentage of OA from 0 to 30 wt% in SLN/NLC, the average size and zeta potential of nanoparticles felled down and entrapment efficiency (EE %) rose dramatically. The obtained micrograph particles showed pronounced spherical shape. Differential Scanning Calorimeter (DSC) measurements indicated that the presence of OA reduced the melting temperature and melting enthalpy of solid lipid in NLC structure. The results reflected good long-term stability of the nanoparticles and the measurements show that the particle size remains lower in NLC compare to SLN formulations, 6 months after production. Dissolution of SP-SLN and SP-NLC was about 5.1 and 7.2 times faster than raw drugs in 120 min respectively. These results indicated that the SP loaded NLC containing 70:30 solid lipid to liquid lipid ratio is a suitable carrier of SP with improved drug EE and steady drug release properties.

Keywords: drug release, lipid nanoparticles, spironolactone, stability

Procedia PDF Downloads 304

Authors: Sarah Nasr, Maha M. A. Nasra, Ossama Y. Abdallah

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The present work aimed to prepare Silymarin loaded MCM-41 type mesoporous silica nanoparticles (MSNs) and to assess the system’s solubility enhancement ability on the pharmacodynamic performance of Silymarin as a hepatoprotective agent. MSNs prepared by soft-templating technique, were loaded with Silymarin, characterized for particle size, zeta potential, surface properties, DSC and XRPD. DSC and specific surface area data confirmed deposition of Silymarin in an amorphous state in MSNs’ pores. In-vitro drug dissolution testing displayed enhanced dissolution rate of Silymarin upon loading on MSNs. High dose Acetaminophen was then used to inflict hepatic injury upon albino male Wistar rats simultaneously receiving either free Silymarin, Silymarin loaded MSNs or blank MSNs. Plasma AST, ALT, albumin and total protein and liver homogenate content of TBARs or LDH as measures of antioxidant drug action were assessed for all animal groups. Results showed a significant superiority of Silymarin loaded MSNs to free drug in almost all parameters. Meanwhile prolonged administration of blank MSNs had no evident toxicity on rats.

Keywords: mesoporous silica nanoparticles, safety, solubility enhancement, silymarin

Procedia PDF Downloads 306

Authors: Arti Bagada, Kantilal Vadalia, Mihir Raval

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Cilnidipine is practically insoluble in water which results in its insufficient oral bioavailability. The purpose of the present investigation was to formulate cilnidipine nanoparticles by nanoprecipitation method to increase the aqueous solubility and dissolution rate and hence bioavailability by utilizing various experimental statistical design modules. Experimental design were used to investigate specific effects of independent variables during preparation cilnidipine nanoparticles and corresponding responses in optimizing the formulation. Plackett Burman design for independent variables was successfully employed for optimization of nanoparticles of cilnidipine. The influence of independent variables studied were drug concentration, solvent to antisolvent ratio, polymer concentration, stabilizer concentration and stirring speed. The dependent variables namely average particle size, polydispersity index, zeta potential value and saturation solubility of the formulated nanoparticles of cilnidipine. The experiments were carried out according to 13 runs involving 5 independent variables (higher and lower levels) employing Plackett-Burman design. The cilnidipine nanoparticles were characterized by average particle size, polydispersity index value, zeta potential value and saturation solubility and it results were 149 nm, 0.314, 43.24 and 0.0379 mg/ml, respectively. The experimental results were good correlated with predicted data analysed by Plackett-Burman statistical method.

Keywords: dissolution enhancement, nanoparticles, Plackett-Burman design, nanoprecipitation

Procedia PDF Downloads 138