Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 159

Search results for: permeation enhancer

159 Conjugated Chitosan-Carboxymethyl-5-Fluorouracil Nanoparticles for Skin Delivery

Authors: Mazita Mohd Diah, Anton V. Dolzhenko, Tin Wui Wong

Abstract:

Nanoparticles, being small with a large specific surface area, increase solubility, enhance bioavailability, improve controlled release and enable precision targeting of the entrapped compounds. In this study, chitosan as polymeric permeation enhancer was conjugated to a polar pro-drug, carboxymethyl-5-fluorouracil (CMFU) to increase the skin drug permeation. Chitosan-CMFU conjugate was synthesized using chemical conjugation process through succinate linker. It was then transformed into nanoparticles via spray drying method. The conjugation was elucidated using Fourier Transform Infrared and Proton Nuclear Magnetic Resonance techniques. The nanoparticle size, size distribution, zeta potential, drug content, skin permeation and retention profiles were characterized. The conjugation was denoted using 1H NMR by new peaks at signal δ = 4.184 ppm (singlet, 2H for CH2) and 7.676-7.688 ppm (doublet, 1H for C6) attributed to CMFU in chitosan-CMFU NMR spectrum. The nanoparticles had profiles of particle size: 93.97 ±35.11 nm, polydispersity index: 0.40 ± 0.14, zeta potential: +18.25 ±2.95 mV and drug content: 6.20 ± 1.98 % w/w. Almost 80 % w/w CMFU in the form of nanoparticles permeated through the skin in 24 hours and close to 50 % w/w permeation occurred in first 1-2 hours. Without conjugation to chitosan and nanoparticulation, less than 40 % w/w CMFU permeated through the skin in 24 hours. The skin drug retention likewise was higher with chitosan-CMFU nanoparticles (15.34 ± 5.82 % w/w) than CMFU (2.24 ± 0.57 % w/w). CMFU, through conjugation with chitosan permeation enhancer and processed in nanogeometry, had its skin permeation and retention degree promoted.

Keywords: carboxymethyl-5-fluorouracil, chitosan, conjugate, skin permeation, skin retention

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158 Microstructure of Hydrogen Permeation Barrier Coatings

Authors: Motonori Tamura

Abstract:

Ceramics coatings consisting of fine crystal grains, with diameters of about 100 nm or less, provided superior hydrogen-permeation barriers. Applying TiN, TiC or Al₂O₃ coatings on a stainless steel substrate reduced the hydrogen permeation by a factor of about 100 to 5,000 compared with uncoated substrates. Effect of the microstructure of coatings on hydrogen-permeation behavior is studied. The test specimens coated with coatings, with columnar crystals grown vertically on the substrate, tended to exhibit higher hydrogen permeability. The grain boundaries of the coatings became trap sites for hydrogen, and microcrystalline structures with many grain boundaries are expected to provide effective hydrogen-barrier performance.

Keywords: hydrogen permeation, tin coating, microstructure, crystal grain, stainless steel

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157 Transdermal Therapeutic System of Lercanıdipine Hydrochloride: Fabrication and in Vivo Evaluation

Authors: Jiji Jose, R. Narayanacharyulu, Molly Mathew, Jisha Prems

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Introduction: Lercanidipine hydrochloride (LD), an effective calcium channel blocker, widely used for the treatment of chronic stable angina and hypertension seems to be potential transdermal therapeutic system candidate, mainly due to its low oral bio availability, short half life and high first-pass metabolism. Objective: To develop transdermal therapeutic systems for LD and to evaluate its in vivo performance in rabbits. Methodology: Transdermal patches of LD were formulated using the polymer blend of eudragit RL100 (ERL) and polyvinyl pyrolidone (PVP) by casting method Propylene glycol (PG) and tween 80 were used as plasticizer and permeation enhancer respectively. The pharmaco kinetic parameters of LD after the administration of transdermal patches was compared with that of oral administration. The study was carried out in a two way crossover design in male New Zealand albino rabbits. Results: The formulation with ERL: PVP ratio 1:4 with 15% w/w PG as plasticizer and 4% w/w tween 80 as permeation enhancer showed the best drug release results. The pharmacokinetic parameters such as Cmax, tmax, mean residence time (MRT) and area under the curve (AUC 0-∞) were significantly different following transdermal administration compared to oral administration. The terminal half life of transdermally administered LD was found to similar that of oral administration. A sustained drug release over a period of 24 hrs was observed after transdermal administration. Conclusion: The fabricated transdermal delivery system have the potential to provide controlled and extended drug release, better bio availability and thus, this may improve the patient compliance.

Keywords: transdermal therapeutic system, lercanidipine hydrochloride, eudragit, skinpermeation

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156 Iontophoretic Drug Transport: An Non-Invasive Transdermal Approach

Authors: Ashish Jain, Shivam Tayal

Abstract:

There has been great interest in the field of Iontophoresis since few years due to its great applications in the field of controlled transdermal drug delivery system. It is an technique which is used to enhance the transdermal permeation of ionized high molecular weight molecules across the skin membrane especially Peptides & Proteins by the application of direct current of 1-4 mA for 20-40 minutes whereas chemical must be placed on electrodes with same charge. Iontophoresis enhanced the delivery of drug into the skin via pores like hair follicles, sweat gland ducts etc. rather than through stratum corneum. It has wide applications in the field of experimental, Therapeutic, Diagnostic, Dentistry etc. Medical science is using it to treat Hyperhidrosis (Excessive sweating) in hands and feet and to treat other ailments like hypertension, Migraine etc. Nowadays commercial transdermal iontophoretic patches are available in the market to treat different ailments. Researchers are keen to research in this field due to its vast applications and advantages.

Keywords: iontophoresis, novel drug delivery, transdermal, permeation enhancer

Procedia PDF Downloads 148
155 Study on Hydrogen Isotope Permeability of High Entropy Alloy Coating

Authors: Long Wang, Yongjin Feng, Xiaofang Luo

Abstract:

Tritium permeation through structural materials is a significant issue for fusion demonstration (DEMO) reactor blankets in terms of fuel cycle efficiency and radiological safety. Reduced activation ferritic (RAFM) steel CLF-1 is a prime candidate for the China’s CFETR blanket structural material, facing high permeability of hydrogen isotopes at reactor operational temperature. To confine tritium as much as possible in the reactor, surface modification of the steels including fabrication of tritium permeation barrier (TPB) attracts much attention. As a new alloy system, high entropy alloy (HEA) contains at least five principal elements, each of which ranges from 5 at% to 35 at%. This high mixing effect entitles HEA extraordinary comprehensive performance. So it is attractive to lead HEA into surface alloying for protective use. At present, studies on the hydrogen isotope permeability of HEA coatings is still insufficient and corresponding mechanism isn’t clear. In our study, we prepared three kinds of HEA coatings, including AlCrTaTiZr, (AlCrTaTiZr)N and (AlCrTaTiZr)O. After comprehensive characterization of SEM, XPS, AFM, XRD and TEM, the structure and composition of the HEA coatings were obtained. Deuterium permeation tests were conducted to evaluate the hydrogen isotope permeability of AlCrTaTiZr, (AlCrTaTiZr)N and (AlCrTaTiZr)O HEA coatings. Results proved that the (AlCrTaTiZr)N and (AlCrTaTiZr)O HEA coatings had better hydrogen isotope permeation resistance. Through analyzing and characterizing the hydrogen isotope permeation results of the corroded samples, an internal link between hydrogen isotope permeation behavior and structure of HEA coatings was established. The results provide valuable reference in engineering design of structural and TPB materials for future fusion device.

Keywords: high entropy alloy, hydrogen isotope permeability, tritium permeation barrier, fusion demonstration reactor

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154 Hydrogen Permeability of BSCY Proton-Conducting Perovskite Membrane

Authors: M. Heidari, A. Safekordi, A. Zamaniyan, E. Ganji Babakhani, M. Amanipour

Abstract:

Perovskite-type membrane Ba0.5Sr0.5Ce0.9Y0.1O3-δ (BSCY) was successfully synthesized by liquid citrate method. The hydrogen permeation and stability of BSCY perovskite-type membranes were studied at high temperatures. The phase structure of the powder was characterized by X-ray diffraction (XRD). Scanning electron microscopy (SEM) was used to characterize microstructures of the membrane sintered under various conditions. SEM results showed that increasing in sintering temperature, formed dense membrane with clear grains. XRD results for BSCY membrane that sintered in 1150 °C indicated single phase perovskite structure with orthorhombic configuration, and SEM results showed dense structure with clear grain size which is suitable for permeation tests. Partial substitution of Sr with Ba in SCY structure improved the hydrogen permeation flux through the membrane due to the larger ionic radius of Ba2+. BSCY membrane shows high hydrogen permeation flux of 1.6 ml/min.cm2 at 900 °C and partial pressure of 0.6.

Keywords: hydrogen separation, perovskite, proton conducting membrane.

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153 Novel Emulgel of Piroxicam for Topical Application with Mentha and Clove Oil

Authors: S. V. Patil, P. S. Dounde, S. S. Patil

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Emulgels have emerged as one of the most interesting topical delivery system as it has dual release control system that is gel and emulsion. The major objective behind this formulation is delivery of hydrophobic drugs to systemic circulation via skin. In fact presence of a gelling agent in water phase converts a classical emulsion in to emulgel. The emulgel for dermatological use has several favorable properties such as being thixotropic, greaseless, easily spreadable, easily removable, emollient, non-staining, water-soluble, longer shelf life, bio-friendly, transparent and pleasing appearance. Various penetration enhancers can potentiate the effect. So this can be used as better topical drug delivery systems over present conventional systems available in market. Piroxicam is a non-steroidal anti-inflammatory drug that has major problems when administered orally; it is an insoluble drug and has irritant effect on gastro intestinal tract lead to ulceration and bleeding. The aim of this study was to overcoming these problems through preparation of topical emulgel of this drug. Emulgel of Piroxicam was prepared using Carbopol 940 along with mentha oil and clove oil as permeation enhancer. The prepared emulgel were evaluated for their physical appearance, pH determination, viscosity, spreadability, in vitro drug release, ex vivo permeation studies. All the prepared formulations showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity and pH value. The emulgel was found to be stable with respect to physical appearance, pH, rheological properties and drug content at all temperature and conditions for three month.

Keywords: emulgel, piroxicam, menthe oil, clove oil

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152 Effect of Hydrogen Content and Structure in Diamond-Like Carbon Coatings on Hydrogen Permeation Properties

Authors: Motonori Tamura

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The hydrogen barrier properties of the coatings of diamond-like carbon (DLC) were evaluated. Using plasma chemical vapor deposition and sputtering, DLC coatings were deposited on Type 316L stainless steels. The hydrogen permeation rate was reduced to 1/1000 or lower by the DLC coatings. The DLC coatings with high hydrogen content had high hydrogen barrier function. For hydrogen diffusion in coatings, the movement of atoms through hydrogen trap sites such as pores in coatings, and crystal defects such as dislocations, is important. The DLC coatings are amorphous, and there are both sp3 and sp2 bonds, and excess hydrogen could be found in the interstitial space and the hydrogen trap sites. In the DLC coatings with high hydrogen content, these hydrogen trap sites are likely already filled with hydrogen atoms, and the movement of new hydrogen atoms could be limited.

Keywords: hydrogen permeation, stainless steels, diamond-like carbon, hydrogen trap sites

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151 Formulation of Film Forming Transdermal Spray Containing Fluconazole Using Full Factorial Design

Authors: Paresh M. Patel, Amit A. Patel, R. H. Parikh

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The present investigation was undertaken to fabricate modified transport fluconazole that belongs to BCS class II and have a poor applicability on topical infection. So to improve topical application, transdermal spray could play a vital role by using ethyl cellulose and Eudragit® S100 as film-forming polymers. Concentration of Eudragit® S100, ethyl cellulose and permeation enhancer (camphor and menthol) were selected as independent variables, whereas drying time, viscosity and in-vitro drug release were selected as dependent variables in factorial design. The viscosity, drying time and in-vitro drug release of the optimize batch B15 was 40.1 cps, 47 sec. and 90.79% respectively. The film of optimized batch was flexible and dermal-adhesive.

Keywords: Eudragit, ethyl cellulose, fluconazole, transdermal spray

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150 Arbutin-loaded Butylglyceryl Dextran Nanoparticles for Topical Delivery

Authors: Mohammad F. Bostanudin, Tan S. Fei, Azwan M. Lazim

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Toward the development of colloidal systems that are able to enhance permeation across the skin, a material combining the non-toxic and non-immunogenic of dextran with alkylglycerols permeation enhancing property has been designed. To this purpose, a range of butylglyceryl dextrans (DEX-OX4) were synthesized via functionalization with n-butylglycidyl ether and the successful functionalization was confirmed by NMR and FT-IR spectroscopies, along with GPC with a degree of modification in the range 6.3–35.7 %. A reduced viscosity and an increased molecular weight of DEX-OX4 were also recorded when compared to that of the native dextran. DEX-OX4 was further formulated into nanocarriers and loaded with α-arbutin prior to be investigated for their particle size, morphology, stability, loading ability, and release profiles. The resulting nanoparticles were found to be close-to-spherical and relatively stable at pH 5 and 7, with size 180–220 nm (ζ-potential -22 to -25 mV), and a loading degree of 11.7 %. Lack of toxicity at application-relevant concentrations and increased permeation across skin biological membrane model were demonstrated by nanoparticles in-vitro results against immortalized skin human keratinocytes cells (HaCaT).

Keywords: butylglycerols, dextran, nanoparticles, transdermal

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149 Iontophoretic Drug Transport of Some Anti-Diabetic Agents

Authors: Ashish Jain, Satish Nayak

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Transdermal iontophoretic drug delivery system is viable drug delivery platform technology and has a strong market worldwide. Transdermal drug delivery system is particularly desirable for therapeutic agents that need prolonged administration at controlled plasma level. This makes appropriateness to antihypertensive and anti-diabetic agents for their transdermal development. Controlled zero order absorption, easily termination of drug delivery and easy to administration also support for popularity of transdermal delivery. In this current research iontophoretic delivery of various anti diabetic agents like glipizide, glibenclamide and glimepiride were carried out. The experiments were carried out at different drug concentrations and different current densities using cathodal iontophoresis. Diffusion cell for iontophoretic permeation study was modified according to Glikfield Design. Pig skin was used for in vitro permeation study and for the in-vivo study New Zealand rabbits were used. At all concentration level iontophoresis showed enhanced permeation rate compared to passive controls. Iontophoretic transports of selected drugs were found to be increased with the current densities. Results showed that target permeation rate for selected drugs could be achieved with the aid of iontophoresis by increasing the area in an appreciable range.

Keywords: transdermal, iontophoresis, pig skin, rabbits, glipizide, glibeclamide

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148 Influence of La0.1Sr0.9Co1-xFexO3-δ Catalysts on Oxygen Permeation Using Mixed Conductor

Authors: Y. Muto, S. Araki, H. Yamamoto

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The separation of oxygen is one key technology to improve the efficiency and to reduce the cost for the processed of the partial oxidation of the methane and the condensation of the carbon dioxide. Particularly, carbon dioxide at high concentration would be obtained by the combustion using pure oxygen separated from air. However, the oxygen separation process occupied the large part of energy consumption. Therefore, it is considered that the membrane technologies enable to separation at lower cost and lower energy consumption than conventional methods. In this study, it is examined that the separation of oxygen using membranes of mixed conductors. Oxygen permeation through the membrane is occurred by the following three processes. At first, the oxygen molecules dissociate into oxygen ion at feed side of the membrane, subsequently, oxygen ions diffuse in the membrane. Finally, oxygen ions recombine to form the oxygen molecule. Therefore, it is expected that the membrane of thickness and material, or catalysts of the dissociation and recombination affect the membrane performance. However, there is little article about catalysts for the dissociation and recombination. We confirmed the performance of La0.6Sr0.4Co1.0O3-δ (LSC) based catalyst which was commonly used as the dissociation and recombination. It is known that the adsorbed amount of oxygen increase with the increase of doped Fe content in B site of LSC. We prepared the catalysts of La0.1Sr0.9Co0.9Fe0.1O3-δ(C9F1), La0.1Sr0.9Co0.5Fe0.5O3-δ(C5F5) and La0.1Sr0.9Co0.3Fe0.7O3-δ(C7F3). Also, we used Pr2NiO4 type mixed conductor as a membrane material. (Pr0.9La0.1)2(Ni0.74Cu0.21Ga0.05)O4+δ(PLNCG) shows the high oxygen permeability and the stability against carbon dioxide. Oxygen permeation experiments were carried out using a homemade apparatus at 850 -975 °C. The membrane was sealed with Pyrex glass at both end of the outside dense alumina tubes. To measure the oxygen permeation rate, air was fed to the film side at 50 ml min-1, helium as the sweep gas and reference gas was fed at 20 ml min-1. The flow rates of the sweep gas and the gas permeated through the membrane were measured using flow meter and the gas concentrations were determined using a gas chromatograph. Then, the permeance of the oxygen was determined using the flow rate and the concentration of the gas on the permeate side of the membrane. The increase of oxygen permeation was observed with increasing temperature. It is considered that this is due to the catalytic activities are increased with increasing temperature. Another reason is the increase of oxygen diffusivity in the bulk of membrane. The oxygen permeation rate is improved by using catalyst of LSC or LSCF. The oxygen permeation rate of membrane with LSCF showed higher than that of membrane with LSC. Furthermore, in LSCF catalysts, oxygen permeation rate increased with the increase of the doped amount of Fe. It is considered that this is caused by the increased of adsorbed amount of oxygen.

Keywords: membrane separation, oxygen permeation, K2NiF4-type structure, mixed conductor

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147 Morphological Characterization and Gas Permeation of Commercially Available Alumina Membrane

Authors: Ifeyinwa Orakwe, Ngozi Nwogu, Edward Gobina

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This work presents experimental results relating to the structural characterization of a commercially available alumina membrane. A γ-alumina mesoporous tubular membrane has been used. Nitrogen adsorption-desorption, scanning electron microscopy and gas permeability test has been carried out on the alumina membrane to characterize its structural features. Scanning electron microscopy (SEM) was used to determine the pore size distribution of the membrane. Pore size, specific surface area and pore size distribution were also determined with the use of the Nitrogen adsorption-desorption instrument. Gas permeation tests were carried out on the membrane using a variety of single and mixed gases. The permeabilities at different pressure between 0.05-1 bar and temperature range of 25-200oC were used for the single and mixed gases: nitrogen (N2), helium (He), oxygen (O2), carbon dioxide (CO2), 14%CO₂/N₂, 60%CO₂/N₂, 30%CO₂/CH4 and 21%O₂/N₂. Plots of flow rate verses pressure were obtained. Results got showed the effect of temperature on the permeation rate of the various gases. At 0.5 bar for example, the flow rate for N2 was relatively constant before decreasing with an increase in temperature, while for O2, it continuously decreased with an increase in temperature. In the case of 30%CO₂/CH4 and 14%CO₂/N₂, the flow rate showed an increase then a decrease with increase in temperature. The effect of temperature on the membrane performance of the various gases is presented and the influence of the trans membrane pressure drop will be discussed in this paper.

Keywords: alumina membrane, Nitrogen adsorption-desorption, scanning electron microscopy, gas permeation, temperature

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146 Penetration Depth Study of Linear Siloxanes through Human Skin

Authors: K. Szymkowska, K. Mojsiewicz- Pieńkowska

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Siloxanes are a common ingredients in medicinal products used on the skin, as well as cosmetics. It is widely believed that the silicones are not capable of overcoming the skin barrier. The aim of the study was to verify the possibility of penetration and permeation of linear siloxanes through human skin and determine depth penetration limit of these compounds. Based on the results it was found that human skin is not a barrier for linear siloxanes. PDMS 50 cSt was not identified in the dermis suggests that this molecular size of silicones (3780Da) is safe when it is used in the skin formulations.

Keywords: linear siloxanes, methyl siloxanes, skin penetration, skin permeation

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145 Combined Effect of Vesicular System and Iontophoresis on Skin Permeation Enhancement of an Analgesic Drug

Authors: Jigar N. Shah, Hiral J. Shah, Praful D. Bharadia

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The major challenge faced by formulation scientists in transdermal drug delivery system is to overcome the inherent barriers related to skin permeation. The stratum corneum layer of the skin is working as the rate limiting step in transdermal transport and reduce drug permeation through skin. Many approaches have been used to enhance the penetration of drugs through this layer of the skin. The purpose of this study is to investigate the development and evaluation of a combined approach of drug carriers and iontophoresis as a vehicle to improve skin permeation of an analgesic drug. Iontophoresis is a non-invasive technique for transporting charged molecules into and through tissues by a mild electric field. It has been shown to effectively deliver a variety of drugs across the skin to the underlying tissue. In addition to the enhanced continuous transport, iontophoresis allows dose titration by adjusting the electric field, which makes personalized dosing feasible. Drug carrier could modify the physicochemical properties of the encapsulated molecule and offer a means to facilitate the percutaneous delivery of difficult-to-uptake substances. Recently, there are some reports about using liposomes, microemulsions and polymeric nanoparticles as vehicles for iontophoretic drug delivery. Niosomes, the nonionic surfactant-based vesicles that are essentially similar in properties to liposomes have been proposed as an alternative to liposomes. Niosomes are more stable and free from other shortcoming of liposomes. Recently, the transdermal delivery of certain drugs using niosomes has been envisaged and niosomes have proved to be superior transdermal nanocarriers. Proniosomes overcome some of the physical stability related problems of niosomes. The proniosomal structure was liquid crystalline-compact niosomes hybrid which could be converted into niosomes upon hydration. The combined use of drug carriers and iontophoresis could offer many additional benefits. The system was evaluated for Encapsulation Efficiency, vesicle size, zeta potential, Transmission Electron Microscopy (TEM), DSC, in-vitro release, ex-vivo permeation across skin and rate of hydration. The use of proniosomal gel as a vehicle for the transdermal iontophoretic delivery was evaluated in-vitro. The characteristics of the applied electric current, such as density, type, frequency, and on/off interval ratio were observed. The study confirms the synergistic effect of proniosomes and iontophoresis in improving the transdermal permeation profile of selected analgesic drug. It is concluded that proniosomal gel can be used as a vehicle for transdermal iontophoretic drug delivery under suitable electric conditions.

Keywords: iontophoresis, niosomes, permeation enhancement, transdermal delivery

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144 Modeling Sorption and Permeation in the Separation of Benzene/ Cyclohexane Mixtures through Styrene-Butadiene Rubber Crosslinked Membranes

Authors: Hassiba Benguergoura, Kamal Chanane, Sâad Moulay

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Pervaporation (PV), a membrane-based separation technology, has gained much attention because of its energy saving capability and low-cost, especially for separation of azeotropic or close-boiling liquid mixtures. There are two crucial issues for industrial application of pervaporation process. The first is developing membrane material and tailoring membrane structure to obtain high pervaporation performances. The second is modeling pervaporation transport to better understand of the above-mentioned structure–pervaporation relationship. Many models were proposed to predict the mass transfer process, among them, solution-diffusion model is most widely used in describing pervaporation transport including preferential sorption, diffusion and evaporation steps. For modeling pervaporation transport, the permeation flux, which depends on the solubility and diffusivity of components in the membrane, should be obtained first. Traditionally, the solubility was calculated according to the Flory–Huggins theory. Separation of the benzene (Bz)/cyclohexane (Cx) mixture is industrially significant. Numerous papers have been focused on the Bz/Cx system to assess the PV properties of membrane materials. Membranes with both high permeability and selectivity are desirable for practical application. Several new polymers have been prepared to get both high permeability and selectivity. Styrene-butadiene rubbers (SBR), dense membranes cross-linked by chloromethylation were used in the separation of benzene/cyclohexane mixtures. The impact of chloromethylation reaction as a new method of cross-linking SBR on the pervaporation performance have been reported. In contrast to the vulcanization with sulfur, the cross-linking takes places on styrene units of polymeric chains via a methylene bridge. The partial pervaporative (PV) fluxes of benzene/cyclohexane mixtures in styrene-butadiene rubber (SBR) were predicted using Fick's first law. The predicted partial fluxes and the PV separation factor agreed well with the experimental data by integrating Fick's law over the benzene concentration. The effects of feed concentration and operating temperature on the predicted permeation flux by this proposed model are investigated. The predicted permeation fluxes are in good agreement with experimental data at lower benzene concentration in feed, but at higher benzene concentration, the model overestimated permeation flux. The predicted and experimental permeation fluxes all increase with operating temperature increasing. Solvent sorption levels for benzene/ cyclohexane mixtures in a SBR membrane were determined experimentally. The results showed that the solvent sorption levels were strongly affected by the feed composition. The Flory- Huggins equation generates higher R-square coefficient for the sorption selectivity.

Keywords: benzene, cyclohexane, pervaporation, permeation, sorption modeling, SBR

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143 The Effect of Particle Porosity in Mixed Matrix Membrane Permeation Models

Authors: Z. Sadeghi, M. R. Omidkhah, M. E. Masoomi

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The purpose of this paper is to examine gas transport behavior of mixed matrix membranes (MMMs) combined with porous particles. Main existing models are categorized in two main groups; two-phase (ideal contact) and three-phase (non-ideal contact). A new coefficient, J, was obtained to express equations for estimating effect of the particle porosity in two-phase and three-phase models. Modified models evaluates with existing models and experimental data using Matlab software. Comparison of gas permeability of proposed modified models with existing models in different MMMs shows a better prediction of gas permeability in MMMs.

Keywords: mixed matrix membrane, permeation models, porous particles, porosity

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142 Development of Polybenzoxazine Membranes on Al2O3 Support for Water-Ethanol Separation via Pervaporation Technique

Authors: Chonlada Choedchun, Ni-on Saelim, Panupong Chuntanalerg, Thanyalak Chaisuwan, Sujitra Wongkasemjit

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Bioethanol is one of the candidates to replace fossil fuels. Membrane technique is one of the attractive processes to produce high purity of ethanol. In this work, polybenzoxazine (PBZ) membrane successfully synthesized from bisphenol-A (BPA), formaldehyde, and two different types of multifunctionalamines: tetraethylenepentamine (tepa), and diethylenetriamine (deta), was evaluated for water-ethanol separation. The membrane thickness was determined by scanning electron microscopy (SEM). Pervaporation technique was carried out to find separation performance. It was found that the optimum PBZ concentration for the preparation of the membranes is 25%. The dipping cycles of PBZ-tepa and PBZ-deta was found to be 4 and 5, giving the total permeation flux of 28.97 and 14.75 g/m2.h, respectively. The separation factor of both membranes was higher than 10,000.

Keywords: polybenzoxazine, pervaporation, permeation flux, separation factor

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141 Transdermal Delivery of Sodium Diclofenac from Palm Kernel Oil Esteres Nanoemulsions

Authors: Malahat Rezaee, Mahiran Basri, Abu Bakar Salleh, Raja Noor Zaliha Raja Abdul Rahman

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Sodium diclofenac is one of the most commonly used drugs of nonsteroidal anti-inflammatory drugs (NSAIDs). It is especially effective in the controlling the severe conditions of inflammation and pain, musculoskeletal disorders, arthritis, and dysmenorrhea. Formulation as nanoemulsions is one of the nanoscience approaches that has been progressively considered in pharmaceutical science for transdermal delivery of the drug. Nanoemulsions are a type of emulsion with particle sizes ranging from 20 nm to 200 nm. An emulsion is formed by the dispersion of one liquid, usually the oil phase in another immiscible liquid, water phase that is stabilized using the surfactant. Palm kernel oil esters (PKOEs), in comparison to other oils, contain higher amounts of shorter chain esters, which suitable to be applied in micro and nanoemulsion systems as a carrier for actives, with excellent wetting behavior without the oily feeling. This research aimed to study the effect of terpene type and concentration on sodium diclofenac permeation from palm kernel oil esters nanoemulsions and physicochemical properties of the nanoemulsions systems. The effect of various terpenes of geraniol, menthone, menthol, cineol and nerolidol at different concentrations of 0.5, 1.0, 2.0, and 4.0% on permeation of sodium diclofenac were evaluated using Franz diffusion cells and rat skin as permeation membrane. The results of this part demonstrated that all terpenes showed promoting effect on sodium diclofenac penetration. However, menthol and menthone at all concentrations showed significant effects (<0.05) on drug permeation. The most outstanding terpene was menthol with the most significant effect for skin permeability of sodium diclofenac. The effect of terpenes on physicochemical properties of nanoemulsion systems was investigated on the parameters of particle size, zeta potential, pH, viscosity and electrical conductivity. The result showed that all terpenes had the significant effect on particle size and non-significant effects on the zeta potential of the nanoemulsion systems. The effect of terpenes was significant on pH, excluding the menthone at concentrations of 0.5 and 1.0%, and cineol and nerolidol at the concentration of 2.0%. Terpenes also had significant effect on viscosity of nanoemulsions exception of menthone and cineol at the concentration of 0.5%. The result of conductivity measurements showed that all terpenes at all concentration except cineol at the concentration of 0.5% represented significant effect on electrical conductivity.

Keywords: nanoemulsions, palm kernel oil esters, sodium diclofenac, terpenes, skin permeation

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140 Effect of Different Model Drugs on the Properties of Model Membranes from Fishes

Authors: M. Kumpugdee-Vollrath, T. G. D. Phu, M. Helmis

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A suitable model membrane to study the pharmacological effect of pharmaceutical products is human stratum corneum because this layer of human skin is the outermost layer and it is an important barrier to be passed through. Other model membranes which were also used are for example skins from pig, mouse, reptile or fish. We are interested in fish skins in this project. The advantages of the fish skins are, that they can be obtained from the supermarket or fish shop. However, the fish skins should be freshly prepared and used directly without storage. In order to understand the effect of different model drugs e.g. lidocaine HCl, resveratrol, paracetamol, ibuprofen, acetyl salicylic acid on the properties of the model membrane from various types of fishes e.g. trout, salmon, cod, plaice permeation tests were performed and differential scanning calorimetry was applied.

Keywords: fish skin, model membrane, permeation, DSC, lidocaine HCl, resveratrol, paracetamol, ibuprofen, acetyl salicylic acid

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139 Al-Ti-W Metallic Glass Thin Films Deposited by Magnetron Sputtering Technology to Protect Steel Against Hydrogen Embrittlement

Authors: Issam Lakdhar, Akram Alhussein, Juan Creus

Abstract:

With the huge increase in world energy consumption, researchers are working to find other alternative sources of energy instead of fossil fuel one causing many environmental problems as the production of greenhouse effect gases. Hydrogen is considered a green energy source, which its combustion does not cause environmental pollution. The transport and the storage of the gas molecules or the other products containing this smallest chemical element in metallic structures (pipelines, tanks) are crucial issues. The dissolve and the permeation of hydrogen into the metal lattice lead to the formation of hydride phases and the embrittlement of structures. To protect the metallic structures, a surface treatment could be a good solution. Among the different techniques, magnetron sputtering is used to elaborate micrometric coatings capable of slowing down or stop hydrogen permeation. In the plasma environment, the deposition parameters of new thin-film metallic glasses Al-Ti-W were optimized and controlled in order to obtain, hydrogen barrier. Many characterizations were carried out (SEM, XRD and Nano-indentation…) to control the composition and understand the influence of film microstructure and chemical composition on the hydrogen permeation through the coatings. The coating performance was evaluated under two hydrogen production methods: chemical and electrochemical (cathodic protection) techniques. The hydrogen quantity absorbed was experimentally determined using the Thermal-Desorption Spectroscopy method (TDS)). An ideal ATW thin film was developed and showed excellent behavior against the diffusion of hydrogen.

Keywords: thin films, hydrogen, PVD, plasma technology, electrochemical properties

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138 Formulation and in vitro Evaluation of Transdermal Delivery of Articaine

Authors: Dinakaran Venkatachalam, Paul Chambers, Kavitha Kongara, Preet Singh

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The objective of this study is to formulate different topical preparations containing articaine and to investigate their permeation through goat skin. Initially, articaine and its hydrochloride salt were compared for in vitro permeation using Franz cell model. Goat skin samples were collected after euthanizing male goat kids purchased from the dairy goat farmers. Subcutaneous fat was removed and the skin was mounted on the donor chamber (orifice area 1.00 cm²) and drugs were applied onto the epidermis. Phosphate buffer saline (pH 7.4) was used to maintain sink condition in the receptor chamber (8 ml) of the Franz cell. Samples (0.4 ml) were collected at various intervals over 24 hours after each sampling equal volume of PBS was replaced in the receptor chamber. Articaine in the collected samples were quantified using LC/MS. The results suggested that articaine free base permeates better than its hydrochloride salt through goat skin. This study results support the fact that local anesthetics in its base form are lipophilic and thus penetrates faster through cell membranes than their salts. Later, articaine free base was formulated either using ethanol and octyl salicylate or dimethyl sulfoxide (DMSO) as penetration enhancers and was compared for in vitro permeation. The transdermal flux of articaine in the formulation containing DMSO was approximately 3.8 times higher than that of the formulation containing ethanol and octyl salicylate. Further studies to evaluate the local anesthetic efficacy of the topical formulation containing articaine for dermal anesthesia in animals have been planned.

Keywords: articaine, dermal anesthesia, local anesthetic, transdermal

Procedia PDF Downloads 155
137 Formulation and Evaluation of TDDS for Sustained Release Ondansetron HCL Patches

Authors: Baljinder Singh, Navneet Sharma

Abstract:

The skin can be used as the site for drug administration for continuous transdermal drug infusion into the systemic circulation. For the continuous diffusion/penetration of the drugs through the intact skin surface membrane-moderated systems, matrix dispersion type systems, adhesive diffusion controlled systems and micro reservoir systems have been developed. Various penetration enhancers are used for the drug diffusion through skin. In matrix dispersion type systems, the drug is dispersed in the solvent along with the polymers and solvent allowed to evaporate forming a homogeneous drug-polymer matrix. Matrix type systems were developed in the present study. In the present work, an attempt has been made to develop a matrix-type transdermal therapeutic system comprising of ondansetron-HCl with different ratios of hydrophilic and hydrophobic polymeric combinations using solvent evaporation technique. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy. The results obtained showed no physical-chemical incompatibility between the drug and the polymers. The patches were further subjected to various physical evaluations along with the in-vitro permeation studies using rat skin. On the basis of results obtained form the in vitro study and physical evaluation, the patches containing hydrophilic polymers i.e. polyvinyl alcohol and poly vinyl pyrrolidone with oleic acid as the penetration enhancer(5%) were considered as suitable for large scale manufacturing with a backing layer and a suitable adhesive membrane.

Keywords: transdermal drug delivery, penetration enhancers, hydrophilic and hydrophobic polymers, ondansetron HCl

Procedia PDF Downloads 241
136 Development of Agomelatine Loaded Proliposomal Powders for Improved Intestinal Permeation: Effect of Surface Charge

Authors: Rajasekhar Reddy Poonuru, Anusha Parnem

Abstract:

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

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135 Gas Permeation Behavior of Single and Mixed Gas Components Using an Asymmetric Ceramic Membrane

Authors: Ngozi Claribelle Nwogu, Mohammed Nasir Kajama, Godson Osueke, Edward Gobina

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A unique sol–gel dip-coating process to form an asymmetric silica membrane with improved membrane performance and reproducibility has been reported. First, we deposited repeatedly a silica solution on top of a commercial alumina membrane support to improve its structural make up. The coated membrane is further processed under clean room conditions to avoid dust impurity and subsequent drying in an oven for high thermal, chemical and physical stability. The resulting asymmetric membrane exhibits a gradual change in the membrane layer thickness. Compared to a single-layer process using only the membrane support, the dual-layer process improves both flux and selectivity. For the scientifically significant difficulties of natural gas purification, collective CO2, CH4 and H2 gas fluxes and separation factors obtained gave reasonably excellent values. In addition, the membrane selectively separated hydrogen as demonstrated by a high concentration of hydrogen recovery.

Keywords: gas permeation, silica membrane, separation factor, membrane layer thickness

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134 Fabrication of Cellulose Acetate/Polyethylene Glycol Membranes Blended with Silica and Carbon Nanotube for Desalination Process

Authors: Siti Nurkhamidah, Yeni Rahmawati, Fadlilatul Taufany, Eamor M. Woo, I Made P. A. Merta, Deffry D. A. Putra, Pitsyah Alifiyanti, Krisna D. Priambodo

Abstract:

Cellulose acetate/polyethylene glycol (CA/PEG) membrane was modified with varying amount of silica and carbon nanotube (CNT) to enhance its separation performance in the desalination process. These composite membranes were characterized for their hydrophilicity, morphology and permeation properties. The experiment results show that hydrophilicity of CA/PEG/Silica membranes increases with the increasing of silica concentration and the decreasing particle size of silica. From Scanning Electron Microscopy (SEM) image, it shows that pore structure of CA/PEG membranes increases with the addition of silica. Membrane performance analysis shows that permeate flux, salt rejection, and permeability of membranes increase with the increasing of silica concentrations. The effect of CNT on the hydrophylicity, morphology, and permeation properties was also discussed.

Keywords: carbon nanotube, cellulose acetate, desalination, membrane, PEG

Procedia PDF Downloads 238
133 Formulation and Ex Vivo Evaluation of Solid Lipid Nanoparticles Based Hydrogel for Intranasal Drug Delivery

Authors: Pramod Jagtap, Kisan Jadhav, Neha Dand

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Risperidone (RISP) is an antipsychotic agent and has low water solubility and nontargeted delivery results in numerous side effects. Hence, an attempt was made to develop SLNs hydrogel for intranasal delivery of RISP to achieve maximum bioavailability and reduction of side effects. RISP loaded SLNs composed of 1.65% (w/v) lipid mass were produced by high shear homogenization (HSH) coupled ultrasound (US) method using glyceryl monostearate (GMS) or Imwitor 900K (solid lipid). The particles were loaded with 0.2% (w/v) of the RISP & surface-tailored with a 2.02% (w/v) non-ionic surfactant Tween® 80. Optimization was done using 32 factorial design using Design Expert® software. The prepared SLNs dispersion incorporated into Polycarbophil AA1 hydrogel (0.5% w/v). The final gel formulation was evaluated for entrapment efficiency, particle size, rheological properties, X ray diffraction, in vitro diffusion, ex vivo permeation using sheep nasal mucosa and histopathological studies for nasocilliary toxicity. The entrapment efficiency of optimized SLNs was found to be 76 ± 2 %, polydispersity index <0.3., particle size 278 ± 5 nm. This optimized batch was incorporated into hydrogel. The pH was found to be 6.4 ± 0.14. The rheological behaviour of hydrogel formulation revealed no thixotropic behaviour. In histopathology study, there was no nasocilliary toxicity observed in nasal mucosa after ex vivo permeation. X-ray diffraction data shows drug was in amorphous form. Ex vivo permeation study shows controlled release profile of drug.

Keywords: ex vivo, particle size, risperidone, solid lipid nanoparticles

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132 Fabrication and Characterization of Folic Acid-Grafted-Thiomer Enveloped Liposomes for Enhanced Oral Bioavailability of Docetaxel

Authors: Farhan Sohail, Gul Shahnaz Irshad Hussain, Shoaib Sarwar, Ibrahim Javed, Zajif Hussain, Akhtar Nadhman

Abstract:

The present study was aimed to develop a hybrid nanocarrier (NC) system with enhanced membrane permeability, bioavailability and targeted delivery of Docetaxel (DTX) in breast cancer. Hybrid NC’s based on folic acid (FA) grafted thiolated chitosan (TCS) enveloped liposomes were prepared with DTX and evaluated in-vitro and in-vivo for their enhanced permeability and bioavailability. Physicochemical characterization of NC’s including particle size, morphology, zeta potential, FTIR, DSC, PXRD, encapsulation efficiency and drug release from NC’s was determined in vitro. Permeation enhancement and p-gp inhibition were performed through everted sac method on freshly excised rat intestine which indicated that permeation was enhanced 5 times as compared to pure DTX and the hybrid NC’s were strongly able to inhibit the p-gp activity as well. In-vitro cytotoxicity and tumor targeting was done using MDA-MB-231 cell line. The stability study of the formulations performed for 3 months showed the improved stability of FA-TCS enveloped liposomes in terms of its particles size, zeta potential and encapsulation efficiency as compared to TCS NP’s and liposomes. The pharmacokinetic study was performed in vivo using rabbits. The oral bioavailability and AUC0-96 was increased 10.07 folds with hybrid NC’s as compared to positive control. Half-life (t1/2) was increased 4 times (58.76 hrs) as compared to positive control (17.72 hrs). Conclusively, it is suggested that FA-TCS enveloped liposomes have strong potential to enhance permeability and bioavailability of hydrophobic drugs after oral administration and tumor targeting.

Keywords: docetaxel, coated liposome, permeation enhancement, oral bioavailability

Procedia PDF Downloads 327
131 Effect of Air Gap Distance on the Structure of PVDF Hollow Fiber Membrane Contactors for Physical CO2 Absorption

Authors: J. Shiri, A. Mansourizadeh, F. Faghih, H. Vaez

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In this study, porous polyvinylidene fluoride (PVDF) hollow fiber membranes are fabricated via a wet phase-inversion Process and used in the gas–liquid membrane contactor for physical CO2 absorption. Effect of different air gap on the structure and CO2 flux of the membrane was investigated. The hollow fibers were prepared using the wet spinning process using a dope solution containing PVDF/NMP/Licl (18%, 78%, 4%) at the extrusion rate of 4.5ml/min and air gaps of 0, 7, 15cm. Water was used as internal and external coagulants. Membranes were characterized using various techniques such as Field Emission Scanning Electron Microscopy (FESEM), Gas permeation test, Critical Water Entry Pressure (CEPw) to select the best membrane structure for Co2 absorption. The characterization results showed that the prepared membrane at which air gap possess small pore size with high surface porosity and wetting resistance, which are favorable for gas absorption application air gap increased, CEPw had a decrease, but the N2 permeation was decreased. Surface porosity and also Co2 absorption was increased.

Keywords: porous PVDF hollow fiber membrane, CO2 absorption, phase inversion, air gap

Procedia PDF Downloads 310
130 Artificial Membrane Comparison for Skin Permeation in Skin PAMPA

Authors: Aurea C. L. Lacerda, Paulo R. H. Moreno, Bruna M. P. Vianna, Cristina H. R. Serra, Airton Martin, André R. Baby, Vladi O. Consiglieri, Telma M. Kaneko

Abstract:

The modified Franz cell is the most widely used model for in vitro permeation studies, however it still presents some disadvantages. Thus, some alternative methods have been developed such as Skin PAMPA, which is a bio- artificial membrane that has been applied for skin penetration estimation of xenobiotics based on HT permeability model consisting. Skin PAMPA greatest advantage is to carry out more tests, in a fast and inexpensive way. The membrane system mimics the stratum corneum characteristics, which is the primary skin barrier. The barrier properties are given by corneocytes embedded in a multilamellar lipid matrix. This layer is the main penetration route through the paracellular permeation pathway and it consists of a mixture of cholesterol, ceramides, and fatty acids as the dominant components. However, there is no consensus on the membrane composition. The objective of this work was to compare the performance among different bio-artificial membranes for studying the permeation in skin PAMPA system. Material and methods: In order to mimetize the lipid composition`s present in the human stratum corneum six membranes were developed. The membrane composition was equimolar mixture of cholesterol, ceramides 1-O-C18:1, C22, and C20, plus fatty acids C20 and C24. The membrane integrity assay was based on the transport of Brilliant Cresyl Blue, which has a low permeability; and Lucifer Yellow with very poor permeability and should effectively be completely rejected. The membrane characterization was performed using Confocal Laser Raman Spectroscopy, using stabilized laser at 785 nm with 10 second integration time and 2 accumulations. The membrane behaviour results on the PAMPA system were statistically evaluated and all of the compositions have shown integrity and permeability. The confocal Raman spectra were obtained in the region of 800-1200 cm-1 that is associated with the C-C stretches of the carbon scaffold from the stratum corneum lipids showed similar pattern for all the membranes. The ceramides, long chain fatty acids and cholesterol in equimolar ratio permitted to obtain lipid mixtures with self-organization capability, similar to that occurring into the stratum corneum. Conclusion: The artificial biological membranes studied for Skin PAMPA showed to be similar and with comparable properties to the stratum corneum.

Keywords: bio-artificial membranes, comparison, confocal Raman, skin PAMPA

Procedia PDF Downloads 435