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Optimization and Characterization of Chitosan Films for Transdermal Delivery of Ondansetron  [PDF]
Asl? Sedef Can,Meryem Sedef Erdal,Sevgi Güng?r,Y?ld?z ?zsoy
Molecules , 2013, DOI: 10.3390/molecules18055455
Abstract: The aim of this study was to develop novel transdermal films of ondansetron HCl with high molecular weight chitosan as matrix polymer and 2-(2-ethoxy-ethoxy) ethanol (Transcutol ?) as plasticizer. In this context, firstly the physicochemical properties of gels used to formulate transdermal films were characterized and, physicochemical properties and bioadhesiveness of the transdermal films prepared with chitosan gels were assessed. The impact of three different types of terpenes, namely limonene, nerolidol and eucalyptol on in vitro skin permeation of ondansetron from transdermal films were also examined. ATR-FTIR measurements were performed to investigate the effects of the chitosan film formulations on in vitro conformational order of stratum corneum intercellular lipids after 24 h permeation study. The results showed that the chitosan gels consisting of Transcutol ? as plasticizer and terpenes as penetration enhancer may be used to prepare transdermal films of ondansetron due to the good mechanical properties and bioadhesiveness of the transdermal films. Eucalyptol (1%) showed higher permeation enhancer effect than the other terpenes and control. ATR-FTIR data confirmed that finding in which eucalyptol induced a blue shift in the both CH2 asymmetric and symmetric absorbance peak positions indicating increased lipid fluidity of stratum corneum.
Development of Chitosan Acetate Films for Transdermal Delivery of Propranolol Hydrochloride
KSY Hemant, HG Shivakumar
Tropical Journal of Pharmaceutical Research , 2010,
Abstract: Purpose: To formulate and evaluate chitosan acetate films designed for transdermal delivery of propranolol hydrochloride. Methods: Chitosan acetate was chemically modified with acetaldehyde and the solution was prepared with 1 % acetic acid, in which was dissolved propranolol hydrochloride, was cast as films in Petri dish and characterised by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and nuclear magnetic resonance (NMR). The films were evaluated for permeability, swelling, and in vitro drug release. Results: Drug content of propranolol hydrochloride in the films ranged from 0.9 to 1.4 mg/cm2 . Swelling was 570 % for chitosan acetate and 180 % for chitosan while drug release through chitosan acetate higher than through chitosan. Permeability coefficient was 6.12 x 10-4 and 0.97 x 10-4 g.cm2 / day for chitosan acetate and chitosan, respectively. FTIR and DSC results indicated that there was no chemical interaction between the drug and the polymers used. NMR spectra showed the appearance of specific peaks for acetate group. Differences between chitosan acetate and chitosan were significant (p < 0.05) with regard to permeability, swelling and in vitro drug release. Conclusion: The films prepared using the synthesised chitosan acetate exhibited superior physicochemical and drug release characteristics to those of chitosan. The results also indicate chitosan acetate films may be suitable for delivering propranolol hydrochloride via the transdermal route which offers some advantages over other routes.
Preparation of alginate coated chitosan microparticles for vaccine delivery
XingYi Li, XiangYe Kong, Shuai Shi, XiuLing Zheng, Gang Guo, YuQuan Wei, ZhiYong Qian
BMC Biotechnology , 2008, DOI: 10.1186/1472-6750-8-89
Abstract: The prepared alginate coated BSA loaded chitosan microparticles had loading efficiency (LE) of 60% and loading capacity (LC) of 6% with mean diameter of about 1 μm. When the weight ratio of alginate/chitosan microparticles was greater than 2, the stable system could be obtained. The rapid charge inversion of BSA loaded chitosan microparticles (from +27 mv to -27.8 mv) was observed during the coating procedure which indicated the presence of alginate layer on the chitosan microparticles surfaces. According to the results obtained by scanning electron microscopy (SEM), the core-shell structure of BSA loaded chitosan microparticles was observed. Meanwhile, in vitro release study indicated that the initial burst release of BSA from alginate coated chitosan microparticles was lower than that observed from uncoated chitosan microparticles (40% in 8 h vs. about 84% in 0.5 h). SDS-polyacrylamide gel electrophoresis (SDS-PAGE) assay showed that alginate coating onto chitosan microparticles could effectively protect the BSA from degradation or hydrolysis in acidic condition for at least 2 h. The structural integrity of alginate modified chitosan microparticles incubated in PBS for 24 h was investigated by FTIR.The prepared alginate coated chitosan microparticles, with mean diameter of about 1 μm, was suitable for oral mucosal vaccine. Moreover, alginate coating onto the surface of chitosan microparticles could modulate the release behavior of BSA from alginate coated chitosan microparticles and could effectively protect model protein (BSA) from degradation in acidic medium in vitro for at least 2 h. In all, the prepared alginate coated chitosan microparticles might be an effective vehicle for oral administration of antigens.Development of an oral antigens (protein, and etc) delivery system for mucosal vaccine is a meaningful challenge for pharmaceutical scientists. The instability and poor absorption of antigens in gastrointestinal tract is major obstacles in the development
Preparation and Characterization of Maleic Anhydride Cross-Linked Chitosan-Polyvinyl Alcohol Hydrogel Matrix Transdermal Patch  [PDF]
Parimal Maji *,Arijit Gandhi,Sougata Jana,Nirmal Maji
Journal of PharmaSciTech , 2013,
Abstract: Transdermal drug delivery systems are polymeric patches containing dissolved or dispersed drugs that deliver therapeutic agents at a constant rate to the human body. Matrix type transdermal patches were prepared using alprazolam as a model drug and employing the combinations of chitosan-polyvinyl alcohol (CS-PVA) cross linked with Maleic anhydride. The transdermal patches were evaluated for their physicochemical properties like thickness, tensile strength, folding endurance, drug content, swellability, surface pH, water vapour transmission, in vitro permeation and skin irritation studies. FTIR study indicated no interaction between drug and polymers. The permeability of alprazolam was increased with increase in PVA content. The in vitro drug permeation followed Higuchi kinetics as its coefficient of correlation value predominates over zero order and first order kinetics. Also the diffusion coefficient of release profiles had a value of nearly 0.5, which indicated Fickian transport diffusion. The patches were found to be free of any skin irritation.
Preparation and Characterization of Water-Soluble Chitosan Nanoparticles as Protein Delivery System
Hong-liang Zhang,Si-hui Wu,Yi Tao,Lin-quan Zang,Zheng-quan Su
Journal of Nanomaterials , 2010, DOI: 10.1155/2010/898910
Abstract: The objective of this study was to investigate the potential of water soluble chitosan as a carrier in the preparation of protein-loaded nanoparticles. Nanoparticles were prepared by ionotropic gelation of water-soluble chitosan (WSC) with sodium tripolyphosphate (TPP). Bovine serum albumin (BSA) was applied as a model drug. The size and morphology of the nanoparticles were investigated as a function of the preparation conditions. The particles were spherical in shape and had a smooth surface. The size range of the nanoparticles was between 100 and 400 nm. Result of the in vitro studies showed that the WSC nanoparticles enhance and prolong the intestinal absorption of BSA. These results also indicated that WSC nanoparticles were a potential protein delivery system.
Microemulsion-based novel transdermal delivery system of tetramethylpyrazine: preparation and evaluation in vitro and in vivo
Zhao JH, Ji L, Wang H, Chen ZQ, Zhang YT, Liu Y, Feng NP
International Journal of Nanomedicine , 2011, DOI: http://dx.doi.org/10.2147/IJN.S23597
Abstract: roemulsion-based novel transdermal delivery system of tetramethylpyrazine: preparation and evaluation in vitro and in vivo Original Research (5838) Total Article Views Authors: Zhao JH, Ji L, Wang H, Chen ZQ, Zhang YT, Liu Y, Feng NP Published Date August 2011 Volume 2011:6 Pages 1611 - 1619 DOI: http://dx.doi.org/10.2147/IJN.S23597 Ji-Hui Zhao, Li Ji, Hui Wang, Zhi-Qiang Chen, Yong-Tai Zhang, Ying Liu, Nian-Ping Feng School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China Objective: To deliver 2,3,5,6-tetramethylpyrazine (TMP) in a relatively large dose through a transdermal route and facilitate the practical application of microemulison in transdermal drug delivery. Methods: The pseudo-ternary phase diagram for microemulsion regions was constructed using isopropyl myristate as oil phase, Labrasol as surfactant, and Plurol Oleique CC 497 as cosurfactant. A uniform experimental design was applied for formulation optimization. In vitro skin permeation experiments of six formulations were undertaken with TMP transdermal patch (EUDRAGIT E100 as matrix) and TMP saturated solution as controls. We prepared TMP-oil dispersed in water-ethylene vinyl acetate-transdermal therapeutic system (TMP-O/W-EVA-TTS) with microemulsion as reservoir and EVA membrane as release liner; pharmacokinetic and brain distribution studies in rats were conducted with TMP transdermal patches as control. Results: The skin fluxes of TMP from microemulsions were 8.2- to 26.7-fold and 0.9- to 4.7-fold higher than those of TMP transdermal patch and TMP saturated solution, respectively, and were strongly affected by the microemulsion composition. The improvement in TMP solubility as well as the skin permeation enhancement effect of microemulsion components contributed mainly to transdermal delivery facilitation. In the pharmacokinetic study, the relative bioavailability of TMP-O/W-EVA-TTS was 350.89% compared with the TMP transdermal patch. Higher and more stable TMP contents in rat plasma were obtained after administration of TMP-O/W-EVA-TTS than after application of TMP transdermal patch. In the brain distribution study, higher rate and extent of TMP distribution to brain, and lower rate of TMP clearance from brain were observed after transdermal administration of TMP-O/W-EVA-TTS than after application of TMP transdermal patch. Conclusion: The novel transdermal delivery system prepared in this study showed a remarkable skin permeation improvement of microemulsion and facilitated its practical application in transdermal drug delivery. With this system as a vehicle, a relatively large dose of TMP could enable successful drug delivery via the transdermal route.
A Biomimetic Chitosan Derivates: Preparation, Characterization and Transdermal Enhancement Studies of N-Arginine Chitosan  [PDF]
Hui-Xia Lv,Zhen-Hai Zhang,Xiao-Pan Wang,Qing-Qing Cheng,Wei Wang,Xu-Hui Huang,Jian-Ping Zhou,Qiang Zhang,Lu-Lu Hou,Wei Huo
Molecules , 2011, DOI: 10.3390/molecules16086778
Abstract: A novel arginine-rich chitosan (CS) derivates mimicked cell penetration peptides; N-Arginine chitosan (N-Arg-CS) was prepared by two reaction methods involving activated L-arginine and the amine group on the chitosan. FTIR spectra showed that arginine was chemically coupled with CS. Elemental analysis estimated that the degrees of substitution (DS) of arginine in CS were 6%, 31.3% and 61.5%, respectively. The drug adefovir was chosen as model and its permeation flux across excised mice skin was investigated using a Franz diffusion cell. The results showed that the most effective enhancer was 2% (w/v) concentration of 10 kDa N-Arg-CS with 6% DS. At neutral pH, the cumulative amount of adefovir permeated after 12 hours was 2.63 ± 0.19 mg cm?2 which was 5.83-fold more than adefovir aqueous solution. Meanwhile N-Arg-CS was 1.83, 2.22, and 2.45 times more effective than Azone, eucalyptus and peppermint, respectively. The obtained results suggest that N-Arg-CS could be a promising transdermal enhancer.
Chitosan–Pluronic nanoparticles as oral delivery of anticancer gemcitabine: preparation and in vitro study
Hosseinzadeh H, Atyabi F, Dinarvand R, Ostad SN
International Journal of Nanomedicine , 2012, DOI: http://dx.doi.org/10.2147/IJN.S26365
Abstract: osan–Pluronic nanoparticles as oral delivery of anticancer gemcitabine: preparation and in vitro study Original Research (4458) Total Article Views Authors: Hosseinzadeh H, Atyabi F, Dinarvand R, Ostad SN Published Date April 2012 Volume 2012:7 Pages 1851 - 1863 DOI: http://dx.doi.org/10.2147/IJN.S26365 Received: 21 September 2011 Accepted: 17 December 2011 Published: 11 April 2012 Hosniyeh Hosseinzadeh1, Fatemeh Atyabi1, Rassoul Dinarvand1, Seyed Naser Ostad2 1Nanotechnology Research Centre, 2Department of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran Abstract: Nanoparticles have proven to be an effective delivery system with few side effects for anticancer drugs. In this study, gemcitabine-loaded nanoparticles have been prepared by an ionic gelation method using chitosan and Pluronic F-127 as a carrier. Prepared nanoparticles were characterized using dynamic light scattering, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), scanning electron microscopy, and transmission electron microscopy. Different parameters such as concentration of sodium tripolyphosphate, chitosan, Pluronic, and drug on the properties of the prepared nanoparticles were evaluated. In vitro drug release was studied in phosphate-buffered saline (PBS; pH = 7.4). The cytotoxicity of the nanoparticles was assayed in the HT-29 colon cancer cell line. The mucoadhesion behavior of the nanoparticles was also studied by mucus glycoprotein assay. The prepared nanoparticles had a spherical shape with positive charge and a mean diameter ranging between 80 to 170 nm. FT-IR and DSC studies found that the drug was dispersed in its amorphous form due to its potent interaction with nanoparticle matrix. Maximum drug encapsulation efficiency was achieved at 0.4 mg/mL gemcitabine while maximum drug loading was 6% obtained from 0.6 mg/mL gemcitabine. An in vitro drug release study at 37°C in PBS (pH = 7.4) exhibited a controlled release profile for chitosan–Pluronic F-127 nanoparticles. A cytotoxicity assay of gemcitabine-loaded nanoparticles showed an increase in the cytotoxicity of gemcitabine embedded in the nanoparticles in comparison with drug alone. The mucoadhesion study results suggest that nanoparticles could be considered as an efficient oral formulation for colon cancer treatment.
TRANSDERMAL DRUG DELIVERY SYSTEM: REVIEW  [PDF]
Vishvakarama Prabhakar,Agarwal Shivendra,Sharma Ritika,Saurabh Sharma
International Research Journal of Pharmacy , 2012,
Abstract: Various new technologies have been developed for the transdermal delivery of some important drugs. Today about 74% of drugs are taken orally and are found not to be as effective as desired. To improve such characters transdermal drug delivery system was emerged. Drug delivery through the skin to achieve a systemic effect of a drug is commonly known as transdermal drug delivery and differs from traditional topical drug delivery. Transdermal drug delivery systems (TDDS) are dosage forms involves drug transport to viable epidermal and or dermal tissues of the skin for local therapeutic effect while a very major fraction of drug is transported into the systemic blood circulation. The adhesive of the transdermal drug delivery system is critical to the safety, efficacy and quality of the product. Topical administration of therapeutic agents offers many advantages over conventional oral and invasive methods of drug delivery. This review article provides an overview of TDDS, its advantages over conventional dosage forms, drug delivery routes across human skin, penetration enhancers, various components of Transdermal patches, types of Transdermal patches, methods of preparation and its physicochemical methods of evaluation.
Microemulsion-based novel transdermal delivery system of tetramethylpyrazine: preparation and evaluation in vitro and in vivo  [cached]
Zhao JH,Ji L,Wang H,Chen ZQ
International Journal of Nanomedicine , 2011,
Abstract: Ji-Hui Zhao, Li Ji, Hui Wang, Zhi-Qiang Chen, Yong-Tai Zhang, Ying Liu, Nian-Ping FengSchool of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of ChinaObjective: To deliver 2,3,5,6-tetramethylpyrazine (TMP) in a relatively large dose through a transdermal route and facilitate the practical application of microemulison in transdermal drug delivery.Methods: The pseudo-ternary phase diagram for microemulsion regions was constructed using isopropyl myristate as oil phase, Labrasol as surfactant, and Plurol Oleique CC 497 as cosurfactant. A uniform experimental design was applied for formulation optimization. In vitro skin permeation experiments of six formulations were undertaken with TMP transdermal patch (EUDRAGIT E100 as matrix) and TMP saturated solution as controls. We prepared TMP-oil dispersed in water-ethylene vinyl acetate-transdermal therapeutic system (TMP-O/W-EVA-TTS) with microemulsion as reservoir and EVA membrane as release liner; pharmacokinetic and brain distribution studies in rats were conducted with TMP transdermal patches as control.Results: The skin fluxes of TMP from microemulsions were 8.2- to 26.7-fold and 0.9- to 4.7-fold higher than those of TMP transdermal patch and TMP saturated solution, respectively, and were strongly affected by the microemulsion composition. The improvement in TMP solubility as well as the skin permeation enhancement effect of microemulsion components contributed mainly to transdermal delivery facilitation. In the pharmacokinetic study, the relative bioavailability of TMP-O/W-EVA-TTS was 350.89% compared with the TMP transdermal patch. Higher and more stable TMP contents in rat plasma were obtained after administration of TMP-O/W-EVA-TTS than after application of TMP transdermal patch. In the brain distribution study, higher rate and extent of TMP distribution to brain, and lower rate of TMP clearance from brain were observed after transdermal administration of TMP-O/W-EVA-TTS than after application of TMP transdermal patch.Conclusion: The novel transdermal delivery system prepared in this study showed a remarkable skin permeation improvement of microemulsion and facilitated its practical application in transdermal drug delivery. With this system as a vehicle, a relatively large dose of TMP could enable successful drug delivery via the transdermal route.Keywords: TMP, microemulsion, EVA membrane, transdermal delivery, pharmacokinetics, brain distribution
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