Cationic polymer-based micro-emulgel with self-preserving ability for transdermal delivery of diclofenac sodium

The objective of the present study was to develop a topical preparation with enhanced skin permeation, high safety and self-preserving ability. Microemulsion (ME) and cationic polymer based micro-emulgel (CPBM) were investigated for the transdermal delivery of diclofenac sodium (DS). Medium-chain tr...

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Veröffentlicht in:Drug delivery 2015-08, Vol.22 (6), p.814-822
Hauptverfasser: Yang, Chunyu, Shen, Yan, Wang, Jue, Ouahab, Ammar, Zhang, Tao, Tu, Jiasheng
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container_end_page 822
container_issue 6
container_start_page 814
container_title Drug delivery
container_volume 22
creator Yang, Chunyu
Shen, Yan
Wang, Jue
Ouahab, Ammar
Zhang, Tao
Tu, Jiasheng
description The objective of the present study was to develop a topical preparation with enhanced skin permeation, high safety and self-preserving ability. Microemulsion (ME) and cationic polymer based micro-emulgel (CPBM) were investigated for the transdermal delivery of diclofenac sodium (DS). Medium-chain triglyceride was selected as the oil phase of ME due to its good solubilization of DS and high safety. Orthogonal test was applied to optimize the formula of ME based on the cumulative skin permeation amount in vitro after preliminary formula test. Chitosan (CS) or polylysine was employed as the cationic polymer in the formula of CPBM. The transdermal delivery of DS was evaluated through in vitro skin permeation test. The results showed that the skin permeation rate of DS from the optimized CPBM (126.17 ± 15.82 μg/cm 2 /h) were 1.86-folds and 5.76-folds higher than that of DS commercial Emulgel and DS control hydrogel, respectively. MEs and the cationic polymer were found to have skin penetration co-enhancing effect when they were combined in the CPBM system. Furthermore, the CPBM showed a good growth inhibition of E. coli and S. aureus. The stability test revealed that the CPBM was stable at room temperature and 4 °C for a period of three months.
doi_str_mv 10.3109/10717544.2014.898111
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Microemulsion (ME) and cationic polymer based micro-emulgel (CPBM) were investigated for the transdermal delivery of diclofenac sodium (DS). Medium-chain triglyceride was selected as the oil phase of ME due to its good solubilization of DS and high safety. Orthogonal test was applied to optimize the formula of ME based on the cumulative skin permeation amount in vitro after preliminary formula test. Chitosan (CS) or polylysine was employed as the cationic polymer in the formula of CPBM. The transdermal delivery of DS was evaluated through in vitro skin permeation test. The results showed that the skin permeation rate of DS from the optimized CPBM (126.17 ± 15.82 μg/cm 2 /h) were 1.86-folds and 5.76-folds higher than that of DS commercial Emulgel and DS control hydrogel, respectively. MEs and the cationic polymer were found to have skin penetration co-enhancing effect when they were combined in the CPBM system. Furthermore, the CPBM showed a good growth inhibition of E. coli and S. aureus. 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subjects Acrylic Resins - chemistry
Administration, Cutaneous
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Cationic polymer
Cations
Chemistry, Pharmaceutical
Chitosan - chemistry
Chromatography, High Pressure Liquid
Diclofenac - administration & dosage
Diclofenac - pharmacokinetics
diclofenac sodium
Drug Delivery Systems - methods
Emulsions - chemistry
Escherichia coli - drug effects
Gels - chemistry
Hydrogen-Ion Concentration
microemulgel
Microscopy, Electron, Transmission
Polylysine - chemistry
self-preserving
Skin Absorption
Staphylococcus aureus - drug effects
topical administration
Triglycerides - chemistry
Viscosity
title Cationic polymer-based micro-emulgel with self-preserving ability for transdermal delivery of diclofenac sodium
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