Study on Penetration Effect of N-trimethyl Chitosan
HE Wen1,ZHANG Mian2,DAI Wen-bing2,WU Yan3
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1.Department of Pharmacy of Renmin Hospital of Wuhan University,Wuhan 430060,China;2.Department of Pharmacy,Wuhan University,Wuhan 430072,China;3.Institude of Pharmacology and Toxicology,Academy of Military Medical Sciences, Beijing 100850,China
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History+
Received
Published
2005-06-16
2006-04-05
Issue Date
2006-04-05
Abstract
OBJECTIVE To study the penetration effect of N-trimethyl chitosan(TMC) and its penetration mechanism.METHODS TMC60 was synthesized by a two-step method using chitosan and methyl-iodide.The degree of quaternization of TMC was determined by 1H-NMR.Attenuated total reflection-fourier transform infrared spectroscopy(ATR-FTIR),combined with the technique of deconvolution was used to study the protein conformation of stratum corneum.The 12 h cumulative penetration was determined on mice skin using testosterone as model drug and azone as comparison.RESULTS The quaternization degree of TMC60 was 67.2%.ATR-FTIR spectra showed that amide II absorption peak of keratin shifted from 1 538.7 cm-1 to 1 536.8 cm-1 after the treatment with TMC60.TMC60 changed the keratin conformation from α-helix to β-sheet or random coil leading to a loose keratin structure,therefore reduced the drug transdermal delivery barrier.The cumulative penetration and the steady penetration rate of TMC60 were both higher than the control sample and the sample treated by Azone(P<0.05).CONCLUSION The results suggest that TMC60 is a potential penetration enhancer for transdermal therapeutic systems.The mechanism is correlated with the influence of TMC60 on keratin.
HE Wen;ZHNG Min;DI Wen-ing;WU Yn.
Study on Penetration Effect of N-trimethyl Chitosan [J]. Chinese Pharmaceutical Journal, 2006, 41(07): 519-522
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