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A Biomimetic Chitosan Derivates: Preparation, Characterization and Transdermal Enhancement Studies of N-Arginine Chitosan
Department of Pharmaceutics, China Pharmaceutical University, No. 24 tongjiaxiang Nanjing, China
Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing, No. 100 shizhijie Nanjing, China
Department of Pharmacy, Fujian Provincial Hospital, China. No.134 dongjie Fuzhou, China
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, No.38 Xueyuan Road Haidian District, Beijing, China
Jiangxi Xierkangtai Pharmaceutical Co. Ltd., North Zone, High-New Technology Industrial Zone, Pingxiang, Jiangxi, China
These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
Received: 11 July 2011; in revised form: 25 July 2011 / Accepted: 1 August 2011 / Published: 9 August 2011
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.
Keywords: biomimetic chitosan derivates; arginine-rich; cell penetration peptides; N-arginine chitosan; transdermal enhancer; adefovir
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Lv, H.-X.; Zhang, Z.-H.; Wang, X.-P.; Cheng, Q.-Q.; Wang, W.; Huang, X.-H.; Zhou, J.-P.; Zhang, Q.; Hou, L.-L.; Huo, W. A Biomimetic Chitosan Derivates: Preparation, Characterization and Transdermal Enhancement Studies of N-Arginine Chitosan. Molecules 2011, 16, 6778-6790.
Lv H-X, Zhang Z-H, Wang X-P, Cheng Q-Q, Wang W, Huang X-H, Zhou J-P, Zhang Q, Hou L-L, Huo W. A Biomimetic Chitosan Derivates: Preparation, Characterization and Transdermal Enhancement Studies of N-Arginine Chitosan. Molecules. 2011; 16(8):6778-6790.
Lv, Hui-Xia; Zhang, Zhen-Hai; Wang, Xiao-Pan; Cheng, Qing-Qing; Wang, Wei; Huang, Xu-Hui; Zhou, Jian-Ping; Zhang, Qiang; Hou, Lu-Lu; Huo, Wei. 2011. "A Biomimetic Chitosan Derivates: Preparation, Characterization and Transdermal Enhancement Studies of N-Arginine Chitosan." Molecules 16, no. 8: 6778-6790.