A Biomimetic Chitosan Derivates: Preparation, Characterization and Transdermal Enhancement Studies of N-Arginine Chitosan

Molecules

Hui-Xia Lv¹  Zhen-Hai Zhang¹  Xiao-Pan Wang¹  Qing-Qing Cheng¹  Wei Wang¹  Xu-Hui Huang¹  Jian-Ping Zhou¹  Qiang Zhang¹  Lu-Lu Hou¹ 

[1] ¹Department of Pharmaceutics, China Pharmaceutical University, No. 24 tongjiaxiang Nanjing, China

关键词: biomimetic chitosan derivates;    arginine-rich;    cell penetration peptides;    N-arginine chitosan;    transdermal enhancer;    adefovir;   

DOI  :  10.3390/molecules16086778

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.