Effect of Molecular Weight and Substitution Degree of Chitosan-poly-arginine on in vitro Transdermal Pene-tration Enhancement
- VernacularTitle:相对分子质量及取代度对寡聚精氨酸壳聚糖体外透皮吸收促进作用的影响
- Author:
Wen HE
;
Bei LIU
;
Xianxi GUO
;
Yi TAN
- Publication Type:Journal Article
- Keywords:
Chitosan;
Poly-arginine;
Molecular weight;
Degree of substitution;
Transdermal penetration enhancement
- From:
China Pharmacist
2014;(12):1996-2000
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To study the effect of molecular weight and degree of substitution (DS) of chitosan-poly-arginine (CS-R9) on transdermal penetration enhancement in vitro. Methods:Low molecular CS, medium molecular CS or high molecular CS was respectively used to synthesize CS-R9 with different molecular weight (LCS-R9-1, MCS-R9 and HCS-R9). Low molecular CS was used to synthesize CS-R9 with various degree of substitution by changing the mole ratio between R9 and CS (LCS-R9-1, LCS-R9-2 and LCS-R9-3). The in vitro transdermal penetration enhancement of the different CS-R9 on tinidazole ( TNZ) was studied using Franz diffusion cells. Results:According to the results of FTIR and 1 H-NMR, a series of target CS-R9 were synthesized including LCS-R9-1 with the DS of 2. 30, MCS-R9 with the DS of 2. 17, HCS-R9 with the DS of 2. 20, LCS-R9-2 with the DS of 8. 05 and LCS-R9-3 with the DS of 15. 87. Compared with the blank control group, Azone group, LCS group, R9 group and LCS+R9 group, LCS-R9-1 could enhance the in vitro transdermal penetration of TNZ significantly (P<0. 05). When the DS was unchanged, LCS-R9-1 and HCS-R9 showed similar enhancement in the first 12h, and the effects were both higher than that of MCS-R9 (P<0. 05). The enhancement of HCS-R9 was decreased during 12-24h, while compared with that of LCS-R9-1, the difference was not notable (P>0. 05). When the molecular weight of CS was unchanged, the effect was increased with the rise of DS in the first 21h, however, after that, the effect was decreased with the rise of DS. Conclusion:Molecular weight and DS both have significant effect on the in vitro transdermal penetration enhancement of CS-R9, and it is valuable to further study the in vivo transdermal penetration enhancement of CS-R9 and underlying mechanisms.
