壳聚糖-环糊精接枝物的制备及其对芍药苷经皮渗透作用研究

Preparation of Chitosan-cyclodextrin Graft and Effects on Transdermal Permeation of Paeoniflorin

目的:制备壳聚糖-环糊精接枝物并考察其对芍药苷经皮渗透的促进作用。方法:两步法合成壳聚糖-环糊精接枝物,利用核磁共振和傅里叶变换-红外光谱仪进行表征,元素分析法测定氨基取代度,并以离体大鼠腹皮为渗透屏障,采用Franz扩散池法进行体外透皮试验,以芍药苷24 h内单位面积的累计透过量为评价指标,考察不同浓度接枝物的促渗效果。结果:成功制备出氨基取代度为7%的壳聚糖-环糊精接枝物,不同浓度接枝物对芍药苷经皮渗透的促进作用不同。24 h内,在质量浓度为0.5%的壳聚糖-环糊精存在下,芍药苷单位面积的累计透过量为384.68μg·cm-2,促渗倍数为1.5865。结论:壳聚糖-环糊精接枝物可促进芍药苷经皮渗透,质量浓度为0.5%时效果最佳。

Objective:To prepare chitosan-cyclodextrin grafts and to investigate their facilitating effects on transdermal permeation of paeoniflorin.Methods:Chitosan-cyclodextrin grafts were synthesized in a two-step process,characterized by nuclear magnetic resonance and Fourier transform-infrared spectroscopy,and the degree of amino substitution was determined by elemental analysis.To test the facilitating effects of the grafts,an in vitro transdermal permeation assay was carried out with isolated rat abdominal skins as the permeability barrier in the Franz diffusion cells using the cumulative permeation amount of paeoniflorin per unit area within 24 h as the evaluation index.Results:A chitosan-cyclodextrin graft with 7%amino substitution was successfully prepared,and the transdermal permeation of paeoniflorin was promoted differently by different concentrations of the graft.The cumulative transmittance of paeoniflorin per unit area in the presence of chitosan-cyclodextrin graft at the concentration of 0.5%by mass was 384.68μg·cm^(-2) within 24 h,and the multiplicity of the promotion of the permeation was 1.5865.Conclusion:Chitosan-cyclodextrin graft can promote paeoniflorin transdermal permeation,with the best effect at a mass concentration of 0.5%.