摘要
为研制丹参酮Ⅱ_A纳米结构脂质载体(Tan Ⅱ_A-NLC),并进行体外透皮研究。该文采用高压均质技术制备Tan Ⅱ_ANLC,运用Box-Behnken设计-效应面法优化处方,并对其进行表征。采用Franze扩散池法评价Tan Ⅱ_A-NLC体外透皮性能。结果显示,以最优处方:脂药比为88、固液脂质比为2、稳定剂用量为1%,制得的Tan Ⅱ_A-NLC粒径为(182±14)nm,多分散指数(PDI)为0.190 6±0.024 5,Zeta电位(-27.8±5.4)m V,包封率(EE)为86.44%±9.26%,载药量(DL)为0.98%±0.18%;体外透皮吸收实验结果显示Tan Ⅱ_A-NLC的24 h药物累积透皮量低于溶液,但其在表皮中的滞留量是溶液的3.18倍。TanⅡ_A-NLC可有效提高Tan Ⅱ_A在表皮层的滞留量,具有广阔的应用前景。
To prepare tanshinone Ⅱ A loaded nanostructured lipid carrier （ Tan ⅡA-NLC） , and study its in vitro transdermal per- meation characteristics. The Tan U Ⅱ-NLC was prepared by high pressure homogenization technology and optimized by Box-Behnken design-response surface method, and it was characterized in terms of morphology, particle size, zeta potention, et al. The transdermai permeation of Tan Ⅱ A-NLC was evaluated by using Franz diffusion cells. The resuhs showed that, the optimal formulation was as fol- lows： drug/lipid materials ratio 88, GMS/MCT ratio 2, emulsifier concentration 1%, average particle size （182 ± 14） nm, polydis- persity index PDI （0. 190 6 ±0. 024 5）, zeta potential （ -27.8 ± 5.4） mV, encapsulation efficiency EE （86.44% ±9. 26% ） and drug loading DL （0. 98%± 0. 18% ）, respectively. The in vitro transdermal permeation results showed that as compared with Tan Ⅱ A solution, Tan Ⅱ A-NLC had lower transdermal permeation amount after applying drug for 24 h, but its retention in the epidermis was3. 18 times that of solution. These results indicated that the prepared Tan Ⅱ A-NLC could effectively increase the regention of Tan Ⅱ A in the epidermis, and had a broad application prospect.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2016年第17期3232-3238,共7页
China Journal of Chinese Materia Medica
基金
国家自然科学基金项目(81573696)
