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丹参酮ⅡA纳米结构脂质载体的制备及其体外透皮渗透特性

[Preparation of tanshinone ⅡA loaded nanostructured lipid carrier and its in vitro transdermal permeation characteristics].

作者信息

Zheng Juan, Shen Cheng-Ying, Pang Jian-Yun, Xu Fang-Chu, Liao Wei-Bo, Hu Chun-Xiao, Xu Ping-Hua, Han Jin, Yuan Hai-Long

机构信息

College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

302 Military Hospital of China, Beijing 100039, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2016 Sep;41(17):3232-3238. doi: 10.4268/cjcmm20161718.

DOI:10.4268/cjcmm20161718
PMID:28920375
Abstract

To prepare tanshinone ⅡA loaded nanostructured lipid carrier (Tan ⅡA-NLC), and study its in vitro transdermal permeation characteristics. The Tan ⅡA-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 transdermal permeation of Tan ⅡA-NLC was evaluated by using Franz diffusion cells. The results showed that, the optimal formulation was as follows: drug/lipid materials ratio 88, GMS/MCT ratio 2, emulsifier concentration 1%, average particle size (182±14) nm, polydispersity 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 ⅡA solution, Tan ⅡA-NLC had lower transdermal permeation amount after applying drug for 24 h, but its retention in the epidermis was 3.18 times that of solution. These results indicated that the prepared Tan ⅡA-NLC could effectively increase the regention of Tan ⅡA in the epidermis, and had a broad application prospect.

摘要

制备丹参酮ⅡA纳米结构脂质载体(TanⅡA-NLC),并研究其体外透皮渗透特性。采用高压均质技术制备TanⅡA-NLC,并通过Box-Behnken设计-响应面法进行优化,对其形态、粒径、ζ电位等进行表征。采用Franz扩散池评价TanⅡA-NLC的透皮渗透情况。结果表明,最佳处方为:药物/脂质材料比88,GMS/MCT比2,乳化剂浓度1%,平均粒径(182±14)nm,多分散指数PDI(0.190 6±0.024 5),ζ电位(-27.8±5.4)mV,包封率EE(86.44%±9.26%),载药量DL(0.98%±0.18%)。体外透皮渗透结果显示,与丹参酮ⅡA溶液相比,TanⅡA-NLC给药24 h后的透皮渗透量较低,但其在表皮中的滞留量是溶液的3.18倍。这些结果表明,所制备的TanⅡA-NLC能有效提高丹参酮ⅡA在表皮中的蓄积量,具有广阔的应用前景。

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