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丹参酮ⅡA纳米结构脂质载体的处方优化及其体外透皮研究
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摘要
为研制丹参酮ⅡA纳米结构脂质载体(Tan ⅡA-NLC),并进行体外透皮研究。本文采用高压均质技术制备Tan ⅡA-NLC,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 HA-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 ⅡA-NLC粒径为182±14 nm,多分散指数(PDI)为0.1906±0.0245,Zeta电位-27.8±5.4 mV,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TanⅡA-NLC的24h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。Tan ⅡA-NLC可有效提高Tan ILA在表皮层的滞留量,具有广阔的应用前景。
To prepare Tan ⅡA loaded nanostructured lipid carrier(Tan ⅡA-NLC),and to study its in vitro skin distribution.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,etc.The transdermal absorption of Tan DA-NLC was evaluated using Franz difiusion cells.The results showed that,the average particle size,PDI,zeta potential,EE and DL of Tan ⅡA-NLC prepared by optimal formulation(the drug/lipid materials ratio was 88,GMS/MCT ratio was 2,and emulsifier concentration was 1%) was.182 ± 14 nm,0.1906 ± 0.0245,-27.8± 5.4 mV,86.44 ± 9.26%,and 0.98 ± 0.18%,respectively.Compared with Tan ⅡA solution,Tan HA loaded NLC had lower amounts of Tan IIA penetrating through the skin after applying drug for 24 h,but had a 3.18 fold higher retention in the epidermis.These results indicate that the prepared Tan ⅡA-NLC has the ability to increase drug concentration in the epidermis,and has a broad application prospects.
引文
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