Pang Jian-Yun, Liu Xiao, Shen Bao-de, Shen Cheng-Ying, Lian Wang-Quan, Liu Juan, Hu Chun-Xiao, Zhong Rui-Na, Xu Run-Chun, Yuan Hai-Long
College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.
Department of Pharmacy, Air Force General Hospital, PLA, Beijing 100142, China.
Zhongguo Zhong Yao Za Zhi. 2017 Jul;42(13):2473-2478. doi: 10.19540/j.cnki.cjcmm.20170507.001.
To increase the permeation and retention of isopsoralen in skin, and improve its bioavailability.Isopsoralen loaded nanostructure liquid carrier (IPRN-NLC) was prepared by high pressure homogenization andoptimized by orthogonal experiment with the encapsulation efficiency, drug loading and average particle size as the evaluation indexes. The in vitro transdermal permeation of IPRN-NLC was evaluated by Franze diffusion cells.The results showed that solid-liquid lipid ratio of optimum IPRN-NLC formulation was 7∶3,drug-lipid ratio of 1∶30, 1% surfactant. Under these conditions, IPRN-NLC had an average encapsulation of （90.25±0.73）%,drug loading of （1.56±0.27）% and an average particle size of (305±1.57) nm.The in vitro transdermal permeation results showed that IPRN-NLC could increase the amount of IPRN permeated though skin, with 3 times of the epidermal retention as compared with IPRN solution. From the results we can know that the IPRN-NLC prepared by high pressure homogenization can improve the permeation andaccumulation of IPRN in the skin, with wide application prospects in the field of transdermal administration.
为提高异补骨脂素在皮肤中的渗透和滞留率，并改善其生物利用度。采用高压均质法制备了载异补骨脂素纳米结构脂质载体（IPRN-NLC），并以包封率、载药量和平均粒径为评价指标，通过正交试验进行优化。采用Franze扩散池评价IPRN-NLC的体外透皮性能。结果表明，最佳IPRN-NLC制剂的固液脂质比为7∶3，药物脂质比为1∶30，表面活性剂用量为1%。在此条件下，IPRN-NLC的平均包封率为（90.25±0.73）%，载药量为（1.56±0.27）%，平均粒径为（305±1.57）nm。体外透皮试验结果表明，IPRN-NLC可增加异补骨脂素透过皮肤的量，其表皮滞留量是异补骨脂素溶液的3倍。结果表明，高压均质法制备的IPRN-NLC可提高异补骨脂素在皮肤中的渗透和蓄积，在透皮给药领域具有广阔的应用前景。
