已发表论文

挥发油调控的甘油脂质体用于促进芍药苷 (Paeoniflorin) 的经皮渗透:处方优化、表征以及离体与在体评价

 

Authors Zhang K, Zhang Y, Li Z, Li N, Feng N

Received 28 February 2017

Accepted for publication 18 April 2017

Published 5 May 2017 Volume 2017:12 Pages 3521—3532

DOI https://doi.org/10.2147/IJN.S135749

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Alexander Kharlamov

Peer reviewer comments 2

Editor who approved publication: Dr Linlin Sun

摘要:本研究制备了一种挥发油调控的新型甘油脂质载体,用其包载芍药苷,以促进芍药苷的经皮渗透,并提高药物在滑膜中的滞留量。本研究采用均匀设计来优化甘油脂质体处方,最终处方包含 5% (w/v) 大豆卵磷脂,0.6% (w/v) 胆固醇与 10% (v/v) 甘油,并加入 2% (v/v) 的透骨草挥发油作为促透剂。挥发油甘油脂质体的体外经皮渗透速率分别为普通甘油脂质体、脂质体与酊剂的 1.4 倍、1.6 倍与 1.7 倍。在体试验表明,与普通甘油脂质体相比,挥发油甘油脂质体可使芍药苷的滑膜滞留量提升 3.1 倍。在体小动物成像试验表明给药 小时后,装载了 Cy5.5 的甘油脂质体在裸鼠膝关节处的荧光强度为普通脂质体的 1.8 倍。透骨草挥发油调控的甘油脂质体展现出良好的经皮渗透性能,并可促进药物在滑膜的滞留,表明其可作为芍药苷的经皮给药载体,用于滑膜病变诱发的类风湿关节炎的治疗。
Keywords: paeoniflorin, transdermal, glycerosomes, liposomes, permeation enhancers, essential oil