Comparative study of liposomes and liposomes-in-polymer hydrogel as transdermal carriers for improving the topical delivery of imperatorin

BAN Junfeng,MO Zhenjie,…,LV Zhufen*

[Abstract]Objective A novel imperatorin (IMP)-liposome-hydrogel formulation was developed to increase skin permeation efficiency and improve the bioavailability of IMP after topical delivery. Methods IMP loading into liposomes was optimized, and liposomes were entrapped in a polymer hydrogel consisting of carbomer. Liposomes were also used as a control formulation. The physical properties and percent encapsulation efficiency were evaluated. The adhesive strength of the gel was tested. The in vitro percutaneous permeability, percutaneous penetration mechanism, and irritant evaluation were investigated. Results Compared to liposomes, the preparation of IMP-liposomes-gel has excellent adhesion properties and sustained drug release on the skin surface. Conclusion These findings suggest developing liposome gels for potential percutaneous drug carrier systems.

[Key words] Imperatorin;  Liposomes;  Liposome gel;  Encapsulation efficiency;  Percutaneous penetration mechanism; Irritant evaluation

欧前胡素脂质体及其凝胶局部经皮递药的比较研究

[摘要]目的 以中药白芷中的有效成分欧前胡素为模型药物，制备其脂质体及脂质体-水凝胶新剂型，以期提高局部用欧前胡素的经皮渗透效率和生物利用度。方法 以欧前胡素脂质体为对照。对欧前胡素脂质体及脂质体-水凝胶的物理性能、包封率、凝胶的胶凝强度，体外透皮性、透皮机制及刺激性进行评价。结果 与脂质体相比，制备的欧前胡素-脂质体-水凝胶具有良好的皮肤表面黏附性能和药物渗透性。结论 以脂质体水凝胶有望成为复方中药经皮递药的新型载体。

[关键词]欧前胡素； 脂质体； 脂质体水凝胶； 经皮递药； 刺激性评价