咪喹莫特负载壳聚糖膜的设计、制备与表征及其经皮给药系统

Design, Development, and Characterization of Imiquimod-Loaded Chitosan Films for Topical Delivery.

机构信息

Department of Experimental and Clinical Pharmacology, College of Pharmacy, University of Minnesota, 308 Harvard Street SE, Minneapolis, Minnesota, 55455, USA.

Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 308 Harvard Street SE, Minneapolis, Minnesota, 55455, USA.

出版信息

AAPS PharmSciTech. 2019 Jan 8;20(2):58. doi: 10.1208/s12249-018-1288-5.

DOI:10.1208/s12249-018-1288-5

PMID:30623265

Abstract

Aldara™ (5% w/w imiquimod) topical cream is approved by the US FDA for the treatment of superficial basal cell carcinoma. However, the cream formulation suffers from dose variability, low drug availability due to the incomplete release, and poor patient compliance. To achieve sustained and complete release of imiquimod, chitosan films were prepared by casting using propylene glycol as a plasticizer. Chitosan films had appropriate physicochemical characteristics for wound dressing and excellent content uniformity and maintained the original physical form of imiquimod. Films were capable of releasing a defined dose of imiquimod over a period of 7 days. The bioactivity of imiquimod was not affected by its entrapment in chitosan matrix as indicated by the results of in vitro growth inhibition assay. In addition, the film formulation showed significantly (p ˂ 0.05) higher drug accumulation in the skin when compared to commercial cream formulation.

摘要

Aldara™（5%咪喹莫特乳膏）获得美国食品药品监督管理局批准，用于治疗表浅基底细胞癌。然而，该乳膏制剂存在剂量变异性、由于不完全释放导致药物利用率低以及患者顺应性差等问题。为了实现咪喹莫特的持续和完全释放，采用丙二醇作为增塑剂，通过浇铸法制备壳聚糖膜。壳聚糖膜具有适合伤口敷料的理化特性，并且药物含量均匀，保持了咪喹莫特的原始物理形态。膜能够在 7 天的时间内释放出规定剂量的咪喹莫特。体外生长抑制试验结果表明，咪喹莫特被包封在壳聚糖基质中并不会影响其生物活性。此外，与商业乳膏制剂相比，该膜制剂在皮肤中的药物蓄积量显著更高（p ˂ 0.05）。