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基于明胶和蜗牛黏液的新型载药成膜贴剂。

Novel drug-loaded film forming patch based on gelatin and snail slime.

机构信息

Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126, Italy.

Department of Pharmacy and BioTechnology, University of Bologna, Via S. Donato 19/2, 40127, Italy.

出版信息

Int J Pharm. 2021 Apr 1;598:120408. doi: 10.1016/j.ijpharm.2021.120408. Epub 2021 Feb 27.

DOI:10.1016/j.ijpharm.2021.120408
PMID:33647415
Abstract

Gelatin-based films enriched with snail slime are proposed as novel biodegradable and naturally bioadhesive patches for cutaneous drug delivery. Films (thickness range 163-248 μm) were stretchable and they adhered firmly onto the wetted skin, especially those with high amount (70% V/V) of snail slime extract. Fluconazole was selected as model drug and added to films containing the highest amount of snail slime. The presence of Fluconazole (4.53 ± 0.07% w/w) did not modify significantly the mechanical properties, the swelling degree and the bioadhesive performances of the films. Structural investigations demonstrated that the crystalline form III of the drug changed to the amorphous one, forming an amorphous solid dispersion. Moreover, snail slime prevented the drug recrystallization over time. In vitro permeation studies showed that film exhibited a cumulative drug concentration (over 60% in 24 h) similar to that of the control solution containing 20% w/V of ethanol. Fluconazole-loaded gelatin films proved to be effective towards clinical isolates of Candida spp. indicating that the drug maintained its remarkable antifungal activity once formulated into gelatin and snail slime-based films. In conclusion, snail slime, thanks to its peculiar composition, has proved to be responsible of optimal skin adhesion, film flexibility and of the formation of a supersaturating drug delivery system able to increase skin permeation.

摘要

以明胶为基质的富含蜗牛黏液的薄膜被提议作为新型可生物降解和天然生物粘附贴片,用于经皮药物传递。这些薄膜(厚度范围为 163-248μm)具有拉伸性,并且能够牢固地粘附在湿润的皮肤上,尤其是那些含有高浓度(70%V/V)蜗牛黏液提取物的薄膜。氟康唑被选为模型药物,并添加到含有最高浓度蜗牛黏液的薄膜中。氟康唑的存在(4.53±0.07%w/w)并没有显著改变薄膜的机械性能、溶胀程度和生物粘附性能。结构研究表明,药物的晶型 III 转变为无定形,形成无定形固体分散体。此外,蜗牛黏液阻止了药物随时间的再结晶。体外渗透研究表明,薄膜在 24 小时内显示出相似的累积药物浓度(超过 60%),类似于含有 20%w/V 乙醇的对照溶液。载氟康唑的明胶薄膜对临床分离的念珠菌属表现出有效,表明药物一旦制成明胶和蜗牛黏液基薄膜,就保持了其显著的抗真菌活性。总之,蜗牛黏液由于其特殊的组成,被证明对最佳皮肤粘附、薄膜柔韧性以及形成超饱和药物传递系统具有重要作用,能够增加皮肤渗透。

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