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工程化聚环氧乙烷颊膜与环糊精:一种老辅料的新作用?

Engineering poly(ethylene oxide) buccal films with cyclodextrin: a novel role for an old excipient?

机构信息

Department of Pharmacy, University of Naples Federico II, Via D. Montesano 49, 80131 Naples, Italy.

出版信息

Int J Pharm. 2013 Aug 16;452(1-2):283-91. doi: 10.1016/j.ijpharm.2013.05.030. Epub 2013 May 22.

DOI:10.1016/j.ijpharm.2013.05.030
PMID:23707963
Abstract

Inspired by the multiple roles cyclodextrins can play in polymeric systems, here we engineered poly(ethylene oxide) (PEO) films with (2-hydroxypropyl)-β-cyclodextrin (CD) as multipurpose ingredient. To shed light on the potential of CD in formulating PEO buccal films for the delivery of poorly water-soluble drugs, we preliminarily assessed thermal and mechanical properties as well as wettability of films prepared at different PEO/CD ratios. PEO/CD platform containing 54% by weight of CD was chosen as the optimized composition since it matched acceptable mechanical properties, in terms of tensile strength and elasticity, with a good wettability. The platform was tested as buccal delivery system for triamcinolone acetonide (TrA), a lipophilic synthetic corticosteroid sparely water soluble. Confocal Raman imaging clearly showed that CD was homogeneously (i.e. molecularly) dispersed in PEO. Nevertheless, homogenous drug distribution in the film without TrA crystallization occurred only in the presence of CD. Finally, CD-containing PEO film placed in simulated buccal fluids provided a useful speed-up of TrA release rate while showing slower dissolution as compared to PEO film. These results, as well as compliance with quality specifications of pharmaceutical manufacturing products, strongly support the soundness of the strategy and prompt toward further applications of PEO/CD films in buccal drug delivery.

摘要

受环糊精在聚合物系统中可以扮演多种角色的启发,我们在这里设计了具有(2-羟丙基)-β-环糊精(CD)作为多功能成分的聚环氧乙烷(PEO)薄膜。为了阐明 CD 在配制用于递送至水难溶性药物的 PEO 口腔膜中的潜力,我们初步评估了不同 PEO/CD 比例下制备的薄膜的热性能、机械性能和润湿性。由于其具有可接受的机械性能(拉伸强度和弹性)和良好的润湿性,因此选择含有 54wt%CD 的 PEO/CD 平台作为优化组成。该平台被测试为三氯醋酸泼尼松龙(TrA)的口腔递送系统,TrA 是一种疏水性合成皮质类固醇,水溶性差。共聚焦 Raman 成像清楚地表明 CD 均匀(即分子水平)分散在 PEO 中。然而,只有在存在 CD 的情况下,才能在薄膜中实现药物的均匀分布而无 TrA 结晶。最后,放置在模拟口腔液中的含 CD 的 PEO 薄膜提供了有用的 TrA 释放速率的加速作用,同时与 PEO 薄膜相比显示出较慢的溶解。这些结果以及符合制药产品制造质量规范,强烈支持该策略的合理性,并促使 PEO/CD 薄膜在口腔递药中的进一步应用。

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