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微囊化技术的最新进展:用于研究口服和透皮药物传递的体内和体外模型。

Advanced progress of microencapsulation technologies: in vivo and in vitro models for studying oral and transdermal drug deliveries.

机构信息

State Key Laboratory of Chirosciences, Department of Applied Biology and Chemical Technology, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.

Centre of Biotechnology, Department of Life Sciences and Biotechnology, University of Ferrara, Ferrara, Italy.

出版信息

J Control Release. 2014 Mar 28;178:25-45. doi: 10.1016/j.jconrel.2013.12.028. Epub 2014 Jan 10.

Abstract

This review provides an overall discussion of microencapsulation systems for both oral and transdermal drug deliveries. Clinically, many drugs, especially proteins and peptides, are susceptible to the gastrointestinal tract and the first-pass metabolism after oral administration while some drugs exhibit low skin permeability through transdermal delivery route. Medicated microcapsules as oral and transdermal drug delivery vehicles are believed to offer an extended drug effect at a relatively low dose and provide a better patient compliance. The polymeric microcapsules can be produced by different microencapsulation methods and the drug microencapsulation technology provides the quality preservation for drug stabilization. The release of the entrapped drug is controlled and prolonged for specific usages. Some recent studies have focused on the evaluation of drug containing microcapsules on potential biological and therapeutic applications. For the oral delivery, in vivo animal models were used for evaluating possible treatment effects of drug containing microcapsules. For the transdermal drug delivery, skin delivery models were introduced to investigate the potential skin delivery of medicated microcapsules. Finally, the challenges and limitations of drug microencapsulation in real life are discussed and the commercially available drug formulations using microencapsulation technology for oral and transdermal applications are shown.

摘要

本文综述了用于口服和透皮药物传递的微胶囊系统。临床上,许多药物,特别是蛋白质和肽类药物,口服后易受到胃肠道和首过代谢的影响,而某些药物经皮给药途径的皮肤透过性较低。载药微胶囊作为口服和透皮药物传递载体,有望以较低的剂量提供延长的药物作用,并提高患者的顺应性。聚合物微胶囊可以通过不同的微囊化方法制备,药物微囊化技术为药物稳定性提供了质量保证。包封药物的释放得到控制和延长,以满足特定用途的需要。一些最近的研究集中在评价含药微胶囊在潜在的生物学和治疗应用方面的作用。对于口服给药,采用体内动物模型来评价含药微胶囊的可能治疗效果。对于透皮药物传递,引入了皮肤传递模型来研究载药微胶囊的潜在皮肤传递。最后,讨论了药物微囊化在实际应用中面临的挑战和局限性,并展示了采用微囊化技术的口服和透皮应用的市售药物制剂。

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