渗透促进剂与眼部生物黏附剂:眼科药物递送的两条新途径。

Penetration enhancers and ocular bioadhesives: two new avenues for ophthalmic drug delivery.

作者信息

Kaur Indu Pal, Smitha R

机构信息

University Institute of Pharmaceutical Sciences, Punjab University, Chandigarh, India.

出版信息

Drug Dev Ind Pharm. 2002 Apr;28(4):353-69. doi: 10.1081/ddc-120002997.

Abstract

This review is focused on the two avenues of development that promise a major impact on future ocular drug therapeutics: bioadhesives, including hydrogels and other agents like carbopols, polyacrylic acids, chitosan, etc., and penetration enhancers, including different surfactants, calcium chelators, etc. The capacity of some polymers to adhere to the mucin coat covering the conjunctiva and the corneal surface of the eye forms the basis for ocular mucoadhesion. These systems markedly prolong the residence time of a drug in the conjunctival sac, since clearence is now controlled by the much slower rate of mucus turnover rather than the tear turnover rate. But improving the corneal drug retention alone is inadequate in bringing about a significant improvement of drug bioavailability. Another approach consists of transiently increasing the pentration characteristics of the cornea with appropriate substances, known as penetration enhancers or absorption promoters. The main aim of this article is to give an insight into the potential application of mucoadhesives and corneal penetration enhancers for the conception of innovative opthalmic delivery appraoches, to decrease the systemic side effects, and create a more focused effect, which may be achieved with lower doses of the drug. Ophthalmic formulations based on these mucoadhesives and penetration enhancers are simple to manufacture and exhibit an excellent tolerance when administered into the cornea. The use of the former considerably prolongs the corneal contact time and the use of the latter increases the rate and amount of drug transport. The various corneal epithelial barriers along with the major routes of transport of drugs are discussed. The article includes a list of the various substances in use or under investigation for the aforementioned properties, along with their mechanisms of action. A fair appraisal of the subject with regard to these two therapeutic approaches and any expected ill effects has been made.

摘要

本综述聚焦于有望对未来眼部药物治疗产生重大影响的两条发展途径

生物黏附剂,包括水凝胶以及卡波姆、聚丙烯酸、壳聚糖等其他制剂,和渗透促进剂,包括不同的表面活性剂、钙螯合剂等。一些聚合物黏附于覆盖眼睛结膜和角膜表面的黏液层的能力构成了眼部黏膜黏附的基础。这些系统显著延长了药物在结膜囊内的停留时间,因为清除现在由慢得多的黏液周转速率而非泪液周转速率控制。但仅改善角膜药物滞留不足以显著提高药物生物利用度。另一种方法是用适当的物质(称为渗透促进剂或吸收促进剂)短暂增加角膜的渗透特性。本文的主要目的是深入了解生物黏附剂和角膜渗透促进剂在创新眼科给药方法概念中的潜在应用,以减少全身副作用,并产生更有针对性的效果,这可以通过较低剂量的药物实现。基于这些生物黏附剂和渗透促进剂的眼科制剂易于制造,并且在角膜给药时表现出优异的耐受性。前者的使用显著延长了角膜接触时间,后者的使用增加了药物转运的速率和量。文中讨论了各种角膜上皮屏障以及药物的主要转运途径。本文列出了因上述特性正在使用或正在研究的各种物质及其作用机制。对这两种治疗方法以及任何预期的不良影响进行了公正的评估。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索