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进一步拧紧螺丝以提高微粒滞留率及相关药物的眼部生物利用度:生物黏附目标。

Turning the screw even further to increase microparticle retention and ocular bioavailability of associated drugs: The bioadhesion goal.

作者信息

Rodríguez Villanueva J, Rodríguez Villanueva L

机构信息

Biomedical Sciences Department, Pharmacy and Pharmaceutical Technology Unit, Pharmacy Faculty, University of Alcalá, Ctra, de Madrid-Barcelona (Autovía A2) Km, 33,600, 28805 Alcalá de Henares, Madrid, Spain.

Pharmacy Faculty, University of Alcalá, Ctra, de Madrid-Barcelona (Autovía A2) Km, 33,600, 28805 Alcalá de Henares, Madrid, Spain.

出版信息

Int J Pharm. 2017 Oct 5;531(1):167-178. doi: 10.1016/j.ijpharm.2017.08.067. Epub 2017 Aug 16.

Abstract

Ocular drug delivery is one of the most fascinating and challenging tasks facing pharmaceutical researchers. Improving drug ocular residence time and/or penetration is complex. Microparticles (MP) provide interesting opportunities to increase ocular bioavailability of drugs and patient compliance brought about by decreased frequency of dosing. However, sustained-release microsphere formulation would fail to accomplish the task of long-lasting drug release unless microspheres remained for a prolonged period at the site of action. Some strategies have been assessed to retain MP at the target site. Among them, improving bioadhesion properties is possibly the one that offers the best technical features to date. In this review, we present the latest scientific communications in the field of MP development and coating to increase bioavailability when MP are destined for ocular treatment. All of these are more or less useful tools that must be considered as an important part of the development process for ocular medication optimization.

摘要

眼部给药是制药研究人员面临的最具吸引力和挑战性的任务之一。提高药物在眼部的停留时间和/或渗透率很复杂。微粒(MP)为提高药物的眼部生物利用度以及因给药频率降低而带来的患者依从性提供了有趣的机会。然而,除非微球在作用部位长时间停留,否则缓释微球制剂将无法完成长效药物释放的任务。已经评估了一些将MP保留在靶部位的策略。其中,改善生物粘附特性可能是迄今为止提供最佳技术特性的策略。在这篇综述中,我们介绍了MP开发和包衣领域的最新科学交流,以提高MP用于眼部治疗时的生物利用度。所有这些或多或少都是有用的工具,必须将其视为眼部药物优化开发过程的重要组成部分。

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