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眼科药物递送系统——最新进展

Ophthalmic drug delivery systems--recent advances.

作者信息

Bourlais C L, Acar L, Zia H, Sado P A, Needham T, Leverge R

机构信息

Laboratoire de Pharmacie Galénique, Biopharmacie et Pharmacie Clinique, Faculté de Pharmacie, Université de Rennes, France.

出版信息

Prog Retin Eye Res. 1998 Jan;17(1):33-58. doi: 10.1016/s1350-9462(97)00002-5.

Abstract

Eye-drops are the conventional dosage forms that account for 90% of currently accessible ophthalmic formulations. Despite the excellent acceptance by patients, one of the major problems encountered is rapid precorneal drug loss. To improve ocular drug bioavailability, there is a significant effort directed towards new drug delivery systems for ophthalmic administration. This chapter will focus on three representative areas of ophthalmic drug delivery systems: polymeric gels, colloidal systems, cyclodextrins and collagen shields. Hydrogels generally offer a moderate improvement of ocular drug bioavailability with the disadvantage of blurring of vision. In situ activated gel-forming systems are preferred as they can be delivered in drop form with sustained release properties. Colloidal systems including liposomes and nanoparticles have the convenience of a drop, which is able to maintain drug activity at its site of action and is suitable for poorly water-soluble drugs. Among the new therapeutic approaches in ophthalmology, cyclodextrins represent an alternative approach to increase the solubility of the drug in solution and to increase corneal permeability. Finally, collagen shields have been developed as a new continuous-delivery system for drugs that provide high and sustained levels of drugs to the cornea, despite a problem of tolerance. It seems that new tendency of research in ophthalmic drug delivery systems is directed towards a combination of several drug delivery technologies. There is a tendency to develop systems which not only prolong the contact time of the vehicle at the ocular surface, but which at the same time slow down the elimination of the drug. Combination of drug delivery systems could open a new directive for improving results and the therapeutic response of non-efficacious systems.

摘要

眼药水是传统剂型,占目前可得眼科制剂的90%。尽管患者接受度良好,但遇到的主要问题之一是药物在角膜前迅速流失。为提高眼部药物生物利用度,人们在致力于开发用于眼部给药的新型药物递送系统。本章将聚焦于眼部药物递送系统的三个代表性领域:聚合物凝胶、胶体系统、环糊精和胶原盾。水凝胶通常能适度提高眼部药物生物利用度,但缺点是会导致视力模糊。原位激活凝胶形成系统更受青睐,因为它们可以以滴剂形式给药并具有缓释特性。包括脂质体和纳米颗粒在内的胶体系统具有滴剂的便利性,能够在作用部位维持药物活性,适用于水溶性差的药物。在眼科新的治疗方法中,环糊精是增加药物在溶液中的溶解度和提高角膜通透性的一种替代方法。最后,胶原盾已被开发为一种新的药物持续递送系统,尽管存在耐受性问题,但能为角膜提供高且持续的药物水平。眼科药物递送系统的新研究趋势似乎是朝着几种药物递送技术的组合发展。有一种开发系统的趋势,这种系统不仅能延长载体在眼表的接触时间,同时还能减缓药物的消除。药物递送系统的组合可能为改善无效系统的效果和治疗反应开辟新的方向。

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