眼科药物输送用微粒。

A Joshi
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引用次数: 51

摘要

微颗粒是悬浮在液体载体介质中的含有药物的小聚合颗粒(可蚀性、不可蚀性或离子交换树脂)。颗粒悬浮液在眼内给药后,颗粒停留在给药部位(死囊、结膜下或玻璃体腔),药物通过扩散、化学反应、聚合物降解或离子交换机制从颗粒中释放出来。几种不同的方法已被用于配制用于眼内和局部应用的微颗粒剂型药物。这些包括可降解的微颗粒,膨胀的黏合剂颗粒,pH响应微颗粒,纳米颗粒/乳胶系统,离子交换树脂等。在玻璃体中注射生物可降解的微颗粒治疗后段感染,并释放可接受水平的药物长达两周已被证明。假定药物通过角膜和非角膜途径从局部滴注进入眼睛。体外和体内研究表明,该剂型具有在眼内持续释放药物的良好前景。然而,必须解决几个配方挑战,包括生产稳定的悬浮液,单位体积均匀剂量,有效的药物包裹,可重复性和大规模生产,均匀粒度等。富有成效的解决技术挑战将导致一个优越的剂型为外用和眼内眼科应用。本文综述了微颗粒眼科给药系统的研究进展及未来面临的挑战。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Microparticulates for ophthalmic drug delivery.

Microparticulates are drug-containing small polymeric particles (erodible, non-erodible or ion-exchange resins) that are suspended in a liquid carrier medium. Upon administration of particle suspension in the eye, the particles reside at the delivery site (cul-de-sac, sub conjunctiva or vitreous cavity) and the drug is released from the particles through diffusion, chemical reaction, polymer degradation, or ion-exchange mechanism. Several distinct approaches have been used to formulate drugs in microparticulate dosage form for intraocular and topical application. These include erodible microparticulates, swelling mucoadhesive particulates, pH responsive microparticulates, nanoparticles/latex systems, ion-exchange resins, etc. Injection of bioerodible microparticulates in the vitreous for treating infections of posterior segment and the release of acceptable levels of drug up to two weeks has been demonstrated. Both corneal and non-corneal routes of drug entry in the eye from topical instillations are postulated. The in vitro and in vivo studies have shown that this dosage form holds great promise for sustained drug release in the eye. However, several formulation challenges, including production of stable suspensions, uniform dose per unit volume, efficient drug entrapment, reproducible and large scale manufacturing, uniform particle size, etc., have to be addressed. Fruitful resolution of technological challenges will result in a superior dosage form for both topical and intraocular ophthalmic application. Recent developments and future challenges of microparticulate ophthalmic drug delivery system are discussed in this review.

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