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基于刺槐豆胶的原位凝胶的研制及其用于治疗细菌性角膜炎的氧氟沙星眼部给药系统的评价。

Development and evaluation of locust bean gum based in situ gel for ocular delivery of ofloxacin for treatment of bacterial keratitis.

机构信息

Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, West Bengal, India.

NSHM Knowledge Campus, Kolkata-Group of Institutions, 124 BL Saha Road, Kolkata 700053, West Bengal, India.

出版信息

Int J Biol Macromol. 2024 Nov;281(Pt 2):136374. doi: 10.1016/j.ijbiomac.2024.136374. Epub 2024 Oct 8.

Abstract

One of the drawbacks of conventional ocular dosage forms is their short residence time in the eye. To address this, we propose an ocular in situ gel that adheres to the eye surface for a prolonged period. Locust bean gum (LBG), a galactomannan polysaccharide, exhibits the desired characteristics to serve as a drug carrier for ocular application. However, the gum has not yet been investigated for ocular drug delivery. In this work, we have developed an LBG based in situ gel loaded with ofloxacin and evaluated its drug delivery efficacy through in vitro and ex vivo tests. To confer temperature sensitivity, LBG was grafted with N-isopropyl acrylamide (NIPAAm), and a series of solutions were made with ofloxacin (0.03 % w/v). The solution turned into a gel when the temperature was raised to 37 °C. The safety and efficacy of the developed in situ gels were validated through experiments on rat eyes infected with clinical strains of bacteria. The developed keratitis was completely healed indicating that the grafted LBG can be used as a potential candidate for the development of ocular in situ gel.

摘要

常规眼部剂型的一个缺点是它们在眼部的停留时间短。为了解决这个问题,我们提出了一种眼部原位凝胶,它可以在眼表面长时间附着。刺槐豆胶(LBG)是一种半乳甘露聚糖多糖,具有作为眼部应用药物载体的理想特性。然而,该胶还没有被用于眼部药物输送的研究。在这项工作中,我们开发了一种载有氧氟沙星的基于 LBG 的原位凝胶,并通过体外和离体试验评估了其药物输送效果。为了赋予温度敏感性,将 LBG 与 N-异丙基丙烯酰胺(NIPAAm)接枝,并制备了一系列含有氧氟沙星(0.03%w/v)的溶液。当温度升高到 37°C 时,溶液变成凝胶。通过对感染临床细菌株的大鼠眼睛进行实验,验证了所开发的原位凝胶的安全性和有效性。开发的角膜炎完全愈合,表明接枝的 LBG 可用作开发眼部原位凝胶的潜在候选物。

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