Development and characterization of in-situ gel for ophthalmic formulation containing ciprofloxacin hydrochloride

S.B. Makwana, V.A. Patel, S.J. Parmar
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引用次数: 112

Abstract

In situ gels are systems which are applied as solutions or suspensions and are capable of undergoing rapid sol-to-gel transformation triggered by external stimulus such as temperature, pH etc. on instillation. The aim of the present study was to formulate and evaluate pH responsive in-situ gel for ophthalmic delivery. Ciprofloxacin hydrochloride is popularly used as a broad spectrum antibiotic in the treatment of corneal ulcers of ocular infections. However, rapid dilution on instillation, wash out, poor retention of drug concentration delimit the therapeutic benefits of the drug when used in form of conventional eye drops. Sodium alginate, an ophthalmic gel forming mucoadhesive polymer was chosen as polymer which undergoes instantaneous gel formation due to formation of calcium alginate by virtue of its interaction with divalent cation (Ca+2) present in lachrymal fluid. Hydroxy Propyl Methyl Cellulose (HPMC K4M and E5 0LV) was further incorporated as a viscosity enhancer in order to achieve the desired consistency so as to facilitate sustained drug release. The developed formulations were evaluated for clarity, pH measurement, gelling capacity, drug content, rheological study, and in vitro drug release. Thus, in situ gel based systems containing gums can be a valuable approach for ophthalmic drug delivery when compared to conventional systems.

Abstract Image

含盐酸环丙沙星眼药原位凝胶的研制与表征
原位凝胶是作为溶液或悬浮液应用的系统,能够在注入时由外部刺激(如温度、pH等)触发快速的溶胶-凝胶转化。本研究的目的是制备和评价pH响应原位凝胶用于眼科给药。盐酸环丙沙星是一种广泛使用的抗生素,用于治疗角膜溃疡和眼部感染。然而,当以常规滴眼液的形式使用时,注射时稀释迅速,冲洗时药物浓度保留不良,限制了药物的治疗益处。海藻酸钠是一种眼用凝胶型黏附聚合物,通过与泪液中的二价阳离子(Ca+2)相互作用而形成海藻酸钙,从而使海藻酸钠瞬间形成凝胶。进一步加入羟丙基甲基纤维素(HPMC K4M和E5 0LV)作为增粘剂,以达到所需的稠度,从而促进药物的持续释放。对所研制的制剂进行了清晰度、pH测量、胶凝能力、药物含量、流变学研究和体外药物释放的评估。因此,与传统系统相比,含有牙龈的原位凝胶系统可以成为眼科药物输送的一种有价值的方法。
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