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Biodegradable hybrid polymeric membranes for ocular drug delivery.

机译:用于眼部药物递送的可生物降解的混合聚合物膜。

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摘要

Ophthalmic delivery systems such as ocular inserts are useful strategies to improve the ocular bioavailability of topically administered drugs. In the present study polyvinyl alcohol and sodium carboxymethylcellulose based ocular inserts were prepared by solution casting for sustained drug delivery of ciprofloxacin for treatment of topical infections. The polymers were esterified and the formation of ester bonds was confirmed by Fourier transform infrared spectroscopy. The inserts had a smooth structure with a surface roughness of 7.3 nm. Inserts were found to be wettable by simulated tear fluid with contact angle <45 degrees . Mechanical testing results indicated that the tensile strength of polyvinyl alcohol-sodium carboxymethylcellulose (10:2 wt.%) inserts was up to 8.9 + or - 1.9 MPa, which is adequate to resist the pressure likely to be exerted during application. In vitro drug release kinetics showed sustained release of ciprofloxacin for up to 48 h from the inserts. Sodium fluorescein-loaded inserts showed higher penetration of the dye in the posterior segment tissues of explanted goat eye balls as compared with an eye drop solution of sodium fluorescein. The inserts were non-toxic to corneal epithelial cells and showed no signs of acute ocular toxicity in in vivo studies in albino rabbits.
机译:眼科递送系统,例如眼用插入物,是改善局部给药药物的眼生物利用度的有用策略。在本研究中,通过溶液流延制备基于环丙沙星的持续药物递送的聚乙烯醇和基于羧甲基纤维素钠的眼用插入物,以治疗局部感染。将聚合物酯化,并通过傅里叶变换红外光谱法确认酯键的形成。刀片具有表面粗糙度为7.3 nm的光滑结构。发现插入物可被接触角<45度的模拟泪液润湿。机械测试结果表明,聚乙烯醇-羧甲基纤维素钠(10:2 wt。%)插入物的拉伸强度高达8.9或-1.9 MPa,足以抵抗施加过程中可能施加的压力。体外药物释放动力学表明环丙沙星从插入物中持续释放长达48小时。与荧光素钠的滴眼液相比,装有荧光素钠的插入物显示出染料在植入的山羊眼球的后节组织中的渗透性更高。插入物对角膜上皮细胞无毒,在白化病兔子的体内研究中没有显示出急性眼毒性的迹象。

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