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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Improved bioavailability of orally delivered insulin using Eudragit-L30D coated PLGA mieroparticles
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Improved bioavailability of orally delivered insulin using Eudragit-L30D coated PLGA mieroparticles

机译：使用Eudragit-L30D涂层PLGA微粒改善口服胰岛素的生物利用度

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Large porous mieroparticles of PLGA entrapping insulin were prepared by solvent evaporation method and evaluated in diabetes induced rat for its efficacy in maintaining blood sugar level from a single oral dose. Incorporation of Eudragit L30D (0.03% w/v) in the external aqueous phase resulted in formation of pH responsive enteric coated polymer particles which release most of the entrapped insulin in alkaline pH. At acidic pH, release of insulin from uncoated PLGA mieroparticles and Eudragit L30D coated PLGA mieroparticles was 31.62±1.8% and 17.5±1.29%, respectively, for initial 30min. However, in 24h, in vitro released insulin from uncoated PLGA and Eudragit coated particles was 96.29±1.01% and 88.30±1%, respectively. Released insulin from composite polymer particles were mostly in monomer form without aggregation and was stable for a month at 37℃. Oral administration of insulin loaded PLGA (50: 50) and Eudragit L30D coated PLGA (50:50) mieroparticles (equivalent to 25IU insulin/kg of animal weight) in alloxan induced diabetic rats resulted in 37.3±11% and 62.7±3.8% reduction in blood glucose level, respectively, in 2h. This effect continued up to 24h in the case of Eudragit L30D coated PLGA mieroparticles. Results demonstrate that use of stabilizers during PLGA particle formulation, large porous particle for quick release of insulin and coating with Eudragit L30D resulted in a novel oral formulation for once a day delivery of insulin.
机译：通过溶剂蒸发法制备了包埋有PLGA胰岛素的大多孔微粒，并在糖尿病诱导的大鼠中评估了单次口服剂量维持血糖水平的功效。在外部水相中加入Eudragit L30D（0.03％w / v）导致形成pH响应型肠溶衣聚合物颗粒，从而在碱性pH下释放出大部分被包裹的胰岛素。在酸性pH值下，最初30分钟内，未包衣的PLGA微粒和Eudragit L30D包衣的PLGA微粒的胰岛素释放分别为31.62±1.8％和17.5±1.29％。然而，在24小时内，未包被PLGA和Eudragit包被颗粒的体外释放胰岛素分别为96.29±1.01％和88.30±1％。从复合聚合物颗粒中释放的胰岛素主要为单体形式，没有聚集，并且在37℃下稳定一个月。在四氧嘧啶诱发的糖尿病大鼠中口服给予胰岛素负载的PLGA（50：50）和Eudragit L30D包被的PLGA（50:50）微粒（相当于25IU胰岛素/ kg动物体重），导致减少37.3±11％和62.7±3.8％血糖水平分别在2h内。对于Eudragit L30D包衣的PLGA微粒，这种效果持续长达24小时。结果表明，在PLGA颗粒配制过程中使用稳定剂，快速释放胰岛素的大多孔颗粒并用Eudragit L30D包衣可产生每天口服一次胰岛素的新型口服制剂。

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