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使用化学改性瓜尔胶共聚物开发用于肠道药物递送的pH敏感纳米颗粒。

Development of pH Sensitive Nanoparticles for Intestinal Drug Delivery Using Chemically Modified Guar Gum Co-Polymer.

作者信息

Varma Vegesna Naga Sravan Kumar, Shivakumar Hosakote Gurumalappa, Balamuralidhara Veerna, Navya Manne, Hani Umme

机构信息

Department of Pharmaceutics, JSS College of Pharmacy, JSS University, Mysore, Karnataka-570015, India.

出版信息

Iran J Pharm Res. 2016 Winter;15(1):83-94.

Abstract

The aim of the research work was to chemically modify guargum (GG) as a pH sensitive co-polymer and formulating intestinal targeting ESO nanoparticles (NPs) using the synthesized co-polymer. Poly acrylamide-grafted-guar gum (PAAm-g-GG) co-polymer was synthesized by free radical polymerization. Chemical modification of PAAm-g-GG by alkaline hydrolysis results in formation of a pH-sensitive co-polymer. The effect of GG and acryl amide (AAm) on grafting was studied. Esomeprazole magnesium (ESO) loaded pH sensitive NPs were prepared by nano-emulsification polymer crosslinking method and characterized. Sixteen formulations were prepared and the concentration of process variables wasvaried to obtain nanoparticles of 200-600 nm. The NPs were found to be homogenous in size distribution. The encapsulation efficiency and drug loading ranged from 33.2% to 50.1% and 12.2% to 17.2% respectively. Particle size, encapsulation efficiency and drug loading increasedalong with co-polymer concentration. In-vitro release studies at pH 1.2 for 2 h, followed by pH 6.8 showed that environment pH significantly affected the drug release. SEM has shown that NPsare spherical with smooth surface. The pH sensitive PAAm-g-GGNPs resisted the initial release of the drug from the drug loaded NPs in acidic pH and delayed the release process to a longer period in alkaline environment.

摘要

该研究工作的目的是对瓜尔胶(GG)进行化学改性,使其成为一种pH敏感共聚物,并使用合成的共聚物制备肠道靶向埃索美拉唑纳米颗粒(NPs)。通过自由基聚合反应合成了聚丙烯酰胺接枝瓜尔胶(PAAm-g-GG)共聚物。通过碱性水解对PAAm-g-GG进行化学改性,从而形成pH敏感共聚物。研究了GG和丙烯酰胺(AAm)对接枝的影响。采用纳米乳化聚合物交联法制备了载有埃索美拉唑镁(ESO)的pH敏感NPs,并对其进行了表征。制备了16种制剂,并改变工艺变量的浓度以获得粒径在200 - 600 nm的纳米颗粒。发现这些NPs的粒径分布均匀。包封率和载药量分别在33.2%至50.1%以及12.2%至17.2%的范围内。粒径、包封率和载药量随共聚物浓度的增加而增加。在pH 1.2下进行2小时的体外释放研究,随后在pH 6.8下进行,结果表明环境pH显著影响药物释放。扫描电子显微镜显示NPs呈球形,表面光滑。pH敏感的PAAm-g-GG NPs在酸性pH下可抑制载药NPs中药物的初始释放,并在碱性环境中将释放过程延迟更长时间。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/30f7/4986109/9f0ab2b2738f/ijpr-15-083-g001.jpg

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