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水解聚丙烯酰胺接枝玉米淀粉基微球:在pH响应型药物递送中的应用。

Hydrolyzed polyacrylamide grafted maize starch based microbeads: application in pH responsive drug delivery.

作者信息

Setty C Mallikarjuna, Deshmukh Anand S, Badiger Aravind M

机构信息

Department of Pharmaceutics, The Oxford College of Pharmacy, 6/9, 1st cross Begur Road, Hongasandra, Bangalore 560068, India.

Department of Pharmaceutics, Shree Dhanvantary Pharmacy College, Kim, Kudsad Road, Surat, Gujarat 394110, India.

出版信息

Int J Biol Macromol. 2014 Sep;70:1-9. doi: 10.1016/j.ijbiomac.2014.06.027. Epub 2014 Jun 24.

Abstract

The present study details the synthesis, characterization and pharmaceutical application of hydrolysed polyacrylamide grafted maize starch (HPam-g-MS) as promising polymeric material for the development of pH responsive microbeads. Different grades of graft copolymer were synthesized by changing the net microwave irradiation time, while keeping all other factors constant. Acute oral toxicity study performed in rodents ensured the bio-safety of graft copolymer for clinical application. Various batches of aceclofenac loaded microbeads were prepared by ionic gelation method using synthesized graft copolymers and evaluated for formulation parameters. FTIR spectroscopy confirmed the chemical compatibility between drug and graft copolymer. Results of in vitro release study (USP type-II) carried out in two different pH media (pH 1.2 acid buffer and pH 7.4 phosphate buffer) showed that release rate of drug from developed microbeads was a function of both: (a) surrounding pH and (b) the matrix composition. The drug release was relatively higher at alkaline pH as compared to acidic pH and this feature is desirable from viewpoint of site specific drug delivery. A direct correlation was observed between percentage grafting and microbeads performance and it presents a scope for further research on application and optimization of HPam-g-MS based microbeads as drug delivery carriers.

摘要

本研究详细阐述了水解聚丙烯酰胺接枝玉米淀粉(HPam-g-MS)作为开发pH响应性微珠的有前景的聚合材料的合成、表征及药物应用。通过改变微波净辐照时间合成了不同等级的接枝共聚物,同时保持所有其他因素不变。在啮齿动物中进行的急性口服毒性研究确保了接枝共聚物用于临床应用的生物安全性。使用合成的接枝共聚物通过离子凝胶法制备了不同批次的载醋氯芬酸微珠,并对其制剂参数进行了评估。傅里叶变换红外光谱(FTIR)证实了药物与接枝共聚物之间的化学相容性。在两种不同pH介质(pH 1.2酸性缓冲液和pH 7.4磷酸盐缓冲液)中进行的体外释放研究(USP II型)结果表明,所制备微珠中药物的释放速率取决于以下两个因素:(a)周围环境的pH值和(b)基质组成。与酸性pH相比,碱性pH下的药物释放相对较高,从定点给药的角度来看,这一特性是理想的。接枝率与微珠性能之间存在直接相关性,这为进一步研究基于HPam-g-MS的微珠作为药物递送载体的应用和优化提供了空间。

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