Polymeric nanoparticle of Ebastine: Formulation, Characterization and in vitro Evaluation

H. Ali, N. Rajab
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引用次数: 1

Abstract

The main aim of this research work was the development and evaluation of polymeric nanoparticle for the bioavailability improvement of Ebastine (EBT) to treat allergic condition. EBT is a piperidine derivative that binds preferentially to peripheral H1 receptors and is a long-acting, non-sedating second-generation histamine receptor antagonist. It is practically insoluble in water (class II, according to BCS). This work aims to formulate and adjust Ebastine polymeric nanoparticles to improve the EBT solubility as well as dissolution rate. For the synthesis of PNPs, the solvent evaporation technique was used, and three different types of stabilizer that used (HPMC E5, Soluplus, tween 80). The particle size analysis indicated that the optimized formula EBT 9 had a reduced nanoparticulate size of 42 nm, with a 90 percent increase in in-vitro dissolution profile compared to 17 percent for the comparison Ebastine powder in 0.1 N HCl media (pH 1.2). As a result, polymeric nanoparticles formulation of weakly water soluble EBS greatly improved the drug's dissolving rate and increased its solubility.
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聚合物纳米颗粒的制备、表征及体外评价
本研究的主要目的是开发和评价聚合物纳米颗粒,提高依巴斯丁(EBT)治疗过敏性疾病的生物利用度。EBT是一种哌啶衍生物,优先结合外周H1受体,是一种长效,非镇静的第二代组胺受体拮抗剂。它几乎不溶于水(根据BCS分类为II类)。本工作旨在制备和调整EBT聚合物纳米颗粒,以提高EBT的溶解度和溶解速度。采用溶剂蒸发法合成PNPs,采用了三种不同类型的稳定剂(HPMC E5, Soluplus, tween 80)。粒径分析表明,优化后的EBT 9的纳米颗粒尺寸减小至42 nm,体外溶出度增加90%,而对照Ebastine粉在0.1 N HCl (pH 1.2)介质中的体外溶出度增加17%。因此,弱水溶性EBS的聚合物纳米颗粒配方大大提高了药物的溶解速度,增加了其溶解度。
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期刊介绍: Journal of Intercultural Ethnopharmacology (2146-8397) Between (2012 Volume 1, Issue 1 - 2018 Volume 7, Issue 1). Journal of Complementary Medicine Research is aimed to serve a contemporary approach to the knowledge about world-wide usage of complementary medicine and their empirical and evidence-based effects. ISSN: 2577-5669
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