Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, GC University Faisalabad, Pakistan.
Department of Chemistry, GC University, Faisalabad, Pakistan.
Pak J Pharm Sci. 2020 Sep;33(5(Supplementary)):2301-2306.
Although ebastine (EBT) can impede histamine-induced skin allergic reaction and persuade long acting selective H1 receptor antagonistic effects but its poor water solubility circumscribed its clinical application. The main objective of this research work was to improve the aqueous solubility and oral bioavailability of EBT by preparing EBT-loaded bilosomes (EBT-PC-SDC-BS). A thin film hydration method was used to prepare ebastine loaded bilosomes. The prepared-formulations were optimized considering size, morphology and entrapment efficiency. The SEM images revealed regular and spherical shape of bilosomes. Average size of the prepared EBT-PC-SDC-BS was 665.8 nm and zeta potential was around-32.9 mV with 89.05 % average entrapment efficiency (EE).Importantly, the solubility of EBT in water was amplified up to 17.9 μg/ml compared to pure drug (2 μg/mL) reflecting a highest solubility increase of 751 %. In vitro drug release results of prepared EBT-PC-SDC-BS exhibited improved release behavior. Finally, it is established from the results that the EBT-PC-SDC-BS could function as a favorable nano-carrier system to improve the solubility as well as dissolution of EBT.
尽管依巴斯汀（EBT）可以抑制组胺引起的皮肤过敏反应，并具有长效选择性 H1 受体拮抗作用，但由于其较差的水溶性限制了其临床应用。本研究工作的主要目的是通过制备载依巴斯汀双层囊泡（EBT-PC-SDC-BS）来提高 EBT 的水溶解度和口服生物利用度。采用薄膜水化法制备载依巴斯汀双层囊泡。考虑到粒径、形态和包封效率对制剂进行了优化。SEM 图像显示双层囊泡呈规则的球形。所制备的 EBT-PC-SDC-BS 的平均粒径为 665.8nm，zeta 电位约为-32.9mV，平均包封效率（EE）为 89.05%。重要的是，与纯药物（2μg/mL）相比，EBT 在水中的溶解度提高到 17.9μg/ml，溶解度提高了 751%。所制备的 EBT-PC-SDC-BS 的体外药物释放结果显示出改善的释放行为。最后，结果表明 EBT-PC-SDC-BS 可以作为一种有利的纳米载体系统，提高 EBT 的溶解度和溶解性能。
