Emami J, Boushehri M S Shetab, Varshosaz J
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences and Isfahan Pharmaceutical Research Center, Isfahan University of Medical Sciences and Health Services, Isfahan, I.R. Iran.
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences and Isfahan Pharmaceutical Research Center, Isfahan University of Medical Sciences and Health Services, Isfahan, I.R. Iran ; Present address: Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, University of Bonn, 3 Gerhard-Domagk str. 53119 Bonn, Germany.
Res Pharm Sci. 2014 Sep-Oct;9(5):301-14.
The purpose of the present study was to develop glipizide controlled release nanoparticles using alginate and chitosan thorough ionotropic controlled gelation method. Glipizide is a frequently prescribed second generation sulfonylurea which lowers the blood glucose in type-two diabetics. Quick absorption of the drug from the gastrointestinal tract along with short half- life of elimination makes it a good candidate for controlled release formulations. Alginate-chitosan nanoparticles (ACNP) are convenient controlled delivery systems for glipizide, due to both the release limiting properties of the system, and the bioadhesive nature of the polymers. In the present study, glipizide loaded alginate-chitosan nanoparticles (GlACNP) were prepared, and the particle characteristics including particle size (PS), zeta potential (ZP), entrapment efficiency (EE%), loading percent (LP), and mean release time (MRT), as well as the morphology of the nanoparticles, the drug-excipient compatibility, and the release kinetics along with the drug diffusion mechanism were evaluated. The results suggested that ionotropic controlled gelation method offers the possibility of preparing the nanoparticles in mild conditions in an aqueous environment, and can lead to the preparation of particles with favorable size, controlled release characteristics, and high entrapment efficiency, serving as a convenient delivery system for glipizide. The particle and release characteristics can be efficiently optimized using the Box-Behnken design. Based on the findings of the present study, it is expected that this novel formulation be a superior therapeutic alternative to the currently available glipizide delivery systems.
本研究的目的是通过离子型控凝法,使用海藻酸盐和壳聚糖制备格列吡嗪控释纳米颗粒。格列吡嗪是一种常用的第二代磺酰脲类药物,可降低2型糖尿病患者的血糖。药物从胃肠道快速吸收以及消除半衰期短,使其成为控释制剂的良好候选药物。海藻酸盐-壳聚糖纳米颗粒(ACNP)是格列吡嗪方便的控释给药系统,这归因于该系统的释放限制特性以及聚合物的生物粘附性质。在本研究中,制备了载格列吡嗪的海藻酸盐-壳聚糖纳米颗粒(GlACNP),并评估了颗粒特性,包括粒径(PS)、zeta电位(ZP)、包封率(EE%)、载药量(LP)和平均释放时间(MRT),以及纳米颗粒的形态、药物-辅料相容性、释放动力学和药物扩散机制。结果表明,离子型控凝法提供了在水性环境中温和条件下制备纳米颗粒的可能性,并可制备出具有良好尺寸、控释特性和高包封率的颗粒,作为格列吡嗪的方便给药系统。使用Box-Behnken设计可以有效地优化颗粒和释放特性。基于本研究的结果,预计这种新型制剂将成为目前可用的格列吡嗪给药系统的一种更优的治疗选择。