Rasheed Qaiser, Ahmad Khan Kamran, Razaque Ghulam, Ahmad Ashfaq, Nawaz Asif, Akhtar Naheed, Ullah Shah Kifayat, Rasul Niazi Zahid, Danish Saeed Muhammad, Alam Anila
Gomal Centre of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, Pakistan.
Faculty of Pharmacy, University of Balochistan, Quetta, Pakistan.
PLoS One. 2025 Jan 9;20(1):e0313523. doi: 10.1371/journal.pone.0313523. eCollection 2025.
Controlled-release microparticles offer a promising avenue for enhancing patient compliance and minimizing dosage frequency. In this study, we aimed to design controlled-release microparticles of Glipizide utilizing Eudragit S100 and Methocel K 100 M polymers as controlling agents. The microparticles were fabricated through a simple solvent evaporation method, employing various drug-to-polymer ratios to formulate different controlled-release batches labeled as F1 to F5. Evaluation of the microparticles encompassed a range of parameters including flow properties, particle size, morphology, percentage yield, entrapment efficiencies, percent drug loading, and dissolution studies. Additionally, various kinetic models were employed to elucidate the drug release mechanism. Furthermore, difference and similarity factors were utilized to compare the dissolution profiles of the tested formulations with a reference formulation. The compressibility index and angle of repose indicated favorable flow properties of the prepared microparticles, with values falling within the range of 8 to 10 and 25 to 29, respectively. The particle size distribution of the microparticles ranged from 95.3 to 126 μm. Encouragingly, the microparticles exhibited high percent yield (ranging from 66 to 77%), entrapment efficiency (80 to 96%), and percent drug loading (46 to 54%). All formulated batches demonstrated controlled drug release profiles extending up to 12 hours, with glipizide release following an anomalous non-Fickian diffusion pattern. However, the drug release profiles of the reference formulation and various polymeric microparticles did not meet the acceptable limits of difference and similarity factors. In-vivo studies revealed sustained hypoglycemic effects over a 12-hour period, indicating the efficacy of the controlled-release microparticles. Overall, our findings suggest the successful utilization of polymeric materials in designing controlled-release microparticles, thereby reducing dosage frequency and potentially improving patient compliance.
控释微颗粒为提高患者依从性和减少给药频率提供了一条有前景的途径。在本研究中,我们旨在利用Eudragit S100和羟丙甲纤维素K100M聚合物作为控释剂来设计格列吡嗪控释微颗粒。微颗粒通过简单的溶剂蒸发法制备,采用不同的药物与聚合物比例来配制标记为F1至F5的不同控释批次。对微颗粒的评估包括一系列参数,如流动性、粒径、形态、产率百分比、包封率、载药百分比和溶出度研究。此外,采用各种动力学模型来阐明药物释放机制。此外,利用差异因子和相似因子将受试制剂的溶出曲线与参比制剂进行比较。压缩性指数和休止角表明所制备的微颗粒具有良好的流动性,其值分别落在8至10和25至29的范围内。微颗粒的粒径分布范围为95.3至126μm。令人鼓舞的是,微颗粒表现出较高的产率百分比(66%至77%)、包封率(80%至96%)和载药百分比(46%至54%)。所有配制批次均显示出长达12小时的控释曲线,格列吡嗪的释放遵循非菲克扩散的异常模式。然而,参比制剂和各种聚合物微颗粒的药物释放曲线未达到差异因子和相似因子的可接受限度。体内研究显示在12小时内具有持续的降血糖作用,表明控释微颗粒的有效性。总体而言,我们的研究结果表明在设计控释微颗粒中成功利用了聚合物材料,从而降低了给药频率并可能提高了患者依从性。