格列美脲负载聚合物纳米粒子的开发与表征:配方设计与评估

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2024-01-20 DOI:10.1007/s12247-024-09812-2
Zaiba Irfan, Muhammad Imran Khan, Muhammad Farhan Sohail, Muhammad Furqan Akhtar, Muhammad Naeem Qaisar, Muhammad Kashif Javed, Fareeha Anwar,  Badarqa-tul-Ayesha, Majid Anwar, Aslam Khan, Faizan Akram
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引用次数: 0

摘要

目的 本研究旨在利用壳聚糖(CTN)、聚乙烯吡咯烷酮(PVP)和吐温 80 开发聚合物纳米粒子(PNPs),以提高水溶性较差的抗糖尿病药物格列美脲(GLM)的溶解度。方法以不同量的 CTN 作为聚合物,PVP 和吐温 80 作为稳定剂,三聚磷酸酯 (TPP) 作为交联剂,开发出 GLM 负载 PNPs,用于提高 GLM 的溶解度和可溶性。采用溶剂蒸发和离子凝胶技术相结合的方法制备了 PNPs。对新制备的 PNPs 进一步进行了表征,包括封装效率(%EE)、相容性研究、平均粒径、形态、热行为、XRD 检查以及在不同生物相关 pH 条件下的溶解研究。傅立叶变换红外研究显示 GLM 与配方复合材料相容。优化后的 PNPs F1PVP 和 F4TW80 的粒度分别为 323 纳米和 149 纳米。扫描电镜显示形成了不规则(片状)颗粒。DSC 和 PXRD 研究表明,PNPs 内部 GLM 的结晶度降低,从而促进了溶解。在生物相关酸性 pH 值为 1.2 和生物相关碱性 pH 值为 6.8 的条件下进行的溶解研究表明,与 GLM 的纯水分散体相比,溶解情况有了显著改善。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Development and Characterization of Glimepiride-Loaded Polymeric Nanoparticles: Formulation Design and Evaluation

Purpose

This study was aimed to develop polymeric nanoparticles (PNPs) using chitosan (CTN), polyvinyl pyrrolidone (PVP), and Tween 80 for dissolution enhancement of poorly water-soluble antidiabetic drug: glimeperide (GLM).

Methods

GLM-loaded PNPs were developed for increasing the dissolution and solubility of GLM by using different amounts of CTN as polymer, PVP, and Tween 80 as stabilizers and tri-polyphosphate (TPP) as a crosslinking agent. PNPs were prepared using a combined approach of solvent evaporation and ionic gelation techniques. The newly fabricated PNPs were further characterized for percent encapsulation efficiency (%EE), compatibility studies, average particle size, morphology, thermal behavior, XRD examination, and dissolution studies at different biorelevant pH conditions.

Results

The prepared PNPs showed % encapsulation efficiency in the range of 55.90 to 93.25%. Fourier transform infrared studies revealed compatibility of GLM with formulation composites. The optimized PNPs F1PVP and F4TW80 showed particle size in nanoscale range 323 nm and 149 nm, respectively. SEM indicated formation of irregular (flakes) shaped particles. DSC and PXRD studies revealed reduction in crystallinity of the GLM inside PNPs thus promoting the dissolution. The dissolution studies at biorelevant acidic pH 1.2 and biorelevant basic pH 6.8 demonstrated remarkable improvement in dissolution profile compared to pure aqueous dispersion of GLM.

Conclusion

Overall results of the study suggested that CTN-based PNPs stabilized with PVP and Tween 80 can act as promising carriers for oral drug delivery of GLM.

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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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