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 F_1PVP and F_4TW80 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.

中文翻译：

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格列美脲负载聚合物纳米颗粒的开发和表征：配方设计和评估

目的

本研究旨在使用壳聚糖 (CTN)、聚乙烯吡咯烷酮 (PVP) 和 Tween 80 开发聚合物纳米粒子 (PNP)，以增强水溶性差的抗糖尿病药物格列美哌胺 (GLM) 的溶出度。

方法

通过使用不同量的 CTN 作为聚合物、PVP 和 Tween 80 作为稳定剂以及三聚磷酸盐 (TPP) 作为交联剂，开发了负载 GLM 的 PNP，以提高 GLM 的溶出度和溶解度。PNP 的制备采用溶剂蒸发和离子凝胶技术相结合的方法。新制备的 PNP 进一步被表征为包封率百分比 (%EE)、相容性研究、平均粒径、形态、热行为、XRD 检查和不同生物相关 pH 条件下的溶出研究。

结果

制备的 PNP 的包封率在 55.90% 至 93.25% 范围内。傅里叶变换红外研究揭示了 GLM 与复合材料配方的兼容性。优化后的 PNP F _1PVP和 F _4TW80的粒径分别在 323 nm 和 149 nm 的纳米级范围内。SEM 表明形成了不规则（片状）形状的颗粒。DSC 和 PXRD 研究表明 PNP 内部 GLM 的结晶度降低，从而促进溶解。在生物相关酸性 pH 1.2 和生物相关碱性 pH 6.8 下的溶出研究表明，与纯 GLM 水分散体相比，溶出曲线显着改善。

结论

研究的总体结果表明，用 PVP 和 Tween 80 稳定的基于 CTN 的 PNP 可以作为 GLM 口服药物递送的有前途的载体。