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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Formulation of spray congealed microparticles with self-emulsifying ability for enhanced glibenclamide dissolution performance
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Formulation of spray congealed microparticles with self-emulsifying ability for enhanced glibenclamide dissolution performance

机译：具有自乳化能力的喷雾凝结微粒配方，可提高格列本脲的溶解性能

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摘要

Purpose: To develop a novel preparation approach of solid Self-Emulsifying Drug Delivery System (s-SEDDS) based on spray congealing as potential drug delivery technology for poorly water-soluble drug Glibenclamide (GBD). Methods: Several systems were formulated using suitable excipients, solid at room temperature, with different hydrophilic-lipophilic balance, such as Myverol, Myvatex, Gelucire (R) 50/13 and Gelucire (R) 44/14. Cremophor (R) EL and Poloxamer 188 were selected as surfactants and PEG 4000 as co-solvent. Results: The screening of the best carrier for s-SEDDS manufacturing revealed that Gelucire (R) 50/13 had greater performance. Then, surfactant-co-solvent systems were developed. Dissolution studies showed that all the formulations promoted the solubilisation performance of the GBD with respect to pure drug; in particular the formulation containing Gelucire (R) 50/13 and PEG 4000 increased the drug solubilisation of five times. These microparticles showed self-dispersibility within 60 min and micelles dimensions around 360 nm. Conclusions: Spray congealing is a promising novel manufacturing technique of solid self-emulsifying systems.
机译：目的：开发一种基于喷雾凝结的固体自乳化药物输送系统（s-SEDDS）的新制备方法，作为水溶性差的药物格列本脲（GBD）的潜在药物输送技术。方法：使用适合的赋形剂配制几种体系，这些赋形剂在室温下为固体，具有不同的亲水-亲脂平衡，例如Myverol，Myvatex，Gelucire（R）50/13和Gelucire（R）44/14。选择Cremophor（R）EL和泊洛沙姆188作为表面活性剂，选择PEG 4000作为助溶剂。结果：筛选用于s-SEDDS的最佳载体表明，Gelucire（R）50/13具有更好的性能。然后，开发了表面活性剂-助溶剂系统。溶出度研究表明，相对于纯药物，所有制剂均能促进GBD的增溶性能。特别地，含有Gelucire 50/13和PEG 4000的制剂使药物溶解度增加了五倍。这些微粒在60分钟内显示出自分散性，胶束尺寸约为360 nm。结论：喷雾凝结是一种有前途的固体自乳化体系的新型制造技术。

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