Abstract: Glibenclamide and lipoic acid are two drugs frequently recommended for the management of diabetes mellitus, and so, the development of a new formulation containing both substances has a great benefit in terms of efficiency and compliance, acting also as a multi-target drug system. Accordingly, the aim of this study was the formulation and physicochemicalcharacterization of new polymeric systems based on chitosan (CS) in whose matrix were encapsulated glibenclamide (Gly) and lipoic acid (LA). The polymeric systems were prepared as microparticles (CS–Gly, CS–LA, and CS–Gly–LA) through ionic gelation method, using pentasodium tripolyphosphate (TPP) as crosslinking agent. The polymeric systems obtained were characterized in terms of particle size and morphology, IR spectroscopy, entrapment efficiency and drug loading, swelling degree, and therelease of the active substances from the chitosan matrix. The polymeric systems obtained were stable systems; the presence of glibenclamide and lipoic acid into the polymer matrix were proved by IR spectroscopy. The entrapment efficiency was 94.66% for Gly and 39.68% for LA. The developed polymeric systems proved a favorable swelling degree and drug release profile, the percentage of release being 88.68% for LA and 75.17% for Gly from CS–Gly–LA systems.

中文翻译：

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载有格列本脲和硫辛酸的基于壳聚糖的递送系统：制剂，表征和动力学释放研究

一个bstract：格列本脲和硫辛酸是经常推荐用于治疗糖尿病的两种药物，因此，开发一种包含这两种物质的新制剂在效率和依从性方面均具有巨大优势，并且还可以作为多目标药物系统。因此，本研究的目的是基于壳聚糖（CS）的新型聚合物体系的配方和物理化学表征，其基质中包封有格列本脲（Gly）和硫辛酸（LA）。使用三聚磷酸五钠（TPP）作为交联剂，通过离子凝胶法将聚合物体系制成微粒（CS–Gly，CS–LA和CS–Gly–LA）。得到的聚合物体系的特征在于粒径和形态，红外光谱，包封率和载药量，溶胀度，以及从壳聚糖基质中释放出活性物质。所获得的聚合物体系是稳定体系。红外光谱证实了格列本脲和硫辛酸存在于聚合物基质中。Gly和LA的包封效率为94.66％和39.68％。发达的聚合物系统证明了良好的溶胀度和药物释放曲线，从CS–Gly–LA系统中，LA的释放百分比为88.68％，Gly的释放百分比为75.17％。