Formulation and evaluation of Albendazole microcapsules for colon delivery using chitosan

Simi SP; Saraswathi R; Sankar C; Krishnan PN; Dilip C; Ameena K

摘要

Objective:To formulate and evaluate Albendazole microcapsules using chitosan, a natural polymer for colon-specific delivery for better treatment of helminthiasis, filariasis, colorectal cancer, avoiding the side effects. Methods:The Albendazole microcapsules were prepared by the use of different concentrations of sodium alginate, chitosan and hydroxypropyl methylcellulose (HPMC). The polysaccharides chitosan reacted with sodium alginate in the presence of calcium chloride to form microcapsules with a polyelectrolyte complex membrane by electrostatic interactions between the two oppositely charged polymers. The microcapsules were then studied for entrapment efficiency, drug-polymer compatibility and surface morphology. In vitro drug release study in presence and absence of cecal content were also studied. Further, kinetic modellings were employed to find out release mechanisms. Results: Albendazole loaded microspheres showd high entrapment efficiency (72.8%) and the microcapsules were free flowing, non aggregated and spherical, between 600 and 1 000μm in diameter. The surface of microcapsules were found to be porous and wavy. The FT-IR spectrum showed that there is no interaction between the polymer and the drug. The in vitro drug release study found to be affected by change in chitosan, sodium alginate and HPMC concentration. The microcapsules with 2.5% sodium alginate and 0.4% chitosan shown minimum release in gastrointestinal simulated condition but shows maximum drug release at the end of 24th hour in presence of cecal content. The rate of drug release follows Korsmeyer-peppas model that was the drug release is by diffusion and erosion. Conclusions:The study reveals that Albendazole loaded chitosan-alginate based microsphere can be used effectively for the colon targeting.

机译：目的：使用壳聚糖（一种用于结肠定位的天然聚合物）来配制和评估阿苯达唑微胶囊，以更好地治疗蠕虫病，丝虫病，大肠癌，避免副作用。方法：采用不同浓度的海藻酸钠，壳聚糖和羟丙基甲基纤维素（HPMC）制备阿苯达唑微胶囊。多糖壳聚糖在氯化钙的存在下与藻酸钠反应，通过两种带相反电荷的聚合物之间的静电相互作用，与聚电解质复合膜形成微囊。然后研究微胶囊的包封率，药物-聚合物相容性和表面形态。还研究了存在和不存在盲肠成分的体外药物释放研究。此外，采用动力学模型找出释放机理。结果：载有阿苯达唑的微球具有较高的包封率（72.8％），微胶囊自由流动，不聚集且呈球形，直径在600至1000μm之间。发现微胶囊的表面是多孔和波浪状的。 FT-IR光谱表明聚合物与药物之间没有相互作用。体外药物释放研究发现受到壳聚糖，藻酸钠和HPMC浓度变化的影响。具有2.5％海藻酸钠和0.4％壳聚糖的微胶囊在胃肠道模拟条件下显示出最小的释放，但是在存在盲肠成分的第24小时结束时显示出最大的药物释放。药物的释放速率遵循Korsmeyer-peppas模型，即药物的释放是通过扩散和侵蚀。结论：研究表明，阿苯达唑负载的壳聚糖-藻酸盐微球可有效用于结肠靶向。

Formulation and evaluation of Albendazole microcapsules for colon delivery using chitosan

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