Effect of formulation variables on drug release from bilosomes; effect of cholesterol concentration

T. Elebyary, Amal Sultan, Sally El-Sayed Abu-Risha, G. E. El Maghraby
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Abstract

Bilosomes are bile salts-containing vesicles that have recently drawn attention as a novel nanocarrier for drugs. Compared to traditional nanocarriers, bilosomes have the advantage of being able to withstand disruption caused by physiological bile salts normally secreted in the gastrointestinal tract. In addition to nonionic surfactants and bile salts, cholesterol is one important ingredient in bilosomes composition. This work investigated the effect of cholesterol concentration on the release rate of the entrapped drug. Tamoxifen was used as a model drug that suffers from poor oral bioavailability due to poor solubility and extensive pre-systemic degradation. Bilosomes composed of Span 60, cholesterol, and bile salts were prepared. Cholesterol was used at two different concentrations of 0.4% and 0.8% w/v, producing formulations BiL1 and BiL2, respectively. The entrapment efficiency and in vitro drug release were evaluated using Franz diffusion cells. Increasing cholesterol concentration reduced drug release. The release efficiency values after 24 hours of release study were 9.7 and 6.8% for BiL1 and BiL2, respectively. This indicates that increasing cholesterol concentration increased the rigidity of the bilosomal membrane and enhanced drug encapsulation. Reduced release would indicate that the vesicles retain the encapsulated drug, which is advantageous, taken into consideration the lymphatic absorption of the vesicles.
配方变量对双糖体药物释放的影响;胆固醇浓度的影响
胆糖体是一种含有胆汁盐的囊泡,最近作为一种新型纳米药物载体引起了人们的关注。与传统的纳米载体相比,胆脂体的优势在于能够抵御通常在胃肠道分泌的生理性胆汁盐所造成的破坏。除了非离子表面活性剂和胆汁盐之外,胆固醇也是双螺旋体成分中的一种重要成分。这项研究探讨了胆固醇浓度对夹带药物释放速率的影响。他莫昔芬(Tamoxifen)被用作一种模型药物,由于溶解性差和广泛的系统前降解,该药物的口服生物利用度较低。研究人员制备了由司盘 60、胆固醇和胆汁盐组成的双酶体。胆固醇的浓度为 0.4% 和 0.8% w/v,分别用于制备 BiL1 和 BiL2。使用弗朗兹扩散细胞对药物的包埋效率和体外药物释放进行了评估。胆固醇浓度增加会减少药物释放。24 小时释放研究后,BiL1 和 BiL2 的释放效率值分别为 9.7% 和 6.8%。这表明胆固醇浓度的增加提高了双体膜的硬度,增强了药物的包裹性。考虑到囊泡的淋巴吸收性,释放量的减少表明囊泡保留了封装的药物,这是有利的。
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