Bile acids have recently been studied for potential applications as formulation excipients and enhancers for drug release; however, some bile acids are not suitable for this application. Unconjugated lithocholic acid (ULCA) has recently shown drug formulation-stabilizing and anti-inflammatory effects. Lipophilic drugs have poor gut absorption after an oral dose, which necessitates the administration of high doses and causes subsequent side effects. Probucol (PB) is a highly lipophilic drug with poor oral absorption that resulted in restrictions on its clinical prescribing. Hence, this study aimed to design new delivery systems for PB using ULCA-based matrices and to test drug formulation, release, temperature, and biological effects. ULCA-based matrices were formulated for PB oral delivery by applying the jet-flow microencapsulation technique using sodium alginate as a polymer. ULCA addition to new PB matrices improved the microcapsule’s stability, drug release in vitro (formulation study), and showed a promising effect in ex vivo study (p < 0.05), suggesting that ULCA can optimize the oral delivery of PB and support its potential application in diabetes treatment.

中文翻译：

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普罗布考细胞靶向制剂的有毒人胆纳米药物增强了药理作用和先进的细胞呼吸作用。

最近研究了胆汁酸作为制剂赋形剂和药物释放促进剂的潜在应用。但是，有些胆汁酸不适合该应用。非共轭石胆酸（ULCA）最近显示出稳定药物制剂和抗炎作用。亲脂性药物口服后肠道吸收不良，需要大剂量给药并引起随后的副作用。普罗布考（PB）是一种高度亲脂性药物，口服吸收差，导致其临床处方受到限制。因此，本研究旨在使用基于ULCA的基质设计用于PB的新递送系统，并测试药物的配方，释放，温度和生物学效应。通过使用藻酸钠作为聚合物的射流微囊化技术，配制了基于ULCA的基质，用于PB口服给药。在新的PB基质中添加ULCA改善了微胶囊的稳定性，药物释放体外（配方研究），并且在离体研究中显示出有希望的效果（p <0.05），表明ULCA可以优化PB的口服给药并支持其在糖尿病治疗中的潜在应用。