Govender Mershen, Choonara Yahya Essop, van Vuuren Sandy, Kumar Pradeep, du Toit Lisa Claire, Pillay Viness
Department of Pharmacy and Pharmacology, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, South Africa.
J Pharm Pharmacol. 2015 Jul;67(7):939-50. doi: 10.1111/jphp.12389. Epub 2015 Feb 2.
The viability of probiotic bacteria during formulation processes and delivery is vital to ensure health benefits. This study focuses on the use of gastro-resistant denatured ovalbumin for the targeted delivery of probiotic Lactobacillus acidophilus to simulated human intestinal and colon conditions through a bi-layered mini-tablet-in-tablet system (BMTTS).
The BMTTS consists of two gastro-resistant ovalbumin mini-tablets containing L. acidophilus suspended in lactose and eudragit S100 for targeted intestinal and colonic delivery respectively. Luminescence has been utilized to ensure probiotic viability during formulation processes in addition to determining all probiotic release profiles. The mechanism of probiotic release from the ovalbumin matrix was ascertained using mathematical modelling and molecular docking studies. Magnetic resonance imaging and differential scanning calorimetry are also included as part of the in-vitro characterization of the ovalbumin system.
The BMTTS was effective in the delivery of L. acidophilus to simulated human intestinal and colon conditions. Formulation processes were furthermore determined to maintain probiotic viability. Statistical analysis of the release data noted a significant effect of pH denaturation on the release properties of ovalbumin. Magnetic resonance imaging results have indicated a decrease in ovalbumin matrix size upon exposure to simulated intestinal fluid. Molecular docking studies carried out depicted the interaction and binding positions inherent to the ovalbumin-pancreatic trypsin interaction complex indicating the possible enzymatic degradation of ovalbumin leading to the release of the probiotic from the protein matrix.
The BMTTS has been determined to be effective in the protection and delivery of probiotic L. acidophilus to simulated human intestinal and colonic conditions. Molecular docking analysis has noted that pancreatin exerts a significant effect on probiotic release from the gastro-resistant ovalbumin matrix.
益生菌在制剂过程和递送过程中的生存能力对于确保健康益处至关重要。本研究聚焦于使用胃抗性变性卵清蛋白，通过双层片内片系统（BMTTS）将益生菌嗜酸乳杆菌靶向递送至模拟的人体肠道和结肠环境。
BMTTS由两片胃抗性卵清蛋白迷你片组成，一片含有悬浮于乳糖中的嗜酸乳杆菌，用于靶向肠道递送，另一片含有尤特奇S100，用于靶向结肠递送。除了确定所有益生菌释放曲线外，还利用发光来确保制剂过程中益生菌的生存能力。使用数学建模和分子对接研究确定了益生菌从卵清蛋白基质中释放的机制。磁共振成像和差示扫描量热法也作为卵清蛋白系统体外表征的一部分。
BMTTS在将嗜酸乳杆菌递送至模拟的人体肠道和结肠环境方面是有效的。此外，确定制剂过程可维持益生菌的生存能力。对释放数据的统计分析表明，pH变性对卵清蛋白的释放特性有显著影响。磁共振成像结果表明，暴露于模拟肠液后卵清蛋白基质尺寸减小。进行的分子对接研究描绘了卵清蛋白 - 胰蛋白酶相互作用复合物固有的相互作用和结合位置，表明卵清蛋白可能发生酶促降解，导致益生菌从蛋白质基质中释放。
已确定BMTTS在将益生菌嗜酸乳杆菌保护并递送至模拟的人体肠道和结肠环境方面是有效的。分子对接分析表明，胰酶对从胃抗性卵清蛋白基质中释放益生菌有显著影响。
