Momoh Mumuni A, Franklin Kenechukwu C, Agbo Chinazom P, Ugwu Calister E, Adedokun Musiliu O, Anthony Ofomata C, Chidozie Omeje E, Okorie Augustine N
Drug Delivery Research Unit, Department of Pharmaceutics, Faculty of Pharmaceutical Sciences University of Nigeria Nsukka, Enugu State, Nigeria.
Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria Nsukka, Enugu State, Nigeria.
Heliyon. 2020 Mar 30;6(3):e03650. doi: 10.1016/j.heliyon.2020.e03650. eCollection 2020 Mar.
Oral delivery of insulin provides a good alternative because it is non-invasive and patient-friendly. However, multiple challenges affected this route. To overcome barriers for oral delivery of insulin, we aimed to develop a novel insulin-loaded microemulsion system based on snail mucin for oral administration. The strategy in the novel system of using mucin loading insulin into the inner core of prepared water in oil microemulsion to provide sustained released, increased in vivo stability and enhanced drug absorption in the gastrointestinal tract. We report how microemulsion composed of varying ratios of snail mucin and Tween® 80 (1:9-9:1) using oil/water emulsion preparation method influenced insulin performance after oral administration. The results obtained include an encapsulation efficiency of above 70 %; in vitro release was sustained over 10 h and evaluations in diabetic rat model shows that insulin-loaded microencapsulation effectively reduced blood glucose levels over a period >8 h after oral administration. Therefore, we suggest that the developed formulation for oral insulin can be a promising alternative dosage form for oral protein delivery.
口服胰岛素是一种很好的替代方法，因为它是非侵入性的，且对患者友好。然而，这条途径面临多重挑战。为了克服胰岛素口服给药的障碍，我们旨在开发一种基于蜗牛黏液的新型载胰岛素微乳系统用于口服给药。在新系统中，采用将黏液素包裹胰岛素于制备好的油包水型微乳内核中的策略，以实现缓释、提高体内稳定性并增强胃肠道药物吸收。我们报告了采用油/水乳化制备方法，由不同比例的蜗牛黏液素和吐温80（1:9 - 9:1）组成的微乳对口服给药后胰岛素性能的影响。获得的结果包括包封率高于70%；体外释放持续超过10小时，在糖尿病大鼠模型中的评估表明，载胰岛素微囊在口服给药后>8小时内有效降低血糖水平。因此，我们认为所开发的口服胰岛素制剂可能是一种有前景的口服蛋白质递送替代剂型。
