Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Bingham University, Karu, Nasarawa State, Nigeria.
Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
Curr Pharm Des. 2024;30(24):1939-1948. doi: 10.2174/0113816128309449240527053640.
Diabetes mellitus is a global disease identified by hyperglycemia due to defects in insulin secretion, insulin action, or both.
The main objective of this research was to evaluate the ability of gelatinized Poly(ethylene glycol) (PEG) microparticles to be used as carriers for oral insulin delivery via double emulsion preparation.
Five different batches of the formulation consisting of gelatin:PEG were prepared as follows: 0:1 (W1), 1:0 (W2), 1:1 (W3), 1:3 (W4), and 3:1 (W5). The prepared microparticles (from insulin-loaded batches) had particle sizes ranging from 19.5 ± 0.32-23.9 ± 0.22 μm and encapsulation and loading capacities ranging from 78.8 ± 0.24-88.9 ± 0.95 and 22.2 ± 0.96-29.7 ± 0.86%, respectively. The minimum and maximum in vitro release rates were 8.0 and 66.0%, respectively, for batches W1 and W2 at 8 h.
Insulin-loaded MPs induced a significant decrease in glucose levels, with a reduction from 100 to 33.35% in batch W5 at 9 h compared to that of subcutaneous insulin (100 to 22.63%). A liver function study showed that the formulation caused no obvious toxicity to the experimental rats.
Gelatinized PEG-based microparticles as insulin delivery systems may open a new window into the development of oral insulin for diabetic treatment.
糖尿病是一种全球性疾病，由于胰岛素分泌、胰岛素作用或两者都有缺陷而导致的高血糖症。
本研究的主要目的是评估明胶化聚乙二醇（PEG）微球作为口服胰岛素传递载体的能力，通过双乳液制备来实现。
制备了由明胶：PEG 组成的 5 种不同批次的制剂：0:1（W1）、1:0（W2）、1:1（W3）、1:3（W4）和 3:1（W5）。从载有胰岛素的批次中制备的微球粒径范围为 19.5±0.32-23.9±0.22μm，包封率和载药量范围分别为 78.8±0.24-88.9±0.95 和 22.2±0.96-29.7±0.86%。W1 和 W2 批次的最小和最大体外释放率分别为 8 小时时的 8.0%和 66.0%。
载有胰岛素的 MPs 显著降低了血糖水平，与皮下胰岛素（从 100%降至 22.63%）相比，W5 批在 9 小时时降低了 100%至 33.35%。肝功能研究表明，该制剂对实验大鼠没有明显的毒性。
作为胰岛素传递系统的明胶化 PEG 基微球可能为开发用于糖尿病治疗的口服胰岛素开辟新的途径。
