制备和表征自乳化药物传递系统（SEDDS），通过疏水离子对复合作用提高盐酸二甲双胍的口服生物利用度。
Preparation and characterisation of self-emulsifying drug delivery system (SEDDS) for enhancing oral bioavailability of metformin hydrochloride using hydrophobic ion pairing complexation.
机构信息
Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Nutrition Health Research Center, Hamadan University of Medical Sciences, Hamadan, Iran.
出版信息
J Microencapsul. 2023 Jan;40(1):53-66. doi: 10.1080/02652048.2023.2170488. Epub 2023 Jan 28.
AIM
The aim of this study was preparation of a self-emulsifying drug delivery system (SEEDS) containing metformin hydrochloride.
METHODS
Hydrophobic ion paired complexes were prepared by electrostatic interaction between metformin and sodium lauryl sulphate (SLS). The nanodroplets were optimised using two-level full factorial methodology and their morphology were examined. release of metformin from SEDDS was evaluated in simulated gastric and intestinal fluids. Finally, the ex efficacy of the optimised formulation in enhancing the intestinal permeability of metformin was evaluated using non-everted intestinal sac.
RESULTS
The data revealed that in weight ratio 1:4(metformin: SLS), the highest recovery was achieved. The physico-chemical properties of the optimised nano-droplets including size, polydispersity index (PdI), zeta potential, and loading efficiency (%) were 192.33 ± 9.9 nm, 0.275 ± 0.051; -1.52 mV, and 93.75 ± 0.77% (w/w), respectively.
CONCLUSIONS
The data obtained from the intestinal transport study demonstrated that SEDDS can significantly enhance the oral permeability of the compound.
目的
本研究旨在制备含有盐酸二甲双胍的自乳化药物传递系统（SEDDS）。
方法
通过静电相互作用将盐酸二甲双胍与十二烷基硫酸钠（SLS）制备成疏水离子对复合物。使用两水平完全析因法对纳米液滴进行优化，并对其形态进行了检查。在模拟胃液和肠液中评估了 SEDDS 中盐酸二甲双胍的释放情况。最后，使用外翻肠囊法评价了优化后的制剂增强盐酸二甲双胍肠道通透性的体外功效。
结果
数据显示，在质量比为 1:4（盐酸二甲双胍：SLS）时，达到了最高的回收率。优化后的纳米液滴的物理化学性质包括粒径、多分散指数（PdI）、Zeta 电位和载药量（%）分别为 192.33±9.9nm、0.275±0.051；-1.52mV 和 93.75±0.77%（w/w）。
结论
肠转运研究获得的数据表明，SEDDS 可以显著提高该化合物的口服渗透性。
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