Self-emulsifying drug delivery systems as a tool to improve solubility and bioavailability of resveratrol.
Self-emulsifying drug delivery systems as a tool to improve solubility and bioavailability of resveratrol.
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DOI：
10.2147/dddt.s95905
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发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Abourehab MA
中科院分区：
文献类型：
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作者：
Balata GF;Essa EA;Shamardl HA;Zaidan SH;Abourehab MA
白藜芦醇是一种非黄酮类多酚化合物，具有广泛的所需生物活性，包括抗氧化、抗炎、抗糖尿病、心脏保护和抗肿瘤活性。然而，人们担心白藜芦醇的生物利用度可能会限制其一些临床用途。因此，本研究的目的是提高白藜芦醇的溶出率和口服降糖降血脂作用。这是使用自乳化药物输送系统实现的。测定了白藜芦醇在各种油、表面活性剂和助表面活性剂中的溶解度。绘制相图以确定使用橄榄油、Tween 80 和丙二醇的有效自乳化区域。对制备的自乳化药物递送系统制剂进行热力学稳定性、乳化效率、液滴尺寸、zeta电位和体外药物释放测试。无沉淀的自乳化时间平均为 17-99 秒，平均液滴尺寸范围为 285 至 823 nm，总体 zeta 电位为 -2.24 至 -15.4 mv。与未加工的药物相比，所有制剂均改善了药物溶出，并且随着油含量的增加溶出参数呈下降趋势。采用优化配方F19，其溶出率为94%，而纯药仅为42%，用于研究白藜芦醇对糖尿病白化大鼠的体内降血糖和降血脂作用，并与不同剂量的纯白藜芦醇的效果进行比较。采用优化配方 F19 10 mg/kg 治疗，对糖尿病诱发的白化大鼠具有显着的降血糖和降血脂作用，其效果与高剂量（20 mg/kg）未加工的白藜芦醇几乎相似。研究得出结论，制剂F19具有良好的乳化性能、均匀的球体尺寸、令人满意的体外药物释放曲线和显着的体内降血糖作用，这为白藜芦醇的未来递送提供了机会。
Resveratrol is a nonflavonoid polyphenolic compound which has a broad range of desirable biological actions which include antioxidant, anti-inflammatory, antidiabetic, cardioprotective, and antitumor activities. However, there is concern that the bioavailability of resveratrol may limit some of its clinical utility. So, the aim of this study was to enhance the dissolution rate and oral hypoglycemic and hypolipidemic effect of resveratrol. This was achieved using self-emulsifying drug delivery system. The solubility of resveratrol was determined in various oils, surfactants, and cosurfactants. Phase diagram was plotted to identify the efficient self-emulsification regions using olive oil, Tween 80, and propylene glycol. The prepared self-emulsifying drug delivery system formulations were tested for thermodynamic stability, emulsification efficiency, droplet size, zeta potential, and in vitro drug release. Self-emulsification time averaged 17–99 seconds without precipitation and the mean droplet sizes ranged from 285 to 823 nm with overall zeta potential of −2.24 to −15.4 mv. All formulations improved drug dissolution in relation to unprocessed drug with a trend of decreased dissolution parameters with increasing oil content. The optimized formula, F19, with dissolution efficiency of 94% compared to only 42% of pure drug was used to study the in vivo hypoglycemic and hypolipidemic effects of resveratrol in diabetic-induced albino rats and comparing these effects with that of pure resveratrol in different doses. Treatment with the optimized formula, F19, at 10 mg/kg had significant hypoglycemic and hypolipidemic effects in diabetic-induced albino rats which were nearly similar to the high dose (20 mg/kg) of unprocessed resveratrol. From the study, it was concluded that formulation F19 has good emulsification property with uniform globule size, satisfactory in vitro drug release profile, and significant in vivo hypoglycemic effects which identify future opportunities for resveratrol delivery.