Abo Enin Hadel A
Pharmaceutics Department, Taif University , Taif , Saudi Arabia and.
Drug Dev Ind Pharm. 2015;41(7):1047-56. doi: 10.3109/03639045.2014.983113. Epub 2014 Nov 18.
The aim is improving the antihyperlipidemic activity of Rosuvastatin Calcium (Rs) through improving its solubility using self-nanoemulsifying drug delivery system (SNEDDS) containing natural oil full of unsaturated fatty acid and omega 3.
A 7 × 3(2) full factorial design was adopted for optimization of oil ratio, Surfactant: Co-surfactant (S:CoS) ratio and oil:S/CoS ratio. Ternary phase diagrams were constructed for optimizing the system with drug loading (10 and 20%). The optimized SNEDD systems were evaluated according to their physical evaluation and drug release. Furthermore, the anti-hyperlipidemia efficacy was compared with commercially marketed product on rates followed by clinical study.
The system containing Tween 80:PEG 400 (3:1) and olive oil:garlic oil (1:1) as an oily phase has droplet size less than 100 nm, ZP (+23.43 ± 2.58 mV), PDI (<0.02) and cloud point (>90 °C). In vitro drug release studies showed remarkable enhancement of the Rs release from Rs-SNEDDS. The antihyperlipidemic effect of Rs-SNEDDS is greater than that of the commercial tablets and the pure drug on rates and in hyperlipidemic patients.
Rs-SNEDDS is a promising drug delivery system for improving the drug solubility and antihyperlipidemic effect using natural oils as (olive oil and garlic oil).
通过使用含有富含不饱和脂肪酸和ω-3的天然油的自纳米乳化药物递送系统（SNEDDS）提高瑞舒伐他汀钙（Rs）的溶解度，从而改善其抗高血脂活性。
采用7×3（2）全因子设计优化油相比例、表面活性剂与助表面活性剂比例（S:CoS）以及油与S/CoS比例。构建三元相图以优化载药量为10%和20%的系统。根据其物理性质评估和药物释放情况对优化后的SNEDD系统进行评价。此外，在高脂血症患者中，将抗高血脂疗效与市售产品进行了速率比较，并进行了临床研究。
以吐温80:聚乙二醇400（3:1）为表面活性剂、橄榄油:大蒜油（1:1）为油相的系统，液滴尺寸小于100nm，ζ电位为（+23.43±2.58mV），多分散指数（PDI）小于0.02，浊点大于90℃。体外药物释放研究表明，Rs-SNEDDS中Rs的释放显著增强。Rs-SNEDDS在高脂血症患者中的抗高血脂作用在速率上大于市售片剂和纯药物。
Rs-SNEDDS是一种有前景的药物递送系统，可利用天然油（如橄榄油和大蒜油）提高药物溶解度和抗高血脂作用。
