Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Alhofuf, Al-Ahsa, 36362, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig, Egypt.
Int J Nanomedicine. 2024 Aug 5;19:7945-7961. doi: 10.2147/IJN.S463750. eCollection 2024.
Monitoring noncommunicable diseases is regarded as a critical concern that has to be managed in order to avoid a wide variety of complications such as increasing blood lipid levels known as dyslipidemia. Statin drugs, mostly, Rosuvastatin (RSV) was investigated for its effectiveness in treating dyslipidemia. However, reaching the most efficient treatment is essential and improving the effect of RSV is crucial. Therefore, a combination therapy was a good approach for achieving significant benefit. Although RSV is hydrophobic, which would affect its absorption and bioavailability following oral administration, overcoming this obstacle was important.
To that end, the purpose of the present investigation was to incorporate RSV into certain lipid-based nanocarriers, namely, nanostructured lipid carrier (NLC) prepared with virgin coconut oil (CCO).
The optimized RSV-NLC formula was selected, characterized and examined for its in vitro, kinetic, and stability profiles. Eventually, the formula was investigated for its in vivo hypolipidemic action.
The optimized NLC formulation showed a suitable particle size (279.3±5.03 nm) with PDI 0.237 and displayed good entrapment efficiency (75.6±1.9%). Regarding in vitro release, it was efficiently prolonged for 24 h providing 93.7±1.47%. The optimized formula was established to be stable after 3 months storage at two different conditions; 4°C and 25°C. Importantly, including CCO in the development of RSV-NLC could impressively enhance lowering total cholesterol level in obese rat models, which endorse the potential synergistic action between RSV and CCO.
The study could elucidate the impact of developing NLC using CCO for improving RSV anti-hyperlipidemic activity.
监测非传染性疾病被认为是一个关键问题，必须加以管理，以避免出现血脂水平升高（即血脂异常）等多种并发症。他汀类药物，主要是瑞舒伐他汀（RSV），因其治疗血脂异常的有效性而受到研究。然而，达到最有效的治疗效果是至关重要的，提高 RSV 的效果是至关重要的。因此，联合治疗是一种实现显著获益的好方法。尽管 RSV 具有疏水性，这会影响其口服后的吸收和生物利用度，但克服这一障碍很重要。
为此，本研究的目的是将 RSV 纳入某些基于脂质的纳米载体中，即使用初榨椰子油（CCO）制备的纳米结构脂质载体（NLC）。
选择、表征和研究了优化的 RSV-NLC 配方，考察了其体外、动力学和稳定性特征。最终，研究了该配方的体内降血脂作用。
优化的 NLC 配方显示出合适的粒径（279.3±5.03nm），PDI 为 0.237，包封效率良好（75.6±1.9%）。体外释放实验表明，其释放时间可延长至 24 小时，达到 93.7±1.47%。该优化配方在 4°C 和 25°C 两种不同条件下储存 3 个月后仍保持稳定。重要的是，在 RSV-NLC 的开发中加入 CCO 可以显著增强肥胖大鼠模型中总胆固醇水平的降低，这支持了 RSV 和 CCO 之间潜在的协同作用。
本研究阐明了使用 CCO 开发 NLC 对提高 RSV 抗高血脂活性的影响。
