■监测非传染性疾病被认为是一个至关重要的问题,必须加以管理,以避免各种并发症,例如称为血脂异常的血脂水平升高。他汀类药物,大多数情况下,研究了瑞舒伐他汀(RSV)治疗血脂异常的有效性。然而,达到最有效的治疗是至关重要的,提高RSV的效果是至关重要的。因此,联合治疗是获得显著获益的良好方法.虽然RSV是疏水性的,这将影响其口服后的吸收和生物利用度,克服这个障碍很重要。
■为此,本研究的目的是将RSV掺入某些基于脂质的纳米载体中,即,用初榨椰子油(CCO)制备的纳米结构脂质载体(NLC)。
■选择了优化的RSV-NLC配方,表征和检查其体外,动力学,和稳定性配置文件。最终,研究了该配方的体内降血脂作用。
■优化的NLC制剂显示出合适的粒度(279.3±5.03nm),PDI为0.237,并显示出良好的包封效率(75.6±1.9%)。关于体外释放,有效延长24小时,提供93.7±1.47%。优化的配方在4°C和25°C两种不同条件下储存3个月后稳定。重要的是,在RSV-NLC的开发中包括CCO可以令人印象深刻地增强肥胖大鼠模型中总胆固醇水平的降低,这证明了RSV和CCO之间的潜在协同作用。
■该研究可以阐明使用CCO开发NLC对改善RSV抗高脂血症活性的影响。
UNASSIGNED: 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.
UNASSIGNED: 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).
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: The study could elucidate the impact of developing NLC using CCO for improving RSV anti-hyperlipidemic activity.