Metwally Mohamed Ali, El-Zawahry El-Yamani Ibrahim, Ali Maher Amer, Ibrahim Diaa Farrag, Sabry Shereen Ahmed, Sarhan Omnia Mohamed
Department of Zoology, Faculty of Science, Al-Azhar University, Cairo 11651, Egypt.
Department of Zoology, Faculty of Science, Zagazig University, Zagazig 44519, Egypt.
Korean J Physiol Pharmacol. 2024 May 1;28(3):275-284. doi: 10.4196/kjpp.2024.28.3.275.
Worldwide, cardiovascular disease is the main cause of death, which accordingly increased by hyperlipidemia. Hyperlipidemia therapy can include lifestyle changes and medications to control cholesterol levels. Statins are the medications of the first choice for dealing with lipid abnormalities. Rosuvastatin founds to control high lipid levels by hindering liver production of cholesterol and to achieve the targeted levels of low-density lipoprotein cholesterol, another lipid lowering agents named ezetimibe may be used as an added therapy. Both rosuvastatin and ezetimibe have low bioavailability which will stand as barrier to decrease cholesterol levels, because of such depictions, formulations of this combined therapy in nanotechnology will be of a great assistance. Our study demonstrated preparations of nanoparticles of this combined therapy, showing their physical characterizations, and examined their behavior in laboratory conditions and vivo habitation. The mean particle size was uniform, polydispersity index and zeta potential of formulations were found to be in the ranges of (0.181-0.72) and (-13.4 to -6.24), respectively. Acceptable limits of entrapment efficiency were affirmed with appearance of spherical and uniform nanoparticles. In vitro testing showed a sustained release of drug exceeded 90% over 24 h. In vivo study revealed an enhanced dissolution and bioavailability from loaded nanoparticles, which was evidenced by calculated pharmacokinetic parameters using triton for hyperlipidemia induction. Stability studies were performed and assured that the formulations are kept the same up to one month. Therefore, nano formulations is a suitable transporter for combined therapy of rosuvastatin and ezetimibe with improvement in their dissolution and bioavailability.
在全球范围内，心血管疾病是主要死因，而高脂血症相应地增加了心血管疾病的发生。高脂血症治疗可包括生活方式改变和控制胆固醇水平的药物治疗。他汀类药物是治疗脂质异常的首选药物。瑞舒伐他汀通过阻碍肝脏胆固醇生成来控制高脂质水平，并达到低密度脂蛋白胆固醇的目标水平，另一种名为依折麦布的降脂药物可作为辅助治疗使用。瑞舒伐他汀和依折麦布的生物利用度都很低，这将成为降低胆固醇水平的障碍，鉴于此描述，纳米技术中这种联合疗法的制剂将有很大帮助。我们的研究展示了这种联合疗法纳米颗粒的制备，展示了它们的物理特性，并在实验室条件和体内环境中研究了它们的行为。平均粒径均匀，制剂的多分散指数和zeta电位分别在(0.181 - 0.72)和(-13.4至-6.24)范围内。包封率的可接受限度通过球形且均匀的纳米颗粒得以确认。体外测试显示药物在24小时内持续释放超过90%。体内研究显示负载纳米颗粒后药物的溶出度和生物利用度提高，这通过使用曲通诱导高脂血症计算药代动力学参数得到证实。进行了稳定性研究并确保制剂在长达一个月的时间内保持不变。因此，纳米制剂是瑞舒伐他汀和依折麦布联合治疗的合适载体，可提高它们的溶出度和生物利用度。
