洛伐他汀纳米粒的设计、优化及体内评价。
Nanoparticles of Lovastatin: Design, Optimization and in vivo Evaluation.
机构信息
Department of Quality Control & Quality Assurance, Holding Company for Biological Products and Vaccines, Cairo, Egypt.
Department of Pharmaceutics, College of Pharmacy, Qassim University, Buraidah, Saudi Arabia.
出版信息
Int J Nanomedicine. 2020 Jun 17;15:4225-4236. doi: 10.2147/IJN.S241120. eCollection 2020.
INTRODUCTION
The aim of the study was to optimize the processing factors of precipitation-ultrasonication technique to prepare nano-sized particles of Lovastatin (LA) for enhancing its solubility, dissolution rate and in vivo bioavailability.
METHODS
LA nanoparticles (LANs) were prepared using precipitation-ultrasonication technique under different processing factors. LANs were characterized in terms of particle size, zeta potential and in vitro release. Stability studies at 4°C, 25°C and 40°C were conducted for optimum formulation. In addition, the in vivo bioavailability of the optimum formula was studied in comparison to a marketed product in white master rats.
RESULTS
The optimized LAN formula (LAN15) had particle size (190±15), polydispersity index (0.626±0.11) and a zeta potential (-25±1.9 mV). The dissolution study of the nanosuspensions showed significant enhancement compared with pure drug. After 50 min, only 20.12±1.85% of LA was dissolved while 99.1±1.09% of LA was released from LAN15. Stability studies verified that nanosuspensions at 4°C and 25°C showed higher stability with no particle growth compared to the samples studied at 40°C. In vivo studies conducted in rats verified that there was 1.45-fold enhancement of C of LAN15 as compared to marketed tablets.
CONCLUSION
Nanoparticle prepared by ultrasonication-assisted precipitation method is a promising formula for enhancing the solubility and hence the bioavailability of Lovastatin.
简介
本研究旨在优化沉淀-超声技术的处理因素，以制备洛伐他汀（LA）纳米颗粒，以提高其溶解度、溶出速率和体内生物利用度。
方法
采用沉淀-超声技术，在不同的处理因素下制备 LA 纳米颗粒（LANs）。从粒径、Zeta 电位和体外释放三个方面对 LANs 进行了表征。在 4°C、25°C 和 40°C 下进行了稳定性研究，以确定最佳配方。此外，与市售产品相比，在白色 master 大鼠中研究了最佳配方的体内生物利用度。
结果
优化的 LAN 配方（LAN15）的粒径为（190±15）nm、多分散指数（0.626±0.11）和 Zeta 电位（-25±1.9 mV）。纳米混悬剂的溶解研究表明，与纯药物相比，其具有显著的增强作用。50 min 后，LA 仅溶解 20.12±1.85%，而 LAN15 中 99.1±1.09%的 LA 释放。稳定性研究表明，与在 40°C 下研究的样品相比，纳米混悬剂在 4°C 和 25°C 下显示出更高的稳定性，没有颗粒生长。在大鼠体内研究中，LAN15 的 C 与市售片剂相比提高了 1.45 倍。
结论
超声辅助沉淀法制备的纳米颗粒是一种有前途的配方，可提高洛伐他汀的溶解度，从而提高其生物利用度。
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