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Nanoparticles of Lovastatin: Design, Optimization and in vivo Evaluation.
International Journal of Nanomedicine ( IF 8 ) Pub Date : 2020-06-17 , DOI: 10.2147/ijn.s241120 Dalia A Gaber 1, 2
International Journal of Nanomedicine ( IF 8 ) Pub Date : 2020-06-17 , DOI: 10.2147/ijn.s241120 Dalia A Gaber 1, 2
Affiliation
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 Cmax 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.
Keywords: hyperlipidemia, HPMC, nano size, factors, antisolvent, bioavailability
中文翻译：
洛伐他汀纳米粒子：设计、优化和体内评估。
引言：本研究的目的是优化沉淀-超声技术的加工因素，制备洛伐他汀（LA）纳米颗粒，以提高其溶解度、溶出度和体内生物利用度。
方法：在不同的加工因素下，使用沉淀-超声技术制备 LA 纳米颗粒 (LANs)。LAN 的特征在于颗粒大小、zeta 电位和体外释放。进行了 4°C、25°C 和 40°C 的稳定性研究以获得最佳配方。此外，还研究了最佳配方的体内生物利用度，并与白色母鼠的市售产品进行了比较。
结果：优化的 LAN 配方 (LAN15) 具有粒径 (190± 15)、多分散指数 (0.626± 0.11) 和 zeta 电位 (- 25± 1.9 mV)。与纯药物相比，纳米混悬剂的溶出度研究显示出显着增强。50 分钟后，只有 20.12±1.85% 的 LA 被溶解，而 99.1±1.09% 的 LA 从 LAN15 中释放出来。稳定性研究证实，与在 40°C 研究的样品相比，在 4°C 和 25°C 下纳米悬浮液表现出更高的稳定性，没有颗粒生长。在大鼠中进行的体内研究证实，与市售片剂相比，LAN15的 C max提高了 1.45 倍。
结论：通过超声辅助沉淀法制备的纳米颗粒是提高洛伐他汀溶解度和生物利用度的有前途的配方。
关键词：高脂血症，HPMC，纳米尺寸，因素，抗溶剂，生物利用度
更新日期：2020-06-30
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 Cmax 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.
Keywords: hyperlipidemia, HPMC, nano size, factors, antisolvent, bioavailability
中文翻译：
洛伐他汀纳米粒子：设计、优化和体内评估。
引言：本研究的目的是优化沉淀-超声技术的加工因素，制备洛伐他汀（LA）纳米颗粒，以提高其溶解度、溶出度和体内生物利用度。
方法：在不同的加工因素下，使用沉淀-超声技术制备 LA 纳米颗粒 (LANs)。LAN 的特征在于颗粒大小、zeta 电位和体外释放。进行了 4°C、25°C 和 40°C 的稳定性研究以获得最佳配方。此外，还研究了最佳配方的体内生物利用度，并与白色母鼠的市售产品进行了比较。
结果：优化的 LAN 配方 (LAN15) 具有粒径 (190± 15)、多分散指数 (0.626± 0.11) 和 zeta 电位 (- 25± 1.9 mV)。与纯药物相比，纳米混悬剂的溶出度研究显示出显着增强。50 分钟后，只有 20.12±1.85% 的 LA 被溶解，而 99.1±1.09% 的 LA 从 LAN15 中释放出来。稳定性研究证实，与在 40°C 研究的样品相比，在 4°C 和 25°C 下纳米悬浮液表现出更高的稳定性，没有颗粒生长。在大鼠中进行的体内研究证实，与市售片剂相比，LAN15的 C max提高了 1.45 倍。
结论：通过超声辅助沉淀法制备的纳米颗粒是提高洛伐他汀溶解度和生物利用度的有前途的配方。
关键词：高脂血症，HPMC，纳米尺寸，因素，抗溶剂，生物利用度
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