Li Zhenbao, Tao Wenhui, Zhang Dong, Wu Chunnuan, Song Binbin, Wang Shang, Wang Tianyang, Hu Mingming, Liu Xiaohong, Wang Yongjun, Sun Yinghua, Sun Jin
School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
Tianjin Medical University Cancer Hospital, Tianjin 300060, China.
Asian J Pharm Sci. 2017 May;12(3):285-291. doi: 10.1016/j.ajps.2016.08.006. Epub 2016 Aug 31.
A biodegradable poly(lactic-co-glycolic acid) loading atorvastatin calcium (AC) nanoparticles (AC-PLGA-NPs) were prepared by probe ultrasonication and evaporation method aiming at improving the oral bioavailability of AC. The effects of experimental parameters, including stabilizer species, stabilizer concentration and pH of aqueous phase, on particle size were also evaluated. The resultant nanoparticles were in spherical shape with an average diameter of 174.7 nm and a narrow particle size distribution. And the drug loading and encapsulation efficiency were about 8% and 71%, respectively. The particle size and polydispersion were almost unchanged in 10 days. The release curves of AC-PLGA-NPs displaying sustained release characteristics indicated that its release mechanisms were matrix erosion and diffusion. The pharmacokinetic study revealed that the C and AUC of AC-PLGA-NPs in rats were nearly 3.7-fold and 4.7-fold higher than that of pure atorvastatin calcium suspension. Our results demonstrated that the delivery of AC-PLGA-NPs could be a promising approach for the oral delivery of AC for enhanced bioavailability.
为提高阿托伐他汀钙(AC)的口服生物利用度,采用探头超声和蒸发法制备了负载阿托伐他汀钙的可生物降解聚乳酸-羟基乙酸共聚物(AC-PLGA)纳米粒。还评估了包括稳定剂种类、稳定剂浓度和水相pH值在内的实验参数对粒径的影响。所得纳米粒呈球形,平均直径为174.7nm,粒径分布窄。药物负载率和包封率分别约为8%和71%。粒径和多分散性在10天内几乎不变。显示出缓释特性的AC-PLGA纳米粒的释放曲线表明其释放机制为基质侵蚀和扩散。药代动力学研究表明,AC-PLGA纳米粒在大鼠体内的Cmax和AUC分别比纯阿托伐他汀钙混悬液高近3.7倍和4.7倍。我们的结果表明,AC-PLGA纳米粒给药可能是一种有前景的口服AC给药方法,可提高生物利用度。