Ozakar Emrah, Cetin Meltem, Ates Orhan, Hacimuftuoglu Ahmet
Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey.
Department of Ophthalmology, Faculty of Medicine, Ataturk University, Erzurum, Turkey.
Pak J Pharm Sci. 2019 Mar;32(2):547-554.
The purpose of the current study was to prepare nifedipine (NF) loaded-PLGA nanoparticles (NPs) using two different methods (nanoprecipitation method (N-2) and emulsion-solvent evaporation method (N-4)) to achieve the sustained release of NF and to reduce its side effects, and also to investigate the in vitro characteristics of NPs (surface morphology, particle size and size distribution, encapsulation efficiency and in vitro release characteristics). SEM images of nanoparticles revealed their approximate spherical shape. The mean particle sizes of the prepared nanoparticles ranged from 294.27±7.93 to 424.92±4.96 nm with almost neutral zeta potential values (close to 0 mV). The percent encapsulation efficiency values of N-2 and N-4 formulations 13.03±1.82% and 18.96±1.95% (p=0.05), respectively. The extents of cumulative drug release from N-2 and N-4 in PB pH 7.4 medium were up to about 100 % in 38 days and 22 days, respectively (when comparing two formulations, p<0.05). PLGA nanoparticles are useful systems for the sustained release of NF, and hence for reducing its side-effects and increasing patient compliance.
本研究的目的是使用两种不同方法(纳米沉淀法(N-2)和乳液-溶剂蒸发法(N-4))制备负载硝苯地平(NF)的聚乳酸-羟基乙酸共聚物(PLGA)纳米颗粒(NPs),以实现NF的缓释并降低其副作用,同时研究NPs的体外特性(表面形态、粒径和粒径分布、包封率和体外释放特性)。纳米颗粒的扫描电子显微镜(SEM)图像显示其近似球形。制备的纳米颗粒的平均粒径范围为294.27±7.93至424.92±4.96 nm,zeta电位值几乎呈中性(接近0 mV)。N-2和N-4制剂的包封率百分比值分别为13.03±1.82%和18.96±1.95%(p = 0.05)。在pH 7.4的磷酸盐缓冲液(PB)介质中,N-2和N-4的累积药物释放程度分别在38天和22天内高达约100%(比较两种制剂时,p<0.05)。PLGA纳米颗粒是用于NF缓释的有用体系,因此可用于减少其副作用并提高患者依从性。