Influence of sonication and in vitro evaluation of nifedipine self-nanoemulsifying drug delivery system

In order to develop a self-nanoemulsifying system, three components, olive oil, Tween 80, and Capmul, were used to construct a ternary phase diagram that helped to find the optimum formulation, which was loaded with nifedipine. The effect of sonication on drug loading was also evaluated. After that, measurement of the droplet size, size distribution, zeta potential, and scanning electron microscopy were conducted for evaluation and characterisation of the formulations. The phase diagram of four formulations showed nanosizes below 200 nm; however, only one was selected to be loaded with nifedipine. The selected formulation had the lowest droplet size of 98 nm and size distribution 0.192, and was composed of 48% Tween 80, 32% Capmul, and 20% olive oil. The nifedipine self-nanoemulsifying drug delivery system (SNEDDS) showed a significant change in the particle size (97 nm) and size distribution (0.257) after sonication. Its zeta potential was -32.3 mV indicating good stability. The SEM photographs of nifedipine showed particles with spherical shape and smooth surface. Finally, a self-nanoemulsifying formulation containing nifedipine, loaded in olive oil, was successfully prepared by mixing the oil with various types of surfactants and co-surfactants. A significant nifedipine self-nanoemulsifying system was developed and significantly improved accordingly.

为开发自纳米乳化系统，本研究以橄榄油、吐温80（Tween 80）及卡普mul（Capmul）三种组分构建三元相图，以此筛选最优处方并负载硝苯地平（nifedipine）。同时评估了超声处理对药物负载量的影响。随后通过测定液滴粒径、粒径分布、ζ电位以及扫描电子显微镜（scanning electron microscopy, SEM）观察，对处方进行表征与评价。基于该三元相图筛选得到四款候选处方，其纳米乳粒径均低于200 nm，但仅选取其中一款用于负载硝苯地平。该优选处方的最小液滴粒径为98 nm，粒径分布系数为0.192，处方组成为48%吐温80、32%卡普mul及20%橄榄油。负载硝苯地平的自纳米乳化给药系统（self-nanoemulsifying drug delivery system, SNEDDS）经超声处理后，粒径显著变为97 nm，粒径分布系数为0.257；其ζ电位为-32.3 mV，表明具备良好的稳定性。硝苯地平的SEM图像显示所得颗粒呈球形且表面光滑。最终，通过将橄榄油与多种表面活性剂及助表面活性剂混合，成功制备了负载硝苯地平的自纳米乳化处方。本研究成功开发了性能优异的硝苯地平自纳米乳化系统，并实现了显著的性能优化。