Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia.
Department of Chemistry, Faculty of Science, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia; Laboratory of Molecular Biomedicine, Institute of Bioscience, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia.
Mater Sci Eng C Mater Biol Appl. 2019 Jan 1;94:841-849. doi: 10.1016/j.msec.2018.10.015. Epub 2018 Oct 4.
Nanoemulsions have been used as a drug carrier system, particularly for poorly water-soluble drugs. Sorafenib is a poorly soluble drug and also there is no parenteral treatment. The aim of this study is the development of nanoemulsions for intravenous administration of Sorafenib. The formulations were prepared by high energy emulsification method and optimized by using Response Surface Methodology (RSM). Here, the effect of independent composition variables of lecithin (1.16-2.84%, w/w), Medium-Chain Triglycerides (2.32-5.68%, w/w) and polysorbate 80 (0.58-1.42%, w/w) amounts on the properties of Sorafenib-loaded nanoemulsion was investigated. The three responses variables were particle size, zeta potential, and polydispersity index. Optimization of the conditions according to the three dependent variables was performed for the preparation of the Sorafenib-loaded nanoemulsions with the minimum value of particle size, suitable rage of zeta potential, and polydispersity index. A formulation containing 0.05% of Sorafenib kept its properties in a satisfactory range over the evaluated period. The composition with 3% Medium-Chain Triglycerides, 2.5% lecithin and 1.22% polysorbate 80 exhibited the smallest particle size and polydispersity index (43.17 nm and 0.22, respectively) with the zeta potential of -38.8 mV was the optimized composition. The fabricated nanoemulsion was characterized by the transmission electron microscope (TEM), viscosity, and stability assessment study. Also, the cytotoxicity result showed that the optimum formulations had no significant effect on a normal cell in a low concentration of the drug but could eliminate the cancer cells. The dose-dependent toxicity made it a suitable candidate for parenteral applications in the treatment of breast cancer. Furthermore, the optimized formulation indicated good storage stability for 3 months at different temperatures (4 ± 2 °C, 25 ± 2 °C and 45 ± 2 °C).
纳米乳已被用作药物载体系统，特别是对于水溶性差的药物。索拉非尼是一种水溶性差的药物，也没有可供注射的治疗方法。本研究的目的是开发用于索拉非尼静脉给药的纳米乳。这些制剂是通过高能乳化法制备的，并通过响应面法（RSM）进行优化。在这里，研究了独立的组成变量，包括卵磷脂（1.16-2.84%，w/w）、中链甘油三酯（2.32-5.68%，w/w）和聚山梨醇酯 80（0.58-1.42%，w/w）的含量对索拉非尼负载纳米乳性质的影响。三个响应变量分别是粒径、Zeta 电位和多分散指数。根据三个依赖变量对条件进行优化，以制备具有最小粒径、合适的 Zeta 电位范围和多分散指数的索拉非尼负载纳米乳。含有 0.05%索拉非尼的制剂在评估期间保持了其性质在令人满意的范围内。含有 3%中链甘油三酯、2.5%卵磷脂和 1.22%聚山梨醇酯 80 的配方表现出最小的粒径和多分散指数（分别为 43.17nm 和 0.22），Zeta 电位为-38.8mV，是优化的配方。所制备的纳米乳通过透射电子显微镜（TEM）、粘度和稳定性评估进行了表征。此外，细胞毒性结果表明，最佳配方在低药物浓度下对正常细胞没有显著影响，但可以消除癌细胞。这种剂量依赖性的毒性使它成为治疗乳腺癌的一种适合的可供注射的候选药物。此外，优化后的配方在不同温度（4±2°C、25±2°C 和 45±2°C）下储存 3 个月时表现出良好的储存稳定性。
