Izadiyan Zahra, Basri Mahiran, Fard Masoumi Hamid Reza, Abedi Karjiban Roghayeh, Salim Norazlinaliza, Shameli Kamyar
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.
Chem Cent J. 2017 Mar 2;11:21. doi: 10.1186/s13065-017-0248-6. eCollection 2017.
The aim of this study is the development of nanoemulsions for intravenous administration of Sorafenib, which is a poorly soluble drug with no parenteral treatment. The formulation was prepared by a high energy emulsification method and optimized by response surface methodology. The effects of overhead stirring time, high shear rate, high shear time, and cycles of high-pressure homogenizer were studied in the preparation of nanoemulsion loaded with Sorafenib. Most of the particles in nanoemulsion are spherical in shape, the smallest particle size being 82.14 nm. The results of the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, a tetrazole reveal that the optimum formulation does not affect normal cells significantly in low drug concentrations but could remove the cancer cells. Finally, a formulation containing Sorafenib retained its properties over a period of 90 days. With characterization, the study of the formulated nanoemulsion has the potential to be used as a parenteral nanoemulsion in the treatment of cancer. Graphical abstractSchematic figure of high pressure homogenizer device.
本研究的目的是开发用于静脉注射索拉非尼的纳米乳剂，索拉非尼是一种难溶性药物，目前尚无肠胃外给药治疗方法。该制剂采用高能乳化法制备，并通过响应面法进行优化。在制备载有索拉非尼的纳米乳剂过程中，研究了顶置搅拌时间、高剪切速率、高剪切时间和高压均质机循环次数的影响。纳米乳剂中的大多数颗粒呈球形，最小粒径为82.14纳米。一种四唑盐，即3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐的结果表明，最佳制剂在低药物浓度下对正常细胞无显著影响，但可清除癌细胞。最后，含有索拉非尼的制剂在90天内保持其性质。通过表征，所制备的纳米乳剂研究有潜力用作治疗癌症的肠胃外纳米乳剂。图形摘要高压均质机装置示意图。
