Department of Clinical Pharmacy, College of Pharmacy, Jazan University, Jazan, Saudi Arabia.
Substance Abuse and Toxicology Research Centre, Jazan University, Jazan, Saudi Arabia.
Drug Deliv. 2020 Dec;27(1):622-631. doi: 10.1080/10717544.2020.1754526.
NLC containing Gefitinib (NANOGEF) was prepared using stearic acid, sesame oil and surfactants (sodium lauryl sulfate and tween 80). NANOGEFs were evaluated for particle size, polydispersity index (PdI), zeta potential, entrapment efficiency (EE), stability, release studies and cytotoxicity studies (MTT assay). The optimized NANOGEF exhibited particle size of 74.06 ± 9.73 d.nm, PdI of 0.339 ± 0.029 and EE of 99.76 ± 0.015%. The TEM study revealed spherical shape of NANOGEF formulations. The slow and sustained release behavior was exhibited by all NANOGEFs. The effects of surfactants were observed not only on particle size but also on zeta potential, entrapment efficiency, stability and release studies. The MTT assay revealed 4.5 times increase in cytotoxicity for optimized NANOGEF (IC = 4.642 µM) when compared with Gefitinib alone (IC = 20.88 µM in HCT-116 cells). Thus NANOGEF may be considered as a potential drug delivery system for the cure of colon cancer.
采用硬脂酸、芝麻油和表面活性剂（硫酸月桂酯和吐温 80）制备了含吉非替尼的 NLC（NANOGEF）。对 NANOGEF 的粒径、多分散指数（PdI）、Zeta 电位、包封效率（EE）、稳定性、释放研究和细胞毒性研究（MTT 测定）进行了评价。优化的 NANOGEF 的粒径为 74.06±9.73 d.nm，PdI 为 0.339±0.029，EE 为 99.76±0.015%。TEM 研究表明 NANOGEF 制剂呈球形。所有 NANOGEF 均表现出缓慢和持续的释放行为。表面活性剂的作用不仅影响粒径，还影响 Zeta 电位、包封效率、稳定性和释放研究。与单独的吉非替尼（HCT-116 细胞中的 IC = 20.88 μM）相比，优化的 NANOGEF（IC = 4.642 μM）的细胞毒性增加了 4.5 倍。因此，NANOGEF 可以被认为是治疗结肠癌的潜在药物传递系统。
