Department of Oncology, Suzhou Ninth People's Hospital, Suzhou, China.
Pharm Dev Technol. 2020 Jun;25(5):640-648. doi: 10.1080/10837450.2020.1727920. Epub 2020 Feb 26.
In this study, RGD coated GEM liposomes were prepared by the emulsification-solvent evaporation method. The and characterizations were done to evaluate the feasibility of application. The mean particle size of the prepared liposomes was found to be 165.6 ± 15.7 nm. The entrapment efficiency and drug loading of the formulation were 82.4% ± 7.2% and 10.1% ± 1.4%, respectively. The liposomes were negatively charged with a zeta potential of -25.8 mV. The surface morphology of RGD-GEM liposomes was spherical and smooth. After three months of storage at different conditions, lyophilized liposomes appeared to be stable since they showed no collapse or contraction. The Weibull model was the most appropriate kinetic model for RGD-GEM liposomes, showing that the release of GEM from the liposomes was in the manners of both dissolution and diffusion. , the additive cytotoxicity of RGD-GEM-LPs in our study was caused by the presence of RGD which is more effective in the treatment of breast cancer devoid of toxicity to normal cells. Liposomes could also significantly extend the role of GEM and showed higher bioavailability than solution.
在这项研究中，通过乳化-溶剂蒸发法制备了 RGD 涂层 GEM 脂质体。对其进行了 和 特性评估，以验证其应用的可行性。结果发现，所制备的脂质体的平均粒径为 165.6±15.7nm。包封率和载药量分别为 82.4%±7.2%和 10.1%±1.4%。脂质体带负电荷，zeta 电位为-25.8mV。RGD-GEM 脂质体的表面形态呈球形且光滑。在不同条件下储存三个月后，冻干脂质体似乎很稳定，因为它们没有塌陷或收缩。Weibull 模型是最适合 RGD-GEM 脂质体的动力学模型，表明 GEM 从脂质体中的释放方式既有溶解也有扩散。此外，本研究中 RGD-GEM-LPs 的附加细胞毒性是由于存在 RGD 所致，RGD 对乳腺癌的治疗更有效，而对正常细胞没有毒性。脂质体还可以显著延长 GEM 的作用时间，并显示出比溶液更高的生物利用度。
