Nanaki Stavroula, Siafaka Panoraia I, Zachariadou Dorothea, Nerantzaki Maria, Giliopoulos Dimitrios J, Triantafyllidis Konstantinos S, Kostoglou Margaritis, Nikolakaki Eleni, Bikiaris Dimitrios N
Laboratory of Polymer Chemistry and Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
Laboratory of General and Inorganic Chemical Technology, Aristotle University of Thessaloniki, GR-54124 Thessaloniki, Macedonia, Greece.
Eur J Pharm Sci. 2017 Mar 1;99:32-44. doi: 10.1016/j.ejps.2016.12.010. Epub 2016 Dec 8.
In this work, high surface area mesoporous silica (SBA-15) was loaded with paclitaxel (taxol, PTX) and was further entrapped into poly(lactic acid-co-glycolic acid) (PLGA) microparticles (MPs). A modified solvent evaporation-emulsion method was used in order to formulate the composite microparticles with sizes of 8-12μm. PTX loaded SBA-15 as well as the PLGA/PTX-SBA-15 composites were characterized in terms of their morphology, crystal structure and thermal properties. Drug content, loading efficiency, particle size and the in-vitro drug release kinetics of the PLGA/PTΧ-SBA-15 microspheres were also investigated. The in vitro release studies were carried out using Simulated Body Fluid (SBF) at 37°C revealing that the prepared formulations present higher dissolution rate than pure PTX and sustained pattern which is ideal for anticancer carriers. Modeling and data analysis of the in vitro drug release was also investigated. It was also shown that all microparticles have low cytotoxicity in HUVE cells. Finally, it was found that drug loaded microparticles are very effective in Human Cervical Adenocarcinoma (HeLa) cells.
在本研究中，将紫杉醇（泰素，PTX）负载于高比表面积介孔二氧化硅（SBA - 15）上，并进一步包封于聚乳酸 - 乙醇酸共聚物（PLGA）微粒（MPs）中。采用改进的溶剂蒸发 - 乳液法制备尺寸为8 - 12μm的复合微粒。对负载PTX的SBA - 15以及PLGA/PTX - SBA - 15复合材料的形态、晶体结构和热性能进行了表征。还研究了PLGA/PTX - SBA - 15微球的药物含量、负载效率、粒径和体外药物释放动力学。在37°C下使用模拟体液（SBF）进行体外释放研究，结果表明所制备的制剂比纯PTX具有更高的溶解速率和持续释放模式，这对于抗癌载体来说是理想的。还对体外药物释放进行了建模和数据分析。结果还表明，所有微粒在人脐静脉内皮细胞（HUVE细胞）中具有低细胞毒性。最后，发现载药微粒对人宫颈腺癌（HeLa细胞）非常有效。
