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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Dual approach utilizing self microemulsifying technique and novel P-gp inhibitor for effective delivery of taxanes
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Dual approach utilizing self microemulsifying technique and novel P-gp inhibitor for effective delivery of taxanes

机译：利用自身微乳化技术和新型P-gp抑制剂的双重方法可有效输送紫杉烷

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摘要

In the present work, concomitant use of self-microemulsifying drug delivery systems (SMEDDS) and a novel third-generation P-gp inhibitor, GF120918 (elacridar), for the effective transport of taxanes (paclitaxel and docetaxel) across an in vitro model of the intestinal epithelium and uptake into tumor cells were investigated. On the basis of solubility studies and ternary phase diagrams, different SMEDDS formulations of taxanes were prepared and characterized. In caco-2 cell permeation study, paclitaxel-loaded SMEDDS along with GF120918 showed a four-fold increase in apparent permeability, while docetaxel-loaded SMEDDS in combination with GF120918 showed a nine-fold increase in permeability, as compared to plain drug solution. Cell uptake studies on A549 cells were performed with microemulsions formed from both SMEDDS formulations loaded with rhodamine 123 dye and showed good uptake than plain dye solution. Confocal laser scanning microscopic images further confirmed the higher uptake of both SMEDDS formulations in the presence of GF120918.
机译：在目前的工作中，伴随使用自微乳化药物递送系统（SMEDDS）和新型第三代P-gp抑制剂GF120918（elacridar），可以有效地跨紫杉烷的体外模型转运紫杉烷类药物（紫杉醇和多西紫杉醇）研究了肠上皮和肿瘤细胞的摄取。根据溶解度研究和三元相图，制备并表征了紫杉烷的不同SMEDDS配方。在caco-2细胞渗透研究中，与普通药物溶液相比，紫杉醇载药的SMEDDS与GF120918的表观通透性增加了四倍，而紫杉醇载药的SMEDDS与GF120918的组合显示出了通透性的九倍。使用由两种装有若丹明123染料的SMEDDS制剂形成的微乳液，对A549细胞进行细胞摄取研究，结果显示，与普通染料溶液相比，该摄取良好。共聚焦激光扫描显微图像进一步证实了在存在GF120918的情况下，两种SMEDDS制剂的摄取量更高。

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