کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5549526 | 1556732 | 2017 | 8 صفحه PDF | دانلود رایگان |
Paclitaxel (PTX) is an important cancer chemotherapeutic drug. To ameliorate the disadvantages of paclitaxel, this study designed liposomes to load paclitaxel, adding the acid-sensitive material cholesteryl hemisuccinate (CHEMS) to increase the accumulation of the drug in the tumor site. To begin, we used a high-performance liquid chromatography (HPLC) method to determine the content of PTX and the encapsulation efficiency. Then, we prepared paclitaxel-loaded acid-sensitive liposomes (PTX ASLs) by a thin-film dispersion method. We investigated the physical and chemical properties of the liposomes. The particle size was 210.8 nm, the polydispersity index (PDI) was 0.182 and the ζ-potential was â31.2âmV. The liposome shape was observed by transmission electron microscopy (TEM), and the results showed that the liposomes were round with a homogenous size distribution. The release characteristics of the liposomes in vitro were studied via a dynamic dialysis method. The results showed that the prepared liposomes had acid sensitivity and sustained release properties. An in vitro cellular uptake assay of MCF-7 cells showed that the cell uptake of coumarin-6-loaded acid-sensitive liposomes was significantly higher than that of free coumarin-6. The cytotoxicity of the PTX ASLs was significantly higher than that of paclitaxel. In conclusion, these results showed that the prepared liposomes had clear acid-sensitive release characteristics and a higher cell uptake rate and cytotoxicity than free PTX. The system is very suitable for targeted cancer therapy with paclitaxel.
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Journal: Asian Journal of Pharmaceutical Sciences - Volume 12, Issue 5, September 2017, Pages 470-477