Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, Heilongjiang 150040, China.
Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, Heilongjiang 150040, China.
Int J Biol Macromol. 2019 Oct 1;138:207-214. doi: 10.1016/j.ijbiomac.2019.07.083. Epub 2019 Jul 12.
In this work, paclitaxel was loaded into porous starch in the form of nanoparticles (PNPS), and the properties of PNPS were investigated by using raw paclitaxel and the system of paclitaxel directly loaded into porous starch (PPS) as control groups. According to the tested results, the drug loading (DL) and encapsulation efficiency (EE) of PNPS were 14.13%±0.27% and 73.92%±0.54%, higher than that of PPS (9.79%±0.31% and 71.17%±0.67%) respectively. Compared with raw paclitaxel and PPS, PNPS exhibited the more prominent dissolution rate and bioavailability, in which the bioavailability of PPS and PNPS were 2.94 and 5.42 times of that of raw paclitaxel respectively. In addition, the IC values of raw paclitaxel, PPS and PNPS on Lewis Lung Carcinoma (LLC) cells were 17,703.41±15.76μM, 95.10±5.32μM and 85.68±7.38μM respectively. Furthermore, the residues of acetone in PPS and PNPS were less than the ICH limit for acetone in class III solvents. To summarize, the preparation of PNPS was a potential method to improve the dissolution and bioavailability of paclitaxel.
在这项工作中，紫杉醇被负载到多孔淀粉中形成纳米颗粒（PNPS），并通过使用原紫杉醇和直接负载到多孔淀粉（PPS）的系统作为对照组来研究 PNPS 的性质。根据测试结果，PNPS 的载药量（DL）和包封率（EE）分别为 14.13%±0.27%和 73.92%±0.54%，高于 PPS 的 9.79%±0.31%和 71.17%±0.67%。与原紫杉醇和 PPS 相比，PNPS 表现出更突出的溶解速率和生物利用度，其中 PPS 和 PNPS 的生物利用度分别是原紫杉醇的 2.94 倍和 5.42 倍。此外，原紫杉醇、PPS 和 PNPS 对 Lewis 肺癌（LLC）细胞的 IC 值分别为 17,703.41±15.76μM、95.10±5.32μM 和 85.68±7.38μM。此外，PPS 和 PNPS 中的丙酮残留量均低于 ICH 对三类溶剂中丙酮的限量。总之，PNPS 的制备是提高紫杉醇溶解和生物利用度的一种潜在方法。
