Abstract
In this study, the PEGylated nanostructured lipid carriers (PEG-NLC) were constructed for the intravenous delivery of 17-allylamino-17-demethoxygeldanamycin (17AAG). 17AAG-PEG-NLC was successfully prepared by the method of emulsion evaporation at a high temperature and solidification at a low temperature using a mixture of glycerol monostearate and PEG2000-stearate as solid lipids, and medium-chain triglyceride as the liquid lipid. The results revealed that the morphology of the NLC was spheroidal. The particle size, zeta potential and entrapment efficiency for 17AAG-PEG-NLC were observed as 189.4 nm, −20.2 mV and 83.42%, respectively. X-ray diffraction analysis revealed that 17AAG existed as amorphous structures in the nanoparticles. In the in vitro release study, the 17AAG from 17AAG-PEG-NLC exhibited a biphasic release pattern with burst release initially and sustained release afterwards. In addition, 17AAG-PEG-NLC showed a significantly higher in vitro antitumor efficacy and longer retention time in vivo than 17AAG solution. These results indicated that 17AAG-PEG-NLC may offer a promising alternative to the current 17AAG formulations for the treatment of solid tumors.
Declaration of interest
This work was supported by the Scientific Research Foundation of Administration of Traditional Chinese Medicine of Heilongjiang Province to Wang Zhi-yong (ZHY12-Z162), the Scientific Research Foundation of Health and Family Planning Commission of Heilongjiang Province to Wang Jing-hua (2014-280), the Scientific Research Fund of Higher Vocational Colleges of Heilongjiang Provincial Education Department to Yang Song-ling (11555091), and the Scientific Research Fund of Heilongjiang Provincial Education Department to Hou Shu-ying (12541560) and Wang Jing-hua (12541566).
The authors report no conflicts of interest.