Deoxycholic acid-grafted PEGylated chitosan micelles for the delivery of mitomycin C
作者：Xiu-Rong Zhang#, Nian-Qiu Shi#(Co-author), Yang Zhao, He-Yun Zhu, Jiao Guan, and Ying Jin
關(guān)鍵字：Biodistribution, mitomycin C,pharmacokinetics, polymeric micelles,synthesis
論文來源：期刊
具體來源：Drug Dev Ind Pharm. 2015 Jun;41(6):916-926.(SCI,IF=2.429)
發(fā)表時(shí)間：2015年
Mitomycin C (MTC) was incorporated to a micelle system preparing from a polymer named deoxycholic acid chitosan-grafted poly(ethylene glycol) methyl ether (mPEG-CS-DA).
mPEG-CS-DA was synthesized and characterized by 1H nuclear magnetic resonance (1H-NMR) and Fourier transform infrared spectroscopy. mPEG-CS-DA formed a core-shell micellar
structure with a critical micelle concentration of 6.57 mg/mL. The mPEG-CS-DA micelles were spherical with a hydrodynamic diameter of about 231 nm. After poly(ethylene glycol)ylation of deoxycholic acid chitosan (CS-DA), the encapsulation efficiency and drug loading efficiency increased from 50.62% to 56.42% and from 20.51% to 24.13%, respectively. The mPEG-CS-DA micelles possessed a higher drug release rate than the CS-DA micelles. For pharmacokinetics, the area under the curve (AUC) of the mPEG-CS-DA micelles was 1.5 times higher than that of MTC injection, and these micelles can enhance the bioavailability of MTC. mPEG-CS-DA micelles reduced the distribution of MTC in almost all normal tissues and had the potential to improve the kidney toxicity caused by MTC injection.
