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TANG Lidan, SHEN Yan, TU Jiasheng. Preparation and stability of poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly(glutamic acid)/poly lysine triblock complex micelle[J]. Journal of China Pharmaceutical University, 2014, 45(3): 301-306. DOI: 10.11665/j.issn.1000-5048.20140309
Citation: TANG Lidan, SHEN Yan, TU Jiasheng. Preparation and stability of poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly(glutamic acid)/poly lysine triblock complex micelle[J]. Journal of China Pharmaceutical University, 2014, 45(3): 301-306. DOI: 10.11665/j.issn.1000-5048.20140309
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Preparation and stability of poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly(glutamic acid)/poly lysine triblock complex micelle

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  • In order to improve the structural stability of the original polymeric micelles based on poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)(mPEG-PLA)copolymer conjugate, the electroneutral polyion complex micelles with equal proportion of poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly(glutamic acid)(mPEG-PLA-PLG)and poly(ethylene glycol)monomethyl ether-poly(D, L-lactic acid)-poly lysine(mPEG-PLA-PLL)were prepared. The enhanced stability of the new micelle was attributed to electrostatic attraction. The target products were obtained by reacting the amino boded terminal hydroxyl group of mPEG-PLA with cyclic carboxylic acid anhydridesof glutamic acid and lysine, respectively through ring opening reaction, and subsequent protecting group removal. Their structures were identified by 1H NMR and IR, and the differences of the critical micelle concentration(CMC)between mPEG-PLA and the modified polymers were measured by fluorescence. Dialysis was empolyed to prepare deoxypodophyllotoxin loaded polymeric micelles. The drug-loading capacity and encapsulation efficiency of mPEG-PLA micelles and electroneutral polyion complex micelle were determined by HPLC. The change of their particle size and drug content in 25 °C water bath were assessed by laser particle analyzer(dynamic light scattering)and HPLC, respectively. Both micelles had low CMC value and similar drug-loading capacity and encapsulation efficiency. However, the stability of the polymer complex micelles was two times higher than that of mPEG-PLA, which represented a significant enhancement.
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