Synthesis and micellar characterization of luteinizing hormone‐releasing hormone poly(ethylene glycol)‐block‐poly(l‐histidine) copolymers

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Abstract
A facile and well‐controlled pathway was introduced to obtain optimal pH‐sensitive luteinizing hormone‐releasing hormone—functionalized poly(ethylene glycol)‐block‐poly(l‐histidine) (LHRH‐PEG‐PHIS) micelles in this paper. The influence of block‐selective solvent, the weight ratio of the selective solvent to common solvent and initial polymer concentration on the self‐assembly of LHRH‐PEG‐PHIS micelles were studied. These factors exerted remarkable influence on the morphology of the resulting micelles. The micelles showed a spherical geometry and an uniform appearance under the following optimal experimental conditions: LHRH‐PEG/PHIS ratio of 1.0 by molar, DMF as the selective solvent and 3.0 mg/mL as initial concentration, 100 W of ultrasonic power. These micelles had a small diameter (about 90 nm), low CMC (10 μg/mL), and pH‐sensitive switch in surface charge and micelles' size. As the pH of the micellar solution decreased from pH 7.4 to 5.5, the zeta potential of the LHRH‐PEG‐PHIS micelles increased from −0.02 mV to 20.7 mV and the diameter of the nanoparticles decreased from 137 nm to 76 nm. After 30 h of incubation at pH 5.0, 6.0, and 7.4 the released free Doxorubicin (DOX) was about 83.18%, 81.26%, and 30.35%, respectively. The LHRH‐PEG‐PHIS micelles could combine the characteristics of active targeting with pH‐triggered drug release promising as intracellular drug delivery carriers. POLYM. ENG. SCI., 55:277–286, 2015. © 2014 Society of Plastics Engineers
Funding Information
  • National Natural Science Foundation of China (30970788)

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