Polymeric micelles for acyclovir drug delivery

• Published in: Colloids and surfaces, B, Biointerfaces Vol. 122; pp. 738 - 745
• Main Authors: Sawdon, Alicia J., Peng, Ching-An
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.10.2014
• Subjects: Acyclovir; Acyclovir - administration & dosage; Antiviral Agents - administration & dosage; Chitosan; Chromatography, Gel; Conjugation; Drug Carriers; Drug delivery systems; Light scattering; Methoxypolyethylene glycol; Micellar drug delivery; Micelles; Microscopy, Electron, Transmission; MPEG encoders; Polymerization; Polymers - chemistry; Proton Magnetic Resonance Spectroscopy; Ring-opening polymerization; Spectroscopy, Fourier Transform Infrared; Video compression; Ring-opening polymerization; Methoxypolyethylene glycol; Chitosan; Acyclovir; Micellar drug delivery
• ISSN: 0927-7765; 1873-4367
• DOI: 10.1016/j.colsurfb.2014.08.011

•Acyclovir was used directly to initiate polymerization of ɛ-caprolactone.•ACV-tagged micelles were self-assembled by conjugation with hydrophilic poly(ethylene glycol) or chitosan.•ACV-tagged polymeric micelles are non-toxic.•ACV-tagged micelles are advantageous in terms of eliminating drug-loading steps, enhancing drug-carrying capacity, and decreasing production cost. Polymeric prodrug micelles for delivery of acyclovir (ACV) were synthesized. First, ACV was used directly to initiate ring-opening polymerization of ɛ-caprolactone to form ACV-polycaprolactone (ACV-PCL). Through conjugation of hydrophobic ACV-PCL with hydrophilic methoxy poly(ethylene glycol) (MPEG) or chitosan, polymeric micelles for drug delivery were formed. 1H NMR, FTIR, and gel permeation chromatography were employed to show successful conjugation of MPEG or chitosan to hydrophobic ACV-PCL. Through dynamic light scattering, zeta potential analysis, transmission electron microscopy, and critical micelle concentration (CMC), the synthesized ACV-tagged polymeric micelles were characterized. It was found that the average size of the polymeric micelles was under 200nm and the CMCs of ACV-PCL-MPEG and ACV-PCL-chitosan were 2.0mgL−1 and 6.6mgL−1, respectively. The drug release kinetics of ACV was investigated and cytotoxicity assay demonstrates that ACV-tagged polymeric micelles were non-toxic.