title: Synthesis and characterization of PHV-block-mPEG diblock copolymer and its formation of amphiphilic nanoparticles for drug delivery.
abstract: Despite the recent research interest in the field of nanoparticles delivery system, their structure modification and transport behavior of various hydrophobic drugs is poorly developed. In this article the synthesis of novel amphiphilic diblock copolymer poly([R]-3-hydroxyvalerate)-block-monomethoxy poly(ethylene glycol) (PHV-block-mPEG) was undertaken by modifying the structure of biodegradable and hydrophobic poly([R]-3-hydroxyvalerate) (PHV) with hydrophilic monomethoxy poly(ethylene glycol) (mPEG). The chemical combination of the two blocks was carried out in the melt using bis(2-ethylhexanoate) tin as transesterification catalyst. The synthesized product was characterized by gel permeation chromatography (GPC), 1H nuclear magnetic resonance (NMR) and differential scanning calorimetry (DSC) analysis. The block copolymer self-assembled into amphiphilic nanoparticles with a core of hydrophobic PHV and a shell of hydrophilic mPEG in aqueous solution. Characterization of the nanoparticles showed the formation of discrete, spherically shaped nanoparticles with mean particle size of 200 +/- 1 nm and zeta potential of -14 +/- 1 mV. A hydrophobic drug thymoquinone was efficiently incorporated into the core hydrophobic domain of the nanoparticles and its release kinetics was studied in vitro. The amphiphilic PEGylated nanoparticles showed biocompatibility when checked in neuronal hippocampal cells of prenatal rat. Our results suggest that the amphiphilic nanoparticles with core-shell structures are potentially useful to develop novel drug carriers.
authors: Nano-Biomaterials Science Laboratory, Division of Applied Life Sciences (BK21), Graduate School and Environmental Biotechnology National Core Research Center, Gyeongsang National University, Jinju 660-701, Republic of Korea.
authors: Mohsin
authors: M
authors: Shah
authors: Mun Hwan
authors: MH
authors: Choi
authors: Najeeb
authors: N
authors: Ullah
authors: Myeong Ok
authors: MO
authors: Kim
authors: Sung Chul
authors: SC
authors: Yoon
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D016227:Benzoquinones / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured; D002850:Chromatography, Gel; D016503:Drug Delivery Systems; D005260:Female; D006624:Hippocampus / Q000187:drug effects; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D018625:Microscopy, Atomic Force; D053758:Nanoparticles / Q000737:chemistry*; D009474:Neurons / Q000187:drug effects; D019906:Nuclear Magnetic Resonance, Biomolecular; D011091:Polyesters / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D014631:Valerates / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D016227:Benzoquinones; D011091:Polyesters; D014631:Valerates; D011092:Polyethylene Glycols; C073314:poly(3-hydroxyvalerate); C028210:monomethoxypolyethylene glycol; C003466:thymoquinone