Facile preparation of pH-responsive polyurethane nanocarrier for oral delivery.
This study reports a novel one pot synthesis of pH-responsive nanocarrier for oral delivery of hydrophobic drug under gastrointestinal tract. Triblock copolymer MPEG-HTPB-MPEG was synthesized coupling of MPEG and HTPB using hexamethylene diisocyanate(HDI) and pH-responsive carboxylic acid group was attached to polybuthadiene backbone by thiol-ene click reaction in a facile and convenient procedure. The MPEG-HTPB (g-COOH)-MPEG block copolymers were self-organized into micelle assemblies in the water. The size and shape of the micelle assemblies were confirmed by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The nanocarriers have high drug loading ability for poorly water-soluble drug. The pH-responsive profile was demonstrated by pH-dependent swelling and in vitro drug release. <10.0% IBU was released under artificial gastric fluid after 2h, whereas an immediate release was observed under artificial intestinal fluid. The XTT assay indicated that the micelle obtained from PEG-HTPB (g-COOH)-PEG triblock copolymer are safe in a wide range of concentrations. The results show that pH-responsive PEG-HTPB (g-COOH)-PEG triblock copolymers are promising nanocarriers for the oral administration of hydrophobic drugs.
Department of polymer, Faculty of Chemistry, Shahid Beheshti University, G.C, 1983963411 Tehran, Iran. Electronic address: M-nabid@sbu.ac.ir.
Mohammad Reza
MR
Nabid
Department of polymer, Faculty of Chemistry, Shahid Beheshti University, G.C, 1983963411 Tehran, Iran.
Ismail
I
Omrani
D000284:Administration, Oral; D002850:Chromatography, Gel; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D000067493:Dynamic Light Scattering; D057446:Hydrodynamics; D006863:Hydrogen-Ion Concentration; D007052:Ibuprofen / Q000494:pharmacology; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000138:chemical synthesis / Q000737:chemistry; D011140:Polyurethanes / Q000138:chemical synthesis / Q000737:chemistry*; D066244:Proton Magnetic Resonance Spectroscopy; D017550:Spectroscopy, Fourier Transform Infrared
D004337:Drug Carriers; D008823:Micelles; D011140:Polyurethanes; D011092:Polyethylene Glycols; D007052:Ibuprofen
HTPB; Nanoparticle; One-pot polymer synthesis; Oral delivery; Polyurethane; Stimuli-responsive