PHEA-graft-polybutylmethacrylate copolymer microparticles for delivery of hydrophobic drugs

International Journal of Pharmaceutics
Mariano LicciardiGaetano Giammona

Abstract

Polymeric microparticles encapsulating two model hydrophobic drugs, beclomethasone dipropionate (BDP) and flutamide (FLU) were prepared by using the high pressure homogenization-solvent evaporation method starting from a oil-in-water emulsion. For the preparation of polymeric microparticles a α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide (PHEA) graft copolymer with comb like structure was properly synthesized via grafting from atom transfer radical polymerization (ATRP) technique, by using two subsequent synthetic steps. In the first step a polymeric multifunctional macroinitiator was obtained by the conjugation of a proper number of 2-bromoisobutyryl bromide (BIB) residues to the PHEA side chains, obtaining the PHEA-BIB copolymer. PHEA-BIB copolymer was then used as macroinitiator for the polymerization via ATRP of the hydrophobic monomer such as butyl methacrylate (BMA) to obtain the α,β-poly(N-2-hydroxyethyl)-D,L-aspartamide-co-(N-2-ethylen-isobutyrate)-graft-poly(butyl methacrylate) copolymer (PHEA-IB-p(BMA)). Spherical microparticles with 1-3 microns diameter were prepared. Microparticles loaded with BDP or FLU were also prepared. In vitro mucoadhesion and enzymatic degradation studies evidenced bioadhesive properties and bio...Continue Reading

References

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Dec 28, 2010·International Journal of Pharmaceutics·Emanuela Fabiola CraparoGennara Cavallaro
Jan 1, 2012·Pharmaceutics·Nicolas AntonThierry F Vandamme

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Citations

Apr 25, 2013·International Journal of Pharmaceutics·Aparna SaigalSui Yung Chan
Feb 13, 2016·Biomacromolecules·Emanuela Fabiola CraparoGennara Cavallaro
Sep 28, 2015·International Journal of Pharmaceutics·Gennara CavallaroAnnalisa Dalmoro
Jun 19, 2015·Pharmaceutical Research·Mariano LicciardiGaetano Giammona
Mar 5, 2013·International Journal of Pharmaceutics·Adriana TrapaniMaria Jose Alonso
Sep 26, 2013·International Journal of Pharmaceutics·Calogero FioricaGaetano Giammona
Jan 26, 2017·International Journal of Pharmaceutics·Gennara CavallaroBarbara Dapas
Jan 9, 2019·AAPS PharmSciTech·Anne TrivinoHarsh Chauhan
Jul 21, 2014·Journal of Materials Chemistry. B, Materials for Biology and Medicine·M LicciardiG Giammona
May 27, 2015·Macromolecular Rapid Communications·Emanuela Fabiola CraparoGennara Cavallaro
Jan 26, 2020·Pharmaceutics·Emanuela Fabiola CraparoGennara Cavallaro
Jan 21, 2015·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Andrea CappelliSalvatore Vomero

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