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Nanoparticles of polyisohexylcyanoaerylate (PIHCA) as carriers of primaquine: formulation, physico-chemical characterization and acute toxicity

Authors
Journal
International Journal of Pharmaceutics
0378-5173
Publisher
Elsevier
Publication Date
Volume
68
Identifiers
DOI: 10.1016/0378-5173(91)90133-9
Keywords
  • Drug Targeting
  • Nanoparticles
  • Polyisohexylcyanoacrylate
  • Primaquine
  • Visceral Leishmaniasis
Disciplines
  • Chemistry

Abstract

Abstract Nanoparticles of polyisohexylcyanoacrylate with bound primaquine were prepared by an emulsion polymerization method and an i.v. formulation was obtained after freeze-drying. Such formulation is intended for drug targeting in visceral leishmaniasis. Drug binding seemed largely dependent on pH and formulation conditions were optimized to obtain a polymeric colloidal suspension containing particles in the 200–250 nm size range and 80–90% drug binding (final content of 10 mg of drug per vial). Aspects such as polymer-drug interaction, in vitro drug release and physicochemical stability were studied. A significant reduction in acute toxicity was demonstrated by using the targeted formulation in NMRI mice.

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