A poly(amidoamine) (PAA) copolymer with β-cyclodextrin was obtained by polyaddition reaction of 6-deoxy-6-amino-β-cyclodextrin (β-CDNH2) and 2-methylpiperazine to 2,2-bis(acrylamido)acetic acid in aqueous medium. This β-CD/PAA copolymer bears β-CD units along the macromolecular chain, is water-soluble and non-cytotoxic. The complexing capacity of β-CD/PAA was determined using an antiviral drug, Acyclovir, as a model of poorly water-soluble drug. Complex formation was confirmed by means of DSC and FTIR analyses. β-CD/PAA can solubilize up to 11% w/w of Acyclovir notably increasing the aqueous solubility of the drug. The in vitro release studies showed the dependence of Acyclovir release rate on the solution pH. The antiviral activity of Acyclovir β-CD/PAA complex was evaluated against herpes simplex virus type I in cell cultures. The Acyclovir β-CD/PAA complex exhibited a higher antiviral activity than the free drug. © 2007 Elsevier B.V. All rights reserved.
Preparation and in vitro evaluation of the antiviral activity of the Acyclovir complex of a beta-cyclodextrin/poly(amidoamine) copolymer / M. Bencini, E. Ranucci, P. Ferruti, F. Trotta, M. Donalisio, M. Cornaglia, D. Lembo, R. Cavalli. - In: JOURNAL OF CONTROLLED RELEASE. - ISSN 0168-3659. - 126:1(2008), pp. 17-25.
|Titolo:||Preparation and in vitro evaluation of the antiviral activity of the Acyclovir complex of a beta-cyclodextrin/poly(amidoamine) copolymer|
BENCINI, MARCO (Primo)
RANUCCI, ELISABETTA (Secondo)
|Parole Chiave:||β-cyclodextrin; Acyclovir; Antiviral activity; Functionalization of polymers; Poly(amidoamine)s; Solubilizing power|
|Settore Scientifico Disciplinare:||Settore CHIM/04 - Chimica Industriale|
|Data di pubblicazione:||2008|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.jconrel.2007.11.004|
|Appare nelle tipologie:||01 - Articolo su periodico|