Effect of polyamidoamine (PAMAM) dendrimers on the in vitro release of water-insoluble nifedipine from aqueous gels |
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Authors: | Bharathi Devarakonda Ning Li Melgardt M de Villiers |
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Institution: | (1) Department of Basic Pharmaceutical Sciences, School of Pharmacy, The University of Louisiana at Monroe, 71209 Monroe, LA;(2) Division of Pharmaceutical Sciences, School of Pharmacy, University of Wisconsin, 53705 Madison, WI |
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Abstract: | The objective of this study was to determine the effect of ethylenediamine core PAMAM dendrimers, on the release of nifedipine
suspended in aqueous gels and to correlate release to the increase in solubility afforded by the dendrimers. Drug release
from aqueous 5% HPMC gels containing nifedipine (2% wt/vol) through 0.2-μm membranes was measured using Enhancer cells and
50% ethanolic solution as the receptor medium. The release from gels containing PAMAM G-3 and G-5 (0.25%–1% wt/vol) was compared
with gels containing the cosolvent isopropyl alcohol (10%–80% vol/vol). PAMAM dendrimers significantly increased the solubility
of nifedipine. This caused a significant increase in the release rate of nifedipine from the gel suspensions. The increase
in drug release depended on the concentration and generation size of the dendrimers added. For higher generations (G-5) lower
concentrations were needed to obtain equivalent increases in release. Although the increase in solubility and release was
not as high as from gels containing high concentrations of the cosolvent isopropyl alcohol, the dendrimers prevented the recrystallization
of the drug that was observed when the gels containing isopropyl alcohol were left open.
Published: October 24, 2005 |
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Keywords: | PAMAM dendrimers Nifedipine Release Gel |
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