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Friday 28 September 2007

Cyclodextrin/carbopol micro-scale interpenetrating networks (ms-IPNs) for drug delivery.

By: Rodriguez-Tenreiro C, Diez-Bueno L, Concheiro A, Torres-Labandeira JJ, Alvarez-Lorenzo C.

J Control Release 2007 Oct;123(1):56-66

Cross-linking of hydroxypropyl-beta-cyclodextrin (HP beta CD) with ethyleneglycol diglycidylether (EGDE) in carbopol dispersions enabled the synthesis of cyclodextrin hydrogels with domains of interpenetrating acrylic microgels (micro-scale-IPNs) in a single step under mild conditions. As carbopol proportion increased, the hardness and compressibility of the ms-IPNs decreased, but their bioadhesion force and pH-responsiveness rose. Control HP beta CD hydrogel and ms-IPNs were loaded with estradiol and ketoconazole by immersion in drug suspensions, some of which were autoclaved to enhance (up to a 50%) drug/cyclodextrin affinity. ms-IPNs prepared with 0.8% or 1.0% carbopol showed the highest loading due to their greater swelling degree and, consequently, mesh size. The total loading of the ms-IPNs greatly exceeded (up to 200-fold) the amount dissolved in their aqueous phase, which highlights the main role of drug complexation with the cross-linked cyclodextrins. The affinity of the drug for HP beta CD sustained the release for several days; the rate being also dependent on carbopol content and on pH of the medium. Therefore, an adequate design of the HP beta CD/carbopol ms-IPNs provides a single material with tunable mechanical properties, in which the complexation ability of cyclodextrins is combined with the bioadhesive and pH-responsive properties of carbopol. The ms-IPNs are potentially useful as vehicles of relatively hydrophobic substances.

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