Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10162399 | Journal of Pharmaceutical Sciences | 2014 | 9 Pages |
Abstract
Temperatureâ and pHâresponsive copolymers were γâray grafted onto polypropylene (PP) to provide its surface with capability to load and to control the release of nonsteroidal antiâinflammatory drugs (NSAIDs) with the aim of being useful as component of drugâeluting medical devices. Poly(N,Nâ²âdimethylaminoethylmethacrylate) (PDMAEMA) or poly(4âvinylpyridine) (P4VP) were grafted onto PP films via a direct method, and then poly(Nâisopropylacrylamide) (PNIPAAm) was grafted applying a preirradiation method. The binary graft copolymers showed hemocompatibility and certain capability to adsorb albumin. (PPâgâDMAEMA)âgâNIPAAm exhibited higher affinity for ibuprofen and, particularly, diclofenac than (PPâgâ4VP)âgâNIPAAm. Sustained release was observed under physiological conditions. Cytotoxicity and antiâinflammatory activity of NSAIDâeluting (PPâgâDMAEMA)âgâNIPAAm films were evaluated on RAW 264.7 macrophage cells. First, dose dependence of antiâinflammatory activity and cytotoxicity of ibuprofen and diclofenac on RAW 264.7 cells were investigated to elucidate the ranges of drug concentration that the graft copolymers should provide. Optimal concentrations of diclofenac and ibuprofen at which they reduce inflammation while maintaining cell viability were determined to be 200 μg/mL and above 400 μg/mL in culture medium. Sequential grafting of DMAEMA and NIPAAm made PP surface to exhibit remarkably high affinity to diclofenac, being able to load and to regulate drug release fulfilling in vitro requirements to avoid inflammatory response. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:1269-1277, 2014
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Authors
Hector Ivan MelendezâOrtiz, Patricia DÃazâRodrÃguez, Carmen AlvarezâLorenzo, Angel Concheiro, Emilio Bucio,