Hydroxyapatite functionalization to trigger adsorption and release of risedronate

[Display omitted] •Tailor-made delivery systems for risedronate as antiresorptive agent are proposed.•Local release on osteoporotic sites to prevent the drawbacks of systemic treatment.•Hydroxyapatite functionalization controls the processes of drug adsorption/release.•Zinc-substituted hydroxyapatit...

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Veröffentlicht in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2017-12, Vol.160, p.493-499
Hauptverfasser: Forte, Lucia, Sarda, Stéphanie, Combes, Christèle, Brouillet, Fabien, Gazzano, Massimo, Marsan, Olivier, Boanini, Elisa, Bigi, Adriana
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Sprache:eng
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Zusammenfassung:[Display omitted] •Tailor-made delivery systems for risedronate as antiresorptive agent are proposed.•Local release on osteoporotic sites to prevent the drawbacks of systemic treatment.•Hydroxyapatite functionalization controls the processes of drug adsorption/release.•Zinc-substituted hydroxyapatite promotes risedronate adsorption.•PEI functionalization of hydroxyapatite modifies adsorption/release mechanisms. Bisphosphonates are widely employed drugs for the treatment of pathologies characterized by excessive bone resorption, and display a great affinity for apatitic supports. In this work we investigate how hydroxyapatite functionalization can influence the processes of adsorption and release of a bisphosphonate, namely risedronate. To this aim, pure hydroxyapatite (HA), hydroxyapatite with a partial substitution of Zn to Ca (ZnHA) and poly-ethylenimine-functionalized hydroxyapatite (HAPEI) were submitted to interaction with risedronate solution. The results indicate that the mechanisms of adsorption and release are greatly influenced by the type of the apatitic support. All the apatitic supports display Langmuir isotherms for risedronate adsorption. However in the case of HAPEI the plateau is not reached even at high equilibrium concentrations in solution. The data suggest that risedronate adsorption on HAPEI mineral-organic support occurs not only through chemisorption on apatitic phase, as on HA and ZnHA, but also through physisorption involved by PEI coating, which modulates also bisphosphonate release. These properties of tailor-made hydroxyapatite supports could be exploited to develop delivery systems for antiresorptive agents directly on osteoporotic sites.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2017.09.055