Synthesis and Evaluation of Water-Soluble Polymeric Bone-Targeted Drug Delivery Systems

Four polymeric bone-targeting conjugates were synthesized based on poly(ethylene glycol) (PEG, two conjugates) and poly[N-(2-hydroxypropyl)methacrylamide] (PHPMA, two conjugates). The well-known bone-targeting compounds, alendronate and aspartic acid peptide, were used as bone-targeting moieties. Fl...

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Veröffentlicht in:	Bioconjugate chemistry 2003-09, Vol.14 (5), p.853-859
Hauptverfasser:	Wang, Dong, Miller, Scott, Sima, Monika, Kopečková, Pavla, Kopeček, Jindřich
Format:	Artikel
Sprache:	eng
Schlagworte:	alendronate Alendronate - chemical synthesis Alendronate - metabolism Animals Binding Sites - physiology Bone and Bones - drug effects Bone and Bones - metabolism D-Aspartic Acid - chemical synthesis D-Aspartic Acid - metabolism Drug Delivery Systems - methods Drug Evaluation, Preclinical - methods fluorescein isothiocyanate hydroxyapatite Male Mice Mice, Inbred BALB C poly[N-(2-hydroxypropyl)methacrylamide] Polymers - administration & dosage Polymers - chemical synthesis Polymers - metabolism Solubility Water - chemistry Water - metabolism
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Zusammenfassung:	Four polymeric bone-targeting conjugates were synthesized based on poly(ethylene glycol) (PEG, two conjugates) and poly[N-(2-hydroxypropyl)methacrylamide] (PHPMA, two conjugates). The well-known bone-targeting compounds, alendronate and aspartic acid peptide, were used as bone-targeting moieties. Fluorescein isothiocyanate (FITC) was attached to the conjugates as a model drug for detection purposes. The bone-targeting potential of these conjugates was tested in vitro with hydroxyapatite (HA) and in mice. The data obtained indicated that these novel delivery systems could specifically accumulate in the bone tissue.
ISSN:	1043-1802 1520-4812
DOI:	10.1021/bc034090j