HPMA copolymer-doxorubicin-gadolinium conjugates: synthesis, characterization, and in vitro evaluation.
This study describes the synthesis, characterization, and in vitro evaluation of N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-gadolinium (Gd)-doxorubicin (Dox) conjugates. Copolymers of HPMA were derivatized to incorporate side chains for Gd chelation and Dox conjugation. The conjugates were characterized by their side chain contents, T(1) relaxivity (r(1)), stability, and in vitro cytotoxicity. High stability and relaxivity of these conjugates coupled with low toxicity show their potential for monitoring the in vivo fate of HPMA-based drug delivery systems by magnetic resonance imaging techniques.
Zarabi
Bahar
B
Department of Pharmaceutical Sciences, University of Maryland, Baltimore, Maryland 21201, USA.
Nan
Anjan
A
Zhuo
Jiachen
J
Gullapalli
Rao
R
Ghandehari
Hamidreza
H
D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004317:Doxorubicin / Q000737:chemistry* / Q000494:pharmacology; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005682:Gadolinium / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D008689:Methacrylates / Q000737:chemistry; D051379:Mice; D041681:NIH 3T3 Cells; D011109:Polymethacrylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
D000903:Antibiotics, Antineoplastic; D004337:Drug Carriers; D008689:Methacrylates; D011109:Polymethacrylic Acids; D004317:Doxorubicin; D005682:Gadolinium; C032802:hydroxypropyl methacrylate