H. Oberoi, N. V. Nukolova, T. Bronich
2011
Citations
0
Influential Citations
2
Citations
Quality indicators
Journal
PMSE preprints. American Chemical Society. Division of Polymeric Materials: Science and Engineering. Meeting
Abstract
The platinum (II) analog, dichloro(1,2-diaminocyclohexane)platinum(II) (DACHPt), the oxaliplatin parent complex, is a potent chemotherapeutic with a wide spectrum of anticancer activity, low toxicity and lack of cross resistance in many cisplatin-resistant cancers1,2. However, its clinical use is restrained by its poor solubility, unfavorable pharmacokinetics and various non-target side effects such as, cumulative peripheral distal neurotoxicity and acute dysesthesias3,4. Polymer micelles with intramicellar cross-linking for structural reinforcement and polyanionic core for platinum (II) encapsulation offer a novel macromolecular platform for carrier based delivery of such compounds. These drug-carrier conjugates acquire new physicochemical, biochemical and pharmacological characteristics, thereby offering the possibly of reducing side effects, increasing drug bioavailability at the target sites and minimizing development of drug resistance5,6. In this study block ionomer complexes (BIC) of poly(ethylene oxide)-b-poly(methacrylic acid) (PEO-b-PMA) and divalent metal cations (Ca2+) were utilized as templates for the synthesis of cross-linked (cl)-micelles7,8. DACHPt was loaded into the cross-linked core of the polymeric micelles. The physicochemical properties, loading efficacy, drug release from the polymer micelles and in vitro cytotoxicity of the formulation were investigated.