A biodegradable graft polymer-drug conjugate (GPDC) was synthesized through copper-catalyzed azide-alkyne click reaction of acetylene-functionalized polylactide with azide-functionalized poly(ethylene oxide) and azide-functionalized paclitaxel. The well-controlled structure of resulting GPDC was verified by 1H NMR and GPC characterizations. With high grafting efficiency, the GPDC had a PTXL loading of 23.5 wt%. DLS analysis indicated that the GPDC exhibited nanoscopic size in water. The release study showed PTXL moieties can be effectively released through the cleavage of the hydrolysable conjugation linkages at pH 7.4. The cytotoxicity study of GPDC revealed that, with the increase of PTXL concentrations, GPDC became more effective in killing MCF-7 cancer cells than free PTXL.

Biodegradable polylactide-g-paclitaxel/poly(ethylene oxide) for drug delivery

244th National Meeting (2012)

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