Injectable poly(organophosphazene)-camptothecin conjugate hydrogels: Synthesis, characterization, and antitumor activities
- Injectable poly(organophosphazene)-camptothecin conjugate hydrogels: Synthesis, characterization, and antitumor activities
- 조정교; 전창주; 구효정; 송수창
- Antitumor activity; Poly(organophosphazene); Thermosensitive hydrogel; Polymer?drug conjugate; Stability of camptothecin
- Issue Date
- European journal of pharmaceutics and biopharmaceutics
- VOL 81, NO 3, 582-590
- The objective of this study is to develop an effective polymer therapeutics involving camptothecin (CPT)
with enhanced efficacy and lessened systemic side-toxicity for cancer treatment. Polymer–CPT conjugates
(PCCs), which consisted of CPT–20-glycinate and poly(organophosphazene) bearing carboxylic acid,
were synthesized, characterized for physicochemical properties, in vitro degradation and CPT release
behaviors from the PCC, and evaluated their anticancer activity. The aqueous solutions of all these PCCs
showed a thermo-responsive sol–gel transition behavior for injectable application near room temperature.
The CPT incorporated into the hydrogel was proven to be stable in vitro over 15 days. The in vitro
cytotoxicity of the PCC was verified to be effective against four kinds of human cancer cell lines. The
in vivo anticancer activity study with HT-29 colon cancer cell xenografted mice showed that the intratumorally
injected PCC hydrogel inhibited the tumor growth more effectively relative to CPT alone ( 29%
vs. 130% in tumor size).
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