Injectable poly(organophosphazene)-camptothecin conjugate hydrogels: synthesis, characterization, and antitumor activities

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Jung-Kyo ChoSoo-Chang Song

Abstract

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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Citations

Oct 12, 2012·Molecular Pharmaceutics·Olga Yu ZolotarskayaHu Yang
Jun 3, 2014·BioMed Research International·Amanda L Baillargeon, Kibret Mequanint
Jun 17, 2014·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Shuxin XuLiandong Deng
Nov 28, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ewa OledzkaMarcin Sobczak
Sep 1, 2015·International Journal of Pharmaceutics·Behrang Shiri VarnamkhastiRassoul Dinarvand
Jul 18, 2016·Drug Discovery Today·Mohammad NorouziDonald W Miller
Aug 26, 2016·Nanomedicine : Nanotechnology, Biology, and Medicine·Lulu WangYancai Wang
Sep 25, 2019·Pharmaceutics·Giuseppe CirilloFrancesca Iemma
Feb 7, 2020·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Zhipeng NiLison Teng
Nov 7, 2013·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Wei HaYan-Ping Shi
Jan 7, 2016·Journal of Materials Chemistry. B, Materials for Biology and Medicine·Liang QiuCai-Yuan Pan
Oct 13, 2020·Advanced Functional Materials·Binglin SuiPeisheng Xu
Aug 1, 2021·International Journal of Pharmaceutics·Diana RafaelIbane Abasolo

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