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

Jung Kyo Cho; Changju Chun; Hyo Jeong Kuh; Soo Chang Song

doi:10.1016/j.ejpb.2012.04.008

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

Jung Kyo Cho
, Changju Chun
, Hyo Jeong Kuh
, Soo Chang Song

Department of Biomedicine & Health Science

Korea Institute of Science and Technology
University of Science and Technology UST
Chonnam National University

Research output: Contribution to journal › Article › peer-review

40 Scopus citations

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). Crown

Original language	English
Pages (from-to)	582-590
Number of pages	9
Journal	European Journal of Pharmaceutics and Biopharmaceutics
Volume	81
Issue number	3
DOIs	https://doi.org/10.1016/j.ejpb.2012.04.008
State	Published - Aug 2012

Bibliographical note

Funding Information:
This research was financially supported by Korea Institute of Science and Technology (KIST) and the Ministry of Education, Science and Technology in Korea. We thank Mr. Yun-Sik Nam, Ms. Chang Won Kim, Ms. Ki Yun Hong, and Mr. Joo-Ho Lee for their kind technical support.

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Antitumor activity
Poly(organophosphazene)
Polymer-drug conjugate
Stability of camptothecin
Thermosensitive hydrogel

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10.1016/j.ejpb.2012.04.008

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title = "Injectable poly(organophosphazene)-camptothecin conjugate hydrogels: Synthesis, characterization, and antitumor activities",

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). Crown",

keywords = "Antitumor activity, Poly(organophosphazene), Polymer-drug conjugate, Stability of camptothecin, Thermosensitive hydrogel",

author = "Cho, \{Jung Kyo\} and Changju Chun and Kuh, \{Hyo Jeong\} and Song, \{Soo Chang\}",

note = "Funding Information: This research was financially supported by Korea Institute of Science and Technology (KIST) and the Ministry of Education, Science and Technology in Korea. We thank Mr. Yun-Sik Nam, Ms. Chang Won Kim, Ms. Ki Yun Hong, and Mr. Joo-Ho Lee for their kind technical support. ",

year = "2012",

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doi = "10.1016/j.ejpb.2012.04.008",

language = "English",

volume = "81",

pages = "582--590",

journal = "European Journal of Pharmaceutics and Biopharmaceutics",

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AU - Chun, Changju

AU - Kuh, Hyo Jeong

AU - Song, Soo Chang

N1 - Funding Information: This research was financially supported by Korea Institute of Science and Technology (KIST) and the Ministry of Education, Science and Technology in Korea. We thank Mr. Yun-Sik Nam, Ms. Chang Won Kim, Ms. Ki Yun Hong, and Mr. Joo-Ho Lee for their kind technical support.

PY - 2012/8

Y1 - 2012/8

N2 - 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). Crown

AB - 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). Crown

KW - Antitumor activity

KW - Poly(organophosphazene)

KW - Polymer-drug conjugate

KW - Stability of camptothecin

KW - Thermosensitive hydrogel

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JO - European Journal of Pharmaceutics and Biopharmaceutics

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

Abstract

Bibliographical note

UN SDGs

Keywords

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