Targeted delivery of curcumin to tumors via PEG-derivatized FTS-based micellar system

Yichao Chen; Xiaolan Zhang; Jianqin Lu; Yixian Huang; Jiang Li; Song Li

doi:10.1208/s12248-014-9595-6

Targeted delivery of curcumin to tumors via PEG-derivatized FTS-based micellar system

Yichao Chen, Xiaolan Zhang, Jianqin Lu, Yixian Huang, Jiang Li, Song Li

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

27 Scopus citations

Abstract

Curcumin and S-trans, trans-farnesylthiosalicylic acid (FTS) are two promising anticancer agents. In this study, we demonstrated that the two agents exerted significant synergy in antitumor activity in various types of cancer cells with combination indices ranging from 0.46 to 0.98 (a value of less than unity indicates synergism). We have further shown that synergistic-targeted co-delivery of the two agents can be achieved via formulating curcumin in polyethylene glycol (PEG)-derivatized FTS-based nanomicellar system. Curcumin formulated in PEG-FTS micelles had small size of around 20 nm. The nanomicellar curcumin demonstrated enhanced cytotoxicity towards several cancer cell lines in vitro. Intravenous application of curcumin-loaded micelle (20 mg kg ^-1 curcumin) led to a significantly more effective inhibition of tumor growth in a syngeneic mouse breast cancer model (4T1.2) than curcumin formulated in Cremophor/EL (P<0.05).

Original language	English (US)
Pages (from-to)	600-608
Number of pages	9
Journal	AAPS Journal
Volume	16
Issue number	3
DOIs	https://doi.org/10.1208/s12248-014-9595-6
State	Published - May 2014
Externally published	Yes

Keywords

S-trans, trans-farnesylthiosalicylic acid
curcumin
dual-functional carrier
micelles
synergy

ASJC Scopus subject areas

Pharmaceutical Science

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10.1208/s12248-014-9595-6

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title = "Targeted delivery of curcumin to tumors via PEG-derivatized FTS-based micellar system",

abstract = "Curcumin and S-trans, trans-farnesylthiosalicylic acid (FTS) are two promising anticancer agents. In this study, we demonstrated that the two agents exerted significant synergy in antitumor activity in various types of cancer cells with combination indices ranging from 0.46 to 0.98 (a value of less than unity indicates synergism). We have further shown that synergistic-targeted co-delivery of the two agents can be achieved via formulating curcumin in polyethylene glycol (PEG)-derivatized FTS-based nanomicellar system. Curcumin formulated in PEG-FTS micelles had small size of around 20 nm. The nanomicellar curcumin demonstrated enhanced cytotoxicity towards several cancer cell lines in vitro. Intravenous application of curcumin-loaded micelle (20 mg kg -1 curcumin) led to a significantly more effective inhibition of tumor growth in a syngeneic mouse breast cancer model (4T1.2) than curcumin formulated in Cremophor/EL (P<0.05).",

keywords = "S-trans, trans-farnesylthiosalicylic acid, curcumin, dual-functional carrier, micelles, synergy",

author = "Yichao Chen and Xiaolan Zhang and Jianqin Lu and Yixian Huang and Jiang Li and Song Li",

note = "Funding Information: This work was supported in part by NIH grants R21CA173887, RO1CA174305, and R01GM102989. We would like to thank Dr. Raman Venkataramanan and Mr. Wenchen Zhao for their help in the HPLC analysis of curcumin.",

year = "2014",

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doi = "10.1208/s12248-014-9595-6",

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T1 - Targeted delivery of curcumin to tumors via PEG-derivatized FTS-based micellar system

AU - Chen, Yichao

AU - Zhang, Xiaolan

AU - Lu, Jianqin

AU - Huang, Yixian

AU - Li, Jiang

AU - Li, Song

N1 - Funding Information: This work was supported in part by NIH grants R21CA173887, RO1CA174305, and R01GM102989. We would like to thank Dr. Raman Venkataramanan and Mr. Wenchen Zhao for their help in the HPLC analysis of curcumin.

PY - 2014/5

Y1 - 2014/5

N2 - Curcumin and S-trans, trans-farnesylthiosalicylic acid (FTS) are two promising anticancer agents. In this study, we demonstrated that the two agents exerted significant synergy in antitumor activity in various types of cancer cells with combination indices ranging from 0.46 to 0.98 (a value of less than unity indicates synergism). We have further shown that synergistic-targeted co-delivery of the two agents can be achieved via formulating curcumin in polyethylene glycol (PEG)-derivatized FTS-based nanomicellar system. Curcumin formulated in PEG-FTS micelles had small size of around 20 nm. The nanomicellar curcumin demonstrated enhanced cytotoxicity towards several cancer cell lines in vitro. Intravenous application of curcumin-loaded micelle (20 mg kg -1 curcumin) led to a significantly more effective inhibition of tumor growth in a syngeneic mouse breast cancer model (4T1.2) than curcumin formulated in Cremophor/EL (P<0.05).

AB - Curcumin and S-trans, trans-farnesylthiosalicylic acid (FTS) are two promising anticancer agents. In this study, we demonstrated that the two agents exerted significant synergy in antitumor activity in various types of cancer cells with combination indices ranging from 0.46 to 0.98 (a value of less than unity indicates synergism). We have further shown that synergistic-targeted co-delivery of the two agents can be achieved via formulating curcumin in polyethylene glycol (PEG)-derivatized FTS-based nanomicellar system. Curcumin formulated in PEG-FTS micelles had small size of around 20 nm. The nanomicellar curcumin demonstrated enhanced cytotoxicity towards several cancer cell lines in vitro. Intravenous application of curcumin-loaded micelle (20 mg kg -1 curcumin) led to a significantly more effective inhibition of tumor growth in a syngeneic mouse breast cancer model (4T1.2) than curcumin formulated in Cremophor/EL (P<0.05).

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Targeted delivery of curcumin to tumors via PEG-derivatized FTS-based micellar system

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