Targeted Delivery of Anticancer Agents via a Dual Function Nanocarrier with an Interfacial Drug-Interactive Motif | Zendy

Xiaolan Zhang | Zendy; Yixian Huang | Zendy; Wenchen Zhao | Zendy; Hao Liu | Zendy; Rebecca T. Marquez | Zendy; Jianqin Lu | Zendy; Peng Zhang | Zendy; Yifei Zhang | Zendy; Jiang Li | Zendy; Xiang Gao | Zendy; Raman Venkataramanan | Zendy; Liang Xu | Zendy; Song Li | Zendy

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Targeted Delivery of Anticancer Agents via a Dual Function Nanocarrier with an Interfacial Drug-Interactive Motif

Author(s) -

Xiaolan Zhang,

Yixian Huang,

Wenchen Zhao,

Hao Liu,

Rebecca T. Marquez,

Jianqin Lu,

Peng Zhang,

Yifei Zhang,

Jiang Li,

Xiang Gao,

Raman Venkataramanan,

Liang Xu,

Song Li

Publication year - 2014

Publication title -

biomacromolecules

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.689

H-Index - 220

eISSN - 1526-4602

pISSN - 1525-7797

DOI - 10.1021/bm501339j

Subject(s) - nanocarriers , paclitaxel , biodistribution , chemistry , pharmacology , doxorubicin , drug , drug delivery , pharmacokinetics , drug carrier , polyethylene glycol , targeted drug delivery , medicine , cancer , in vitro , biochemistry , chemotherapy , organic chemistry

We have developed a dual-function drug carrier, polyethylene glycol (PEG)-derivatized farnesylthiosalicylate (FTS). Here we report that incorporation of a drug-interactive motif (Fmoc) into PEG5k-FTS2 led to further improvement in both drug loading capacity and formulation stability. Doxorubicin (DOX) formulated in PEG5k-Fmoc-FTS2 showed sustained release kinetics slower than those of DOX loaded in PEG5k-FTS2. The maximum tolerated dose of DOX- or paclitaxel (PTX)-loaded PEG5k-Fmoc-FTS2 was significantly higher than that of the free drug. Pharmacokinetics and biodistribution studies showed that DOX/PEG5k-Fmoc-FTS2 mixed micelles were able to retain DOX in the bloodstream for a significant amount of time and efficiently deliver the drug to tumor sites. More importantly, drug (DOX or PTX)-loaded PEG5k-Fmoc-FTS2 led to superior antitumor activity over other treatments including drugs formulated in PEG5k-FTS2 in breast cancer and prostate cancer models. Our improved dual function carrier with a built-in drug-interactive motif represents a simple and effective system for targeted delivery of anticancer agents.

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