4.7 Article

Improved Tumor Targeting of Polymer-Based Nanovesicles Using Polymer-Lipid Blends

Journal

BIOCONJUGATE CHEMISTRY
Volume 22, Issue 10, Pages 2021-2029

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/bc200214g

Keywords

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Funding

  1. National Institute of Health (NCI) [R21 CA125088, R21 EB013226]
  2. American Cancer Society [RSG-07-005-01]
  3. NSF
  4. DOD of the Office of the Congressionally Directed Medical Research [W81XWH-07-1-0457]

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Block copolymer-based vesicles have recently garnered a great deal of interest as nanoplatforms for drug delivery. and molecular imaging applications to their unique structural properties. These nanovesicles have been shown to direct their cargo to disease sites either through enhanced permeability and retention or even more efficiently via active targeting. Here, we show that the efficacy of nanovesicle targeting can be significantly improved when prepared from polymer-lipid blends compared with block copolymer alone. Polymer-lipid hybrid nanovesicles were produced from the aqueous coassembly of the cliblock copolymer, poly(ethylene oxide)-block-poly-butadiene (PEO-PBD), and the phospholipid, hydrogenated soy phosphatidylcholine(HSPC). The PEG-based vesicles, 117 nm in diameter, were functionalized with either folic acid or anti-HER2/neu affibodies as targeting ligands to confer specificity for cancer cells. Our results revealed that nanovesicles prepared from polymer-lipd blends led to significant improvement in cell binding compared to nanovesicles prepared from block copolymer alone in both in vitro cell studies and murine tumor models'. Therefore, it is envisioned that nanovesicles composed of polymer-lipid blends may constitute a preferred embodiment for targeted drug delivery and molecular imaging applications.

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