Enhanced anticancer activity of nanopreparation containing an MMP2-sensitive PEG-drug conjugate and cell-penetrating moiety

• DOI: 10.1073/pnas.1304987110
• Publication Date: 2013-09-24T05:25:39Z
• Authors: Lin Zhu; Tao Wang; Federico Perche; Anton Taigind; Vladimir P. Torch...
• Keywords: Nanocarriers; Internalization; Cell-penetrating peptide; PEGylation; Conjugate

Significance The clinical outcomes of anticancer drugs are compromised by their poor physicochemical properties, low tumor targeting, insufficient bioavailability, and side effects. Matrix metalloproteinase 2 (MMP2) has been found overexpressed in most cancers responsible for cell proliferation metastasis. In this study, a self-assembling MMP2-sensitive paclitaxel-containing micellar nanopreparation was developed. Several major drug delivery strategies, including self-assembly, PEGylation, the enhanced permeability retention effect, stimulus sensitivity, cell-penetrating moiety, concept prodrug, were used collaborative fashion to design nanoparticle. showed superior internalization, antitumor efficacy over its nonsensitive counterpart, free paclitaxel conventional micelles. This uniquely engineered nanoparticle potential effective intracellular into cancer cells.