Enhanced Melanoma‐Targeted Therapy by “Fru‐Blocked” Phenyboronic Acid‐Modified Multiphase Antimetastatic Micellar Nanoparticles

• DOI: 10.1002/advs.201800229
• Publication Date: 2018-07-13T11:24:12Z
• Authors: Yang Long; Zhengze Lu; Ling Mei; Man Li; Kebai Ren; Xuhui Wang; Jiajing Tang; Zhirong Zhang; Qin He
• Keywords: Nanocarriers

Abstract Metastasis remains the main driver of mortality in patients suffering from cancer because refractoriness resulting multi‐phase metastatic cascade. Herein, a multifunctional self‐delivering PBA‐LMWH‐TOS nanoparticle (PLT NP) is established that acts as both nanocarrier and anti‐metastatic agent with effects on most hematogenous metastases cancers. The hydrophilic segment (low molecular weight heparin, LMWH) inhibits interactions between tumor cells platelets. hydrophobic ( d ‐α‐tocopheryl succinate, TOS) could inhibit expression matrix metalloproteinase‐9 (MMP‐9) B16F10 which first reported this article. Surprisingly, even blank NPs showed excellent capacity three mouse models by acting different phases Moreover, overexpression sialic acid (SA) residues implicated malignant phenotypes Thus, these 3‐aminophenylboronic (PBA)‐modified doxorubicin (DOX)‐loaded offer an efficient approach for treatment solid melanomas metastases. Furthermore, simple pH‐sensitive “Fructose (Fru)‐blocking” coping strategy to reduce NP distribution normal tissues distinctly increases accumulation melanoma tumors. These micellar consisting biocompatible materials promising clinical therapy highly invasive tumors