In this study， a synthetic high-density lipoprotein (sHDL)， peptide-based nanocarrier loaded with docetaxel (DTX) was constructed， against breast cancer. The thermodynamic and molecular dynamic analyses were conducted to examine the stability of nanoparticles synthesized from mimetic peptide 5?A and various types of phospholipids. Furthermore， the cellular uptake and fluorescence imaging analysis experiments， with scavenger receptor B-I (SR-BI) were carried out to examine the tumor-targeting ability of sHDL. The nanoparticles were investigated for their pharmacodynamic and cytotoxic effects to show their effectivity as anti-tumor agents. The results showed that the synthesized sHDL nanoparticles exhi... More
In this study， a synthetic high-density lipoprotein (sHDL)， peptide-based nanocarrier loaded with docetaxel (DTX) was constructed， against breast cancer. The thermodynamic and molecular dynamic analyses were conducted to examine the stability of nanoparticles synthesized from mimetic peptide 5?A and various types of phospholipids. Furthermore， the cellular uptake and fluorescence imaging analysis experiments， with scavenger receptor B-I (SR-BI) were carried out to examine the tumor-targeting ability of sHDL. The nanoparticles were investigated for their pharmacodynamic and cytotoxic effects to show their effectivity as anti-tumor agents. The results showed that the synthesized sHDL nanoparticles exhibited a high payload of DTX， sustained drug release properties， and excellent biocompatibility. Moreover， DTX-sHDL nanoparticles enhanced the uptake of DTX， increased the cytotoxicity against MCF-7 cells， and reduced the off-target side-effects to normal cells. Finally， experiments in 4T1 cell line-bearing mice indicate that inhibition of tumor growth by DTX-sHDL nanoparticles was superior to that of free DTX group. Thus， the sHDL nanoparticles are a promising drug delivery vehicle for improving the efficacy of anti-cancer drugs.
