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Title: Improving breast cancer therapy using doxorubicin loaded solid lipid nanoparticles: Synthesis of a novel arginine-glycine-aspartic tripeptide conjugated, pH sensitive lipid and evaluation of the nanomedicine in vitro and in vivo. Author: Zheng G, Zheng M, Yang B, Fu H, Li Y. Journal: Biomed Pharmacother; 2019 Aug; 116():109006. PubMed ID: 31152925. Abstract: Breast cancer is the leading cause of cancer mortality in women worldwide. To overcome the toxic side effects and multidrug resistance (MDR) during doxorubicin (DOX) chemotherapy, an arginine-glycine-aspartic (RGD) tripeptide modified, pH-sensitive solid lipid nanoparticles (SLNs) is employed in this study. In this study, a RGD conjugated, pH sensitive lipid was synthesized using glycerin monostearate (GMS) and adipic acid dihydrazide (HZ) as lipid materials and named RGD-HZ-GMS. RGD-HZ-GMS was applied to encapsulate DOX to construct a RGD modified, DOX loaded SLNs (RGD-DOX-SLNs). To evaluate the anticancer effect of RGD-DOX-SLNs, breast cancer cell line (MCF-7 cells) and DOX resistant cell line (MCF-7/ADR cells) were used. in vivo tumor suspension and toxicity effects were evaluated on mice bearing MCF-7/ADR cells breast cancer model. RGD-DOX-SLNs had a uniformly spherical shape. The mean particle size and zeta potential of the RGD-DOX-SLNs was 96.3 nm and 35.6 mV, respectively. RGD-DOX-SLNs showed 5.58 fold higher area under the plasma concentration - time curve (AUC) compared with DOX solution. Terminal half life (T1/2) and peak concentration (Cmax) of RGD-DOX-SLNs was 10.85 h and 39.12 ± 2.71 L/kg/h. in vitro and in vivo antitumor results indicate that RGD-DOX-SLNs might be a promising novel lipid carrier which could improve breast cancer therapy.[Abstract] [Full Text] [Related] [New Search]