Carrier-Free Nanoparticles via Coassembly of Paclitaxel and Gambogic Acid with Folate-Functionalized Albumin for Targeted Tumor Treatment

Abstract

Various traditional drug delivery systems usually have complex compositions and exhibit relatively low drug loading (<10 wt %) due to a lack of affinity with drugs, leading to the potential adverse effects of overdosed carrier materials and manufacturing costs. Herein, carrier-free nanoparticles with ultrahigh drug loading, reduced drug toxicity, and targeting delivery ability are developed by the adsorption of folate-functionalized albumin (FA-HSA) and drugs. Hydrophobic drugs paclitaxel (PTX) and gambogic acid (GA) form carrier-free PTX/GA via coassembly, followed by the adsorption of FA-HSA on the surface of PTX/GA to fabricate PTX/GA@FA-HSA with high drug loading capacity and the targeting ability via the FA-folate receptor (FR)-mediated recognition pathway. PTX/GA@FA-HSA exhibits a spherical core–shell nanostructure and a diameter of 130.0 ± 1.4 nm. Compared to the traditional drug delivery systems, PTX/GA@FA-HSA exhibits high drug loading (∼81.5%) due to two drugs acting as both the carriers and the cargos. Experimental results demonstrate that both PTX and GA in PTX/GA@FA-HSA can be delivered and internalized into MDA-MB-231 cells via the FA-FR-mediated recognition pathway. Meanwhile, PTX/GA@FA-HSA exhibited enhanced tumor targeting ability and negligible side effects in MDA-MB-231 tumor-bearing nude mice, which provides an insight for designing advanced carrier-free nanocarriers with targeting ability.