Carrier-Free Nanoparticles\nvia Coassembly of Paclitaxel\nand Gambogic Acid with Folate-Functionalized Albumin for Targeted\nTumor Treatment

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