Nanoparticulate
drug carriers exploit the enhanced permeability of
tumor vasculature to achieve selective delivery of chemotherapeutic drugs. For this purpose, nanoparticles (NPs) need to circulate with a long half-life, enter
tumors via the permeable vasculature and stay in
tumors via favorable interactions with
tumor cells. To fulfill these requirements,
albumin-coated nanocrystal formulation of
paclitaxel (PTX), Cim-
F-alb, featuring high
drug loading content, physical stability in serum, and surface-bound
albumin in its native conformation is prepared. The pharmacokinetic and biodistribution (PK/BD) profiles of Cim-
F-alb in a mouse model of B16F10
melanoma show that Cim-
F-alb exhibits a longer plasma half-life and a greater PTX deposition in
tumors than
Abraxane by ≈1.5 and ≈4.6 fold, respectively. Biolayer interferometry analysis indicates that Cim-
F-alb has less interaction with
serum proteins than nanocrystals lacking
albumin coating, indicating the protective effect of the surface-bound
albumin against opsonization in the initial deposition phase. With the advantageous PK/BD profiles, Cim-
F-alb shows greater and longer-lasting anticancer efficacy than
Abraxane at the equivalent dose. This study demonstrates the significance of controlling circulation stability and surface property of NPs in efficient
drug delivery to
tumors and enhanced anticancer efficacy.