The Role of Payload Hydrophobicity in Nanotherapeutic Pharmacokinetics.

Although drug delivery with nanovectors is regarded as one of the paradigm-shifting advances in modern medicine, the compatibility and performance of drug-vector formulations have not been systematically studied in terms of their physicochemistry and pharmacokinetics ( PKs). The drug delivery systems ( DDSs), currently available in clinics or trials, were analyzed based on hydrophobicity and anatomical therapeutic chemical ( ATC) classification of drug payloads. Four major types of DDSs differentiated based on DDS structure and drug hydrophobicity, where payload hydrophobicity decreased: micelles, serum albumin, liposome membrane, and liposome interior. A strong relationship between the increase in half-life in DDS formulation and drug hydrophobicity was found with up to 200-fold greater increase for hydrophilic drugs. The analysis results seemingly integrated PKs, ATC, and hydrophobicity to reinforce the development or optimization of drug delivery vectors and their formulations. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:2147-2156, 2014 [ABSTRACT FROM AUTHOR]