title: The role of payload hydrophobicity in nanotherapeutic pharmacokinetics.
abstract: 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.
authors.affiliation: Houston Methodist Research Institute, Department of Nanomedicine, Houston, Texas, 77030.
authors.forename: Povilas
authors.initials: P
authors.lastname: Norvaisas
authors.affiliation: Houston Methodist Research Institute, Department of Nanomedicine, Houston, Texas, 77030. Electronic address: aziemys@hostonmethodist.com.
authors.forename: Arturas
authors.initials: A
authors.lastname: Ziemys
mesh_terms: D055598:Chemical Phenomena; D003627:Data Interpretation, Statistical; D062313:Databases, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D057927:Hydrophobic and Hydrophilic Interactions; D008081:Liposomes; D008823:Micelles; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism; D010599:Pharmacokinetics; D011485:Protein Binding; D012709:Serum Albumin / Q000737:chemistry / Q000378:metabolism
chemical_list: D004337:Drug Carriers; D008081:Liposomes; D008823:Micelles; D004364:Pharmaceutical Preparations; D012709:Serum Albumin
keywords: albumin; formulation; formulation vehicles; lipoproteins; liposomes; log P; micelles; nanoparticles; pharmacokinetics; physicochemical