title: Influence of drug physicochemical characteristics on in vitro transdermal absorption of hydrophobic drug nanosuspensions.
abstract: The purpose of this paper was to study the influence of drug physicochemical characteristics on in vitro transdermal absorption of hydrophobic drug nanosuspensions. Four drug nanosuspensions were produced by high-pressure homogenization technique, which were the same in stabilizer and similar in particle size. Differential scanning calorimetry and powder X-ray diffraction analysis showed that the crystalline state of the nanocrystals did not change. In vitro permeation study demonstrated that the drug nanosuspensions have a higher rate of permeation that ranged from 1.69- to 3.74-fold compared to drug microsuspensions. Correlation analysis between drug physicochemical properties and Jss revealed that log P and pKa were factors that influenced the in vitro transdermal absorption of hydrophobic drug nanosuspensions, and drugs with a log P value around 3 and a higher pKa value (when pKa < pH+2) would gain higher Jss in this paper.
authors.affiliation: a Department of Pharmacy and.
authors.forename: Cheng-Ying
authors.initials: CY
authors.lastname: Shen
authors.affiliation: b Animal Laboratory Center , 302 Military Hospital , Beijing , China , and.
authors.forename: Rui-Sheng
authors.initials: RS
authors.lastname: Li
authors.affiliation: a Department of Pharmacy and.
authors.forename: Bao-de
authors.initials: BD
authors.lastname: Shen
authors.affiliation: a Department of Pharmacy and.
authors.forename: Gang
authors.initials: G
authors.lastname: Shen
authors.affiliation: c School of Biomedical Sciences, Huaqiao University , Quanzhou , Fujian , China.
authors.forename: Li-Qiang
authors.initials: LQ
authors.lastname: Wang
authors.affiliation: a Department of Pharmacy and.
authors.forename: Juan
authors.initials: J
authors.lastname: Zheng
authors.affiliation: a Department of Pharmacy and.
authors.forename: Xiao-Rong
authors.initials: XR
authors.lastname: Li
authors.affiliation: a Department of Pharmacy and.
authors.forename: Hong-Yan
authors.initials: HY
authors.lastname: Min
authors.affiliation: a Department of Pharmacy and.
authors.forename: Jin
authors.initials: J
authors.lastname: Han
authors.affiliation: a Department of Pharmacy and.
authors.forename: Hai-Long
authors.initials: HL
authors.lastname: Yuan
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D055598:Chemical Phenomena / Q000187:drug effects; D057927:Hydrophobic and Hydrophilic Interactions / Q000187:drug effects; D008297:Male; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism*; D009924:Organ Culture Techniques; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption / Q000187:drug effects / Q000502:physiology*; D014961:X-Ray Diffraction
keywords: Correlation analysis; drug physicochemical characteristics; nanosuspension; permeation rate; transdermal absorption