title: In vitro enhancement of lactate esters on the percutaneous penetration of drugs with different lipophilicity.
abstract: Lactate esters are widely used as food additives, perfume materials, medicine additives, and personal care products. The objective of this work was to investigate the effect of a series of lactate esters as penetration enhancers on the in vitro skin permeation of four drugs with different physicochemical properties, including ibuprofen, salicylic acid, dexamethasone and 5-fluorouracil. The saturated donor solutions of the evaluated drugs in propylene glycol were used in order to keep a constant driving force with maximum thermodynamic activity. The permeability coefficient (K(p)), skin concentration of drugs (SC), and lag time (T), as well as the enhancement ratios for K(p) and SC were recorded. All results indicated that lactate esters can exert a significant influence on the transdermal delivery of the model drugs and there is a structure-activity relationship between the tested lactate esters and their enhancement effects. The results also suggested that the lactate esters with the chain length of fatty alcohol moieties of 10-12 are more effective enhancers. Furthermore, the enhancement effect of lactate esters increases with a decrease of the drug lipophilicity, which suggests that they may be more efficient at enhancing the penetration of hydrophilic drugs than lipophilic drugs. The influence of the concentration of lactate esters was evaluated and the optimal concentration is in the range of 5-10 wt.%. In sum, lactate esters as a penetration enhancer for some drugs are of interest for transdermal administration when the safety of penetration enhancers is a prime consideration.
authors.affiliation: School of Materials Science and Engineering, Tianjin University, 300072, Tianjin, China.
authors.forename: Jianhua
authors.initials: J
authors.lastname: Zhang
authors.forename: Mei
authors.initials: M
authors.lastname: Liu
authors.forename: Hongjian
authors.initials: H
authors.lastname: Jin
authors.forename: Liandong
authors.initials: L
authors.lastname: Deng
authors.forename: Jinfeng
authors.initials: J
authors.lastname: Xing
authors.forename: Anjie
authors.initials: A
authors.lastname: Dong
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D004952:Esters; D007773:Lactates / Q000737:chemistry*; D008297:Male; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D051381:Rats; D012867:Skin / Q000737:chemistry*; D012869:Skin Absorption
chemical_list: D004337:Drug Carriers; D004952:Esters; D007773:Lactates; D004364:Pharmaceutical Preparations