AAPS PharmSciTech

, Volume 11, Issue 2, pp 894–903 | Cite as

In vitro Enhancement of Lactate Esters on the Percutaneous Penetration of Drugs with Different Lipophilicity

  • Jianhua Zhang
  • Mei Liu
  • Hongjian Jin
  • Liandong Deng
  • Jinfeng Xing
  • Anjie Dong
Research Article

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.

Key words

lactate esters penetration enhancer percutaneous permeation rat skin transdermal drug delivery system 

Notes

ACKNOWLEDGMENTS

This project was supported by the National Natural Science Foundation of China (Number 30672554).

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Copyright information

© American Association of Pharmaceutical Scientists 2010

Authors and Affiliations

  • Jianhua Zhang
    • 1
  • Mei Liu
    • 2
  • Hongjian Jin
    • 2
  • Liandong Deng
    • 2
  • Jinfeng Xing
    • 2
  • Anjie Dong
    • 1
    • 2
  1. 1.School of Materials Science and EngineeringTianjin UniversityTianjinChina
  2. 2.School of Chemical Engineering and TechnologyTianjin UniversityTianjinChina

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