Publication

A study of the percutaneous absorption-enhancing effects of cyclodextrin derivatives in rats

VOLLMER, U., MULLER, BW., PEETERS, J., MESENS, J., WILFFERT, B. & Peters, T., Jan-1994, In : Journal of Pharmacy and Pharmacology. 46, 1, p. 19-22 4 p.

Research output: Contribution to journalArticleAcademicpeer-review

  • U VOLLMER
  • BW MULLER
  • J PEETERS
  • J MESENS
  • B WILFFERT
  • Thies Peters

2-Hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) and 2,6-dimethyl-beta-cyclodextrin (D-beta-CyD) were studied for transdermal penetration enhancement of the cytochrome P450 inhibitor liarozole by an in-vivo transdermal absorption rat model. The mode of action of penetration enhancement was investigated by differential scanning calorimetry (DSC). In-vivo, HP-beta-CyD, as a 20% aqueous solution, increased the absorption of liarozole approximately threefold and a 20% aqueous solution of D-beta-CyD decreased the percutaneous absorption of liarozole in blood by a factor of 0.6. However, pretreatment with D-beta-CyD (20%, 4 h) enhanced the transdermal absorption 9.4-fold. In the DSC experiments the thermal profile of human stratum corneum was practically unchanged after treatment with HP-beta-CyD, but treatment with D-beta-CyD revealed an interaction of D-beta-CyD with the protein and lipid fraction. Thus the results from DSC and those from the permeability experiments revealed that D-beta-CyD acts as a transdermal absorption enhancer by changing the stratum corneum barrier whereas HP-beta-CyD influences the partitioning behaviour of the drug in the skin.

Original languageEnglish
Pages (from-to)19-22
Number of pages4
JournalJournal of Pharmacy and Pharmacology
Volume46
Issue number1
Publication statusPublished - Jan-1994

    Keywords

  • STRATUM-CORNEUM, TRANSPORT, MECHANISM

ID: 13858400