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Influence of Bile Acids on Clindamycin Hydrochloride Skin Permeability: In Vitro and In Silico Preliminary Study
Dragana Zaklan1, Dušan Nešić2, Darko Mitrović2
1Department of Pharmacy, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, 21000, Novi Sad, Serbia. dragana.zaklan@mf.uns.ac.rs.
European Journal of Drug Metabolism and Pharmacokinetics
|February 9, 2024
Summary
Bile acids, cholic acid (CA) and deoxycholic acid (DCA), enhance topical clindamycin hydrochloride skin penetration. This study demonstrates bile acids as promising excipients for improved topical drug delivery and efficacy.
Area of Science:
- Pharmaceutical Sciences
- Dermatology
- Drug Delivery
Background:
- Topical clindamycin formulations suffer from poor bioavailability and limited skin penetration, hindering therapeutic efficacy.
- Penetration enhancement is a key strategy to improve topical drug delivery.
- Bile acids, cholic acid (CA) and deoxycholic acid (DCA), are investigated for their potential as penetration enhancers.
Purpose of the Study:
- To assess the influence of CA and DCA on clindamycin hydrochloride skin permeability.
- To evaluate the interaction of clindamycin and bile acids with skin ATP-binding cassette (ABC) transporters in silico.
Main Methods:
- In vitro skin parallel artificial membrane permeability assay (skin-PAMPA) at pH 5.5 and 6.5.
- Spectrophotometric determination of clindamycin hydrochloride concentrations.
- In silico prediction of drug-transporter interactions using Vienna LiverTox.
Main Results:
- Both CA and DCA increased clindamycin hydrochloride permeability across the skin-PAMPA membrane.
- The enhancing effect was more pronounced with CA and at pH 6.5.
- Bile acids may facilitate clindamycin transport via skin ABC transporters.
Conclusions:
- Bile acids show potential as penetration-enhancing excipients for topical clindamycin formulations.
- Further research can leverage bile acids to improve topical drug delivery and therapeutic outcomes.
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