Percutaneous release of caffeine from microemulsion, emulsion and gel dosage forms

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 68; no. 2; pp. 446 - 451
• Main Authors: Bolzinger, M.-A., Briançon, S., Pelletier, J., Fessi, H., Chevalier, Y.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01-02-2008; Elsevier Science; Elsevier
• Subjects: Animals; Biological and medical sciences; Caffeine; Caffeine - chemistry; Caffeine - pharmacokinetics; Chemical Sciences; Dosage Forms; Emulsions; Female; Galenic pharmacology; General pharmacology; Hypodermis; Life Sciences; Male; Medical sciences; Microemulsion; or physical chemistry; Percutaneous penetration; Pharmaceutical sciences; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Skin - metabolism; Swine; Theoretical and; Topical delivery; Percutaneous penetration; Microemulsion; Topical delivery; Hypodermis; Caffeine; Pharmaceutical technology; CNS stimulant; Psychotropic; Percutaneous route; Respiratory analeptic; Colloidal gel; Local administration; Emulsion; Penetration; Dosage form; Xanthine derivatives; Release; Topical administration
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2007.10.018

The transport of caffeine to the hypodermis by an alcohol-free o/w microemulsion was investigated and compared with an aqueous gel and an o/w emulsion. The microemulsion was well characterized and
in vitro diffusion measurements through pig skin having the hypodermis either kept or removed were performed in static Franz cells. The microemulsion allowed delivery of a large fraction of the caffeine in the hypodermis: 23% of caffeine reached the hypodermis after 24
h diffusion, 1.3-fold larger than from the emulsion and gel dosage forms. Half this amount was stored in the hypodermis, the other half continuing its diffusion to the receptor compartment of the Franz cell.