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. 2005 Sep 2;7(1):E218–E223. doi: 10.1208/aapsj070120

Release and permeation kinetics of caffeine from bioadhesive transdermal films

Sara Nicoli 1, Paolo Colombo 1, Patrizia Santi 1,
PMCID: PMC2751510  PMID: 16146342

Abstract

The aim of this work was to investigate, in vitro, the kinetics of release and permeation of caffeine, chosen as model drug, from bioadhesive transdermal films. These films are not self-adhesive but become adhesive when applied to wet skin. Permeation experiments were performed from films with different drug loadings using rabbit ear skin as barrier. In order to characterize the release kinetics of caffeine from the film, a polyethylene membrane, impregnated with isopropyl myristate was employed. The data obtained in the present work suggest that caffeine release from transdermal bioadhesive films was controlled either by the permeability characteristics of the skin or by the film itself, depending on drug loading. When drug loading is low (ie, caffeine is dissolved in the polymers constituting the film), the control resides in the skin. When caffeine loading exceeds its solubility in the film, the permeation profile is not linear, but shows a sort of burst effect in the early times of permeation, probably owing to the presence of solid drug and/or to a certain degree of “conserved supersaturation” in the solid phase.

Keywords: transdermal, caffeine, permeation kinetics, controlled release, skin

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References

  • 1.Zhai H, Maibach HI. Occlusion vs skin barrier function. Skin Res Technol. 2002;8:1–6. doi: 10.1046/j.0909-752x.2001.10311.x. [DOI] [PubMed] [Google Scholar]
  • 2.Colombo P, Catellani PL, Padula C, Santi P, Colombo G. Film for Dermal and Transdermal Administration of Drugs. WO 02/30402. April 18, 2002.
  • 3.Padula C, Colombo G, Nicoli S, Catellani PL, Massimo G, Santi P. Bioadhesive film for the transdermal delivery of lidocaine: in vitro and in vivo behavior. J Control Release. 2003;88:277–285. doi: 10.1016/S0168-3659(03)00015-4. [DOI] [PubMed] [Google Scholar]
  • 4.Nicoli S, Amoretti V, Colombo P, Santi P. Bioadhesive transdermal film containing caffeine. Skin Pharmacol Appl Skin Physiol. 2004;17:119–123. doi: 10.1159/000077237. [DOI] [PubMed] [Google Scholar]
  • 5.Amato M, Isenschmid M, Huppi P. Percutaneous caffeine application in the treatment of neonatal apnea. Eur J Pediatr. 1991;150:592–594. doi: 10.1007/BF02072214. [DOI] [PubMed] [Google Scholar]
  • 6.Conney AH, Lu YP, Lou YR, Huang MT. Inhibitory effects of tea and caffeine on UV-induced carcinogenesis: relationship to enhanced apoptosis and decreased tissue fat. Eur J Cancer Prev. 2002;11:S28–S36. [PubMed] [Google Scholar]
  • 7.Bertin C, Zunino H, Pitter JC, et al. A double-blind evaluation of the activity of an anti-cellulite product containing retinol, caffeine, and ruscogenine by a combination of several non-invasive methods. J Cosmet Sci. 2001;52:199–210. [PubMed] [Google Scholar]
  • 8.Mandel HG. Update on caffeine consumption, disposition and action. Food Chem Toxicol. 2002;40:1231–1234. doi: 10.1016/S0278-6915(02)00093-5. [DOI] [PubMed] [Google Scholar]
  • 9.Anderson BJ, Gunn TR, Holford NH, Johnson R. Caffeine overdose in a premature infant: clinical course and pharmacokinetics. Anaesth Intensive Care. 1999;27:307–311. doi: 10.1177/0310057X9902700316. [DOI] [PubMed] [Google Scholar]
  • 10.Monti D, Giannelli R, Chetoni P, Burgalassi S. Comparison of the effect of ultrasound and of chemical enhancers on transdermal permeations of caffeine and morphine through hairless mouse skin in vitro. Int J Pharm. 2001;229:131–137. doi: 10.1016/S0378-5173(01)00830-4. [DOI] [PubMed] [Google Scholar]
  • 11.Dias M, Farinha A, Faustino E, Hadgraft J, Pais J, Toscano C. Topical delivery of caffeine from some commercial formulations. Int J Pharm. 1999;182:41–47. doi: 10.1016/S0378-5173(99)00067-8. [DOI] [PubMed] [Google Scholar]

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