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In vitro transdermal delivery of the major catechins and caffeine from extract of Camellia sinensis.

Abstract

The aim of this study was to investigate the feasibility of the transdermal delivery of catechins and caffeine from green tea extract. Drug-in-adhesive patches containing 1.35, 1.03, 0.68, and 0.32 mg cm(-2) green tea extract were formulated and the dissolution of (-)-epigallocatechin gallate (EGCg), (-)-epigallocatechin (EGC) and (-)-epicatechin (EC) from these was determined. Transdermal delivery was determined across full thickness pig ear skin from saturated solutions of green tea extract in pH 5.5 citrate-phosphate buffer, polyethylene glycol 400 and a 50:50 mixture of the citrate phosphate buffer and polyethylene glycol in addition to patches containing 1.35 mg cm(-2) green tea extract. Dissolution experiments indicated first order release which was dose dependent in respect of the loading level, although the amounts permeated were not always proportional to the amounts in the formulation. The highest percentage permeation of EGCg was found to be from the patch formulation. EGCg, EGC and EC were all successfully delivered transdermally from saturated solutions and adhesive patches containing green tea extract in this study. There was some evidence for the dermal metabolism of EGCg, but after 24 h 0.1% permeated from the patches containing 1.35 mg cm(-2) green tea extract. This was equivalent to the percentage absorbed after intragastric administration of green tea extract in rats. In addition, the concentration of EGCg in the Franz cell receptor chamber after 24 h permeation from the 0.9 cm diameter patch containing 1.35 mg cm(-2) was within the range of Cmax plasma levels achieved after oral dosing of 2.2-4.2 gm(-2) green tea extract. Caffeine was also delivered at concentrations above those previously reported.

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  • Authors+Show Affiliations

    ,

    Welsh School of Pharmacy, Cardiff University, Cardiff CF10 3XF, UK.

    , ,

    Source

    International journal of pharmaceutics 283:1-2 2004 Sep 28 pg 45-51

    MeSH

    Administration, Cutaneous
    Animals
    Caffeine
    Camellia sinensis
    Catechin
    Chemistry, Pharmaceutical
    Plant Extracts
    Rats
    Swine
    Tea

    Pub Type(s)

    Journal Article
    Research Support, Non-U.S. Gov't

    Language

    eng

    PubMed ID

    15363500

    Citation

    Batchelder, Rachel J., et al. "In Vitro Transdermal Delivery of the Major Catechins and Caffeine From Extract of Camellia Sinensis." International Journal of Pharmaceutics, vol. 283, no. 1-2, 2004, pp. 45-51.
    Batchelder RJ, Calder RJ, Thomas CP, et al. In vitro transdermal delivery of the major catechins and caffeine from extract of Camellia sinensis. Int J Pharm. 2004;283(1-2):45-51.
    Batchelder, R. J., Calder, R. J., Thomas, C. P., & Heard, C. M. (2004). In vitro transdermal delivery of the major catechins and caffeine from extract of Camellia sinensis. International Journal of Pharmaceutics, 283(1-2), pp. 45-51.
    Batchelder RJ, et al. In Vitro Transdermal Delivery of the Major Catechins and Caffeine From Extract of Camellia Sinensis. Int J Pharm. 2004 Sep 28;283(1-2):45-51. PubMed PMID: 15363500.
    * Article titles in AMA citation format should be in sentence-case
    TY - JOUR T1 - In vitro transdermal delivery of the major catechins and caffeine from extract of Camellia sinensis. AU - Batchelder,Rachel J, AU - Calder,Richard J, AU - Thomas,Chris P, AU - Heard,Charles M, PY - 2004/01/22/received PY - 2004/06/06/revised PY - 2004/06/07/accepted PY - 2004/9/15/pubmed PY - 2005/1/26/medline PY - 2004/9/15/entrez SP - 45 EP - 51 JF - International journal of pharmaceutics JO - Int J Pharm VL - 283 IS - 1-2 N2 - The aim of this study was to investigate the feasibility of the transdermal delivery of catechins and caffeine from green tea extract. Drug-in-adhesive patches containing 1.35, 1.03, 0.68, and 0.32 mg cm(-2) green tea extract were formulated and the dissolution of (-)-epigallocatechin gallate (EGCg), (-)-epigallocatechin (EGC) and (-)-epicatechin (EC) from these was determined. Transdermal delivery was determined across full thickness pig ear skin from saturated solutions of green tea extract in pH 5.5 citrate-phosphate buffer, polyethylene glycol 400 and a 50:50 mixture of the citrate phosphate buffer and polyethylene glycol in addition to patches containing 1.35 mg cm(-2) green tea extract. Dissolution experiments indicated first order release which was dose dependent in respect of the loading level, although the amounts permeated were not always proportional to the amounts in the formulation. The highest percentage permeation of EGCg was found to be from the patch formulation. EGCg, EGC and EC were all successfully delivered transdermally from saturated solutions and adhesive patches containing green tea extract in this study. There was some evidence for the dermal metabolism of EGCg, but after 24 h 0.1% permeated from the patches containing 1.35 mg cm(-2) green tea extract. This was equivalent to the percentage absorbed after intragastric administration of green tea extract in rats. In addition, the concentration of EGCg in the Franz cell receptor chamber after 24 h permeation from the 0.9 cm diameter patch containing 1.35 mg cm(-2) was within the range of Cmax plasma levels achieved after oral dosing of 2.2-4.2 gm(-2) green tea extract. Caffeine was also delivered at concentrations above those previously reported. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/15363500/In_vitro_transdermal_delivery_of_the_major_catechins_and_caffeine_from_extract_of_Camellia_sinensis_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378517304003436 DB - PRIME DP - Unbound Medicine ER -