Abstract
Epigallocatechin-3-gallate (EGCG) is the most studied catechin in green tea (Camellia sinensis). EGCG and green tea are cancer preventive in many animal models, and numerous mechanisms have been proposed in cell lines. EGCG is poorly bioavailable in man and rodents. We hypothesized that transdermal delivery of EGCG could result in improved bioavailability. Following application of EGCG transdermal gel (50 mg kg-1, t.d.) to SKH-1 mice, EGCG was observed in the epidermis (1365.7-121.0 ng g-1) and dermis (411.2-42.6 ng g-1). The maximum plasma concentration (Cmax) of EGCG was 44.5 ng mL-1. The t1/2 (94.4 h) and AUC0→24h (881.5 ng mL-1 h) of EGCG were greater than values previously reported for oral EGCG. The t1/2 and area under the concentration-time curve up to 24h (AUC0→24h) in the liver, small intestine and colon were 21.3-74.6 h and 715-2802 ng g-1 h, respectively. Stability studies showed that the transdermal formulation was stable at 4°C and had a half-life (t1/2) of 47.1 and 20.2 h at 25°C and 37°C, respectively. These data indicate that transdermal EGCG is useful for delivering prolonged levels of EGCG to plasma and tissues, and may provide an alternative to tea consumption as a dosage form of EGCG.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 599-604 |
| Number of pages | 6 |
| Journal | Journal of Pharmacy and Pharmacology |
| Volume | 58 |
| Issue number | 5 |
| DOIs | |
| State | Published - May 1 2006 |
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All Science Journal Classification (ASJC) codes
- Pharmacology
- Pharmaceutical Science
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Transdermal delivery of (-)-epigallocatechin-3-gallate, a green tea polyphenol, in mice. / Lambert, Joshua D.; Kim, Dou Hwan; Zheng, Ruijin; Yang, Chung S.
In: Journal of Pharmacy and Pharmacology, Vol. 58, No. 5, 01.05.2006, p. 599-604.Research output: Contribution to journal › Article
TY - JOUR
T1 - Transdermal delivery of (-)-epigallocatechin-3-gallate, a green tea polyphenol, in mice
AU - Lambert, Joshua D.
AU - Kim, Dou Hwan
AU - Zheng, Ruijin
AU - Yang, Chung S.
PY - 2006/5/1
Y1 - 2006/5/1
N2 - Epigallocatechin-3-gallate (EGCG) is the most studied catechin in green tea (Camellia sinensis). EGCG and green tea are cancer preventive in many animal models, and numerous mechanisms have been proposed in cell lines. EGCG is poorly bioavailable in man and rodents. We hypothesized that transdermal delivery of EGCG could result in improved bioavailability. Following application of EGCG transdermal gel (50 mg kg-1, t.d.) to SKH-1 mice, EGCG was observed in the epidermis (1365.7-121.0 ng g-1) and dermis (411.2-42.6 ng g-1). The maximum plasma concentration (Cmax) of EGCG was 44.5 ng mL-1. The t1/2 (94.4 h) and AUC0→24h (881.5 ng mL-1 h) of EGCG were greater than values previously reported for oral EGCG. The t1/2 and area under the concentration-time curve up to 24h (AUC0→24h) in the liver, small intestine and colon were 21.3-74.6 h and 715-2802 ng g-1 h, respectively. Stability studies showed that the transdermal formulation was stable at 4°C and had a half-life (t1/2) of 47.1 and 20.2 h at 25°C and 37°C, respectively. These data indicate that transdermal EGCG is useful for delivering prolonged levels of EGCG to plasma and tissues, and may provide an alternative to tea consumption as a dosage form of EGCG.
AB - Epigallocatechin-3-gallate (EGCG) is the most studied catechin in green tea (Camellia sinensis). EGCG and green tea are cancer preventive in many animal models, and numerous mechanisms have been proposed in cell lines. EGCG is poorly bioavailable in man and rodents. We hypothesized that transdermal delivery of EGCG could result in improved bioavailability. Following application of EGCG transdermal gel (50 mg kg-1, t.d.) to SKH-1 mice, EGCG was observed in the epidermis (1365.7-121.0 ng g-1) and dermis (411.2-42.6 ng g-1). The maximum plasma concentration (Cmax) of EGCG was 44.5 ng mL-1. The t1/2 (94.4 h) and AUC0→24h (881.5 ng mL-1 h) of EGCG were greater than values previously reported for oral EGCG. The t1/2 and area under the concentration-time curve up to 24h (AUC0→24h) in the liver, small intestine and colon were 21.3-74.6 h and 715-2802 ng g-1 h, respectively. Stability studies showed that the transdermal formulation was stable at 4°C and had a half-life (t1/2) of 47.1 and 20.2 h at 25°C and 37°C, respectively. These data indicate that transdermal EGCG is useful for delivering prolonged levels of EGCG to plasma and tissues, and may provide an alternative to tea consumption as a dosage form of EGCG.
UR - http://www.scopus.com/inward/record.url?scp=33646445159&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33646445159&partnerID=8YFLogxK
U2 - 10.1211/jpp.58.5.0004
DO - 10.1211/jpp.58.5.0004
M3 - Article
C2 - 16640828
AN - SCOPUS:33646445159
VL - 58
SP - 599
EP - 604
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
SN - 0022-3573
IS - 5
ER -