Transdermal Absorption and Skin Metabolism of Viprostol, A Synthetic Prostaglandin E<sub>2</sub>Analogue

Nicolau, G.; Yacobi, Avraham

doi:10.3109/03602538909030304

Cited by 5 publications

(1 citation statement)

References 29 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Studies of drug metabolism in the skin are often conducted via the tissue homogenate model (23)(24)(25)(26)(27) because of the difficulties in separating cutaneous from systemic metabolism with in vivo experimental models. Fresh human tissue samples can be obtained readily from surgical procedures and, if processed immediately and stored under appropriate conditions for the particular enzyme(s), the enzyme activity is maintained.…”

Section: Comparative Metabolism Of Pge I In Human Placenta Homogenatementioning

confidence: 99%

Metabolism studies on transdermal prostaglandin E1 in human foreskin in vitro

Földvári

Oguejiofor

1997

European Journal of Drug Metabolism and Pharmacokinetics

View full text Add to dashboard Cite

The metabolism of prostaglandin E1 (PGE1) in solution and in transdermal liposomal formulations was investigated in vitro by incubation with homogenates from human foreskin (HSH), with rabbit lung (RLH) and human placenta (HPH) and heat denatured homogenates as controls, PGE1 and its metabolites and degradation products were analyzed by reversed phase HPLC. Metabolism of PGE1 in HSH was negligible up to 5 h whereas at 24 h, 83 +/- 1%, 92 +/- 2%, and 84 +/- 3% of the initial drug content remained from two different liposomal PGE1 and the free drug incubations, respectively. In HPH, 65 +/- 4% and 5 +/- 3% of initial PGE1 content remained, whereas in RLH, 73 +/- 2% and 60 +/- 3% PGE1 remained after 1 h and 24 h, respectively. The major metabolite was 15-ketoPGE1 in all homogenates. The specific 15-hydroxyprostaglandin dehydrogenase (15-OHPGDH) enzyme activities in HSH, RLH and HPH were found to be 0.22, 1.65, 5.29 nmol 15-ketoPGE1/h/mg homogenate protein, respectively. In conclusion, 15-OHPGDH activity was demonstrated in human foreskin. Encapsulation of PGE1 into liposomes can provide protection from skin metabolism. Based on our in vitro data, we predict that in vivo transdermal delivery of PGE1 is not limited by cutaneous metabolism.

show abstract

Section: Comparative Metabolism Of Pge I In Human Placenta Homogenatementioning

confidence: 99%

Metabolism studies on transdermal prostaglandin E1 in human foreskin in vitro

Földvári

Oguejiofor

1997

European Journal of Drug Metabolism and Pharmacokinetics

View full text Add to dashboard Cite

show abstract

Anti‐Elastase and Anti‐Hyaluronidase Activities of Saponins and Sapogenins from Hedera helix, Aesculus hippocastanum, and Ruscus aculeatus: Factors Contributing to their Efficacy in the Treatment of Venous Insufficiency

Facino

Carini

Stefani

et al. 1995

Archiv der Pharmazie

140

View full text Add to dashboard Cite

Triterpene and steroid saponins and sapogenins of medicinal plants (Aesculus hippocastanum L., Hedera helix L., Ruscus aculeatus L.) are claimed to be effective for the treatment/prevention of venous insufficiency. In this work we evaluated the inhibitory effects of these plant constituents on the activity of elastase and hyaluronidase, the enzyme systems involved in the turnover of the main components of the perivascular amorphous substance. The results evidence that for Hedera helix L., the sapogenins only non-competitively inhibit hyaluronidase activity in a dose-dependent fashion, showing comparable IC50 values (hederagenin IC50 = 280.4 microM; oleanolic acid IC50 = 300.2 microM); both the saponins hederacoside C and alpha-hederin are very weak inhibitors. The same behaviour is observed for serine protease porcine pancreatic elastase: the glycosides are devoid of inhibitory action, while genins are potent competitive inhibitors (oleanolic acid IC50 = 5.1 microM; hederagenin IC50 = 40.6 microM). Constituents from Aesculus hippocastanum L. show inhibitory effects only on hyaluronidase, and this activity is mainly linked to the saponin escin (IC50 = 149.9 microM), less to its genin escinol (IC50 = 1.65 mM). By contrast, ruscogenins from Ruscus aculeatus L., ineffective on hyaluronidase activity, exhibit remarkable anti-elastase activity (IC50 = 119.9 microM; competitive inhibition). The mechanism of elastase inhibition by triterpene and steroid aglycones, with a nitroanilide derivative as substrate, is discussed.

show abstract

Skin Metabolism

Nicolau¹,

Yacobi²

1993

Topical Drug Bioavailability, Bioequivalence, and Penetration

View full text Add to dashboard Cite

Transdermal Absorption and Skin Metabolism of Viprostol, A Synthetic Prostaglandin E₂Analogue

Cited by 5 publications

References 29 publications

Metabolism studies on transdermal prostaglandin E1 in human foreskin in vitro

Metabolism studies on transdermal prostaglandin E1 in human foreskin in vitro

Anti‐Elastase and Anti‐Hyaluronidase Activities of Saponins and Sapogenins from Hedera helix, Aesculus hippocastanum, and Ruscus aculeatus: Factors Contributing to their Efficacy in the Treatment of Venous Insufficiency

Skin Metabolism

Contact Info

Product

Resources

About

Transdermal Absorption and Skin Metabolism of Viprostol, A Synthetic Prostaglandin E2Analogue

Cited by 5 publications

References 29 publications

Metabolism studies on transdermal prostaglandin E1 in human foreskin in vitro

Metabolism studies on transdermal prostaglandin E1 in human foreskin in vitro

Anti‐Elastase and Anti‐Hyaluronidase Activities of Saponins and Sapogenins from Hedera helix, Aesculus hippocastanum, and Ruscus aculeatus: Factors Contributing to their Efficacy in the Treatment of Venous Insufficiency

Skin Metabolism

Contact Info

Product

Resources

About

Transdermal Absorption and Skin Metabolism of Viprostol, A Synthetic Prostaglandin E₂Analogue