Decylglucoside-based microemulsions for cutaneous localization of lycopene and ascorbic acid.
Cutaneous delivery of combinations of antioxidants offers the possibility of enhanced protection against UV-radiation. In this study, we investigated the potential of sugar-based microemulsions containing monoglycerides to promote simultaneous cutaneous delivery of lycopene and ascorbic acid, and increase tissue antioxidant activity. Lycopene and ascorbic acid were incorporated (0.04% and 0.2% (w/w), respectively) in decylglucoside-based microemulsions containing isopropyl myristate mixed with monocaprylin (ME-MC), monolaurin (ME-ML) or monoolein (ME-MO) as oil phase. The microemulsions increased lycopene delivery into porcine ear skin by 3.3- to 8-fold compared to a drug solution. The effect of microemulsions on ascorbic acid cutaneous delivery was more modest (1.5-3-fold), and associated with an approximately 2-fold increase in transdermal delivery. According to their penetration-enhancing ability, the microemulsions were ranked ME-MC>ME-MO>ME-ML. This superiority of ME-MC coincided with a stronger effect in decreasing skin electrical resistance. After 18 h of treatment, the viability of bioengineered skin treated with ME-MC was 2.2-times higher compared to Triton-X100 (moderate irritant), demonstrating that ME-MC is less cytotoxic. Skin treatment with ME-MC containing both antioxidants increased the tissue antioxidant activity by 10.2-fold, but no synergism between the antioxidants was observed.
Albany College of Pharmacy and Health Sciences, Albany, NY 12208, USA.
Dominique
D
Pepe
Jessica
J
Phelps
Kevin
K
Lewis
Jared
J
Dujack
Katrina
K
Scarlett
Sumaya
S
Jahan
Emilee
E
Bonnier
Tatjana
T
Milic-Pasetto
Martha A
MA
Hass
Luciana B
LB
Lopes
D000279:Administration, Cutaneous; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D001205:Ascorbic Acid / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002210:Caprylates / Q000737:chemistry; D002338:Carotenoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems; D004655:Emulsions; D005079:Excipients / Q000737:chemistry; D005960:Glucosides / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry; D007848:Laurates / Q000737:chemistry; D000077276:Lycopene; D050178:Monoglycerides / Q000737:chemistry; D009226:Myristates / Q000737:chemistry; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013552:Swine
D000975:Antioxidants; D002210:Caprylates; D004655:Emulsions; D005079:Excipients; D005960:Glucosides; D005989:Glycerides; D007848:Laurates; D050178:Monoglycerides; D009226:Myristates; C008205:isopropyl myristate; C020777:monolaurin; D002338:Carotenoids; C005953:monoolein; D001205:Ascorbic Acid; D000077276:Lycopene; C025343:monooctanoin