Effects of dimethylformamide and L-menthol permeation enhancers on transdermal delivery of quercetin

• Published in: Pharmaceutical development and technology Vol. 12; no. 5; p. 481
• Main Authors: Olivella, Mónica S, Lhez, Lucía, Pappano, Nora B, Debattista, Nora B
• Format: Journal Article
• Language: English
• Published: England 01.01.2007
• Subjects: Acrylic Resins; Adjuvants, Pharmaceutic - pharmacology; Administration, Cutaneous; Algorithms; Animals; Antioxidants - administration & dosage; Antioxidants - pharmacokinetics; Diffusion; Dimethylformamide - pharmacology; Drug Delivery Systems - methods; Menthol - pharmacology; Molecular Structure; Permeability - drug effects; Polyvinyls - chemistry; Quercetin - administration & dosage; Quercetin - pharmacokinetics; Skin - drug effects; Skin - metabolism; Skin Absorption - drug effects; Swine
• ISSN: 1083-7450
• DOI: 10.1080/10837450701481207

In this work a feasibility study of transdermal delivery system for quercertin (Q) in carbopol gel through abdominal hairless pig skin in vitro was performed. Dimethylformamide (DMF) and L-menthol (M) were selected as enhancers. Permeation experiences were carried out by using Franz-type diffusion cells. Phosphate saline buffer (pH 7.4) was used in the receptor compartments. All the system was maintained at 32 +/- 0.5 degrees C with a circulating water jacket and magnetic stirring (180 rpm). Samples were analysed by UV-VIS spectrophotometer at 255 nm. Flux (Jm) values, permeation (P) and diffusion (D) coefficients were obtained. Results of Q in CG permeation experiences with different percentages of DMF and M showed that 16.7% DMF and 1.95% L-menthol enhancers were the best quantities for the system tested. Enhancer effect can be attributed to direct action on membrane structure by promoting its distension. Therefore, enhancer substitutes for water in pores, improving active principal permeation through pig skin. M significantly increases Q permeation about 17 times higher than control. The results of permeation experiments with M and DMF using the same enhancer concentration (1.42%) conclude that M action is 9 times higher than DMF, approximately, indicating that M is an effective enhancer for a transdermal therapeutic system of Q in CG as vehicle.