Hydrophile Lipophile Balance Number and transdermal transportation efficiency of vitamin C, E and coenzyme Q10 derivatives

Accession number;07A0095810
Title;Hydrophile Lipophile Balance Number and transdermal transportation efficiency of vitamin C, E and coenzyme Q10 derivatives
Author; WATANABE YUKIO (Meisei Univ., Coll. of Sci. and Eng.) SUZUKI HARUE (Suzukikeiseigeka(kyotoshi)) UEDA TOYOTOSHI (Meisei Univ., Coll. of Sci. and Eng.)
Journal Title;Aesthetic Dermatol
Journal Code:L5200A
ISSN:1341-5530
VOL.16;NO.4;PAGE.287-300(2006)
Figure&Table&Reference;FIG.13, TBL.1, REF.32
Pub. Country;Japan
Language;Japanese
Abstract;We have aimed at devising a new delivery system for medicines and supplements. Derivatives of vitamin C, E, and coenzyme Q10 were examined concerning the relationship between the HLB (hydrophile lipophile balance) number and transdermal transportation efficiency into the skin. Non-invasive vibrational spectroscopies, IR-ATR (infrared attenuated total reflection), and NIR-DR (near-infrared diffusive reflection) methods were used in order to evaluate the concentration of transported materials in the skin. Vitamin C derivatives of sodium L-ascorbyl-2-phosphate (hereafter abbreviated as APS) and sodium L-ascorbyl-2-phosphate-6-palmitate (APPS) were examined. APPS contains both a hydrophilic group and a hydrophobic group, since APS has been modified to APPS by deriving palmitic acid ester at the 6-OH position. APPS has an HLB number of around 9.03, while APS has that of 20. The iontophoretic efficiency of APPS is higher than APS. Vitamin E derivatives of DL-.ALPHA.-tocopheryl N,N-dimethylglycinate (DL-.ALPHA.-TDMG) and .ALPHA. -tocopheryl acetate (.ALPHA.-TA) were examined concerning their transdermal transportation efficiency. Their HLB numbers are 2.28 and zero, respectively. .ALPHA.-TA is hydrophobic, while DL-.ALPHA.-TDMG has a hydrophilic terminal group of dimethylglycine/HCl. The iontopheretic efficiency of .ALPHA.-TA is lower than that of DL-.ALPHA.-TDMG. Coenzyme Q10 (CoQ10) is hydrophobic and a portion of benzoquinone is also hydrophobic. CoQ10 has been modified to a reduced form of CoQ10 (CoH2Q10) by NaBH4. CoH2Q10 has a hydroquinone structure with a hydrophilic property. Supersonic perforation led to transportion of a greater amount of CoH2Q10 into the skin than CoQ10. The balance between hydrophilic and hydrophobic group in the transported material is an important factor for its effective transportation into the skin. (author abst.)