Pentane-1,5-diol as a percutaneous absorption enhancer.
Propylene glycol (propane-1,2-diol) is the only diol widely used in dermatology. Pentane-1,5-diol is mainly used as a plasticizer in cellulose products and adhesives, in dental composites and in brake fluid compositions and as a preservative for grain. However, pentane-1,5-diol is also an effective solvent, water-binding substance, antimicrobial agent and preservative and may therefore replace several ingredients in a skin composition. The release of tri-iodothyroacetic acid (TRIAC) and percutaneous absorption of hydrocortisone and mometasone furoate with either pentane-1,5-diol or propane-1,2-diol and 2-methyl-pentane-2,4-diol (hexylene glycol), respectively, as enhancers was compared. The release of TRIAC was 21% higher when pentane-1,5-diol was used as an enhancer instead of propane-1,2-diol. The percutaneous absorption of hydrocortisone through the skin was increased 12 times with propane-1,2-diol compared to 4.4 times with pentane-1,5-diol. However, the percutaneous absorption of hydrocortisone into the skin was 50% higher with pentane-1,5-diol compared to propane-1,2-diol. There was no significant difference, between the original mometasone furoate cream, with 2-methyl-pentane-2,4-diol, and the new cream with pentane-1,5-diol in the amount of mometasone furoate that was absorbed into the skin and through the skin. However, the cosmetic properties of the new mometasone furoate cream was superior to the original mometasone furoate cream, for examples, no bad odour, more even texture, goes better into the skin and has less greasiness. Pentane-1,5-diol can be used as a technology platform, which adds a series of desirable properties to dermatological preparations and enhances product usability. This will result in improved formulations for a series of major and commonly used dermatological drugs. When used in pharmaceutical topical preparations, pentane-1,5-diol will increase the percutaneous absorption of the active substance and it is an efficient antimicrobial agent that will act as an effective preservative in topical formulations. Pentane-1,5-diol is cosmetically attractive, has low risk for skin and eye irritation compared to other diols, low toxicity risk and no bad odour.
Faergemann
Jan
J
Department of Dermatology, Sahlgrenska University Hospital, SE-41345, Gothenburg, Sweden. jan.faergemann@derm.gu.se
Wahlstrand
Björn
B
Hedner
Thomas
T
Johnsson
Jörgen
J
Neubert
Reinhard H H
RH
Nyström
Lena
L
Maibach
Howard
H
D000279:Administration, Cutaneous; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage; D002626:Chemistry, Pharmaceutical; D006018:Glycols / Q000494:pharmacology*; D006801:Humans; D006854:Hydrocortisone / Q000008:administration & dosage; D066298:In Vitro Techniques; D000068656:Mometasone Furoate; D010420:Pentanes; D011244:Pregnadienediols / Q000008:administration & dosage; D011310:Preservatives, Pharmaceutical / Q000494:pharmacology*; D019946:Propylene Glycol / Q000494:pharmacology; D012869:Skin Absorption / Q000187:drug effects*; D012997:Solvents / Q000494:pharmacology*; D014284:Triiodothyronine / Q000031:analogs & derivatives / Q000737:chemistry
D000893:Anti-Inflammatory Agents; D006018:Glycols; D010420:Pentanes; D011244:Pregnadienediols; D011310:Preservatives, Pharmaceutical; D012997:Solvents; D000068656:Mometasone Furoate; D014284:Triiodothyronine; C578469:1,5-pentanediol; C010642:3,3',5-triiodothyroacetic acid; D019946:Propylene Glycol; D006854:Hydrocortisone