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Enhancement of bioavailability by lowering of fat content in topical formulations.
Br J Dermatol. 2009 Mar; 160(3):552-6.BJ

Abstract

BACKGROUND

The cosmetic properties of topical formulations are important parameters for the adherence to treatment, where modern oil-in-water emulsions are considered more acceptable compared with ointments. After application of an emulsion to the skin, the concentration of active ingredients in the formulation residue on the skin will increase, due to evaporation of volatile ingredients.

OBJECTIVES

The aim of the present study was to investigate the effect of changes in vehicle fatty content on the skin penetration of two active ingredients: benzyl nicotinate (BN) and betamethasone valerate (BV).

METHODS

Formulations containing 0.5% BN and 0.3% BV in vehicles with different lipid content (10-80%) were applied in a randomized and double-blind manner to the forearm of healthy volunteers. The changes in skin colour (erythema and blanching) were then monitored visually and with a new noninvasive instrument.

RESULTS

The BN formulation containing 10% fat induced erythema more rapidly and with higher intensity than the formulations with higher fat content. Increased efficacy was also observed from the low-fat content formulation of BV, which gave more blanching than the formulations with high fat content.

CONCLUSIONS

The rate of penetration of the active ingredients was inversely related to the lipid content, i.e. simple changes of the cosmetic properties by modifications of the lipid content may affect the efficacy of a formulation.

Authors+Show Affiliations

Research & Development, ACO Hud Nordic AB, Box 622, SE-194 26 Upplands Väsby, Sweden.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19120336

Citation

Wirén, K, et al. "Enhancement of Bioavailability By Lowering of Fat Content in Topical Formulations." The British Journal of Dermatology, vol. 160, no. 3, 2009, pp. 552-6.
Wirén K, Frithiof H, Sjöqvist C, et al. Enhancement of bioavailability by lowering of fat content in topical formulations. Br J Dermatol. 2009;160(3):552-6.
Wirén, K., Frithiof, H., Sjöqvist, C., & Lodén, M. (2009). Enhancement of bioavailability by lowering of fat content in topical formulations. The British Journal of Dermatology, 160(3), 552-6. https://doi.org/10.1111/j.1365-2133.2008.08981.x
Wirén K, et al. Enhancement of Bioavailability By Lowering of Fat Content in Topical Formulations. Br J Dermatol. 2009;160(3):552-6. PubMed PMID: 19120336.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhancement of bioavailability by lowering of fat content in topical formulations. AU - Wirén,K, AU - Frithiof,H, AU - Sjöqvist,C, AU - Lodén,M, Y1 - 2008/12/11/ PY - 2009/1/6/entrez PY - 2009/1/6/pubmed PY - 2009/4/23/medline SP - 552 EP - 6 JF - The British journal of dermatology JO - Br J Dermatol VL - 160 IS - 3 N2 - BACKGROUND: The cosmetic properties of topical formulations are important parameters for the adherence to treatment, where modern oil-in-water emulsions are considered more acceptable compared with ointments. After application of an emulsion to the skin, the concentration of active ingredients in the formulation residue on the skin will increase, due to evaporation of volatile ingredients. OBJECTIVES: The aim of the present study was to investigate the effect of changes in vehicle fatty content on the skin penetration of two active ingredients: benzyl nicotinate (BN) and betamethasone valerate (BV). METHODS: Formulations containing 0.5% BN and 0.3% BV in vehicles with different lipid content (10-80%) were applied in a randomized and double-blind manner to the forearm of healthy volunteers. The changes in skin colour (erythema and blanching) were then monitored visually and with a new noninvasive instrument. RESULTS: The BN formulation containing 10% fat induced erythema more rapidly and with higher intensity than the formulations with higher fat content. Increased efficacy was also observed from the low-fat content formulation of BV, which gave more blanching than the formulations with high fat content. CONCLUSIONS: The rate of penetration of the active ingredients was inversely related to the lipid content, i.e. simple changes of the cosmetic properties by modifications of the lipid content may affect the efficacy of a formulation. SN - 1365-2133 UR - https://www.unboundmedicine.com/medline/citation/19120336/Enhancement_of_bioavailability_by_lowering_of_fat_content_in_topical_formulations_ L2 - https://doi.org/10.1111/j.1365-2133.2008.08981.x DB - PRIME DP - Unbound Medicine ER -