Klin Farmakol Farm. 2021;35(4):126-129 | DOI: 10.36290/far.2021.029

The Importance of Penetration Enhancers choice in Topical Products

Jiří Slíva
Department of Pharmacology, Third Faculty of Medicine, Charles University, Prague

Topical products are widely used in the treatment of pain or inflammatory and degenerative conditions. Their undeniable advantage is sufficiently proven clinical efficacy and also a generally favourable safety profile due to their minimal systemic exposure compared to orally used products. It was also demonstrated that exact formulation used is critical for topical analgesic in management of pain conditions. This brief overview emphasizes the important role of different excipients like penetration enhancers which chemical properties suggesting a different disrupting effect on the skin barrier. It summarizes the well-known properties of the skin as a key barrier to any pharmacological effects and focuses on a differences in using different excipients like penetration enhancers.

Keywords: penetration enhancer, oleyl lalcohol, oleic acid, skin barrier.

Published: January 4, 2022  Show citation

ACS AIP APA ASA Harvard Chicago Chicago Notes IEEE ISO690 MLA NLM Turabian Vancouver
Slíva J. The Importance of Penetration Enhancers choice in Topical Products. Klin Farmakol Farm. 2021;35(4):126-129. doi: 10.36290/far.2021.029.
Download citation

References

  1. Barton AFM. CRC Handbook of Solubility Parameters and Other Cohesion Parameters, Second Edition. 2017; 1-739. Go to original source...
  2. Boelsma E, Tanojo HE, Boddé HE, Ponec M. Assessment of the Potential Irritancy of Oleic Acid on Human Skin: Evaluation In Vitro and In Vivo. Toxicol Vitr, 1996; 10: 729-742. Go to original source... Go to PubMed...
  3. Boncheva M, Damien F, Normand V. Molecular organization of the lipid matrix in intact Stratum corneum using ATR-FTIR spectroscopy. Biochim Biophys Acta, 2008; 1778, 5: 1344-1355. Go to original source... Go to PubMed...
  4. Cordero J, Camacho M, Obach R et al. In vitro based index of topical anti-inflammatory activity to compare a series of NSAIDs. Eur J Pharm Biopharm, 2001; 51: 135-142. Go to original source... Go to PubMed...
  5. Derry S, Moore RA, Gaskell H, McIntyre M, Wiffen PJ. Topical NSAIDs for acute musculoskeletal pain in adults. Cochrane Database Syst Rev, 2015; CD007402. Go to original source...
  6. Hagen M, Baker M. Skin penetration and tissue permeation after topical administration of diclofenac. Curr Med Res Opin, 2017; 33: 1623-1634. Go to original source... Go to PubMed...
  7. Ibrahim SA, Li SK. Effects of chemical enhancers on human epidermal membrane: Structure-enhancement relationship based on maximum enhancement (E(max)). J Pharm Sci, 2009; 98: 926-944. Go to original source... Go to PubMed...
  8. Paudel KS, Milewski M, Swadley CL, Brogden NK, Ghosh P, Stinchcomb AL. Challenges and opportunities in dermal/transdermal delivery. Ther Deliv, 2010; 1: 109-131. Go to original source... Go to PubMed...
  9. Pradal J et all. Importance of the formulation in the skin delivery of topical diclofenac: not all topical diclofenac formulations are the same. J Pain Res. 2019; 12: 1149-1154. Go to original source... Go to PubMed...
  10. Pradal J et all. Comparison of Skin Permeation and Putative Anti-Inflammatory Activity of Commercially Available Topical Products Containing Ibuprofen and Diclofenac. J Pain Res. 2020; Nov 4, 13: 2805-2814. Go to original source... Go to PubMed...
  11. Public Assessment Report DE/H/5493+6245+6603/001-002/DC for Diclofenac AbZ Schmerzgel Diclox / Diclox forte Diclofenac-ratiopharm, 2020. Available online at: https://mri.cts-mrp.eu/Human/Downloads/DE_H_5493_002_PAR.pdf. Last accessed: 27 May 2021.
  12. Rao P, Knaus EE. Evolution of nonsteroidal anti-inflammatory drugs (NSAIDs): cyclooxygenase (COX) inhibition and beyond. J Pharm Pharm Sci, 2008; 11: 81s-110s. Go to original source... Go to PubMed...
  13. Tanojo H, Junginger HE, Bodde HE. In vivo human skin permeability enhancement by oleic acid: Transepidermal water loss and Fourier-transform infrared spectroscopy. J Control Release, 1997; 47: 31-39. Go to original source...
  14. Wiffen PJ, Xia J. Systematic review of topical diclofenac for the treatment of acute and chronic musculoskeletal pain. Curr Med Res Opin, 2020; 36: 637-650. Go to original source... Go to PubMed...
  15. Williams AC, Barry BW. Penetration enhancers. Advanced Drug Delivery Reviews, 2012; 64: 128-137. Go to original source...
  16. Zhang Q, Saad P, Mao G, Walters RM, Mack Correa MC, Mendelsohn R, Flach CR. Infrared spectroscopic imaging tracks lateral distribution in human stratum corneum. Pharm Res, 2014; 31: 2762-2773. Go to original source... Go to PubMed...




Clinical Pharmacology and Pharmacy

Madam, Sir,
please be aware that the website on which you intend to enter, not the general public because it contains technical information about medicines, including advertisements relating to medicinal products. This information and communication professionals are solely under §2 of the Act n.40/1995 Coll. Is active persons authorized to prescribe or supply (hereinafter expert).
Take note that if you are not an expert, you run the risk of danger to their health or the health of other persons, if you the obtained information improperly understood or interpreted, and especially advertising which may be part of this site, or whether you used it for self-diagnosis or medical treatment, whether in relation to each other in person or in relation to others.

I declare:

  1. that I have met the above instruction
  2. I'm an expert within the meaning of the Act n.40/1995 Coll. the regulation of advertising, as amended, and I am aware of the risks that would be a person other than the expert input to these sites exhibited


No

Yes

If your statement is not true, please be aware
that brings the risk of danger to their health or the health of others.