Next Article in Journal
Attenuation of Benign Prostatic Hyperplasia by Optimized Tadalafil Loaded Pumpkin Seed Oil-Based Self Nanoemulsion: In Vitro and In Vivo Evaluation
Next Article in Special Issue
Investigation of Silicone-Containing Semisolid in Situ Film-Forming Systems Using QbD Tools
Previous Article in Journal
Validation of an Ex Vivo Permeation Method for the Intestinal Permeability of Different BCS Drugs and Its Correlation with Caco-2 In Vitro Experiments
Open AccessArticle

Mechanistic Evaluation of Enhanced Curcumin Delivery through Human Skin In Vitro from Optimised Nanoemulsion Formulations Fabricated with Different Penetration Enhancers

1
Therapeutics Research Centre, University of Queensland Diamantina Institute, University of Queensland, Woolloongabba, QLD 4102, Australia
2
Faculty of Pharmacy, Helwan University, Helwan 11795, Egypt
3
School of Pharmacy and Biomedical Sciences, Curtin Health Innovation Research Institute, Curtin University, Perth 6845, Australia
4
School of Pharmacy and Medical Sciences, University of South Australia, Adelaide 5000, Australia
5
Therapeutics Research Centre, Basil Hetzel Institute for Translational Medical Research, The Queen Elizabeth Hospital, Adelaide 5011, Australia
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(12), 639; https://doi.org/10.3390/pharmaceutics11120639
Received: 18 October 2019 / Revised: 24 November 2019 / Accepted: 25 November 2019 / Published: 1 December 2019
Curcumin is a natural product with chemopreventive and other properties that are potentially useful in treating skin diseases, including psoriasis and melanoma. However, because of the excellent barrier function of the stratum corneum and the relatively high lipophilicity of curcumin (log P 3.6), skin delivery of curcumin is challenging. We used the principles of a Quality by Design (QbD) approach to develop nanoemulsion formulations containing biocompatible components, including Labrasol and Lecithin as surfactants and Transcutol and ethanol as cosurfactants, to enhance the skin delivery of curcumin. The nanoemulsions were characterised by cryo-SEM, Zeta potential, droplet size, pH, electrical conductivity (EC) and viscosity (η). Physicochemical long-term stability (6 months) was also investigated. The mean droplet sizes as determined by dynamic light scattering (DLS) were in the lower submicron range (20–50 nm) and the average Zeta potential values were low (range: −0.12 to −2.98 mV). Newtonian flow was suggested for the nanoemulsions investigated, with dynamic viscosity of the nanoemulsion formulations ranging from 5.8 to 31 cP. The droplet size of curcumin loaded formulations remained largely constant over a 6-month storage period. The inclusion of terpenes to further enhance skin permeation was also examined. All nanoemulsions significantly enhanced the permeation of curcumin through heat-separated human epidermal membranes, with the greatest effect being a 28-fold increase in maximum flux (Jmax) achieved with a limonene-based nanoemulsion, compared to a 60% ethanol in water control vehicle. The increases in curcumin flux were associated with increased skin diffusivity. In summary, we demonstrated the effectiveness of nanoemulsions for the skin delivery of the lipophilic active compound curcumin, and elucidated the mechanism of permeation enhancement. These formulations show promise as delivery vehicles for curcumin to target psoriasis and skin cancer, and more broadly for other skin delivery applications. View Full-Text
Keywords: skin permeation; permeation enhancers; curcumin; nanoemulsions; cutaneous drug delivery; Quality by Design principles skin permeation; permeation enhancers; curcumin; nanoemulsions; cutaneous drug delivery; Quality by Design principles
Show Figures

Graphical abstract

MDPI and ACS Style

Yousef, S.A.; Mohammed, Y.H.; Namjoshi, S.; Grice, J.E.; Benson, H.A.E.; Sakran, W.; Roberts, M.S. Mechanistic Evaluation of Enhanced Curcumin Delivery through Human Skin In Vitro from Optimised Nanoemulsion Formulations Fabricated with Different Penetration Enhancers. Pharmaceutics 2019, 11, 639.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop