Optimization and Characterization of Thymoquinone-Loaded Liposomes with Enhanced Topical Anti-inflammatory Activity
Thymoquinone, the major constituent of Nigella sativa oil has been found to have a promising topical anti-inflammatory activity; however, exaggerated heat and photo-sensitivity and lipophilicity prevent the best use of this promising product. The present work aimed to formulate an ideal thymoquinone liposomal system for topical delivery. Different liposomal systems were developed using thin film hydration method by applying different cholesterol molar concentrations, different total lipid molar concentrations, and different drug-to-lipid ratios. Morphological characterization of the prepared formulae was performed using polarized light, scanning electron microscope, and transmission electron microscope. The optimized formula (F12) was selected on the basis of enhanced permeation through the skin and was incorporated into chitosan gel for topical application. The gel formulation was clear with suitable skin permeation and exhibited acceptable rheological properties. Using carrageenan-induced paw edema in rats, the developed chitosan gel (F12) showed significant superior in vivo anti-inflammatory activity over the chitosan gel of the TQ (p < 0.05) and comparable effect to the marketed indomethacin gel. As a conclusion, results revealed the potential of formulating thymoquinone as liposomal formulation in enhancing the anti-inflammatory effect compared to the TQ solution.
KEY WORDSliposomes thymoquinone skin enhanced drug deposition, enhanced stability
The authors wish to thank the Lipoid GmbH company (Germany) for the generous gift of Phospholipon 90H. Also, we are indebted to Dr. Rehab Refaee (Department of Histology, Faculty of Medicine, Minia University) for her contribution concerning the histology of skin observation.
This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.
- 2.Aljabre S. In vitro antifungal activity of thymoqyuinone against Scopulariopsis brevicaulis. Arab J Pharm Sci. 2005;3:27–33.Google Scholar
- 17.New RC. Preparation of liposomes. In: New RRC, editors. Liposomes, a practical approach. Oxford etc: IRZ press; 1990. p. 33–104.Google Scholar
- 24.Morris CJ. Carrageenan-induced paw edema in the rat and mouse. Methods Mol Biol. 2003;225:115–21.Google Scholar
- 30.Sinko PJ, Singh Y. Martin’s physical pharmacy and pharmaceutical sciences: physical chemical and biopharmaceutical principles in the pharmaceutical sciences. Sixth edition; 2011.Google Scholar
- 37.New R. Characterization of liposomes. In: New R, (editor) Liposomes—a practical approach. Oxford: IRL Press; 1990. p. 105–62.Google Scholar
- 44.Li X, Chen D, Le C, Zhu C, Gan Y, Hovgaard L, et al. Novel mucus-penetrating liposomes as a potential oral drug delivery system: preparation, in vitro characterization, and enhanced cellular uptake. Int J Nanomed. 2011;6(3):151–62.Google Scholar
- 49.Orienti I, Luppi B, Zecchi V. Chitosan and its N-carboxyethyl and N-aminoethyl derivatives as vehicles for topical formulations. J Cosmet Sci. 1999;50(5):307–14.Google Scholar
- 52.Paranjothy K. Gels as topical applications. Indian Drugs. 1994;31:224.Google Scholar