EXTRACTION OF A WATER SOLUBLE BIOACTIVE HYPOXOSIDE AND ITS DEVELOPMENT INTO AN ETHOSOMAL SYSTEM FOR DEEP DERMAL DELIVERY
Keywords:
Hypoxoside, Rooperol, Transdermal, Skin Cancer, AntioxidantAbstract
Objective: This study was aimed to extract Hypoxoside, a water soluble phytochemical, from the corms of Hypoxis hemerocallidea, and incorporate it into a suitable transdermal carrier system to increase its penetrability and deep dermal delivery for potential antioxidant and anticancer activity.
Methods: The extraction of Hypoxis hemerocallidea corms was carried out by continuous hot extraction method. This extract (20 mg/ml) was loaded into ethosomal vesicular system by cold method and optimized by varying proportions of lecithin and ethanol. The optimized system was then subjected to characterization in terms of particle size, polydispersity index (PDI), entrapment efficiency and invitro permeation and penetration studies.
Results: The optimized vesicle with size of 176.2±11 nm, PDI of 0.231 and entrapment efficiency of 74.2±2.3% was obtained which showed a sustained release pattern of the hypoxoside from the vesicular system. Confocal laser scanning microscopy (CLSM) demonstrated that the vesicles were able to efficiently traverse the skin to a depth of 117.29 µm whereas the mechanism of vesicle-skin interaction was confirmed by histopathological study.
Conclusion: The study indicated that with the development of an efficient delivery system a water soluble phytochemical with antioxidant and anticancer properties can be efficiently delivered to the skin.
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References
Drewes SE, Khan F. The african potato (Hypoxis hemerocallidea): a chemical-historical perspective: review article. S Afr J Sci 2004;100:425-30.
Owira PM, Ojewole JA. African potato’ (Hypoxis hemerocallidea corm): a plantâ€medicine for modern and 21st century diseases of mankind?–a review. Phytother Res 2009;23:147-52.
Ojewole JAO. Antinociceptive, anti-inflammatory and antidiabetic properties of Hypoxis hemerocallidea Fisch. and C. A. Mey. (Hypoxidaceae) corm [‘African Potato’] aqueous extract in mice and rats. J Ethnopharmacol 2005;103:126-34.
Ojewole JA. Anticonvulsant activity of Hypoxis hemerocallidea Fisch. and CA Mey. (Hypoxidaceae) corm (‘African potato’) aqueous extract in mice. Phytother Res 2008;22:91-6.
Muwanga C. An assessment of extracts, and actives as natural antibiotic, and immune modulation phytotherapies. MSc. Dissertation. University of the Western Cape, Cape Town; 2006.
Bettolo GB, Patamia M, Nicoletti M, Galeffi C, Messana I. Research on African medicinal plants—II: Hypoxoside, a new glycoside of uncommon structure from hypoxis obtusa busch. Tetrahedron 1982;38:1683-7.
Drewes S, Liebenberg RW. Rooperol and its derivates; 1987.
Theron EJ, Albrecht CF, Kruger PB, Jerkins K, Van Der Merwe MJ. Glucosidase activity in fetal bovine serum renders the plant glucoside hypoxoside, Cytotoxic Toward B16-F10-B1-6 mouse melanoma cells. In vitro Cell Dev Biol: Anim 1994;30:115-9.
Jun H, Shi-wen Z. New research on development of solid lipid nanoparticles. J Med Coll PLA 2007;22:385-90.
Muller RH, Petersen RD, Hommoss A, Pardeike J. Nanostructured lipid carriers (NLC) in cosmetic dermal products. Adv Drug Delivery Rev 2007;59:522-30.
Kong M, Park HJ. Stability investigation of hyaluronic acid based nanoemulsion and its potential as transdermal carrier. Carbohydr Polym 2011;83:1303–10.
Akiladevi D, Basak S. Ethosomes: A non-Invasive approach for transdermal drug delivery. Int J Curr Pharm Res 2010;2:1-4.
Touitou E Godin B, Dayan N, Weiss C, Piliponsky A, Levi-Schaffer F. Intracellular delivery mediated by an ethosomal carrier. Biomaterials 2001;22:3053-9.
Ainbinder D, Paolino D, Fresta M, Touitou E. Drug delivery applications with ethosomes. J Biomed Nanotechnol 2010;6:558-68.
Heinrich M, Barnes J, Gibbons S. Williamson EM. Fundamentals of pharmacognosy and Phytotherapy, Elsevier Health Sciences; 2012.
Touitou Elka. "Compositions for applying active substances to or through the skin; 1996.
Kalia YN, Guy RH. Modeling transdermal drug release. Adv Drug Delivery Rev 2001;48:159-72.
Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm 2010;67:217-23.
Touitou E, Godin B, Weiss C. Enhanced delivery of drug into and across the skin by ethosomal carriers. Drug Dev Res 2002;50:406-15.