Formulation and Evaluation of a Novel Itraconazole-Clotrimazole Topical Emulgel for the Treatment of Sporotrichosis

Author(s): Letícia L. Noronha, Patricia G. Ferreira, Carolina G.S. Lima, Luana P. Borba-Santos, Sonia Rozental, Marcela de Moraes, Fernando C. da Silva, Vitor F. Ferreira*, Débora O. Futuro.

Journal Name: Current Pharmaceutical Design

Volume 26 , Issue 14 , 2020

Become EABM
Become Reviewer


In recent years, the development of new pharmaceutical formulations for the treatment of sporotrichosis has become a relevant research field. In this work, we aimed to develop an emulgel containing itraconazole and clotrimazole to ensure therapeutic effectiveness against Sporothrix brasiliensis. The topical use of a formulation that combines both drugs represents an interesting option for the complementary treatment of sporotrichosis. The emulgel formulation was prepared and evaluated for its zeta potential, viscosity, in vitro antifungal activity and stability at different storage conditions. The results showed that the newly developed emulgel displayed promising physicochemical characteristics, as well as a good in vitro inhibitory activity against S. brasiliensis yeasts. The results obtained in this work suggest that the emulgel containing itraconazole and clotrimazole might highly be efficient and a complementary therapy to oral administration in the treatment of sporotrichosis.

Keywords: Emulgel, sporotrichosis, itraconazole, clotrimazole, topical drug delivery systems, viscosity.

Chakrabarti A, Bonifaz A, Gutierrez-Galhardo MC, Mochizuki T, Li S. Global epidemiology of sporotrichosis. Med Mycol 2015; 53(1): 3-14.
[] [PMID: 25526781]
Borba-Santos LP, Rodrigues AM, Gagini TB, et al. Susceptibility of Sporothrix brasiliensis isolates to amphotericin B, azoles, and terbinafine. Med Mycol 2014; 00(0): 1-11.
[PMID: 25394542]
Kauffman CA, Bustamante B, Chapman SW, Pappas PG. Clinical practice guidelines for the management of sporotrichosis: 2007 update by the Infectious Diseases Society of America. Clin Infect Dis 2007; 45(10): 1255-65.
[] [PMID: 17968818]
Ajazuddin AA, Alexander A, Khichariya A, et al. Recent expansions in an emergent novel drug delivery technology: Emulgel. J Control Release 2013; 171(2): 122-32.
[] [PMID: 23831051]
Gagini T, Borba-Santos LP, Messias Rodrigues A, Pires de Camargo Z, Rozental S. Clotrimazole is highly effective in vitro against feline Sporothrix brasiliensis isolates. J Med Microbiol 2017; 66(11): 1573-80.
[] [PMID: 28984226]
Ferreira PG, Noronha L, Teixeira R, et al. Investigation of a microemulsion containing clotrimazole and itraconazole for transdermal delivery for the treatment of sporotrichosis. J Pharm Sci 2020; 109(2): 1026-34.
[] [PMID: 31604084]
Ting Y, Jiang Y, Lan Y, et al. Viscoelastic emulsion improved the bioaccessibility and oral bioavailability of crystalline compound: a mechanistic study using in vitro and in vivo models. Mol Pharm 2015; 12(7): 2229-36.
[] [PMID: 25984595]
Raikos V, Ranawana V. Designing emulsion droplets of foods and beverages to enhance delivery of lipophilic bioactive components e a review of recent advances. Int J Food Sci Technol 2017; 52(1): 68-80.
Eswaraiah S, Swetha K, Lohita M, Preethi PJ, Priyanka B, Reddy KK. Emulgel: review on novel approach to topical drug delivery. Asian J Pharm Res 2014; 4(1): 4-11.
Sohail M, Naveed A, Abdul R, Gulfishan , Muhammad Shoaib Khan H, Khan H. An approach to enhanced stability: Formulation and characterization of Solanum lycopersicum derived lycopene based topical emulgel. Saudi Pharm J 2018; 26(8): 1170-7.
[] [PMID: 30532638]
Naga Sravan Kumar Varma V, Maheshwari PV, Navya M, Reddy SC, Shivakumar HG, Gowda DV. Calcipotriol delivery into the skin as emulgel for effective permeation. Saudi Pharm J 2014; 22(6): 591-9.
[] [PMID: 25561873]
Srivastava N, Patel DK, Rai VK, Pal A, Yadav NP. Development of emulgel formulation for vaginal candidiasis: Pharmaceutical characterization, in vitro and in vivo evaluation. J Drug Deliv Sci Technol 2018; 48: 490-8.
Pant S, Badola A, Baluni S, Pant W. A review on emulgel novel approach for topical drug delivery system. World J Pharm Pharm Sci 2015; 4: 1728-43.
Ferreira PG, Lima CGS, Noronha LL, et al. Development and characterization of emulgels for treatment of chronic wounds. Asian J Pharm Technol Innov 2017; 5(25): 40-8.
Ferreira PG, Guimarães de Souza Lima C, Noronha LL, et al. Development of a method for the quantification of clotrimazole and itraconazole and study of their stability in a new microemulsion for the treatment of sporotrichosis. Molecules 2019; 24(12): 233.
[] [PMID: 31242573]
Resolution Nº 318, Diário Oficial da União (Brazil), published 2019, Ed 216, section 1, page 97 Available at:.
Gary W. Method for antifungal disk diffusion susceptibility testing of yeasts: M44. 3rd ed. Wayne, PA: Clinical and Laboratory Standards Institute 2018.
Alam MA, Alzahrani KA, Abdelgalil AA, Al-janoobi FI, Al-agamy MH, Al-mohizea A. In-vitro efficacies of topical microemulsions of clotrimazole and ketoconazole; and in-vivo performance of clotrimazole microemulsion. J Drug Deliv Sci Technol 2017; 39: 408-16.
Negussie AH, Miller JL, Reddy G, Drake SK, Wood BJ, Dreher MR. Synthesis and in vitro evaluation of cyclic NGR peptide targeted thermally sensitive liposome. J Control Release 2010; 143(2): 265-73.
[] [PMID: 20067811]
Maha E. Elmataeeshy, Magda S. Sokar, Mohammed Bahey-El-Din, Dalia S. Shaker. Enhanced transdermal permeability of Terbinafine through novel nanoemulgel formulation; Development, in vitro and in vivo characterization. Fut J Pharm Sci 2018; 4: 18-28.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2020
Page: [1566 - 1570]
Pages: 5
DOI: 10.2174/1381612826666200406081249
Price: $65

Article Metrics

PDF: 11