Advancing the Understanding of Itraconazole: Skin Levels, Minimum Inhibitory Concentration, and the Role of Super Bioavailable Formulation in Recalcitrant Dermatophytosis

Main Article Content

Navya Pandey
Gauri Bhale
Mohan Kale

Abstract

Clinical therapy of recalcitrant dermatophytosis—a chronic fungal skin illness caused by dermatophytes—is tough. Alternative treatments are needed when traditional antifungals fail. Itraconazole, a common antifungal, treats resistant dermatophytosis. This review examines itraconazole skin levels, MIC data, and highly bioavailable itraconazole for recalcitrant dermatophytosis. The review examines extremely bioavailable itraconazole in this difficult condition.


This review paper introduces recalcitrant dermatophytosis, discusses itraconazole and its mechanism of action, examines skin levels and MIC data, explores super bioavailable itraconazole, and evaluates its role in the disease.


This review underlines the importance of itraconazole skin levels due to its lipophilicity and delayed keratin turnover. Itraconazole's MIC values against dermatophytes show its efficacy against diverse species. The paper also highlights hyper bioavailable itraconazole's increased pharmacokinetics and solubility, which increase systemic exposure and absorption.


The review paper also examines trials on ultra bioavailable itraconazole in recalcitrant dermatophytosis, which showed superior clinical and mycological cure rates, faster time to cure, and greater rates of complete cure. Super bioavailable itraconazole safety is briefly discussed.


This review highlights the importance of itraconazole and its extremely bioavailable formulation in treating recalcitrant dermatophytosis. It stresses appropriate skin levels and covers hyper bioavailable itraconazole as an alternate treatment for recalcitrant dermatophytosis.

Article Details

How to Cite
Pandey, N. ., Bhale, G. ., & Kale, M. . (2023). Advancing the Understanding of Itraconazole: Skin Levels, Minimum Inhibitory Concentration, and the Role of Super Bioavailable Formulation in Recalcitrant Dermatophytosis. Journal of Coastal Life Medicine, 11(1), 3318–3322. Retrieved from https://www.jclmm.com/index.php/journal/article/view/894
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References

Gupta AK, Foley KA, Versteeg SG. New Antifungal Agents and New Formulations Against Dermatophytes. Mycopathologia. 2017;182(1-2):127-141. doi:10.1007/s11046-016-0045-0

Bhatia VK, Sharma PC. Epidemiological studies on Dermatophytosis in human patients in Himachal Pradesh, India. Springerplus. 2014;3:134. Published 2014 Mar 19. doi:10.1186/2193-1801-3-134

Mahajan S, Tilak R, Kaushal SK, Mishra RN, Pandey SS. Clinico-mycological study of dermatophytic infections and their sensitivity to antifungal drugs in a tertiary care center. Indian J Dermatol Venereol Leprol. 2017;83(4):436-440. doi:10.4103/ijdvl.IJDVL_519_16

Rajagopalan M, Inamadar A, Mittal A, Miskeen AK, Srinivas CR, Sardana K, Godse K, Patel K, Rengasamy M, Rudramurthy S, Dogra S. Expert Consensus on The Management of Dermatophytosis in India (ECTODERM India). BMC Dermatol. 2018 Jul 24;18(1):6. doi: 10.1186/s12895-018-0073-1. PMID: 30041646; PMCID: PMC6057051.

Fuller LC, Barton RC, Mohd Mustapa MF, Proudfoot LE, Punjabi SP, Higgins EM. British Association of Dermatologists' guidelines for the management of tinea capitis 2014. Br J Dermatol. 2014;171(3):454-463. doi:10.1111/bjd.13196

Dogra S, Uprety S. The menace of chronic and recurrent dermatophytosis in India: Is the problem deeper than we perceive?. Indian Dermatol Online J. 2016;7(2):73-76. doi:10.4103/2229-5178.178102

Haria M, Bryson HM, Goa KL. Itraconazole. A reappraisal of its pharmacological properties and therapeutic use in the management of superficial fungal infections [published correction appears in Drugs 1996 Aug;52(2):253]. Drugs. 1996;51(4):585-620. doi:10.2165/00003495-199651040-00006

Van Cutsem J, Van Gerven F, Van de Ven MA, Borgers M, Janssen PA. Itraconazole, a new triazole that is orally active in aspergillosis. Antimicrob Agents Chemother. 1984;26(4):527-534. doi:10.1128/AAC.26.4.527

Verma S, Madhu R. The great Indian epidemic of superficial dermatophytosis: An appraisal. Indian J Dermatol. 2017;62(3):227-236.

Bohn M, Kraemer KT. Dermatopharmacology of ciclopirox nail lacquer topical solution 8% in the treatment of onychomycosis. J Am Acad Dermatol. 2000;43(4 Suppl):S57-S69. doi:10.1067/mjd.2000.109072.

Dias MF, Bernardes-Filho F, Quaresma-Santos MV, Amorim AG, Schechtman RC, Azulay DR. Treatment of superficial mycoses: review. Part II. An Bras Dermatol. 2013 Nov-Dec;88(6):937-44. doi: 10.1590/abd1806-4841.20132018. PMID: 24474103; PMCID: PMC3900345..

Gupta AK, Fleckman P, Baran R. Ciclopirox nail lacquer topical solution 8% in the treatment of toenail onychomycosis. J Am Acad Dermatol. 2000;43(4 Suppl):S70-S80. doi:10.1067/mjd.2000.109071.

Adimi P, Hashemi SJ, Mahmoudi M, Mirhendi H, Shidfar MR, Emmami M, Rezaei-Matehkolaei A, Gramishoar M, Kordbacheh P. In-vitro Activity of 10 Antifungal Agents against 320 Dermatophyte Strains Using Microdilution Method in Tehran. Iran J Pharm Res. 2013 Summer;12(3):537-45. PMID: 24250660; PMCID: PMC3813282.

Espinel-Ingroff A, Arthington-Skaggs BA, Iqbal N, et al. Multicenter evaluation of proposed standardized procedure for antifungal susceptibility testing of filamentous fungi. J Clin Microbiol. 2007;45(6):1811-1818.

Hay R. Therapy of Skin, Hair and Nail Fungal Infections. Journal of Fungi. 2018; 4(3):99. https://doi.org/10.3390/jof4030099.

Kumar M, Tiwari A, Asdaq SMB, Nair AB, Bhatt S, Shinu P, Al Mouslem AK, Jacob S, Alamri AS, Alsanie WF, Alhomrani M, Tiwari V, Devi S, Pathania A, Sreeharsha N. Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation. Saudi J Biol Sci. 2022 Jan;29(1):1-10. doi: 10.1016/j.sjbs.2021.11.006. Epub 2021 Nov 12. PMID: 35002390; PMCID: PMC8717166..

Qumber M, Alruwaili NK, Bukhari SN, Alharbi KS, Imam SS, Afzal M, Alsuwayt B, Mujtaba A, Ali A. BBD-based development of itraconazole loaded nanostructured lipid carrier for topical delivery: in vitro evaluation and antimicrobial assessment. Journal of pharmaceutical innovation. 2021 Mar;16:85-98.

Shegokar R, Müller RH. Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives. Int J Pharm. 2010;399(1-2):129-139.

Nene S, Shah S, Rangaraj N, Mehra NK, Singh PK, Srivastava S. Lipid based nanocarriers: A novel paradigm for topical antifungal therapy. Journal of Drug Delivery Science and Technology. 2021 Apr 1;62:102397.

Alsarra IA, Alanazi FK, Ahmed SM, et al. Comparative study of itraconazole-cyclodextrin inclusion complex and its commercial product. Arch Pharm Res. 2010;33(7):1009-1017. doi:10.1007/s12272-010-0706-3.