Study of in vitro drug release and percutaneous absorption of fluconazole from topical dosage forms

AAPS PharmSciTech

Volumn 11, Issue 2, 2010, Pages 986-993

  Salerno, Claudia ^a   Carlucci, Adriana M ^a   Bregni, Carlos ^a  

^a UNIVERSIDAD DE BUENOS AIRES   (Argentina)

Author keywords

Fluconazole; In vitro drug permeation; Lipogel; Percutaneous absorption; Topical microemulsion

Indexed keywords

CELLULOSE DERIVATIVE; DIETHYLENE GLYCOL MONOETHYL ETHER; ESTER DERIVATIVE; FLUCONAZOLE; PROPYLENE GLYCOL; SOLVENT; ANTIFUNGAL AGENT; DRUG CARRIER; EMULSION;

ANTIFUNGAL ACTIVITY; ARTICLE; CANDIDA ALBICANS; CLINICAL EVALUATION; DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG PENETRATION; DRUG RELEASE; DRUG SOLUBILITY; HYDROGEL; IN VITRO STUDY; MICROEMULSION; MYCOSIS; NONHUMAN; PRIORITY JOURNAL; SKIN LEISHMANIASIS; SKIN PENETRATION; THICKNESS; ABSORPTION; ANIMAL; CHEMISTRY; DIFFUSION; DOSE RESPONSE; EMULSION; METABOLISM; PROCEDURES; SKIN; SKIN ABSORPTION; SWINE; TOPICAL DRUG ADMINISTRATION;

ABSORPTION; ADMINISTRATION, TOPICAL; ANIMALS; ANTIFUNGAL AGENTS; DIFFUSION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG CARRIERS; DRUG COMPOUNDING; EMULSIONS; FLUCONAZOLE; SKIN; SKIN ABSORPTION; SWINE;

EID: 77954834268     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-010-9457-1     Document Type: Article

References (38)

1. Dash AK, Elmquist WF. Analytical profiles of drug substances and excipients. Harry G Britain, Founding Florey Academic Press 2001; Vol 27 pp 70-113.
2. Martindale The Extra Pharmacopea. 31st Ed p. 404.
3. Mathy FX, Ntivunwa D, Verbeeck RK, Pre'at V. Fluconazole distribution in rat dermis following intravenous and topical application: a microdialysis study. J Pharm Sci. 2005;94(4):770-80.
4. Wildfeuer A, Faergemann J, Laufen H, Pfaff G, Zimmermann T, Seidl HP, et al. Bioavailability of fluconazole in the skin after oral medication. Mycoses. 1994;37(3-4):127-30.
5. Faergemann J. Pharmacokinetics of fluconazole in skin and nails. J Am Acad Dermatol. 1999;40(6 Pt 2): S14-20.
6. Klimke K, Schäfer-Korting M. Effect of keratin on the efficacy of fluconazole. Mycoses. 1997;40 Suppl 1:43-6.
7. Remington. The science and practice of pharmacy. A R Gennaro Editor. 2000. 20th Ed, p. 1552.
8. Lesher JL. Oral therapy of common superficial fungal infections of the skin. J Am Acad Dermatol. 1999;40: S31-4.
9. Reithinger R, Dujardin JC, Louzir H, Pirmez C, Alexander B, Brooker S. Cutaneous leishmaniasis. Lancet Infect Dis. 2007;7(9):581-96.
10. Laffitte E, Genton B, Panizzon RG. Cutaneous leishmaniasis caused by Leishmania tropica: treatment with oral fluconazole. Dermatology. 2005;210:249-51.
11. Baron S, Laube S, Raafat F, Moss C. Cutaneous leishmaniasis in a Kosovan child treated with oral fluconazole. Clin Exp Dermatol. 2004;29:546-7.
12. Alrajhi AA, Ibrahim EA, De Vol EB, Khairat M, Faris RM, Maguire JH. Fluconazole for the treatment of cutaneous leishmaniasis caused by Leishmania major. N Engl J Med. 2002;346:891-5.
13. Croft SL, Seifert K, Yardley V. Current scenario of drug development for leishmaniasis. Indian J Med Res. 2006;123:399-410.
14. Soto J, Toledo JT, Gutierrez P, Arboleda M, Nicholls RS, Padilla JR, et al. Treatment of cutaneous leishmaniasis with a topical antileishmanial drug (WR279396): phase 2 pilot study. Am J Trop Med Hyg. 2002;66:147-51.
15. Armijos RX, Weigel MM, Calvopina M, Mancheno M, Rodriguez R. Comparison of the effectiveness of two topical paromomycin treatments versus meglumine antimoniate for New World cutaneous leishmaniasis. Acta Trop. 2004;91:153-60.
16. Neal RA, Allen S, McCoy N, Olliaro P, Croft SL. The sensitivity of Leishmania species to aminosidine. J Antimicrob Chemother. 1995;35:577-84.
17. Grogl M, Schuster BG, Ellis WY, Berman JD. Successful topical treatment of murine cutaneous leishmaniasis with a combination of paromomycin and gentamicin. J Parasitol. 1999;85:354-9.
18. Soto J, Fuya P, Herrera R, Berman J. Topical Paromomycin/ methylbenzethonium chloride plus parenteral meglumine antimonate as treatment for American cutaneous leishmaniasis: controlled study. Clin Infect Dis. 1998;26:56-8.
19. Arana BA, Mendoza CE, Rizzo NR, Kroeger A. Randomized, controlled, double-blind trial of topical treatment of cutaneous leishmaniasis with paromomycin plus methylbenzethonium chloride ointment in Guatemala. Am J Trop Med Hyg. 2001;65(5):466-70.
20. Ayub AC, Gomes A D M, Lima M V C, Vianna-Soares CD, Ferreira L A M. Topical Delivery of fluconazole: in vitro skin penetretion and permeation using emulsions as dosage forms. Drug Dev Ind Pharm. 2007;33:273-80.
21. Al-Abdely HM, Graybill JR, Loebenberg D, Melby PC. Efficacy of the triazole SCH 56592 against Leishmania amazonensis and Leishmania donovani in experimental murine cutaneous and visceral leishmaniases. Antimicrob Agents Chemother. 1999;43:2910-4.
22. El Laithy HM, El-Shaboury K M F. The development of cutina lipogels and gel microemulsion for topical administration of fluconazole. AAPS PharmSciTech. 2002;3(4) 35:3-9.
23. Murdan S, Gregoriadis G, Florence AT. Novel sorbitan monostearate organogels. J Pharm Sci. 1999;88(6):608-14.
24. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev. 2002;54 Suppl 1:77-98.
25. Talegaonkar S, Azeem A, Ahmad FJ, Khar RK, Pathan SA, Khan ZI. Microemulsions: a novel approach to enhanced drug delivery. Recent patents on drug delivery and formulation. 2008;2(3):238-57.
26. Rozman B, Gasperlin M, Tinois-Tessoneaud E, Pirot F, Falson F. Simultaneous absorption of vitamins C and E from topical microemulsions using reconstructed human epidermis as a skin model. Eur J Pharm Biopharm. 2009;72(1):69-75.
27. Göger NG, Aboul-Enein HY. Quantitative determination of fluconazole in capsules and IV solutions by UV spectrophotometric methods. Anal lett. 2001;34(12):2089-98.
28. Thakker KD, Chwern WH. Development and validation of in vitro release test for semisolid dosage forms-Case study. Dissolution Technol. May 2003;10-15.
29. Zatz JL, Segers JD. Techniques for measuring in vitro release from semisolids. Dissolution Technol. February 1998;3-17.
30. FDA Guidance for Industry: SUPAC-SS Nonsterile Semisolid Dosage Forms. scale-up and postappraoval changes: chemistry, manufacturing, and controls; in vitro release testing and in vivo bioequivalence documentation. http://www.fda.gov/cder/guidance.htm. May 1997.
31. European Comission Scientific Committee On Consumer Products (Sccp). Opinion on basic criteria for the in vitro assessment of dermal absorption of cosmetic ingredients. http://ec.europa.eu/health/ph-risk/committees/04-sccp/ docs/sccp-s-03pdf. Updated March 2006.
32. European Commission Health & Consumer Protection Directorate General Sanco/222/2000 rev. 7 19 March 2004 Guidance Document on Dermal Absorption. http://www.efsa.europa.eu/cs/BlobServer/DocumentSet/SANCO-222-2000-rev7pdf? ssbinary=true
33. Alberti I, Kalia YN, Naik A, Bonny J, Guy RH. Effect of ethanol and isopropyl myristate on the availability of topical terbinafine in human stratum corneum, in vivo. Int J Pharm. 2001;219:11-9.
34. Yang W, Wiederhold NP, Williams RO. Drug delivery strategies for improved azole antifungal action. Expert Opin Drug Deliv. 2008;5(11):1199-216.
35. Thachrodi D, Panduranga Roo K. Transdermal absorption of nifedipine from microemulsiions of lipophilic skin penetration enhancers. Int J Pharm. 1994;111:235-40.
36. Harrison JE, Watkinson AC, Green DM, Hadgraft J, Brain K. The relative effect of Azone and Transcutol on permeant diffusivity and solubility in human stratum corneum. Pharm Res. 1996;13(4):542-6.
37. Trottet L, Merly C, Mirza M, Hadgraft J, Davis AF. Effect of finite doses of propylene glycol on enhancement of in vitro percutaneous permeation of loperamide hydrochloride. Int J Pharm. 2004;274:213-9.
38. Vidal Mussi S, Fernandes AP, Miranda Ferreira LA. Comparative study of the efficacy of formulations containing fluconazole or paromomycin for topical treatment of infections by Leishmania (Leishmania) major and Leishmania (Leishmania) amazonensis. Parasitology Res. 2007. doi:10.1007/s00436-006-0394-6 http://www.springerlink.com/content/b7002028121u8273/fulltext.html. (Pubitemid 46450539)