Development and Evaluation of New Microemulsion-Based Hydrogel Formulations for Topical Delivery of Fluconazole

AAPS PharmSciTech

Volumn 16, Issue 4, 2015, Pages 889-904

  Coneac, Georgeta ^a   Vlaia, Vicenţiu ^a   Olariu, Ioana ^a   Muţ, Ana Maria ^a   Anghel, Dan Florin ^b   Ilie, Cornelia ^b   Popoiu, Călin ^a   Lupuleasa, Dumitru ^c   Vlaia, Lavinia ^a  

^a VICTOR BABES UNIVERSITY OF MEDICINE AND PHARMACY   (Romania)

^b INSTITUTE OF PHYSICAL CHEMISTRY   (Romania)

^c CAROL DAVILA UNIVERSITY OF MEDICINE AND PHARMACY   (Romania)

Author keywords

fluconazole; in vitro skin permeation; microemulsion; microemulsion loaded hydrogel; topical

Indexed keywords

CARBOMER; DIETHYLENE GLYCOL MONOETHYL ETHER; FLUCONAZOLE; KETOCONAZOLE; METHYL PARABEN; PROPYL PARABEN; PROPYLENE GLYCOL; WATER; ANTIFUNGAL AGENT; EMULSION; HYDROGEL;

ANTIFUNGAL ACTIVITY; ARTICLE; CANDIDA ALBICANS; CONTROLLED STUDY; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; FLOW KINETICS; HYDROGEL; IN VITRO STUDY; MICROEMULSION; NONHUMAN; PH; PRIORITY JOURNAL; VISCOSITY; ZETA POTENTIAL; ANIMAL; EMULSION; PIG; TOPICAL DRUG ADMINISTRATION;

ADMINISTRATION, TOPICAL; ANIMALS; ANTIFUNGAL AGENTS; EMULSIONS; FLUCONAZOLE; HYDROGELS; IN VITRO TECHNIQUES; SWINE;

EID: 84937815637     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-014-0275-8     Document Type: Article

References (58)

1. Lawrence MJ, Rees GD. Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev. 2012;64(Suppl):175–93.
2. Tenjarla S. Microemulsions: an overview and pharmaceutical applications. Crit Rev Ther Drug Carrier Syst. 1999;16(5):461–521.
3. Eccleston GM. Emulsions and microemulsions. In: Swarbrick J, editor. Encyclopedia of pharmaceutical technology, vol. 3. 3rd ed. New York: Informa Healthcare; 2007. p. 1548–65.
4. Lawrence MJ, Warisnoicharoen W. Recent advances in microemulsions as drug delivery vehicles. In: Torchilin VP, editor. Nanoparticulates as drug carriers. London: Imperial College Press; 2006. p. 125–39. 148–154.
5. Heuschkel S, Goebel A, Neubert RHH. Microemulsions—modern colloidal carrier for dermal and transdermal drug delivery. J Pharm Sci. 2008;97(2):603–31.
6. Kogan A, Garti N. Microemulsions as transdermal drug delivery vehicles. Adv Colloid Interf Sci. 2006;123–126:369–85.
7. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv Drug Deliv Rev. 2002;54 Suppl 1:S77–98.
8. Kreilgaard M, Pedersen EJ, Jaroszewski JW. NMR characterisation and transdermal drug delivery potential of microemulsion systems. J Control Release. 2000;69(3):421–33.
9. El Maghraby GM. Transdermal delivery of hydrocortisone from eucalyptus oil microemulsion: effects of cosurfactants. Int J Pharm. 2008;355(1–2):285–92.
10. Park ES, Cui Y, Yun BJ, Ko IJ, Chi SC. Transdermal delivery of piroxicam using microemulsions. Arch Pharm Res. 2005;28(2):243–8.
11. Yuan Y, Li S, Mo F, Zhong D. Investigation of microemulsion system for transdermal delivery of meloxicam. Int J Pharm. 2006;321:117–23.
12. Zhao X, Liu JP, Zhang X, Li Y. Enhancement of transdermal delivery of theophylline using microemulsion vehicle. Int J Pharm. 2006;327(1–2):58–64.
13. Shah RR, Magdum CS, Wadkar KA, Naikwade NS. Fluconazole topical microemulsion: preparation and evaluation. Res J Pharm Technol. 2009;2(2):353–7.
14. Kweon JH, Chi SC, Park ES. Transdermal delivery of diclofenac using microemulsions. Arch Pharm Res. 2004;27(3):351–6.
15. Chen HB, Chang XL, Weng T, Zhao X, Gao Z, Yang Y, et al. A study of microemulsion systems for transdermal delivery of triptolide. J Control Release. 2004;98(3):427–36.
16. Žabka M, Hukel’ová M, Čuchorová M, Starýchová L. Effect of microemulsion on liberation of indomethacin from hydrophilic and lipophilic gel. Acta Fac Pharm Univ Comen. 2012;LIX:81–8.
17. Desai K-GH. Enhanced skin permeation of rofecoxib using topical microemulsion gel. Drug Dev Res. 2004;63(1):33–40.
18. Hathout RM, Elshafeey AH. Development and characterization of colloidal soft nano-carriers for transdermal delivery and bioavailability enhancement of an angiotensin II receptor blocker. Eur J Pharm Biopharm. 2012;82(2):230–40.
19. Abdulkarim MF, Abdullah GZ, Chitneni M, Salman IM, Ameer OZ, Yam MF, et al. Topical piroxicam in vitro release and in vivo anti-inflammatory and analgesic effects from palm oil esters-based nanocream. Int J Nanomedicine. 2010;5:915–24.
20. Sintov AC, Shapiro L. New microemulsion vehicle facilitates percutaneous penetration in vitro and cutaneous drug bioavailability in vivo. J Control Release. 2004;95(2):173–83.
21. Zhang J, Michniak-Kohn B. Investigation of microemulsion microstructures and their relationship to transdermal permeation of model drugs: ketoprofen, lidocaine, and caffeine. Int J Pharm. 2011;421(1):34–44.
22. Sintov AC, Brandys-Sitton R. Facilitated skin penetration of lidocaine: combination of a short-term iontophoresis and microemulsion formulation. Int J Pharm. 2006;316(1–2):58–67.
23. Zhu W, Yu A, Wang W, Dong R, Wu J, Zhai G. Formulation design of microemulsion for dermal delivery of penciclovir. Int J Pharm. 2008;360(1–2):184–90.
24. Ustündağ Okur N, Apaydin S, Karabay Yavaşoğlu NÜ, Yavaşoğlu A, Karasulu HY. Evaluation of skin permeation and anti-inflammatory and analgesic effects of new naproxen microemulsion formulations. Int J Pharm. 2011;416(1):136–44.
25. Aggarwal N, Goindi S, Khurana R. Formulation, characterization and evaluation of an optimized microemulsion formulation of griseofulvin for topical application. Colloids Surf B: Biointerfaces. 2013;105:158–66.
26. Araújo LMPC, Thomazine JA, Lopez RFV. Development of microemulsions to topically deliver 5-aminolevulinic acid in photodynamic therapy. Eur J Pharm Biopharm. 2010;75(1):48–55.
27. Zadeh BSM, Moghimi H, Santos P, Hadgraft J, Lane ME, Rahim F. Formulation of microemulsion system for improvement of nitrofurazone permeation through silicon membrane as burn wound imitating coverage. Int J Pharmacol. 2010;6(3):264–70.
28. Tsai YH, Lee KF, Huang YB, Huang CT, Wu PC. In vitro permeation and in vivo whitening effect of topical hesperetin microemulsion delivery system. Int J Pharm. 2010;388:257–62.
29. Djordjevic L, Primorac M, Stupar M. In vitro release of diclofenac diethylamine from caprylocaproyl macrogolglycerides based microemulsions. Int J Pharm. 2005;296:73–9.
30. Yuan JS, Ansari M, Samaan M, Acosta EJ. Linker-based lecithin microemulsions for transdermal delivery of lidocaine. Int J Pharm. 2008;349:130–43.
31. Tian Q, Ren F, Xu Z, Xie Y, Zhang S. Preparation of high solubilizable microemulsion of naproxen and its solubilization mechanism. Int J Pharm. 2012;426:202–10.
32. Pathan IB, Setty CM. Nanoemulsion system for transdermal delivery of tamoxifen citrate: design, characterization, effect of penetration enhancers and in vivo studies. Dig J Nanomater Biosci. 2012;7(4):1373–87.
33. Gennaro AR, editor. Remington. The science and practice of pharmacy. 21st ed. London: Pharmaceutical Press; 2005. p. 1671.
34. Sweetman SC, editor. Martindale: the complete drug reference. 36th ed. London: Pharmaceutical Press; 2009. p. 404.
35. Dash AK, Elmquist WF. Fluconazole. In: Britain HG, editor. Analytical profiles of drug substances and excipients, vol. 27. London: Academic; 2001. p. 70–113.
36. 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.
37. Faergemann J. Pharmacokinetics of fluconazole in skin and nails. J Am Acad Dermatol. 1999;40(6 Pt 2):S14–20.
38. 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.
39. Jadhav KR, Shetye SL, Kadam VJ. Design and evaluation of microemulsion based drug delivery system. Int J Adv Pharm Sci. 2010;1:156–66.
40. Rohit RS, Chandrakant SM, Kiran AW, Nilofar SN. Fluconazole topical microemulsion: preparation and evaluation. Res J Pharm Technol. 2009;2(2):353–7.
41. Mitkari BV, Korde SA, Mahadik KR, Kokare CR. Formulation and evaluation of topical liposomal gel for fluconazole. Indian J Pharm Educ Res. 2010;44(4):324–33.
42. Lalit SK, Panwar AS, Darwhekar G, Jain DK. Formulation and evaluation of fluconazole amphiphilogel. Der Pharm Lett. 2011;3(5):125–31.
43. Bachhav YG, Patravale VB. Microemulsion based vaginal gel of fluconazole: formulation, in vitro and in vivo evaluation. Int J Pharm. 2009;365:175–9.
44. Abdel-Mottaleb MMA, Mortada ND, Elshamy AA, Awad GAS. Preparation and evaluation of fluconazole gels. Egypt J Biomed Sci. 2007;23(1):266–86.
45. Salerno C, Carlucci AM, Bregni C. Study of in vitro drug release and percutaneous absorption of fluconazole from topical dosage forms. AAPS PharmSciTech. 2010;11(2):986–93.
46. Zhao SS, Du Q, Cao D-Y. Preparation of liposomal fluconazole gel and in vitro transdermal delivery. J Chin Pharm Sci. 2007;16:116–8.
47. El-Laithy HM, El-Shaboury KMF. The development of Cutina lipogels and gel microemulsion for topical administration of fluconazole. AAPS PharmSciTech. 2002;3(4):77–85.
48. Azeem A, Rizwa M, Ahmad FJ, Iqbal Z, Khar RK. Nanoemulsion components screening and selection: a technical note. AAPS PharmSciTech. 2009;10(1):69–77.
49. Shakeel F, Ramadan W. Transdermal delivery of anticancer drug caffeine from water-in-oil nanoemulsions. Colloids Surf B Biointerfaces. 2010;75:356–62.
50. Schmidts T, Nocker P, Lavi G, Kuhlmann J, Czermak P, Runkel F. Development of an alternative, time and cost saving method of creating pseudoternary diagrams using the example of microemulsion. Colloids Surf A. 2009;340:187–92.
51. Siepmann J, Peppas NA. Higuchi equation: derivation, applications, use and misuse. Int J Pharm. 2011;418(1):6–12.
52. Ghosh PK, Majithiya RJ, Umrethia ML, Murthy RSR. Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability. AAPS PharmSci Tech. 2006;10(1):69–77.
53. European Directorate for the Quality of Medicines & HealthCare. European pharmacopoeia. 7th ed. Strasbourg: Council of Europe; 2010. p. 674.
54. Sirotti C, Coceani N, Colombo I, Lapasin R, Grassi M. Modeling of drug release from microemulsions: a peculiar case. J Membr Sci. 2002;204:401–12.
55. Godin B, Touitou E. Transdermal skin delivery: predictions for humans from in vivo, ex vivo and animal models. Adv Drug Deliv Rev. 2007;59(11):1152–61.
56. Simon GA, Maibach HI. The pig as an experimental animal model of percutaneous permeation in man: qualitative and quantitative observations—an overview. Skin Pharmacol Appl Ski Physiol. 2000;13(5):229–34.
57. Barbero AM, Frasch HF. Pig and guinea pig skin as surrogates for human in vitro penetration studies: a quantitative review. Toxicol In Vitro. 2009;23(1):1–13.
58. Schmook FP, Meingassner JG, Billich A. Comparison of human skin or epidermis models with human and animal skin in in-vitro percutaneous absorption. Int J Pharm. 2001;215(1–2):51–60.