PREPARATION, CHARACTERIZATION, AND OPTIMIZATION OF MICROEMULSION FOR TOPICAL DELIVERY OF ITRACONAZOLE
Abstract
Microemulsions (ME) have been proved to increase the cutaneous absorption of both lipophilic and hydrophilic medicaments when compared to conventional vehicles (emulsions, pure oils, aqueous solutions). Hence the aim of present investigation is to prepare, characterize and optimize microemulsion of Itraconazole (ITZ). Itraconazole is an anti fungal agent, most widely used in the ringworm infection. It is classified as class III drug as per BCS classification. It indicates lower permeability through skin. Therefore objective of the research is to improve permeability of Itraconazole through skin. Microemulsion was prepared using eucalyptus oil, tween 20 and methanol as oil phase, surfactant and co-surfactant respectively. Pseudo ternary phase diagrams were constructed to find out optimum ratio of oil: Smix (surfactant: Co-Surfactant): water. A 32 full factorial design was applied for the optimization of prepared microemulsion. Microemulsion was evaluated for globule size, zeta potential, in-vitro diffusion study etc. Results of globule size measurements and zeta potential indicated ME7 had high stability then other formulation of microemulsion. For the optimization transdermal flux and %Q6 was selected as dependant variables. Results of optimization study also revealed ME 7 as optimized microemulsion for high permeability to the skin. Further ME7 was compared to marketed Itraconazole preparation (ITASPORE) and evaluated using similarity factor F2. Results of F2 value was not near to 100 indicated there is no similarity in diffusion profiles of ME7 and ITASPORE. Hence, indirectly it suggest there was increased in permeability of drug by preparing microemulsion.Keywords:
Microemulsion, Factorial Design, Eucalyptus oil, Tween 20, Desirability AnalysisDOI
https://doi.org/10.22270/jddt.v8i2.1731References
Alam S, Iqbal Z, Ali A, Khar R, Ahmad F, Akhter S, Microemulsion as a potential transdermal carrier for poorly water soluble antifungal drug itraconazole, Journal of Dispersion Science and Technology. 2009, 31(1), 84-94.
Fahima MH, Dalia SS, Mohamed KG, Mohamed N, and Aliaa I, Formulation, Characterization, and Clinical Evaluation of Microemulsion Containing Clotrimazole for Topical Delivery, AAPS PharmSciTech, Vol. 12, No. 3, 2011, 879-886.
Mandal S, Mandal SS, Research Paper Microemulsion Drug Delivery System: A Platform for Improving Dissolution Rate of Poorly Water Soluble Drug, Int J Pharm Sci Nanotech, 2011, 3(4), 1214-9.
Patel P, Monpara M, Mandal S, Patel N, KSR, Formulation and evaluation of microemulsion based gel of itraconazole, Pharmagene, 2013, 1(2), 32-6.
Hong JY, Kim J-K, Song YK, Park JS, Kim CK, A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption. Journal of controlled release, 2006, 110(2), 332-8.
Lee EA, Heo SK, Choi MJ, Chung SJ, Shim CK, Kim DD, Formulations of itraconazole for topical skin delivery, Journal of Pharmaceutical Investigation, 2007, 37(3), 167-71.
Rhee YS, Park CW, Nam TY, Shin YS, Chi SC, Park ES, Formulation of parenteral microemulsion containing itraconazole, Archives of pharmacal research, 2007, 30(1), 114-23.
Mukherjee S, Ray S, Thakur R, Design and evaluation of itraconazole loaded solid lipid nanoparticulate system for improving the antifungal therapy, Pak J Pharm Sci, 2009, 22(2), 131-8.
Silva JA, Bedor DC, Damasceno BP, Oliveira AG, Egito EST, Santana DP, Physicochemical characterization and development of a microemulsion system for transdermal use, Journal of Dispersion Science and Technology, 2009, 31(1), 1-8.
Jadhav K, Shetye S, Kadam V, Design and evaluation of microemulsion based drug delivery system, International journal of Advances in pharmaceutical Sciences, 2010, 1(2), 25-30.
Lee EA, Balakrishnan P, Song CK, Choi JH, Noh GY, Park CG, Microemulsion-based hydrogel formulation of itraconazole for topical delivery, Journal of pharmaceutical investigation, 2010, 40(5), 305-11.
Mandal S, Microemulsion drug delivery system: design and development for oral bioavailability enhancement of lovastatin, SA Pharmaceutical Journal. 2010, 78(3), 44-50.
Patel V, Kukadiya H, Mashru R, Surti N, Mandal S, Development of microemulsion for solubility enhancement of clopidogrel, Iranian Journal of Pharmaceutical Research, 2010, 327-34.
Guimarães GP, Reis MYdFA, Silva DTCd, Mendonça Junior FJB, Converti A, Pessoa Jr A, Antifungal activity of topical microemulsion containing a thiophene derivative, Brazilian Journal of Microbiology, 2014, 45(2), 545-50.
Kaewbanjong J, Amnuaikit T, Boonme P, Formulation and Characterization of Clotrimazole Microemulsions and Microemulsion-Based Gels. International Journal of Nanoscience, 2014, 13(04), 1440-005.
Maqsood I, Masood MI, Bashir S, Nawaz HMA, Anjum AA, Shahzadi I, Preparation and in vitro evaluation of Nystatin micro emulsion based gel, Pak J Pharm Sci, 2015, 28(5), 1587-93.
Kumar N, D-optimal experimental approach for designing topical microemulsion of itraconazole: Characterization and evaluation of antifungal efficacy against a standardized Tinea pedis infection model in Wistar rats, European Journal of Pharmaceutical Sciences, 2015, 67, 97-112.
Published
Abstract Display: 1682 
PDF Downloads: 1931 How to Cite
Issue
Section
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
How to Cite
.