Development of Miconazole nitrate loaded micellar gel for improved topical delivery

Manish Kumar

Abstract


The objective of the present investigation was to develop micellar gel of miconazole nitrate using amphiphilic block co-polymer pluronic F-127. Miconazole nitrate was entrapped into the micelles at critical micelle concentration by dialysis method and F2 was selected as best formulation based on a micelle size of 82.6 nm, entrapment efficiency of 96% and cumulative drug permeation amounting to 86 ± 0.31%. The spherical micelles as revealed by TEM were incorporated into gel. The gel with a pH of 6.16 and viscosity of 6942 ± 1.1cp displayed cumulative in vitro drug permeation 86.5 ± 0.01%. CLSM images upholded the assumption that the higher delivery observed for micellar gel in porcine skin was primarily due to penetration pathway. Thus the prepared micelles loaded gel represented higher permeability in the treatment of deep seated infection.

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References


J.E. Bennett, Antimicrobial Agents: Antifungal Agents The Pharmacological Basis of Therapeutics, J.G. Hardman, L.E. Limbird, and A. Goodman Gillman, Eds. (McGraw-Hill, New York, NY, 9th ed., 1175–1190 (2001).

Patel R., Patel H., Formulation and Evaluation of Carbopol Gel Containing Liposomes of ketoconazole. (Part-II) Baria, Int.J. Drug Delivery Tech, 1:42 – 45 (2009).

Tenjarla S., Preparation characterization, and Evaluation of Miconazole – Cyclodextrin Complexes for Improved Oral and Topical Delivery, J. Pharm. Sci. 87: 425–429 (1998).

Pedersen M., Formation and Antimycotic Effect of Cyclo dextrin Inclusion Complexes of Econazole and Miconazole, Int. J. Pharm, 90:247–254 (1993).

Zhang, L., Pornpattananangkul D.; Hu, C. M.J., Huang, C.-M., Development of Nanoparticles for Antimicrobial Drug Delivery. Curr. Med. Chem., 17: 585-594 (2010).

Piemi M.P., Positively and Negatively Charged Submicron Emulsions for Enhanced Topical Delivery of Antifungal Drugs, J. Control Release , 58:177–187 (1999).

Wehrle P., Wehrle D., Sequential Statistical Optimization of a Positively Charged Submicron Emulsion of Miconazole, Pharm. Dev. Technol., 97–111(1996).

Karine M., Robert G., Michael M., Colloidal Drug Delivery Systems – Recent Advances with Polymeric Micelles. , Chimia 62: 832-840 (2008).

Trimaille,T., Mondon K., Gurny R., Möller M., Novel polymeric micelles for hydrophobc drug delivery based on biodegradable poly (hexyl-substituted lactides,) Int. J. Pharm., 147-154 (2006).

Jain N.K., Controlled and Novel drug delivery, CBS publisher & distributors. 1st edition, pp. 381-383 (2004).

Nakamura H., Sano A., Matsuura K., Determination of critical micelles concentration of anionic surfactant by capillary electrophoresis using 2-Naphthalene methanol as a marker for micelles formation, Analytical sciences., 14:379 (1998).

Patist A., Bhagwat S.S., Penfield K.W., Aikens P., On the measurement of critical micelle concentration of pure and technical- grade nonionic surfactant, J. surfactant and detergent., 3:53-58 (2000).

Wu Y., Yang W.C., Hu J., Fu S., Chitosan nanoparticles as a novel delivery system for ammonium glycyrrhizinate. Int. J. Pharm., 295:235-245, (2005).

Barakat N.S., Optimization of physical characterization, skin permeation of naproxen from glycofurol- based topical gel, Asian J Pharm, 3:154-62, (2012).

Jiang W., Wang Y.D., Gan Q.. Preparation and Characterization of Copolymer Micelles Formed by Poly (ethylene glycol)-Polylactide Block Copolymers as Novel Drug Carriers., CJPE,6:289-295 (2006).

Sinnko J. Martin’s “Physical Pharmacy and Pharmaceutical Sciences,” 5th Ed., Lippincott Williams & Wilkins, Baltimore, 473 (2006).

Sezgin. Z, Yüksel N, Baykara T., Preparation and characterization of polymeric micelles for solubilization of poorly soluble anticancer drugs. Eur J Pharm Biopharm., 64:3,261-80 (2006).

Pople P. V., Singh K. K., Development and evaluation of topical formulation containing solid lipid nanoparticles of vitamin A., AAPS PharmSciTech, 7:4,E1-E7 (2006).

Pardeike J., Hommoss A., Muller R. H., Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. Int. J. Pharm., 366:170-184 (2009).

Nagarajan R., Solubilization of hydrocarbons and resulting aggregate shape transitions in aqueous solutions of Pluronic (PEO-PPO-PEO) block copolymers, Colloids Surfaces B Biointerfaces, 16:55–72 (1999).

Hurter P.N., Scheutjens J.M.H.M., Hatton H.A.,Molecular modeling of micelle formation and solubilization in block copolymer micelles. 1. A self-consistent mean-field lattice theory,Macromolecules., 5592–5601, (1993).

Hurter P.N., Scheutjens J.M.H.M., Hatton H.A.,Molecular modeling of micelle formation and solubilization in block copolymer micelles. 2. Lattice theory for monomers with internal degrees of freedom, Macromolecules, 26:5030–5040, (1993).

Alexandridis,P., Holzwarth J.F., Hatton T.A., Micellization of poly (ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymers in aqueous solutions: thermo- dynamics of copolymer association, Macromolecules.,27:2414–2425,1994.

Alexandridis P., Athanassiou V., Fukuda S., Hatton T.A., Surface activity of poly(ethylene oxide)-block-poly- (propylene oxide)-block-poly(ethylene oxide) copolymers, Langmuir.,10:2604–2612, (1994).

Kumar P., Mohan C., Kanamsrinivasan,, Uma Shankar M., Gulati M., Physiochemical Characterization and Release Rate Studies of Solid Dispersions of Ketoconazole with Pluronic F127 and PVP K-30., Iran J Pharm Res., 10:685–694, (2011).

Kim I.S., Kim S.H., Development of a polymeric nanoparticulate drug delivery system. In vitro characterization of nanoparticles based on sugar-containing conjugates. Int. J Pharm., 245: 67-73 (2002).

Gref R.., Minamitake Y., Peracchia M.T., Trubetskoy V., Torchilin, V., Langer R. Biodegradable long-circulating polymeric nanospheres., Science., 263:1600–603, (1994).

Jeong Y.I., Cheon, J.B., Kim S.H., Nah J.W., Lee Y.M., Sung Y.K., Akaike T., Cho C.S., Clonazepam release from core-shell type nanoparticles in vitro., J Controlled Release. , 51:169–178, (1998).

Torchilin V.P., Micellar nanocarriers: pharmaceutical perspectives. , Pharm Res, 24:1-16, (2007)


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