DESIGN AND IN VITRO CHARACTERIZATION OF FLUTRIMAZOLE MICROSPHERES LOADED TOPICAL EMULGEL
DESIGN AND INVITRO CHARACTERIZATION OF FLUTRIMAZOLE MICROSPHERES LOADED TOPICAL EMULGEL
DOI:
https://doi.org/10.22159/ajpcr.2019.v12i9.34341Keywords:
Flutrimazole, Microsphere loaded topical gel, Controlled release, Fourier transform infraredAbstract
Objective: Flutrimazole is a topical antifungal agent which displays potent broad spectrum in vitro activity against dermatophytes, filamentous fungi, and yeasts. The purpose of the present study is to formulate and evaluate microspheres loaded topical gel containing flutrimazole as model drug microspheres were prepared using aqueous ionotropic gelation method.
Methods: Different polymers, the different drug to polymer(s) ratio(s) and other parameters were screened to study their effects on the properties of microspheres and to optimize each parameter. The controlled release emulgel was formulated by changing the polymer ratio. Fourier transform infrared study confirmed the purity of the drug, concede no interaction between the drug and excipients and analyze the parameters affecting the morphology and other characteristics of the resultant products employing scanning electron microscopy.
Results: Microspheres loaded topical gel has been shown that encapsulation and controlled release of flutrimazole could reduce the side effect while also reducing percutaneous absorption when administered to the skin. The microspheres obtained were subjected to the preformulation studies such as bulk density, tapped density, angle of repose, Carr’s index, and Hausner’s ratio the results obtained were within the limit. The microspheres were characterized by percentage yield, drug entrapment efficiency, and particle size analysis, then the optimized microspheres formulation were incorporated into the gel prepared with various polymer(s) ratio(s) and were evaluated by parameters such as visual inspection, pH measurement, spreadability studies, viscosity, and in vitro drug release using Franz diffusion cell.
Conclusion: The result of studies revealed that the optimized batch shows 97.24% release in 12 h and stable for around there. The microsphere loaded gel has advantages such as efficient absorption and more drug retention time.
Downloads
References
Rang HP, Dale MM, Ritter JM, Flower RJ. Anti-inflammatory and immunosuppressant drugs. In: Rang and Dale’s Pharmacology. 6th ed., Ch. 14. Edinburgh: Elsevier Publications; 2008. p. 226-45.
Chien YW. Concepts and system design for rate-controlled drug delivery. Novel Drug Delivery System. 2nd ed., Ch. 1. New York: Marcel Dekker, Inc.; 1992. p. l-42.
Das S, Das MK. Synthesis and characterisation of thiolated jackfruit seed starch as a colonic drug delivery carrier. Int J Appl Pharm 2019;11:53-62.
Rang HP, Dale MM, Ritter JM, Flower RJ. Anti-inflammatory and immunosuppressant drugs. In: Rang and Dale’s Pharmacology. 6th ed., Ch. 14. Edinburgh: Elsevier Publications; 2008. p. 226-45.
Chen X, Peng L, Gao J, Novel topical drug delivery systems and their potential use in scars treatment. Asian J Pharm Sci 2012;7:155-67.
Sigh RP, Parpani S, Narke R, Chavan R. Emulgel: Arecent approach for topical drug delivery system. Asian J Pharm Res Dev 2014;2:13-5.
Chien YW. Rate-controlled drug delivery systems. Indian J Pharm Sci 1988;4:63-5.
Gurulningappa S, Hallur MS. Anti-inflammatory assays of extracts of medicinal plants. Indian J Pharm Sci 2002;64:498-500.
Singh M, Mittal V. Formulation and evaluation of herbal gel containing ethanolic extract of Ipomoea fistulosa. Int J Sci Res 2014;3:25-9.
Dixit G, Misal G, Gulkari V, Upadhye K. Formulation and evaluation of polyherbal gel for anti-inflammatory activity. Int J Pharm Sci Res 2013;4:1186-91.
Gohel MC, Parikh RK, Amin AF, Surati AK. Preparation and formulation optimization of sugar crosslinking gelatin microspheres of diclofenac sodium. Indian J Pharm Sci 2005;67:575-81.
Rouge N, Buri P, Doelker E. Drug absorption sites in the gastrointestinal tract and dosage forms for site specific delivery. Int J Pharm 1996;136:117-39.
Lee TW, Robinson JR. Controlled release drug-delivery systems. In: Remington’s Pharmaceutical Sciences. 20th ed., Ch. 47. Pennsylvania: Mack Publishing Company; 2000. p. 903-29.
Cevc G, Vierl U. Nanotechnology and the transdermal route: A state of the art review and critical appraisal. J Control Release 2010;141:277-99.
Bhandke SE. Formulation and development of repaglinide microparticles by ionotropic gelation techniques. Indian J Pharm Educ Res 2006;
Desai S, Vidyasagar G, Shah V, Desai D. Preparation and in-vitro characterization of mucoadhesive microspheres of midazolam: Nose to brain administration. Asian J Pharm Clin Res 2011;4:100-2. Gavini E, Hegge AB, Rassu G, Sanna V, Testa C, Pirisino G, et al. Nasal administration of carbamazepine using chitosan microspheres: In vitro/ in vivo studies. Int J Pharm 2006;307:9-15.
Alexander A, Dwivedi S, Ajazuddin, Giri TK, Saraf S, Saraf S, et al. Approaches for breaking the barriers of drug permeation through transdermal drug delivery. J Control Release 2012;164:26-40.
Doddayya H, Srishailgouda SP, Reddy BT, Kumar P, Rajagopal HU, Shree MV. Formulation and evaluation of brain-targeted nasal selegiline hydrochloride microspheres. Int J Pharm Biomed Res 2014;5:61-8.
Kumar JR, Muralidharan S, Ramasamy S. Microsponges enriched Gel (Megs): Anovel strategy for opthalmic drug delivery system containing ketotifen. J Pharm Res 2013;5:97-102.
Chadawar V, Shaji J. Microsponge delivery system. Curr Drug Deliv 2007;4:123-9.
Rashmi M. Topical Gel: A Review; 2008. Available from: http://www. pharmainfo.com.
Okur NU, Apaydın 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;416:136-44.
Sharma S. Topical preparations are used for the localized effects at the site of their application by virtue of drug penetration into the underlying layers of skin or mucous membranes. Pharm Rev 2008;6:1-10.
Zhao L, Wang Y, Zhai Y, Wang Z, Liu J, Zhai G, et al. Ropivacaine loaded microemulsion and microemulsion-based gel for transdermal delivery: Preparation, optimization, and evaluation. Int J Pharm 2014;477:47-56. Elmowafy M, et al. ???. Beni-Suef Univ J Basic Appl Sci 2017;6:184-91.
Kasting GB. Kinetics of finite dose absorption through skin 1. Vanillylnonanamide. J Pharm Sci 2001;90:202-12.
El-Hadidy GN, Ibrahim HK, Mohamed MI, El-Milligi MF. Microemulsions as vehicles for topical administration of voriconazole: Formulation and in vitro evaluation. Drug Dev Ind Pharm 2012;38:64-72.
Jyothi D, Koland M. Formulation and evaluation of an herbal anti-inflammatory gel containing Trigonella foenum-greacum seed extract. Int J Pharm Pharm Sci 2016;8:41-4.
Bhaskar K, Anbu J, Ravichandiran V, Venkateswarlu V, Rao YM. Lipid nanoparticles for transdermal delivery of flurbiprofen: Formulation, in vitro, ex vivo and in vivo studies. Lipids Health Dis 2009;8:6.
Mohamed MI. Topical emulsion gel composition comprising diclofenac sodium. Am Assoc Pharm Sci 2004;6:1-7.
Zuckerman JM. Macrolides and ketolides: Azithromycin, clarithromycin, telithromycin. Infect Dis Clin North Am 2004;18:621-49, 11.
Murthy SN, Hiremath SR. Physical and chemical permeation enhancers in transdermal delivery of terbutaline sulphate. AAPS PharmSciTech 2001;2:E-TN1.
Mohamed MI. Optimization of chlorphenesin emulgel formulation. AAPS J 2004;6:e26.
Ansel HC, Allen LV Jr., Popovich NG. Pharmaceutical Dosage Forms and Drug Delivery Systems. 7th ed. New York: Lippincott Williams and Wilkins; 1999.
Bonacucina G, Cespi M, Palmieri GF. Characterization and stability of emulsion gels based on acrylamide/sodium acryloyldimethyl taurate copolymer. AAPS PharmSciTech 2009;10:368-75.
Kumar L, Verma R. In vitro evaluation of topical gelprepared using natural polymer. Int J Drug Deliv 2010;2:58-63.
Gupta A, Mishra AK, Singh AK, Gupta V, Bansal P. Formulation and evaluation of topical gel of diclofenac sodiumusing different polymers. Drug Invent Today 2010;2:250-25.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.
