THERMOSENSITIVE MUCOADHESIVE PLURONIC-BASED IN-SITU VAGINAL GEL OF SERTACONAZOLE
Abstract
The purpose of this study is to develop thermosensitive mucoadhesive pluronics based in-situ gel of sertaconazole for treatment of vulvovaginal candidiasis, with the aim to prolong residence time in vagina, control drug release, and enhance efficacy as well as improvement in patient compliance. In-situ gel formulations of sertaconazole were formulated usingdifferent concentration of pluronic-127 alone and in combination with pluronic-68 as thermosensitive polymer and HPMC K4M also added as mucoadhesive polymer. The prepared formulations were evaluated for their gelation temperature, gelling capacity, rheological properties, mucoadhesive properties, microbiological studies and in vitro release studies. It was found that the viscosity and mucoadhesive force increased as theconcentration of pluronic-127 increasedand in vitro drug release decreased. In conclusion, HPMC K4M was able to improve the sustain release property of pluronics indicating that the combination of HPMC K4M and pluronics may find use in development of vaginal in-situgel drug delivery system with prolong local residence time and thus better clinical outcome.
Keywords:
Thermoreversible, mucoadhesion, sertaconazole, pluronics, in-situgel
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References
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2. Marodi L, Johnston RB.Invasive Candida species disease in infants and children: occurrence, risk factors, management, and innate host defense mechanisms.Curr Opin Pediatr 2007;19(6):693-97.
3. AgutJ, PalacinC, SalgadoJ, CasasE, SacristanA, Ortiz JA.Direct membranedamaging effect of Sertaconazole on Candidaalbicans as a mechanism of its fungicidal activity.ArzneimittelForsch 1992;42(5A):721-24.
4. Carrillo-Munoz AJ, Quindos G, Del Valle O, Santos P, Giusiano G, Guardia C et al.In vitroantifungal activity of sertaconazole nitrate against recent isolates of onychomycosis causative agents.J Chemother 2008;20(4):521-23.
5. Palacin C, Tarrago C, Ortiz JA.Sertaconazole: pharmacology of a gynecological antifungal agent.Int J Gynaecol Obstet 2000;71(1):37-46.
6. Albert C, Fernández JM, Sacristán A, OrtizJA.Physicochemical properties, analytical determinations and stability osertaconazole nitrate.Arzneimittel Forsch 1992;42:695-98.
7. Chang JY, Oh Y-K, Choi HG, Kim YB, Kim C-K.Rheological evaluation of thermo sensitive and mucoadhesive vaginal gels in physiological conditions.Int J Pharm2002;241:155-63.
8. Qiu Y, Park K. Environment-sensitive hydrogels for drug delivery.Adv Drug Deliv Rev2001;53:321-39.
9. Mauck CK, Katz D, Sandefer EP, Nasution MD, Henderson M, Digenis GA et al. Vaginal distribution of Replens and K-Y jelly using three imaging techniques.Contraception 2008;77:195-204.
10. Schmolka IR.Artificial skin 1, Preparation and properties of pluronic F-127 gels for treatment of burns.J Biomed Mater Res 1972;6(6):571-82.
11. Choi HG, Jung JH, Ryu JM, Yoon SJ, Oh YK, Kim CK. Development of in-situ gelling and mucoadhesive acetaminophen liquid suppository. Int J Pharm 1998;165(1):33-44.
12. Kwon KW,Park MJ, Hwang J, Char K.Effects of alcohol addition on gelation in aqueous solution of poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymer.Polymer Journal 2001;33(5):404-10.
13. Yu GE, Deng Y, Dalton S, Wang QG, Attwood D, Price C et al.Micellization and gelation of triblock copoly(oxyethylene oxypropylene oxyethylene) F127.J Chem Soc -Faraday Trans 1992;88(17):2537-44.
14. Gupta A, Garg S, Khar RK. Measurement of Bioadhesive Strength of Mucoadhesive Buccal Tablets: Design of an In vitro Assembly. Indian Drugs 1993;30(4):152-55.
15. Higuchi T. Mechanism of sustain action medication. Theoretical analysis of solid drugs dispersed in solid matrices.J Pharm Sci 1963;52(12):1145-49.
16. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983;15(1):25-35.
17. Nakamura F, Ohta R, Machida Y, Nagai T.In vitro and in vivo nasal mucoadhesion of some water-soluble polymers.Int J Pharm 1996;134(1):173-81.
18. Lu WY, Liu Y, Zhu YY, Wei G. Effect of carrageenan on poloxamer-based in-situ gel for vaginal use: Improved in vitro and in vivo sustained-release properties.Eur J Pharm Sci 2009;37(3-4):306-12.
19. Sultana Y, Aqil M, Ali A. Ion-Activated GelriteR-Based in-situ Ophthalmic Gels of Pefloxacin Mesylate: Comparison with Conventional Eye Drops.Drug Deliv2006;13(3):215-19.
20. Cabana A, Ait-Kadi A, Juhasz J. Study of the gelation process of polyethylene oxide-poly propylene oxide-polyethylene oxide copolymer (poloxamer 407) aqueous solutions. J Colloid Interface Sci 1997;190:307-12.
21. Jain N, Aswal V, Goyal P, Bahadur P. Micellar structure of an ethylene oxide-propylene oxide block copolymer: a small-angle neutron scattering study. J Phys Chem 1998;102: 8452-60.
22. Rashad AL, Toffler WL, Wolf N, Thoraburg K, Kirk EP, Ellis G et al. Vaginal P02 in healthy women and in women infected with Trichomoniasis vaginalis: Potential implications for metronidazole therapy. Am J Obestet Gynecol 1992;166:620-24.
23. Edsman K, Carlfors J, Petersson R. Rheological evaluation of poloxamer as an in-situ gel for ophthalmic use. Eur J Pharm Sci1998;6:105-12.
24. Maheshwari M, Paradker A, Yamamura S. Preparation and characterization of pluronic-colloidal silicone dioxide composite particles as a liquid crystal precursor. AAPS PharmSciTech 2006;7(4):E70-E76.
25. Charrueau C, Tuleu C, Astre V, Grossiord J-L, Chaumeil J-L. Poloxamer 407 as a thermogelling and adhesive polymer for rectal administration of short-chain fatty acids. Drug Dev Ind Pharm 2001;27:351-57.
26. Alexandridis P, Hatton TA. Poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) block copolymer surfactants in aqueous solutions and at interfaces: thermodynamic, structure, dynamic and modeling. Colloids Surf A Physicochem Eng Asp1995;96(1-2):1-46.
27. Mendenhall W, Sincich T, editors. A Second Course in Business Statistics: Regression Analysis. 3rd ed. San Francisco, CA: Dellen Publishing Co; 1989.p.141-226.
Published
30/04/2019
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How to Cite
[1]
A. P. P. Anita P. Patel, J. K. P. Jayvadan K. Patel, and B. M. Bharat Mishra, “THERMOSENSITIVE MUCOADHESIVE PLURONIC-BASED IN-SITU VAGINAL GEL OF SERTACONAZOLE ”, Int J Indig Herb Drug, pp. 11-21, Apr. 2019.
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Research Articles
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