Mucoadhesive, thermosensitive, prolonged-release vaginal gel for clotrimazole: β-cyclodextrin complex

AAPS PharmSciTech

Volumn 7, Issue 2, 2006, Pages

  Bilensoy, Erem ^a   Rouf, M Abdur ^a   Vural, Imran ^a   Şen, Murat ^a   Hincal, A Atilla ^a  

^a HACETTEPE UNIVERSITY   (Turkey)

Author keywords

Clotrimazole; Cyclodextrin; Mucoadhesive; Prolonged release; Thermosensitive; Vaginal

Indexed keywords

BETA CYCLODEXTRIN; CARBOPOL 934; CITRIC ACID; CLOTRIMAZOLE; HYDROXYPROPYLMETHYLCELLULOSE; KLEPTOSE; POLOXAMER; AGENTS USED INTRAVAGINALLY; ANTIFUNGAL AGENT; BETA CYCLODEXTRIN DERIVATIVE; TISSUE ADHESIVE;

ARTICLE; COMPLEX FORMATION; CONTROLLED RELEASE FORMULATION; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG SOLUBILITY; DRUG STABILITY; DRUG STRUCTURE; GEL; GELATION; HEAT SENSITIVITY; IN VITRO STUDY; INFRARED SPECTROPHOTOMETRY; MINIMUM INHIBITORY CONCENTRATION; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PH; PRECIPITATION; PROTON NUCLEAR MAGNETIC RESONANCE; SCANNING ELECTRON MICROSCOPY; CHEMISTRY; DELAYED RELEASE FORMULATION; DIFFUSION; DRUG COMBINATION; DRUG SCREENING; FEMALE; HUMAN; MATERIALS TESTING; MUCOSA; TEMPERATURE; VAGINA; VAGINITIS;

ANTIFUNGAL AGENTS; BETA-CYCLODEXTRINS; CLOTRIMAZOLE; DELAYED-ACTION PREPARATIONS; DIFFUSION; DRUG COMBINATIONS; DRUG EVALUATION, PRECLINICAL; FEMALE; HUMANS; MATERIALS TESTING; MUCOUS MEMBRANE; TEMPERATURE; TISSUE ADHESIVES; VAGINA; VAGINAL CREAMS, FOAMS, AND JELLIES; VAGINITIS;

EID: 84869298534     PISSN: 15309932     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/pt070238     Document Type: Article

References (30)

1. Ritter W, Patzschke K, Krause U, Stettendorf S. Pharmacokinetic fundamentals of vaginal treatment with clotrimazole. Chemotherapy. 1982;28:37-42.
2. Sawyer PR, Brogden RN, Pinder RM, Speight TM, Avery GS. Clotrimazole: a review of its antifungal activity and therapeutic efficacy. Drugs. 1975;9:424-447.
3. Deshpande AA, Rhodes CT, Danish M. Intravaginal drug delivery. Drug Dev Ind Pharm. 1992;18:1225-1279.
4. Wolfsson AD. Intravaginal drug delivery technologies. In: Rathbone M, ed. Modified-Release Drug Delivery Technology. New York, NY. Marcel Dekker; 2002:759-774.
5. Hardy E, Jimenes AL, de Padua KS, Zanewald LJD. Women's preferences for vaginal antimicrobial contraceptives, III: choice of a formulation, applicator and packaging. Contraception. 1998; 58:245-249.
6. Ceschel GC, Maffei P, Lombardi Borgia S, Ronchi C, Rossi S. Development of a mucoadhesive dosage form for vaginal administration. Drug Dev Ind Pharm. 2001;27:541-547.
7. Chang JY, Oh YK, Choi H, Kim YB, Kim CK. Rheological evaluation of thermosensitive and mucoadhesive vaginal gels in physiological conditions. Int J Pharm. 2002;241:155-163.
8. Chang JY, Oh YK, Kong HS, et al. Prolonged antifungal effects of clotrimazole-containing mucoadhesive thermosensitive gels in vaginitis. J Control Release. 2002;82:39-50.
9. Chu JS, Amidon GL, Weiner ND, Goldberg AH. Mixture experimental design in the development of a mucoadhesive gel formulation. Pharm Res. 1991;8:1401-1407.
10. Park H, Robinson JR. Physicochemical properties of water insoluble polymers important to mucin/epithelial adhesion. J Control Release. 1985;2:47-57.
11. Veyries ML, Couarrazze G, Geiger S, et al. Controlled release of vancomycin from poloxamer 407 gels. Int J Pharm. 1999;192:183-193.
12. Desai SD, Blanchard J. Pluronic F127-based ocular delivery system containing biodegradable polyisobutylcyanoacrylate nanocapsules of pilocarpine. Drug Deliv. 2000;7:201-207.
13. Bochot A, Fattal E, Grossiord JL, Puisieux F, Couvreur P. Characterization of a new ocular delivery system based on a dispersion of liposomes in a thermosensitive gel. Int J Pharm. 1998; 162:119 -127.
14. Kim EY, Gao ZG, Park JS, Li H, Han K. rhEGF/HP-β-CD complex in poloxamer gel for ophthalmic delivery. Int J Pharm. 2002; 233:159-167.
15. Thompson DO. Cyclodextrins - enabling excipients: their present and future use in pharmaceuticals. Crit Rev Ther Drug Carrier Syst. 1997;14:1-104.
16. Loftsson T, Brewster ME. Pharmaceutical applications of cyclodextrins, I: drug solubilization and stabilization. J Pharm Sci. 1996;85:1017-1025.
17. Challa R, Alka A, Javed A, Khar RK. Cyclodextrins in drug delivery: an updated review. AAPS PharmSciTech. 2005;6:E329-E357.
18. Hedges AR. Industrial applications of cyclodextrins. Chem Rev. 1998;98:2035-2044.
19. 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;165:33-44.
20. Miyazaki S, Nakamura T, Takada, M. Thermo-sensitive sol-gel transition of Pluronic F-127. Yakuzaigaku. 1991;51:36-43.
21. Schneider HJ, Hacket F, Rüdiger V, Ikeda H. NMR studies of cyclodextrins and cyclodextrin complexes. Chem Rev. 1998; 98:1755-1785.
22. 1H NMR studies. J Pharm Pharmacol. 1997;49:944-948.
23. Djedaini F, Perly B. Anthraquinone sulphonate as a general-purpose shift reagent for the NMR analysis of cyclodextrins. Magnet Res Chem. 1990;28:372-374.
24. Djedaini F, Perly B. Nuclear magnetic resonance investigation of the stoichiometries in β-cyclodextrin:steroid inclusion complexes. J Pharm Sci. 1991;80:1157-1161.
25. Van Doome, H, Bosch EH, Lerk CF. Formation and antimicrobial activity of complexes of beta-cyclodextrin and some antimycotic imidazole derivatives. Pharm Weekbl Sci. 1988;10:80-85.
26. Blanco-Fuente H, Esteban-Fernandez B, Blanco-Mendez J, Otero-Espinar FJ. Use of β-cyclodextrins to prevent modifications of the properties of carbopol hydrogels due to carbopol-drug interactions. Chem Pharm Bull (Tokyo). 2002;50:40-46.
27. Boulmedarat L, Grossiord JL, Fattal E, Bochot A. Influence of methyl β-cyclodextrin and liposomes on rheological properties of Carbopol®974 NF gels. Int J Pharm. 2003;254:59-64.
28. Anderson BC, Pandit NK, Mallapragada S. Understanding drug release from poly(ethylene oxide)-b-poly(propylene oxide)-b-poly (ethylene oxide) gels. J Control Release. 2001;70:157-167.
29. Stella VJ, Rao VM, Zannou EE, Zia V. Mechanisms of drug release from cyclodextrin complexes. Adv Drug Deliv Rev. 1999;36:3-16.
30. Memisoglu E, Bochot A, Ozalp M, Sen M, Duchene D, Hincal AA. Direct formation of nanospheres from amphiphilic β-cyclodextrin inclusion complexes. Pharm Res. 2003;20:117-125.