Abstract | OBJECTIVES: METHODS: Aqueous thermosensitive formulations containing 1% of econazole nitrate and poloxamer 407 and/or 188 were prepared and their rheological, mechanical and drug-release properties determined at 20 ± 0.1°C and/or 37 ± 0.1°C. Based on their biologically suitable thermorheological properties, formulations containing the mixtures of poloxamer 407 and 188 in ratios of 15:15 (F1), 15:20 (F2) and 20:10 (F3) were chosen for comprehensive analysis. KEY FINDINGS: Formulations based on F3 exhibited typical gel-type mechanical spectra (G' > G″) at 37°C whereas formulations based on F1 and F2 exhibited properties akin to weakly cross-linked gels. Texture profile analysis demonstrated that F3 showed the highest cohesiveness, adhesiveness, hardness and compressibility. No statistically significant differences (P > 0.5) were observed in the release of econazole nitrate from the formulations at pH 4.5, which in all cases followed anomalous diffusion kinetics. Formulations based on 20% poloxamer 407:10% poloxamer 188 were chosen for in-vivo studies and were shown to be effective for the treatment of the vaginal candidiasis. Histopathologic evaluation also supported the effectiveness of the thermosensitive formulation administered intravaginally. CONCLUSION: By careful engineering of the rheological properties, in-situ thermosensitive gel formulations of econazole nitrate were prepared and were shown to be efficacious in the treatment of vaginal candidiasis.
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Authors | Esra Baloglu, Sinem Yaprak Karavana, Zeynep Ay Senyigit, Süleyha Hilmioglu-Polat, Dilek Yesim Metin, Osman Zekioglu, Tamer Guneri, David S Jones |
Journal | The Journal of pharmacy and pharmacology
(J Pharm Pharmacol)
Vol. 63
Issue 10
Pg. 1274-82
(Oct 2011)
ISSN: 2042-7158 [Electronic] England |
PMID | 21899542
(Publication Type: Evaluation Study, Journal Article, Research Support, Non-U.S. Gov't)
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Copyright | © 2011 The Authors. JPP © 2011 Royal Pharmaceutical Society. |
Chemical References |
- Dosage Forms
- Gels
- Poloxamer
- Econazole
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Topics |
- Animals
- Candida
(isolation & purification)
- Candidiasis
(drug therapy, microbiology)
- Chemistry, Pharmaceutical
- Dosage Forms
- Econazole
(administration & dosage, pharmacology, therapeutic use)
- Female
- Gels
- Poloxamer
- Rats, Wistar
- Rheology
- Vagina
(drug effects, microbiology, pathology)
- Vaginitis
(drug therapy, microbiology)
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