Fluconazole-Loaded Ibuprofen In Situ Gel-Based Oral Spray for Oropharyngeal Candidiasis Treatment

被引:5
作者
Khaing, Ei Mon [1 ]
Senarat, Setthapong [2 ,3 ]
Jitrangsri, Kritamorn [3 ,4 ]
Phaechamud, Thawatchai [1 ,3 ]
机构
[1] Silpakorn Univ, Fac Pharm, Dept Ind Pharm, Nakhon Pathom 73000, Thailand
[2] Ubon Ratchathani Univ, Fac Pharmaceut Sci, Div Pharmaceut Chem & Technol, Ubon Ratchathani 34190, Thailand
[3] Silpakorn Univ, Fac Pharm, Nat Bioact & Mat Hlth Promot & Drug Delivery Syst, Nakhon Pathom 73000, Thailand
[4] Walailak Univ, Sch Engn & Technol, Dept Chem Engn & Pharmaceut Chem, Nakhon Srithammarat 80160, Thailand
关键词
fluconazole; ibuprofen; in situ gel; oral spray; oropharyngeal candidiasis; METHYL-PYRROLIDONE NMP; NILE RED; ALBICANS; DOXYCYCLINE; FORMULATION; RELEASE; VITRO;
D O I
10.1208/s12249-024-02804-y
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Oral candidiasis is a fungal infection affecting the oral mucous membrane, and this research specifically addresses on a localized treatment through fluconazole-loaded ibuprofen in situ gel-based oral spray. The low solubility of ibuprofen is advantageous for forming a gel when exposed to an aqueous phase. The 1% w/w fluconazole-loaded in situ gel oral sprays were developed utilizing various concentrations of ibuprofen in N-methyl pyrrolidone. The prepared solutions underwent evaluation for viscosity, surface tension, contact angle, water tolerance, gel formation, interface interaction, drug permeation, and antimicrobial studies. The higher amount of ibuprofen reduced the surface tension and retarded solvent exchange. The use of 50% ibuprofen as a gelling agent demonstrated prolonged drug permeation for up to 24 h. The incorporation of Cremophor EL in the formulations resulted in increased drug permeation and exhibited effective inhibition against Candida albicans, Candida krusei, Candida lusitaniae, and Candida tropicalis. While the Cremophor EL-loaded formulation did not exhibit enhanced antifungal effects on agar media, its ability to facilitate the permeation of fluconazole and ibuprofen suggested potential efficacy in countering Candida invasion in the oral mucosa. Moreover, these formulations demonstrated significant thermal inhibition of protein denaturation in egg albumin, indicating anti-inflammatory properties. Consequently, the fluconazole-loaded ibuprofen in situ gel-based oral spray presents itself as a promising dosage form for oropharyngeal candidiasis treatment.
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页数:21
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