The main aim and objective of this research was to develop and evaluate Fluconazole loaded nanosponges and formulate them as suitable topical gels for delivering the drug systemically after topical application. Fluconazole (FLZ) is a potent triazole anti fungistatic drug; topical administration of novel Fluconazole resulted in systemic absorption, for improved therapeutic effect and better dispersibility as compared to conventional topical formulation. Fluconazole (FLZ) nanosponges prepared by using emulsion solvent diffusion method to improve topical permeation. Nanosponges were formulated successfully using ethyl cellulose and Eudragit RS 100 as polymer, polyvinyl alcohol as the surfactant, and dichloromethane as solvent. The optimised batch of fluconazole loaded nanosponges used to prepare topical gel using different concentrations of carbopol gel. The prepared nanosponges were evaluated by various tests like production yield, drug entrapment efficiency, FTIR, particle size, zeta potential, SEM study. The entrapment efficiency and production yield were excellent. Based on the entrapment efficiency and production yield,out of ten formulations batches of nanosponges was evaluated and from that batch F3 was optimised.Optimized batch F3 containing FLZ and EC in the ratio of 1:3 showed optimum physicochemical and release characteristics. The optimised batch F3 of ethyl cellulose shows highest entrapment efficiency as 97.97% and production yield as 93.85% resp. A complex Fourier transform infrared (FTIR) study examines the formation in the nanosponge structure. The nanosponges had particle size in the range of 234.95 to 374.26 nm. The Zeta Potential was strong enough to produce stable formulations. The zeta potential of optimised batch nanosponges was found to be 25.05. SEM analysis of optimized batch F3 confirms that nanosponges were spherical in size with a porous and smooth surface. The formulated fluconazole topical gel were characterized for pH, actual drug content, viscosity, spreadability, In -Vitro drug release study. The in -vitro drug release showed maximum drug release of topical gel i.e. 88.34% in 8 hours. The present study demonstrates that, an antifungal drug Fluconazole is formulated in the form of nanosponges topical gel for the antifungal activity and can be best suitable approach in novel drug delivery system than conventional gel. Hence it is concluded that above topical gel formulation of fluconazole loaded nanosponges can be used in treatment of fungal infection.
机构:
Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, BrazilUniv Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
de Vargas, Bethania Andrade
Bidone, Juliana
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Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, BrazilUniv Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
Bidone, Juliana
Oliveira, Laura Karsburg
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Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, BrazilUniv Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
Oliveira, Laura Karsburg
Koester, Leticia Scherer
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Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, BrazilUniv Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
Koester, Leticia Scherer
Bassani, Valquiria Linck
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Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, BrazilUniv Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
Bassani, Valquiria Linck
Teixeira, Helder Ferreira
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Univ Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, BrazilUniv Fed Rio Grande do Sul, Fac Farm, Programa Posgrad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
机构:
Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Yu, Hongmei
Zhang, Baoxi
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Zhang, Baoxi
Liu, Meiju
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Liu, Meiju
Xing, Wenhui
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Xing, Wenhui
Hu, Kun
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Hu, Kun
Yang, Shiying
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Yang, Shiying
He, Guorong
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Chinese Acad Med Sci, Inst Materia Med, Beijing City Key Lab Drug Target Identificat & Dru, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
He, Guorong
Gong, Ningbo
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Gong, Ningbo
Du, Guanhua
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Chinese Acad Med Sci, Inst Materia Med, Beijing City Key Lab Drug Target Identificat & Dru, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
Du, Guanhua
Lu, Yang
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Chinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R ChinaChinese Acad Med Sci, Peking Union Med Coll, Inst Materia Med, Beijing Key Lab Polymorph Drugs, Beijing 100050, Peoples R China
机构:
Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Ashtiani, Sahar Yazdani
Nasrollahi, Saman Ahmad
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Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Nasrollahi, Saman Ahmad
Naeimifar, Atefeh
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Univ Tehran Med Sci, Sch Pharm, Dept Pharmaceut, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Naeimifar, Atefeh
Kashani, Aubid Nassiri
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Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Kashani, Aubid Nassiri
Samadi, Aniseh
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Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Samadi, Aniseh
Yadangi, Somayeh
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Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Yadangi, Somayeh
Aboutaleb, Ehsan
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Guilan Univ Med Sci, Sch Pharm, Dept Pharmaceut, Rasht, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Aboutaleb, Ehsan
Abdolmaleki, Poorya
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Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Abdolmaleki, Poorya
Dinarvand, Rassoul
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Univ Tehran Med Sci, Sch Pharm, Dept Pharmaceut, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
Dinarvand, Rassoul
Firooz, Alireza
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Univ Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, IranUniv Tehran Med Sci, Ctr Res & Training Skin Dis & Leprosy, Pharmaceut Cosmeceut & Hyg Formulat Lab, Tehran, Iran
机构:
Dubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab EmiratesDubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab Emirates
Salem, Yasmein Yaser
Hoti, Gjylije
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Univ Turin, Dept Chem, Via P Giuria 7, I-10125 Turin, Italy
Univ Turin, Dept Drug Sci & Technol, Via P Giuria 9, I-10125 Turin, ItalyDubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab Emirates
Hoti, Gjylije
Sammour, Rana M. F.
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Dubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab EmiratesDubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab Emirates
Sammour, Rana M. F.
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Caldera, Fabrizio
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Cecone, Claudio
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Matencio, Adrian
Shahiwala, Aliasgar F.
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Dubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab EmiratesDubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab Emirates
Shahiwala, Aliasgar F.
Trotta, Francesco
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Univ Turin, Dept Chem, Via P Giuria 7, I-10125 Turin, ItalyDubai Pharm Coll Girls, Dept Pharmaceut, Al Muhaisanah 1, Al Mizhar, Dubai, U Arab Emirates
机构:
Int Med Univ, Dept Pharmaceut Technol, Kuala Lumpur 57000, Malaysia
CSIR, Cent Drug Res Inst, Pharmaceut Div, Lucknow 226031, Uttar Pradesh, IndiaBundelkhand Univ, Inst Pharm, Jhansi, Uttar Pradesh, India