title: A vaginal drug delivery model.
abstract: Efficient drug delivery at vaginal cavity is often a challenge owing to its peculiar physiological variations including vast differences in pH. Keeping in view this attribute of the target site, the current work was aimed at developing formulation strategies which could overcome this and successfully deliver molecules like itraconazole through SLNs. Optimized SLNs with the given composition was selected for further development into mucoadhesive and thermosensitive gel. Stearic acid and Compritol 888 (1:1, w/w ratio) as lipid, a mixture of 3% Poloxomer 188 and 0.5% sodium taurocholate as surfactant and organic to aqueous ratio of 10:50 was taken. Carbopol 934 and Pluronic F 127 were taken for the development of gel. Optimized gel exhibited a desired gelling temperature (35 °C); viscosity (0.920 PaS) and appreciable in vitro drug release (62.2% in 20 h). MTT assay did not show any cytotoxic effect of the gel. When evaluated in vivo, it did not exhibit any irritation potential despite appreciable bioadhesion. A remarkable decrease in CFUs was also observed in comparison with control and marketed formulation when evaluated in rat infection model. Thus, the proposed study defines the challenges for developing a suitable formulation system overcoming the delivery barriers of the vaginal site.
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy, Jamia Hamdard , New Delhi , India.
authors.forename: Mohd Aamir
authors.initials: MA
authors.lastname: Mirza
authors.affiliation: b Product Development Cell , National Institute of Immunology , New Delhi , India.
authors.forename: Amulya K
authors.initials: AK
authors.lastname: Panda
authors.affiliation: c Laboratory of Chemical Glycobiology , National Institute of Immunology , New Delhi , India.
authors.forename: S
authors.initials: S
authors.lastname: Asif
authors.affiliation: c Laboratory of Chemical Glycobiology , National Institute of Immunology , New Delhi , India.
authors.forename: Devina
authors.initials: D
authors.lastname: Verma
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy, Jamia Hamdard , New Delhi , India.
authors.forename: Sushama
authors.initials: S
authors.lastname: Talegaonkar
authors.affiliation: d Department of Biosciences , Jamia Millia Islamia , New Delhi , India , and.
authors.forename: Nikhat
authors.initials: N
authors.lastname: Manzoor
authors.affiliation: d Department of Biosciences , Jamia Millia Islamia , New Delhi , India , and.
authors.forename: Amber
authors.initials: A
authors.lastname: Khan
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy, Jamia Hamdard , New Delhi , India.
authors.forename: Farhan Jalees
authors.initials: FJ
authors.lastname: Ahmed
authors.affiliation: e Department of Microbiology , Hamdard Institute of Medical Sciences and Research, Jamia Hamdard , New Delhi , India.
authors.forename: Mridu
authors.initials: M
authors.lastname: Dudeja
authors.affiliation: a Department of Pharmaceutics , Faculty of Pharmacy, Jamia Hamdard , New Delhi , India.
authors.forename: Zeenat
authors.initials: Z
authors.lastname: Iqbal
mesh_terms: D000179:Acrylates / Q000737:chemistry; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D005260:Female; D005782:Gels / Q000008:administration & dosage* / Q000737:chemistry; D017964:Itraconazole / Q000008:administration & dosage / Q000737:chemistry; D023421:Models, Animal; D020442:Poloxamer / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013501:Surface-Active Agents / Q000737:chemistry; D013696:Temperature; D014621:Vagina / Q000378:metabolism*; D014783:Viscosity
chemical_list: D000179:Acrylates; D000935:Antifungal Agents; D004337:Drug Carriers; D005782:Gels; D013501:Surface-Active Agents; D020442:Poloxamer; D017964:Itraconazole; C453622:carbopol 934P
keywords: Antifungal; MTT assay; bioadhesive; itraconazole; poloxamer; solid lipid nanoparticles; thermosensitive gel; x-ray diffraction