title: Novel microparticulate systems for the vaginal delivery of nystatin: development and characterization.
abstract: To develop more effective antifungal microparticulate therapeutic systems for the treatment of Candida vaginitis, microparticles containing nystatin were elaborated by emulsification/internal gelation method. Three types of microparticles were successfully prepared, alginate microparticles, chitosan and poloxamer 407 coated alginate microparticles. DSC and FT-IR studies were performed to test the efficacy of the method. After physicochemical characterization, mean particle sizes ranged from 36.088 μm to 56.146 μm. The encapsulation efficiency was found to be similar for alginate and chitosan coated microparticles and lower for poloxamer 407 coated. Optimal mucoadhesive properties in all kind of microparticles where exhibited. Release studies showed the best kinetic parameters for poloxamer 407 coated microparticles. After ex vivo permeation studies through porcine vaginal mucosa, and determination of the amount of nystatin retained as well as microbiologic studies performed, it could be inferred that the developed microparticulate systems offered an antifungal effect against Candida albicans without toxic systemic absorption.
authors.affiliation: Pharmacy and Pharmaceutical Technology Department, Faculty of Pharmacy, University of Granada, Campus of Cartuja, Street s/n, 18071 Granada, Spain.
authors.forename: M J
authors.initials: MJ
authors.lastname: Martín-Villena
authors.forename: F
authors.initials: F
authors.lastname: Fernández-Campos
authors.forename: A C
authors.initials: AC
authors.lastname: Calpena-Campmany
authors.forename: N
authors.initials: N
authors.lastname: Bozal-de Febrer
authors.forename: M A
authors.initials: MA
authors.lastname: Ruiz-Martínez
authors.forename: B
authors.initials: B
authors.lastname: Clares-Naveros
mesh_terms: D000042:Absorption; D000282:Administration, Intravaginal; D000464:Alginates / Q000737:chemistry / Q000648:ultrastructure; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D002152:Calorimetry, Differential Scanning; D002176:Candida albicans / Q000187:drug effects*; D002177:Candidiasis / Q000188:drug therapy / Q000382:microbiology; D002214:Capsules / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry; D020099:Coated Materials, Biocompatible / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D005260:Female; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D008826:Microbial Sensitivity Tests; D009092:Mucous Membrane / Q000378:metabolism; D009761:Nystatin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D034421:Sus scrofa; D014627:Vaginitis / Q000188:drug therapy / Q000382:microbiology
chemical_list: D000464:Alginates; D000935:Antifungal Agents; D002214:Capsules; D020099:Coated Materials, Biocompatible; D004337:Drug Carriers; D006603:Hexuronic Acids; D020442:Poloxamer; D009761:Nystatin; D020723:Glucuronic Acid; D048271:Chitosan