Double-layered mucoadhesive tablets containing nystatin.
The objective of this work was to design a mucoadhesive tablet with a potential use in the treatment of oral candidosis. A 2-layered tablet containing nystatin was formulated. Lactose CD (direct compression), carbomer (CB), and hydroxypropylmethylcellulose (HPMC) were used as excipients. Tablets were obtained through direct compression. Properties such as in vitro mucoadhesion, water uptake, front movements, and drug release were evaluated. The immediate release layer was made of lactose CD (100 mg) and nystatin (30 mg). The CB:HPMC 9:1 mixture showed the best mucoadhesion properties and was selected as excipient for the mucoadhesive polymeric layer (200 mg). The incorporation of nystatin (33.3 mg) in this layer affected the water uptake, which, in turn, modified the erosion front behavior. Nystatin showed a first-order release. The polymeric layer presented an anomalous kinetic (n = 0.82) when this layer was individually evaluated. The mucoadhesive tablet formulated in this work releases nystatin quickly from the lactose layer and then in a sustained way, during approximately 6 hours, from the polymeric layer. The mixture CB:HPMC 9:1 showed good in vitro mucoadhesion. A swelling-diffusion process modulates the release of nystatin from this layer. A non-Fickian (anomalous) kinetic was observed.
Llabot
Juan Manuel
JM
Departamento de Farmacia, Facultad de Ciencias Quimicas, Universidad Nacional de Cordoba, Cordoba, Argentina.
Manzo
Ruben Hilario
RH
Allemandi
Daniel Alberto
DA
D000180:Acrylic Resins / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D000268:Adhesiveness; D000284:Administration, Oral; D000935:Antifungal Agents / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D002180:Candidiasis, Oral / Q000188:drug therapy; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D004058:Diffusion; D004339:Drug Compounding; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D065347:Hypromellose Derivatives; D007785:Lactose / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D009761:Nystatin / Q000737:chemistry* / Q000378:metabolism / Q000627:therapeutic use; D012995:Solubility; D013607:Tablets; D013997:Time Factors; D014867:Water / Q000378:metabolism
D000180:Acrylic Resins; D000935:Antifungal Agents; D003692:Delayed-Action Preparations; D013607:Tablets; D014867:Water; D009761:Nystatin; D065347:Hypromellose Derivatives; C006903:carbopol 940; D008747:Methylcellulose; D007785:Lactose