Formulation, characterization and in vivo evaluation of novel edible dosage form containing nebivolol HCl

Abstract

The objective of this investigation was to develop a novel oral edible gel dosage form for nebivolol hydrochloride, with suitable rheological characteristics that can provide a means of administering the drug to dysphagic and geriatric patients. Edible gels were prepared using low acetylated gellan gum and sodium citrate in different concentrations. The effect of concentration of the solution on gelation time, viscosity, and drug release was studied. Optimized formulation had "spoon thick" consistency that is considered suitable for dysphagic patients as suggested by National Dysphagia Diet Task Force. The optimized formulation containing gellan gum (0.4 % w/v) and sodium citrate (0.3 % w/v) showed more than 95% drug release in 20 minutes. This formulation also showed significantly better pharmacokinetic profile when compared to marketed conventional tablets in New Zealand white rabbits (n = 3). Optimized formulation was found stable for 6 months when stored at 25 °C ± 0.2 °C/60 ± 5% RH. From this study, it can be concluded that the novel edible gel dosage form containing nebivolol hydrochloride may prove to be more efficacious in the treatment of hypertension in dysphagic patients.Uniterms: Edible gel/pharmaceutics. Nebivolol HCl/delivery. Dysphagia/drugs administration.O objetivo deste trabalho foi desenvolver um gel comestível para veiculação de cloridrato de nebivolol, com características reológicas adequadas, que podem fornecer meio de administrar o fármaco em casos de disfagia orofaríngea e pacientes geriátricos. Géis comestíveis foram preparados utilizando goma gelana de baixa acetilação e citrato de sódio, em diferentes concentrações. Estudou-se o efeito da concentração da solução no tempo de gelificação, a viscosidade e a liberação do fármaco. A formulação otimizada apresentava consistência de pudim, o que é considerado adequado para pacientes disfágicos como sugerido pela National Dysphagia Diet Task Force. A formulação otimizada contendo 0,4% (m/v) de goma gelana e 0,3% (m/v) de citrato de sódio mostrou que mais de 95% de fármaco foi liberado em 20 minutos. Esta formulação também mostrou, significativamente, melhor perfil farmacocinético, quando comparado com os comprimidos convencionais comercializados administrados a coelhos brancos neozelandeses (n = 3). A formulação otimizada manteve-se estável durante 6 meses, armazenada a 25 o C ± 0,2 °C/60 ± 5% de UR. A partir deste estudo, conclui-se que a nova forma de gel comestível contendo cloridrato de nebivolol pode ser mais eficaz no tratamento de hipertensão em pacientes portadores de disfagia.

Investigation of the Potential of Nebivolol Hydrochloride-Loaded Chitosomal Systems for Tissue Regeneration: In Vitro Characterization and In Vivo Assessment

“…The DSC scan of pure NVH exhibited a melting endothermic peak at 228 °C, corresponding to its melting point [ 89 , 90 ]. CSL exhibited broad spectrum endothermic peaks in the temperature ranges of 70–120 °C corresponding to polymeric dehydration of the typical polysaccharide and 215–225 °C corresponding to hydrogen-bonded lactate dimers within the CSL matrix [ 91 ].…”

Computational Tools Assisted Formulation Optimization of Nebivolol Hydrochloride Loaded Plga Nanoparticles by 32 Factorial Designs

“…The numerical value of PDI ranges from 0.0 (for a perfectly uniform sample with respect to the particle size) to 1.0 (for a highly polydisperse sample with multiple particle size populations). In drug delivery applications using lipid-based carriers, a PDI of 0.3 and below is considered to be acceptable and indicates a homogenous population of vesicles [25]. The PDI value nanoparticles shown in table 3 and it is 0.3 for most of the formulation indicates that particles are more homogeneous distributed in the formulation.…”

Hibiscus Rosa Sinensis Loaded Solid Lipid Nanoparticles and in Vivo Wound Healing Activity in Wistar Albino Rats

“…After the gels have been set in container, all gels were evaluated for homogeneity by visual inspection. They were evaluated for their appearance and presence of visible aggregates [27] Grittiness .…”

“…The pH measurement was done in triplicate and average values are noted [28] Viscosity Viscosity of formulated gels was measured using Brookfield DV-II+Pro viscometer (spindle number LV4) at the rotation speed of 50 rpm at room temperature. All the measurements were made in triplicate and average values were noted [27,29] Extrudability .…”