Objective: The study aims to prepare and evaluate Nicorandil mucoadhesive microspheres to improve the oral physicochemical properties of nicorandil and mucoadhesion to extend the residence time at the absorption site. Methods: Nicorandil mucoadhesive microsphere was prepared by emulsion cross-linking method using fenugreek gum, karaya gum as polymer, and glutaraldehyde as a cross-linking agent. Drug entrapment efficiency, particle size, % swelling index, mucoadhesion study, differential scanning calorimetry, powder x-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were used to characterize the microspheres. Results: The characterization studies indicated the formation of mucoadhesive microspheres. The nicorandil mucoadhesive microspheres particle size is130.83±0.48, entrapment efficiency 66.91±0.54, swelling index 82.69±0.40, % mucoadhesion 95.22±0.13 and in vitro drug release was found to be 89.96±0.17 % at the end of 12 h. Conclusion: This research work successfully formed nicorandil mucoadhesive microspheres formulation using the emulsion cross-linking method. Encapsulation efficiency and other physicochemical and functional characterization of microspheres suggested the successful formation of nicorandil mucoadhesive microspheres.
Objective: The study aims to prepare and evaluate febuxostat nanosuspension to improve oral bioavailability. Methods: Febuxostat nanosuspension was prepared by the solvent-antisolvent method, followed by a lyophilization technique using PVP K-30 as a stabilizer and sodium lauryl sulfate as a surfactant. Drug content, differential scanning calorimetry, powder x-ray diffraction, Fourier transform infrared spectroscopy, and in vitro dissolution studies were used to characterize the nanosuspension. Results: The results of the characterization studies indicated the formation of nanosuspension. The lyophilized FXT NS particle size is 2170.2 nm, the PDI value is 0.63, the negative zeta potential is 1.6 mV, and the drug content is 19.02%. Functional characterization studies demonstrated that the particle size reduced due to the interaction between the stabilizer and surfactant. Conclusion: It can be concluded that the prepared febuxostat nanosuspension enhances the aqueous solubility of FXT and improves its oral bioavailability.
Objective: To improve ATN's solubility, permeability, and dissolution rate of pentaerythritol-eudragit®RS100 co-processed excipients (CE) and their potential as a solid dispersion carrier (ATN-CE-SD). Methods: The ATN-CE-SD was prepared using the solvent evaporation technique. The pure ATN, physical mixture, CE carrier, and optimized ATN-CE-SD was physicochemically characterized using Scanning electron microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, powder x-ray diffractometry, solubility, and in vitro dissolution was used to evaluate solid dispersions. Results: Physical and chemical analysis showed that ATN-CE-SD formed via the involvement of weak intermolecular forces of attraction between CE carrier and ATN. The prepared solid dispersion showed the drug content around ~ 96.94 % w/w, indicating that the solvent evaporation method improved the encapsulation of ATN and, thus, enhanced its drug content. Compared to pure ATN (~ 0.11 mg/ml), ATN-CE-SD (1:2) significantly increased the aqueous solubility by around ~ 25-fold (~ 2.78 mg/ml), indicating solid dispersion improves the solubility of ATN. ATN-CE-SD enhanced the rate of dissolution of ATV (~ 65 %) compared to pure ATN (~ 25 %) and PM (~ 34 %). Likewise, ATN-CE-SD (1:2) improved the rate and extent of ATN (~ 60 %) across the biological membrane compared to pure ATN (~ 22 %) and PM (~ 32 %). The ATN-CE-SD (1:2) improved the dissolution efficiency by around ~ (57.31%) compared to pure ATN (~ 7.02%) and PM (~ 20.43%). According to the study, co-processed excipients could serve as a promising solid dispersion carrier and improve ATN's water solubility, permeability, and dissolution rate. Conclusion: Based on the results, it is possible to use synthetic solid dispersion carriers as alternatives to improve the low water solubility and permeability of ATN.
Objective: The objective of the study was to design and formulate ferulic acid (FA) phytosomes converted in to functionalised soft nanoparticles by using the solvent evaporation method to increase resistance time, improve the bioavailability and half-life of ferulic acid. Methods: FA is a BCS-II drug, which has low solubility and high permeability. The functionalised soft nanoparticles was prepared by the solvent evaporation method followed by the particle size and zeta potential, Fourier Transform Infra-Red (FTIR), Powder x-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM). It indicates good result for the complexation rate. PXRD showed good powder diffraction results with having good flow property. Particle size and zeta potential had a good result of-12.05±120 improved by the cationic polymer. The complex was evaluated by the study of drug loading, entrapment efficiency, histopathological study and mucoadhesive property for the final formulation of the microspheres system. Also, the formulation were evaluated for the In vitro drug dissolution study for rate of the extent of drug release. Ex-vivo drug diffusion study by using goat nasal mucosa using pH 6.6 for evaluating rate of the extent of drug diffusion through nasal mucosa. Results: The results of the characterization studies indicated the designing of functionalised phytosomal soft nanoparticles (FPSN). The FPSN particle size and zeta potential had a good result of-12.05±120. The FTIR spectra of the complex showed a characteristic peak at 3652.8 cm-1(OH-stretching) which indicate that the shifting and interaction between the FA and soya phospholipid complex (SPC 3). The P-XRD, SEM, In vitro dissolution showed good powder diffraction results with having good flow property. The complex is evaluated by the study of drug loading. Also formulation were evaluated for the In vitro drug dissolution study for rate of the extent of drug release. The result of the above studies was Drug loading increased at 44.42 %. The Ex-vivo permeation study ferulic acid-phytosomal soft nanoparticle (FALC-PSN) showed characteristic in the drug diffusion at 80.04 %, which indicate that the drug had increases its aqueous solubility and also change with the structural morphology. Conclusion: It can be concluded that the ferulic acid phytosomal soft nanoparticles (FAPSN) enhance the solubility of the FA and increased the bioavailability and retention time to target liver cancer.
Objective: Chitosan-based pregabalin microsphere (CBPM) formulation was prepared to improve in vitro mucoadhesion and absorption of pregabalin via intranasal administration. Methods: The CBPM formulations were prepared using the inotropic gelation method and optimized using the Box-behnken design. The optimized CBPM formulation was physico-chemically characterized using scanning electron microscopy, thermal analysis, Fourier transform infrared spectrometry and powder x-ray diffraction. Additionally, the CBPM formulation was characterized for functional parameters such as in vitro mucoadhesion, in vitro drug release, ex vivo permeability across the sheep nasal mucosa and in vivo anticonvulsant activity in pentylenetetrazol (PTZ)-induced seizures model in mice. Results: The design-optimized CBPM exhibited a 91.45 % inclusion efficiency of pregabalin in the microspheres. The Physico-chemical analysis of the individual components and the optimized formulation confirmed the formation of CBPM. The in vitro mucoadhesion study revealed ~80% mucoadhesive of the CBPM to the sheep nasal mucosa. The in vitro dissolution profiles of CBPM was significantly higher (~97%) than that of pure pregabalin (~70%). The CBPM displayed a higher rate and extent of permeability (~90%) than pure pregabalin (~76%) across the sheep nasal mucosa. The in vivo anticonvulsant activity showed that intranasal administration of CBPM resulted in significant (P<0.01) protection against PTZ-induced convulsions in mice. Conclusion: The chitosan-based microsphere intranasal formulation could be employed as promising delivery for rapid pregabalin absorption.
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