Formulation, Development and Evaluation of Febuxostat Loaded Microsponges

: Febuxostat is a novel, orally administered, powerful, non-purine, xanthine oxidase inhibitor used for treating gout and ceaseless tophaceous gout. The drug exhibits low bioavailability (about 49%) which is ascribed to its dissolution rate limited absorption. The aim of the current work was to provide a novel strategy to improve the dissolution profile and thus, bioavailability of Febuxostat. Formulation of fast dissolving tablets (FDT) is anticipated to provide immediate release of drug, which in turn, will improve its dissolution profile to provide the initial surge in plasma concentration required in acute gout attack. Incorporation of co-processed excipients in a tablet is known to improve the compressibility and disintegration characteristics of the tablets, which, in turn, result in enhanced in vitro drug release and improved bioavailability. A combination of crospovidone (it rapidly wicks saliva into the tablet to create the volume development and hydrostatic weight important to give quick disintegration) and microcrystalline cellulose (highly compressible ingredient with good wicking and absorbing capacity) was, therefore, used as co-processed excipients. The tablets were prepared by direct compression technique with the application of a 32 randomized full factorial design. The prepared tablets were able to release more than 80% of the drug within 10 minutes of the start of dissolution testing and were able to show better drug release profile in comparison to available marketed formulation.

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“…Melting point of Febuxostat was found to be in a range of 206° to 208°C which was in agreement with the available literature [ 24 ].…”

Section: Resultssupporting

confidence: 90%

Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients

Kaur

Mittal

Gulati

et al. 2020

DDF

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“…The collected solution was transferred to glass vials and kept frozen for 24 h at − 80 °C in an ultra-cold deep freezer. Thereafter, the samples were freeze-dried using a lyophilizer (Christ Alpha 1–2 LD, Osterode am Harz, Germany) for 24 h to yield a dry powder and stored in airtight containers for further investigation [ 31 ].…”

Section: Methodsmentioning

confidence: 99%

“…Quantitative determination was performed by UV spectrophotometer at λ max 315 nm for the released quantity of FBX. Each measurement was performed in triplicate, and the graph of cumulative percent drug release versus time was plotted [ 31 ].…”

Section: Particle Size Polydispersity Index (Pdi) and Surface Charge ...mentioning

confidence: 99%

Febuxostat ternary inclusion complex using SBE7-βCD in presence of a water-soluble polymer: physicochemical characterization, in vitro dissolution, and in vivo evaluation

Sakran,

Abdel-Hakim,

Teiama

et al. 2024

Drug Deliv. and Transl. Res.

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Febuxostat (FBX), a potent xanthine oxidase inhibitor, is widely used as a blood uric acid-reducing agent and has recently shown a promising repurposing outcome as an anti-cancer. FBX is known for its poor water solubility, which is the main cause of its weak oral bioavailability. In a previous study, we developed a binary system complex between FBX and sulfobutylether-β-cyclodextrin (SBE7-βCD) with improved dissolution behavior. The aim of the current study was to investigate the effect of incorporating a water-soluble polymer with a binary system forming a ternary one, on further enhancement of FBX solubility and dissolution rate. In vivo oral bioavailability was also studied using LC–MS/MS chromatography. The polymer screening study revealed a marked increment in the solubility of FBX with SBE7-βCD in the presence of 5% w/v polyethylene glycol (PEG 6000). In vitro release profile showed a significant increase in the dissolution rate of FBX from FBX ternary complex (FTC). Oral in vivo bioavailability of prepared FTC showed more than threefold enhancement in Cmax value (17.05 ± 2.6 µg/mL) compared to pure FBX Cmax value (5.013 ± 0.417 µg/mL) with 257% rise in bioavailability. In conclusion, the association of water-soluble polymers with FBX and SBE7-βCD system could significantly improve therapeutic applications of the drug. Graphical Abstract

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“…BCS class II drugs, such as FXT are difficult to formulate due to their extremely poor water (H 2 O) solubility [ 9 ]. Different formulation strategies, including the use of microsponges [ 10 ], nanosponges [ 11 ], polymeric nanoparticles [ 12 ], ternary solid dispersion [ 13 ], nanoemulsion [ 14 ], self-nanoemulsifying formulations [ 15 , 16 ], self-microemulsifying formulation [ 17 ], ethosomes [ 18 ], and nanostructure lipid carriers [ 19 ] have been used to enhance the fundamental and physicochemical characteristics of FXT.…”

Section: Introductionmentioning

confidence: 99%

Solubility and Thermodynamic Properties of Febuxostat in Various (PEG 400 + Water) Mixtures

et al. 2022

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The solubility of the poorly soluble medicine febuxostat (FXT) (3) in various {polyethylene glycol 400 (PEG 400) (1) + water (H2O) (2)} mixtures has been examined at 298.2–318.2 K and 101.1 kPa. FXT solubility was measured using an isothermal method and correlated with “van’t Hoff, Apelblat, Buchowski–Ksiazczak λh, Yalkowsky–Roseman, Jouyban–Acree, and Jouyban–Acree-van’t Hoff models”. FXT mole fraction solubility was enhanced via an increase in temperature and PEG 400 mass fraction in {(PEG 400 (1) + H2O (2)} mixtures. Neat PEG 400 showed the highest mole fraction solubility of FXT (3.11 × 10–2 at 318.2 K), while neat H2O had the lowest (1.91 × 10–7 at 298.2 K). The overall error value was less than 6.0 % for each computational model, indicating good correlations. Based on the positive values of apparent standard enthalpies (46.72–70.30 kJ mol−1) and apparent standard entropies (106.4–118.5 J mol−1 K−1), the dissolution of FXT was “endothermic and entropy-driven” in all {PEG 400 (1) + H2O (2)} mixtures examined. The main mechanism for FXT solvation in {PEG 400 (1) + H2O (2)} mixtures was discovered to be an enthalpy-driven process. In comparison to FXT-H2O, FXT-PEG 400 showed the strongest molecular interactions. In conclusion, these results suggested that PEG 400 has considerable potential for solubilizing a poorly soluble FXT in H2O.

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Formulation, Development and Evaluation of Febuxostat Loaded Microsponges

Cited by 5 publications

References 3 publications

Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients

Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients

Febuxostat ternary inclusion complex using SBE7-βCD in presence of a water-soluble polymer: physicochemical characterization, in vitro dissolution, and in vivo evaluation

Solubility and Thermodynamic Properties of Febuxostat in Various (PEG 400 + Water) Mixtures

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