PREPARATION AND IN VITRO EVALUATION OF BUTENAFINE HCL NANOSUSPENSION
DOI:
https://doi.org/10.22159/ijap.2026v18i2.56008Keywords:
Nanosuspension, Solubility enhancement, Antifungal, Soluplus®, NanotechnologyAbstract
Objective: One of the significant problems associated with poorly soluble drugs is low bioavailability. Butenafine HCl is classified as BCS Class II by the biopharmaceutical classification system, with low solubility and high permeability. Objectives: Formulation as a nanosuspension is an attractive and promising alternative to solve low solubility problems and low bioavailability
Methods: A nanosuspension of Butenafine HCL was generated utilizing a bottom-up method through the solvents/anti-solvents procedure characterized by particle size analysis, polydisperse index, and entrapment efficacy, and then the selected formula was described by dissolution testing, differential scanning calorimetry, X-ray powder diffraction, FTIR, and FESEM. Nanosuspensions were prepared via the solvent/anti-solvent procedure, using different polymer types and ratios.
Results: Butenafine solubilized in PBS with 1% soluplus, PVP, PEG 400, and poloxamer was 14.32±0.011, 6±0.01, 10.48±0.012, and 2.025±0.001. To form a nanosuspension with particle sizes ranging from 78 to 516 ±0.01 nm, entrapment up to 96%, and a Drug content of 99%. Particle size of optimum formula, consisting of Butenafine HCL and soluplus® in a ratio of drug: stabilizer (Soluplus®):co-stabilizer (PEG400) is (1:8:2.5) measured in nanostructure, and it was equal to 78.3±0.03 with a PDI 0.2511±0.13, which is in the nanosized range, drug content of optimum formula 99.6±0.013, and entrapment was 96±0.012. Osmolarity adjusted to a range of 280 to 310 mOsm/Kg. The release of the drug after 120 min was 95%. FTIR spectra show a distinct peak for the drug, indicating no chemical interaction between BF and Soluplus®. DSC shows a slight shift in the melting point to 220.50 °C due to the presence of cryoprotectants. PXRD shows amorphous formation due to nanosuspension, and FESEM shows the size and shape of the nanosuspension, in which the size of the particle by FESEM was 72.9 nm, which is close to the measured particle size. The stability study of the optimal formula after three months showed a particle size of 78 nm at 5 °C and 80 nm at 25 °C.
Conclusion: Using soluplus as a stabilizer at various concentrations successfully produced a nanosuspension of Butenafine HCl. The best formula, consisting of Butenafine HCL and soluplus® in a ratio of drug: stabilizer (Soluplus®):co-stabilizer (PEG400) is 1:8:2.5.
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