DEVELOPMENT, CHARACTERIZATION AND EVALUATION OF NANOCRYSTALS OF NITROFURANTOIN

Nitrofurantoin is a broad-spectrum bactericidal antibiotic that affects both gram-negative and gram-positive bacteria. Nitrofurantoin exhibits bacteriostatic or bactericidal effects by inhibiting the synthesis of DNA, RNA, protein, and cell wall synthesis. Nanocrystals of NFT were prepared by a cold high-pressure homogenization technique. To improve the dissolution rate, the drug was formulated in a nanocrystal by using an emulsion diffusion method, high-pressure homo-genization or sonication. NFT was dispersed in aqueous surfactant solution containing poloxamer 188, PVPK 30, and HPMC E3 under continuous stirring. Poloxamer 188 was used as a surfactant for the preparation of the NCs. Formulation NC9B3 has a mean particle size 231 ± 9 nm with polydispersity index 0.09 ± 0.02, which indicates a very narrow particle size distribution.  % Entrapment efficiency was 98.3 ± 0.7 slow drug release profile indicates the homogeneous dispersion of NFT in the lipid matrix. NCs have crystalline nature with rough surfaces, which has been confirmed using SEM analysis. XRPD spectra show the reduction in the crystalline behavior of the drug and the lipid after the formation of the NCs. There was no significant change in the mean particle size and polydispersity index after 6-month storage at 25 °C / 60% RH.