Formulation, Optimization And Characterization Of Nanostructured Lipid Carrier Of Nitrofurantoin

Nitrofurantoin is effective against many urinary tract pathogens. It acts as bacteriostatic and/or bactericidal by inhibiting DNA-RNA protein& cell wall synthesis. Nanostructured Lipid Carriers (NLCs) of NFT was prepared by Hot Homogenization Process. Glyceryl Monostearate and Miglyol 812 were heated at 80ºC temperature on hot plate. In the melted lipid, drug was added with continuous stirring at high speed homogenization. Formulation NLC12B has % Entrapment efficiency 89.1 ± 0.5, PDI 0.11 ± 0.01 and mean particle size 237 ± 7nm represents narrow particle size distribution. Spherical feature of NLCs with better uniformity without aggregation of Nitrofurantoin loaded NLC was confirmed by TEM. Moreover, efficient miscibility of drug in lipids was confirmed by the absence of intense and characteristic peak of NFT in XRPD. After 6 month storage at 2-8°C there was no significant changes in the PDI as well as mean particle size.

Formulation

Nitrofurantoin is a broad-spectrum bactericidal antibiotic that affects both Gramnegative and Gram-positive bacteria. Nitrofurantoin exhibits bacteriostatic or bactericidaleffects by inhibiting the synthesis of DNA, RNA, protein and cell wall synthesis. Nanocrystals ofNFT were prepared by Cold High Pressure Homogenization Technique. NFT was dispersed inaqueous surfactant solution containing Poloxamer 188, PVPK 30 and HPMC E3 undercontinuous stirring. Poloxamer 188 was used as a surfactant for the preparation of the NCsFormulation NC9B3 have mean particle size 231 ± 9nm with Polydispersity index 0.09 ± 0.02which indicates very narrow particle size distribution. % Entrapment efficiency was 98.3± 0.7Slow drug release profile indicates the homogeneous dispersion of NFT in lipid matrix. NCshave crystalline nature with rough surfaces which has been confirmed using SEM analysis.XRPD spectra show the reduction in crystalline behaviour of the drug and the lipid afterformation of the NCs. There was no significant change in the mean particle size andPolydispersity index after 6 month storage at 25°C/60% RH