Norfloxacin mixed solvency based solid dispersions: An in-vitro and in-vivo investigation

Abstract

Norfloxacin (NF) is a synthetic fluoro-quinolone molecule that is used for the treatment of urinary tract infections. However, due to its poor aqueous solubility, it has low oral bioavailability. The aim of the present study was to improve the aqueous solubility and dissolution profile of NF by formulating its mixed-solvency based solid dispersions (SDs). The NF-loaded SDs were prepared by a solvent evaporation technique using urea, sodium benzoate and a niacinamide hydrotropic mixture. The prepared SDs were evaluated regarding their solubility, mean particle size, in-vitro drug release and oral bioavailability. The optimized batch showed a high percentage yield of 99.04% , with a mean particle size of 132.91 m. Optimized SDs Exhibit 96.48% drug release. The oral bioavailabilities of NF from the optimized SDs, drug alone and marketed formulation were evaluated in Wistar rats at a dose of 20.0 mg/kg. In comparison to the drug alone, approximately 6.90-and 5.0-fold increases in AUC and C max , respectively, were observed for NF from mixed-solvency based SDs. The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability.

Thermal, spectroscopic and antimicrobial activity characterization of some norfloxacin complexes

“…Fluorine (F) and the piperazine group give an extra stabilization to the ternary complex norfloxacin-enzyme-DNA because it interacts with the enzyme; this stabilization is responsible for the effectiveness potential antibacterial action. However, this compound presents poor aqueous solubility that causes a low oral bioavailability, generating a poor metabolization of norfloxacin [5,6]. Garnayak and Patel [4] have reported that less than 10% of the drug containing norfloxacin as active principle is metabolized, part of the drug excreted by renal excretion and a fraction of the drug remained unaltered by the metabolism.…”

Norfloxacin Loaded Lipid Polymer Hybrid Nanoparticles for Oral Administration: Fabrication, Characterization, In Silico Modelling and Toxicity Evaluation

“…The blood samples were centrifuged at 7000 rpm at 4 °C for 20 min to separate plasma. Separated plasma samples were analyzed via the high performance liquid chromatography method as previously reported [28].…”

Advanced development of a non-ionic surfactant and cholesterol material based niosomal gel formulation for the topical delivery of anti-acne drugs

“…The samples were stored in USP type-1 flint vials and hermetically sealed with bromo butyl rubber plugs with aluminum caps. 25…”