Potentiating the solubility of BCS class II drug zaltoprofen using nanodispersion technology

The aim of this work was to formulate zaltoprofen (ZLT) loaded polyvinyl pyrrolidone K30 (PVP K30) nanodispersions to improve the solubility of ZLT. By varying the concentrations of PVP K30 and poloxamer 407 (1:1, 1:2, 2:1 and 2:2) different trials of ZLT nanodispersions were developed by solvent evaporation technique. The effects of formulation variables on the particle size, zeta potential, drug content, and encapsulation efficiency of ZLT loaded nanodispersions (ZLTNDs) were investigated. The average particle size, zeta potential, drug content and entrapment efficiency of ZLT nanodispersions (ZLTNDs-4) were 285.40 +/- 16.41 nm, -19.06 +/- 1.50 mV, 73.11 +/- 0.16 mg, and 91.37 +/- 0.22%, respectively. The spherical shape of the nanodispersion was verified by Transmission Electron Microscope (TEM) analysis. Further the developed formulation was characterized using Fourier Transform Infrared Spectroscopy and Differential scanning calorimetry (DSC) analysis. The in vitro release studies revealed maximum ZLT release 95.78 +/- 0.85% compared to pure ZLT 36.47 +/- 0.84%. The in vitro anti-inflammatory effect of pure ZLT, ZLTNDs-4 and standard drug (diclofenac sodium) was tested by protein denaturation assay, and the results exhibited superior anti-inflammatory activity of ZLTNDs-4 was 33.33 +/- 1.00%). The anti- angiogenesis assay (CAM assay) results indicated that absence of vascular inhibition compared to pure ZLT. The results of the present work can be used to enhance the poorly aqueous soluble of ZLT and may be extended for other hydrophobic compounds, benefiting the pharmaceutical industries, etc.

Automated summary

The aim of this study was to improve the solubility of zaltoprofen (ZLT) by formulating ZLT loaded polyvinyl pyrrolidone K30 (PVP K30) nanodispersions. Different formulations of ZLT nanodispersions were developed by varying the concentrations of PVP K30 and poloxamer 407. The effects of formulation variables on the properties of ZLT nanodispersions were investigated. The results showed that the developed ZLT nanodispersion (ZLTNDs-4) had small particle size, high drug content, and good anti-inflammatory activity compared to pure ZLT.