Abstract
Purpose: The
objective of this study was to develop, characterize, and comparatively
investigate the ketotifen fumarate (KF) nanosuspensions (NSS) to
enhance the permeability of KF.
Methods: In the
present work, the NSP and NSE were prepared by
double-emulsion solvent evaporation/nanoprecipitation methods with poly (D,Llactide-co-glycolide) and Eudragit RL100
polymers, respectively. The loading efficiency, particle size, and
polydispersity index of prepared different NSs were evaluated with scanning
electron microscopy (SEM), X-ray diffraction, differential scanning calorimetry
(DSC), Fourier transform infrared spectroscopy (FTIR), and in vitro release and
transcorneal permeation . NSs were also
compared on the basis of particle size and polydispersity index.
Results: Particle
size, polydispersity index, and loading efficiency of NSP1 and NSE3
showed the best value (158 nm, 117 nm, 0.21, 0.43 and 43%, 95.23%,
respectively). SEM showed spherical globules and DSC results showed the
reduction in crystallinity. The NSE3 formulations demonstrated
significantly (p<0.05) higher drug release rates than the NSP1
due to increases in the surface area. Comparative studies showed that NSE
release and permeability are higher than NSP.
Conclusion: It is concluded that both NSP and NSE
provide a useful dosage form for the ocular drug delivery which can enhance the
permeability of KF.