Preparation of amorphous cefuroxime axetil nanoparticles by sonoprecipitation for enhancement of bioavailability.
The aim of the present work was to prepare amorphous discreet nanoparticles by sonoprecipitation method for enhancing oral bioavailability of cefuroxime axetil (CA), a poorly water-soluble drug. CA nanoparticles (SONO-CA) were prepared by sonoprecipitation and compared with particles obtained by precipitation without sonication (PPT-CA) and amorphous CA obtained by spray drying. Spray drying present broad particle size distribution (PSD) with mean particle size of 10 microm and low percent yield, whereas, precipitation without sonication resulted in large amorphous aggregates with broad PSD. During sonoprecipitation, particle size and yield improve with an increase in the amplitude of sonication and lowering the operation temperature due to instantaneous supersaturation and nucleation. The overall symmetry and purity of CA molecule was maintained as confirmed by FTIR and HPLC, respectively. All the three methods resulted in the formation of amorphous CA with only sonoprecipitation resulting in uniform sized nanoparticles. Sonoprecipitated CA nanoparticles showed enhanced dissolution rate and oral bioavailability in Wistar rat due to an increased solubility attributed to combination of effects like amorphization and nanonization with increased surface area and reduced diffusion pathway.
Dhumal
Ravindra S
RS
Department of Pharmaceutics, Poona College of Pharmacy and Research Centre, Bharati Vidyapeeth University, Erandawane, Pune, Maharashtra, India.
Biradar
Shailesh V
SV
Yamamura
Shigeo
S
Paradkar
Anant R
AR
York
Peter
P
D000284:Administration, Oral; D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002444:Cefuroxime / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D011232:Chemical Precipitation; D002626:Chemistry, Pharmaceutical; D018360:Crystallography, X-Ray; D005260:Female; D008297:Male; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D033362:Powder Diffraction; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D013010:Sonication; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods
D000900:Anti-Bacterial Agents; D002444:Cefuroxime; C040738:cefuroxime axetil