Albendazole nanocrystals: Optimization, spectroscopic, thermal and anthelmintic studies

• Published in: Journal of drug delivery science and technology 2018-02, Vol.43, p.369-378
• Main Authors: Koradia, Krishna D., Parikh, Rajesh H., Koradia, Hiral D.
• Format: Article
• Language: English
• Subjects: Anthelmintic bioassay; Antisolvent precipitation; Differential scanning calorimetry; Fourier transform infrared spectroscopy; Nanocrystals; X-ray diffraction
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2017.11.003

Albendazole is a broad spectrum anthelmintic. Its efficacy is often limited by poor intestinal absorption mainly due to its low aqueous solubility. One of the best approaches to enhance aqueous solubility and dissolution of drug is nanoparticles. In the present study nanocrystals of albendazole were prepared by antisolvent precipitation technique followed by spray drying. The nanocrystals were optimized using 32 full factorial design considering stabilizer concentration and stirring speed as independent variable and dissolution efficiency as dependent variable. The prepared formulations were subjected for spectroscopic, thermal and dissolution studies. The results of FTIR showed that the drug was compatible with the excipients. The dissolution from nanocrystals was much more faster then pure albendazole. The particle size of nanocrystals was 277 nm. The XRD showed that there were no significant difference in the diffraction pattern of pure Albendazole and nanocrystals, crystalline habit modification happened in the nanocrystals. The lower melting point and enthalpy in physical mixture and in nanocrystals compare to pure Albendazole was reported in DSC study. TEM image of nanocrystals indicated rectangular nanoparticles. Gas chromatography study showed that the amount of residual solvent was less than the permissible limits. The optimized nanocrystals showed better anthelmintic activity compared to pure Albendazole. [Display omitted]