The novel oral imatinib microemulsions: physical properties, cytotoxicity activities and improved Caco-2 cell permeability


Gundogdu E., Karasulu H. Y. , Koksal C. , Karasulu E.

JOURNAL OF MICROENCAPSULATION, vol.30, no.2, pp.132-142, 2013 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 30 Issue: 2
  • Publication Date: 2013
  • Doi Number: 10.3109/02652048.2012.704952
  • Title of Journal : JOURNAL OF MICROENCAPSULATION
  • Page Numbers: pp.132-142

Abstract

The objective of this study was to formulate imatinib (IM) loaded to water-in-oil (w/o) microemulsions as an alternative formulation for cancer therapy and to evaluate the cytotoxic effect of microemulsions Caco-2 and MCF-7. Moreover, permeability studies were also performed with Caco-2 cells. W/o microemulsion systems were developed by using pseudo-ternary phase diagram. According to cytotoxicity studies, all formulations did not exert a cytotoxic effect on Caco-2 cells. Furthermore, all formulations had a significant cytotoxic effect on MCF-7 cells and the cytotoxic effect of M3IM was significantly more than that of other microemulsions and IM solution (p<0.05). The permeability studies of IM across Caco-2 cells showed that permeability value from apical to basolateral was higher than permeability value of other formulations. In conclusion, the microemulsion formulations as a drug carrier, especially M3IM formulation, may be used as an effective alternative breast cancer therapy for oral delivery of IM.