The novel oral imatinib microemulsions: physical properties, cytotoxicity activities and improved Caco-2 cell permeability.
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.
Department of Biopharmaceutics and Pharmacokinetics, Ege University, Izmir, Turkey. evren.gundogdu@ege.edu.tr
Evren
E
Gundogdu
Hatice Yesim
HY
Karasulu
Cinel
C
Koksal
Ercüment
E
Karasulu
D000970:Antineoplastic Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D001549:Benzamides / Q000493:pharmacokinetics* / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy*; D018938:Caco-2 Cells; D004655:Emulsions; D005260:Female; D006801:Humans; D000068877:Imatinib Mesylate; D010539:Permeability; D010879:Piperazines / Q000493:pharmacokinetics* / Q000494:pharmacology; D011743:Pyrimidines / Q000493:pharmacokinetics* / Q000494:pharmacology
D000970:Antineoplastic Agents; D001549:Benzamides; D004655:Emulsions; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate