Magnetoliposomes as carriers for promising antitumor thieno[3, 2-b]pyridin-7-arylamines: photophysical and biological studies. Issue 25 (7th March 2017)

• Record Type: Journal Article
• Authors: Rodrigues, Ana Rita O.; Almeida, B. G.; Rodrigues, Juliana M.; Queiroz, Maria João R. P.; Calhelha, R. C.; Ferreira, Isabel C. F. R.; Pires, A.; Pereira, A. M.; Araújo, J. P.; Coutinho, Paulo J. G.; Castanheira, Elisabete M. S.
• Is Part Of: RSC advances. Volume 7:Issue 25(2017)
• Page Start: 15352
• Page End: 15361
• Publication Date: 2017-03-07
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c7ra00447h
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Magnetoliposomes containing MnFe2 O4 nanoparticles were used as nanocarriers for new potent antitumor thieno[3, 2- b ]pyridin-7-arylamines, inhibiting the growth of human tumor cells. Abstract : Magnetoliposomes containing superparamagnetic manganese ferrite nanoparticles were tested as nanocarriers for two new promising antitumor drugs, a N -(3-methoxyphenyl)thieno[3, 2- b ]pyridin-7-amine (1 ) and a N -(2-methoxy-phenyl)thieno[3, 2- b ]pyridin-7-amine (2 ). The fluorescence emission of both compounds was studied in different polar and non-polar media, evidencing a strong intramolecular charge transfer character of the excited state of both compounds. These in vitro potent antitumor thienopyridine derivatives were successfully incorporated in both aqueous and solid magnetoliposomes, with encapsulation efficiencies higher than 75%. The magnetic properties of magnetoliposomes containing manganese ferrite nanoparticles were measured for the first time, proving a superparamagnetic behaviour. Growth inhibition assays on several human tumor cell lines showed very low GI50 values for drug-loaded aqueous magnetoliposomes, comparing in most cell lines with the ones previously obtained using the neat compounds. These results are important for future drug delivery applications using magnetoliposomes in oncology, through a dual therapeutic approach (simultaneous chemotherapy and magnetic hyperthermia).