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Encapsulation of nor-beta-lapachone into poly(d,l)-lactide-: Co -glycolide (PLGA) microcapsules: Full characterization, computational details and cytotoxic activity against human cancer cell lines

: Costa, M.P.; Feitosa, A.C.S.; Oliveira, F.C.E.; Cavalcanti, B.C.; Dias, G.G.; Caetano, E.W.S.; Sales, F.A.M.; Freire, V.N.; Fiore, S. di; Fischer, R.; Ladeira, L.O.; Silva Junior, E.N. da; Pessoa, C.


Medicinal chemistry communications : MedChemComm 8 (2017), Nr.10, S.1993-2002
ISSN: 2040-2503
ISSN: 2040-2511
Fraunhofer IME ()

In this work, we characterize nor-β-lapachone-loaded (NβL-loaded) microcapsules prepared using an emulsification/solvent extraction technique. Features such as surface morphology, particle size distribution, zeta potential, optical absorption, Raman and Fourier transform infrared spectra, thermal analysis data, drug encapsulation efficiency, drug release kinetics and in vitro cytotoxicity were studied. Spherical microcapsules with a size of 1.03 ± 0.46 μm were produced with an encapsulation efficiency of approximately 19%. Quantum DFT calculations were also performed to estimate typical interaction energies between a single nor-β-lapachone molecule and the surface of the microparticles. The NβL-loaded PLGA microcapsules exhibited a pronounced initial burst release. After the in vitro treatment with NβL-loaded microcapsules, a clear phagocytosis of the spheres was observed in a few minutes. The cytotoxic activity against a set of cancer cell lines was investigated .