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Issue 10, 2017
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Encapsulation of nor-β-lapachone into poly(d,l)-lactide-co-glycolide (PLGA) microcapsules: full characterization, computational details and cytotoxic activity against human cancer cell lines

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Abstract

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.

Graphical abstract: Encapsulation of nor-β-lapachone into poly(d,l)-lactide-co-glycolide (PLGA) microcapsules: full characterization, computational details and cytotoxic activity against human cancer cell lines

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Supplementary files

Article information


Submitted
19 Apr 2017
Accepted
06 Sep 2017
First published
07 Sep 2017

Med. Chem. Commun., 2017,8, 1993-2002
Article type
Research Article

Encapsulation of nor-β-lapachone into poly(D,L)-lactide-co-glycolide (PLGA) microcapsules: full characterization, computational details and cytotoxic activity against human cancer cell lines

M. P. Costa, A. C. S. Feitosa, F. C. E. Oliveira, B. C. Cavalcanti, G. G. Dias, E. W. S. Caetano, F. A. M. Sales, V. N. Freire, S. Di Fiore, R. Fischer, L. O. Ladeira, E. N. da Silva Júnior and C. Pessoa, Med. Chem. Commun., 2017, 8, 1993
DOI: 10.1039/C7MD00196G

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