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

Marcília P Costa; Anderson C S Feitosa; Fátima C E Oliveira; Bruno C Cavalcanti; Gleiston G Dias; Ewerton W S Caetano; Francisco A M Sales; Valder N Freire; Stefano Di Fiore; Rainer Fischer; Luiz O Ladeira; Eufrânio N da Silva Júnior; Claudia Pessoa

doi:10.1039/c7md00196g

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

Medchemcomm. 2017 Sep 7;8(10):1993-2002. doi: 10.1039/c7md00196g. eCollection 2017 Oct 1.

Authors

Marcília P Costa¹, Anderson C S Feitosa², Fátima C E Oliveira², Bruno C Cavalcanti², Gleiston G Dias³, Ewerton W S Caetano^{4

5}, Francisco A M Sales^{4

5}, Valder N Freire⁶, Stefano Di Fiore⁷, Rainer Fischer^{7

8}, Luiz O Ladeira⁹, Eufrânio N da Silva Júnior³, Claudia Pessoa^{2

10}

Affiliations

¹ Pharmacy Course , Federal University of Piauí , 64049-550 Teresina , PI , Brazil.
² Department of Physiology and Pharmacology , Federal University of Ceará , 60430-270 Fortaleza , CE , Brazil . Email: cpessoa@ufc.br.
³ Institute of Exact Sciences , Department of Chemistry , Federal University of Minas Gerais , Belo Horizonte , 31270-901 , MG , Brazil . Email: eufranio@ufmg.br ; Tel: +55 31 34095720.
⁴ Department of Secondary School and Teachers College , Federal Institute of Ceará , 60040-531 Fortaleza , CE , Brazil.
⁵ Federal Institute of Ceará , 63503-790 Iguatu , CE , Brazil.
⁶ Department of Physics , Federal University of Ceará , 60455-760 Fortaleza , CE , Brazil.
⁷ Fraunhofer Institute for Molecular Biology and Applied Ecology IME , 52074 , Aachen , Germany.
⁸ Institute for Molecular Biotechnology , RWTH Aachen University , 52074 Aachen , Germany.
⁹ Institute of Exact Sciences , Department of Physics , Federal University of Minas Gerais , Belo Horizonte , 31270-901 , MG , Brazil.
¹⁰ Oswaldo Cruz Foundation (Fiocruz) , 60180-900 Fortaleza , CE , Brazil.

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.