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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.


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.

SUBMITTER: Costa MP 

PROVIDER: S-EPMC6071939 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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

Costa Marcília P MP   Feitosa Anderson C S ACS   Oliveira Fátima C E FCE   Cavalcanti Bruno C BC   Dias Gleiston G GG   Caetano Ewerton W S EWS   Sales Francisco A M FAM   Freire Valder N VN   Di Fiore Stefano S   Fischer Rainer R   Ladeira Luiz O LO   da Silva Júnior Eufrânio N EN   Pessoa Claudia C  

MedChemComm 20170907 10


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 <i>in vitro</i> cytotoxicity were studied. Spherical microcapsules with a size of 1.03 ± 0.46 μm were produced with an encapsulati  ...[more]

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