title: Controlled Release of Nor-β-lapachone by PLGA Microparticles: A Strategy for Improving Cytotoxicity against Prostate Cancer Cells.
abstract: Prostate cancer is one of the most common malignant tumors in males and it has become a major worldwide public health problem. This study characterizes the encapsulation of Nor-β-lapachone (NβL) in poly(d,l-lactide-co-glycolide) (PLGA) microcapsules and evaluates the cytotoxicity of the resulting drug-loaded system against metastatic prostate cancer cells. The microcapsules presented appropriate morphological features and the presence of drug molecules in the microcapsules was confirmed by different methods. Spherical microcapsules with a size range of 1.03 ± 0.46 μm were produced with an encapsulation efficiency of approximately 19%. Classical molecular dynamics calculations provided an estimate of the typical adsorption energies of NβL on PLGA. Finally, the cytotoxic activity of NβL against PC3M human prostate cancer cells was demonstrated to be significantly enhanced when delivered by PLGA microcapsules in comparison with the free drug.
authors.affiliation: Department of Physiology and Pharmacology, Federal University of Cear&#225;, 60430-270 Fortaleza, CE, Brazil. marciliapc@ufpi.edu.br.|Department of Pharmacy, Federal University of Piau&#237;, 64049-550 Teresina, PI, Brazil. marciliapc@ufpi.edu.br.
authors.forename: Marcilia P
authors.initials: MP
authors.lastname: Costa
authors.affiliation: Department of Physiology and Pharmacology, Federal University of Cear&#225;, 60430-270 Fortaleza, CE, Brazil. acs_feitosa@yahoo.com.br.
authors.forename: Anderson C S
authors.initials: AC
authors.lastname: Feitosa
authors.affiliation: Department of Physiology and Pharmacology, Federal University of Cear&#225;, 60430-270 Fortaleza, CE, Brazil. cassiadefatima3006@gmail.com.
authors.forename: Fátima C E
authors.initials: FC
authors.lastname: Oliveira
authors.affiliation: Department of Physiology and Pharmacology, Federal University of Cear&#225;, 60430-270 Fortaleza, CE, Brazil. nunim_br@yahoo.com.br.
authors.forename: Bruno C
authors.initials: BC
authors.lastname: Cavalcanti
authors.affiliation: Department of Chemistry, Federal University of Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil. eufranio@ufmg.br.
authors.forename: Eufrânio N
authors.initials: EN
authors.lastname: da Silva
authors.affiliation: Department of Chemistry, Federal University of Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil. diasgg@yahoo.com.br.
authors.forename: Gleiston G
authors.initials: GG
authors.lastname: Dias
authors.affiliation: Department of Physics, Federal University of Cear&#225;, 60455-760 Fortaleza, CE, Brazil. adilson.sales@gmail.com.
authors.forename: Francisco A M
authors.initials: FA
authors.lastname: Sales
authors.affiliation: Department of Physics, Federal University of Cear&#225;, 60455-760 Fortaleza, CE, Brazil. brunolopesdesousa@gmail.com.
authors.forename: Bruno L
authors.initials: BL
authors.lastname: Sousa
authors.affiliation: Department of Analytical Chemistry and Physical Chemistry, Federal University of Cear&#225;, 60455-760 Fortaleza, CE, Brazil. itoliberato@gmail.com.
authors.forename: Ito L
authors.initials: IL
authors.lastname: Barroso-Neto
authors.affiliation: Department of Physiology and Pharmacology, Federal University of Cear&#225;, 60430-270 Fortaleza, CE, Brazil. cpessoa@ufc.br.|Oswaldo Cruz Foundation (Fiocruz), 60180-900 Fortaleza, CE, Brazil. cpessoa@ufc.br.
authors.forename: Cláudia
authors.initials: C
authors.lastname: Pessoa
authors.affiliation: Department of Secondary School and Teachers College, Federal Institute of Cear&#225;, 60040-531 Fortaleza, CE, Brazil. ewcaetano@gmail.com.
authors.forename: Ewerton W S
authors.initials: EW
authors.lastname: Caetano
authors.affiliation: Fraunhofer Institute for Molecular Biology and Applied Ecology IME, 52074, Aachen, Germany. stefano.difiore@ime.fraunhofer.de.
authors.forename: Stefano
authors.initials: S
authors.lastname: Di Fiore
authors.affiliation: Fraunhofer Institute for Molecular Biology and Applied Ecology IME, 52074, Aachen, Germany. rainer.fischer@ime.fraunhofer.de.|Institute for Molecular Biotechnology, RWTH Aachen University, 52074 Aachen, Germany. rainer.fischer@ime.fraunhofer.de.
authors.forename: Rainer
authors.initials: R
authors.lastname: Fischer
authors.affiliation: Department of Physics, Federal University of Minas Gerais, 31340-550 Belo Horizonte, MG, Brazil. loladeira@gmail.com.
authors.forename: Luiz O
authors.initials: LO
authors.lastname: Ladeira
authors.affiliation: Department of Analytical Chemistry and Physical Chemistry, Federal University of Cear&#225;, 60455-760 Fortaleza, CE, Brazil. vnffreire@gmail.com.
authors.forename: Valder N
authors.initials: VN
authors.lastname: Freire
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D001572:Benzofurans / Q000008:administration & dosage* / Q000737:chemistry; D002214:Capsules / Q000737:chemistry; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D016503:Drug Delivery Systems; D006801:Humans; D020128:Inhibitory Concentration 50; D019344:Lactic Acid / Q000737:chemistry; D008297:Male; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D009285:Naphthoquinones / Q000008:administration & dosage* / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011471:Prostatic Neoplasms; D013059:Spectrum Analysis, Raman
chemical_list: D000970:Antineoplastic Agents; D001572:Benzofurans; D002214:Capsules; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D009285:Naphthoquinones; C574726:nor-beta-lapachone; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid
keywords: PLGA microcapsules; cancer; lapachol; naphthoquinone; nor-β-lapachone; prostate