Improving Encapsulation of Hydrophilic Chloroquine Diphosphate into Biodegradable Nanoparticles: A Promising Approach against Herpes Virus Simplex-1 Infection
Tábata Loíse Cunha Lima,
Renata de Carvalho Feitosa,
Emanuell dos Santos-Silva,
Alaine Maria dos Santos-Silva,
Emerson Michell da Silva Siqueira,
Paula Renata Lima Machado,
Alianda Maira Cornélio,
Eryvaldo Sócrates Tabosa do Egito,
Matheus de Freitas Fernandes-Pedrosa,
Kleber Juvenal Silva Farias,
Arnóbio Antônio da Silva-Júnior
Affiliations
Tábata Loíse Cunha Lima
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Renata de Carvalho Feitosa
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Emanuell dos Santos-Silva
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Alaine Maria dos Santos-Silva
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Emerson Michell da Silva Siqueira
Graduate Program in Development and Technological Innovation in Medicines, Federal University of Rio Grande do Norte (UFRN), Natal 59.072-570, Brazil
Paula Renata Lima Machado
Department of Clinical Analysis and Toxicology, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Alianda Maira Cornélio
Department of Morphology, Federal University of Rio Grande do Norte, UFRN, Natal 59.072-570, Brazil
Eryvaldo Sócrates Tabosa do Egito
Graduate Program in Health Sciences, Federal University of Rio Grande do Norte (UFRN), Natal 59.072-570, Brazil
Matheus de Freitas Fernandes-Pedrosa
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Kleber Juvenal Silva Farias
Department of Clinical Analysis and Toxicology, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Arnóbio Antônio da Silva-Júnior
Laboratory of Pharmaceutical Technology and Biotechnology, Department of Pharmacy, Federal University of Rio Grande do Norte, UFRN, Gal. Gustavo Cordeiro de Farias, Petrópolis, Natal 59.072-570, Brazil
Chloroquine diphosphate (CQ) is a hydrophilic drug with low entrapment efficiency in hydrophobic nanoparticles (NP). Herpes simplex virus type 1 (HSV-1) is an enveloped double-stranded DNA virus worldwide known as a common human pathogen. This study aims to develop chloroquine-loaded poly(lactic acid) (PLA) nanoparticles (CQ-NP) to improve the chloroquine anti- HSV-1 efficacy. CQ-NP were successfully prepared using a modified emulsification-solvent evaporation method. Physicochemical properties of the NP were monitored using dynamic light scattering, atomic force microscopy, drug loading efficiency, and drug release studies. Spherical nanoparticles were produced with modal diameter of <300 nm, zeta potential of −20 mv and encapsulation efficiency of 64.1%. In vitro assays of CQ-NP performed in Vero E6 cells, using the MTT-assay, revealed different cytotoxicity levels. Blank nanoparticles (B-NP) were biocompatible. Finally, the antiviral activity tested by the plaque reduction assay revealed greater efficacy for CQ-NP compared to CQ at concentrations equal to or lower than 20 µg mL−1 (p < 0.001). On the other hand, the B-NP had no antiviral activity. The CQ-NP has shown feasible properties and great potential to improve the antiviral activity of drugs.
