Designing structural features of novel benznidazole-loaded cationic nanoparticles for inducing slow drug release and improvement of biological efficacy

Santos-Silva, Alaine M. dos; Caland, Lilia Basílio de; Oliveira, Ana Luiza C. de S. L.; Araújo-Júnior, Raimundo F. de; Fernandes-Pedrosa, Matheus de Freitas; Cornélio, Alianda Maira; Silva-Júnior, Arnóbio Antônio da

doi:10.1016/j.msec.2017.04.053

Cited by 27 publications

(17 citation statements)

References 51 publications

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“…Considering the emulsification-solvent evaporation method, the EE% level superior to 60% is considered excellent, which induced a slow drug release profile adjusted by the parabolic diffusion mathematical model ( r ≥ 0.95) (Table 2). This fact suggested a diffusion-controlled transport of CQ from the polymeric matrix of NP [43]. In addition, it is important to note that, on the best of our knowledge, no data in the literature describes the slow chloroquine release from PLA nanoparticles.…”

Section: Discussionmentioning

confidence: 99%

“…This ability of colloidal nanocarriers to preserve the entrapped drug into the polymeric matrix is a promising characteristic for drug targeting intended for specific affected cell or tissue, mainly considering the internalization of nanoparticles by endocytosis [43,56,57].…”

Section: Discussionmentioning

confidence: 99%

“…The pairwise comparisons of the analytical data were performed using the Student’s t-test. For the antiviral assay and cell viability, the multiple comparisons were performed using analysis of variance (ANOVA) at p = 0.05 significance level, followed by Bonferroni’s test and Dunnett’s test [43,44].…”

Section: Methodsmentioning

confidence: 99%

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Improving Encapsulation of Hydrophilic Chloroquine Diphosphate into Biodegradable Nanoparticles: A Promising Approach against Herpes Virus Simplex-1 Infection

et al. 2018

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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.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Improving Encapsulation of Hydrophilic Chloroquine Diphosphate into Biodegradable Nanoparticles: A Promising Approach against Herpes Virus Simplex-1 Infection

et al. 2018

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“…The preparation of monodisperse colloidal systems (PDI < 0.2) is important to predict their behavior and interaction with biological surfaces, mainly the capacity to overcome biological membranes [ 40 , 41 ]. Generally, the size of SLN ranges from 100 to 400 nm, yet negative zeta potential values between −20 and −40 mV were observed due to the nature of lipids used [ 42 , 43 ].…”

Section: Resultsmentioning

confidence: 99%

Phytol-Loaded Solid Lipid Nanoparticles as a Novel Anticandidal Nanobiotechnological Approach

et al. 2020

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Phytol is a diterpene alcohol and can be found as a product of the metabolism of chlorophyll in plants. This compound has been explored as a potential antimicrobial agent, but it is insoluble in water. In this study, we describe a novel approach for an interesting anticandidal drug delivery system containing phytol. Different formulations of phytol-loaded solid lipid nanoparticles (SLN) were designed and tested using a natural lipid, 1,3-distearyl-2-oleyl-glycerol (TG1). Different compositions were considered to obtain three formulations with 1:10, 1:5, and 1:3 w/w phytol/TG1 ratios. All the formulations were prepared by emulsification solvent evaporation method and had their physicochemical properties assessed. The biocompatibility assay was performed in the HEK-293 cell line and the antifungal efficacy was demonstrated in different strains of Candida ssp., including different clinical isolates. Spherical and uniform SLN (<300 nm, PdI < 0.2) with phytol-loading efficiency >65% were achieved. Phytol-loaded SLN showed a dose-dependent cytotoxic effect in the HEK-293 cell line. The three tested formulations of phytol-loaded SLN considerably enhanced the minimal inhibitory concentration of phytol against 15 strains of Candida spp. Considering the clinical isolates, the formulations containing the highest phytol/TG1 ratios showed MICs at 100%. Thus, the feasibility and potential of phytol-loaded SLN was demonstrated in vitro, being a promising nanocarrier for phytol delivery from an anticandidal approach.

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“…Mechanistically, the nitro group of BNZ is reduced in cells to an amino group, which produces ROS and subsequently induces cell apoptosis [3,4]; therefore, it may also be a potential anticancer drug. Recently, we demonstrated the improved biological efficacy of BNZ in human HT-29 colorectal cancer cells through the use of stable, biocompatible, and small-sized cationic nanoparticles (NPs) [5].…”

Section: Introductionmentioning

confidence: 99%

Self-Assembled Benznidazole-Loaded Cationic Nanoparticles Containing Cholesterol/Sialic Acid: Physicochemical Properties, In Vitro Drug Release and In Vitro Anticancer Efficacy

Santos-Silva

Caland

Nascimento

et al. 2019

IJMS

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Cationic polymeric nanoparticles (NPs) have the ability to overcome biological membranes, leading to improved efficacy of anticancer drugs. The modulation of the particle-cell interaction is desired to control this effect and avoid toxicity to normal cells. In this study, we explored the surface functionalization of cationic polymethylmethacrylate (PMMA) NPs with two natural compounds, sialic acid (SA) and cholesterol (Chol). The performance of benznidazole (BNZ) was assessed in vitro in the normal renal cell line (HEK-293) and three human cancer cell lines, as follows: human colorectal cancer (HT-29), human cervical carcinoma (HeLa), and human hepatocyte carcinoma (HepG2). The structural properties and feasibility of NPs were evaluated and the changes induced by SA and Chol were determined by using multiple analytical approaches. Small (<200 nm) spherical NPs, with a narrow size distribution and high drug-loading efficiency were prepared by using a simple and reproducible emulsification solvent evaporation method. The drug interactions in the different self-assembled NPs were assessed by using Fourier transform-infrared spectroscopy. All formulations exhibited a slow drug-release profile and physical stability for more than 6 weeks. Both SA and Chol changed the kinetic properties of NPs and the anticancer efficacy. The feasibility and potential of SA/Chol-functionalized NPs has been demonstrated in vitro in the HEK-293, HepG2, HeLa, and HT-29 cell lines as a promising system for the delivery of BNZ.

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Designing structural features of novel benznidazole-loaded cationic nanoparticles for inducing slow drug release and improvement of biological efficacy

Cited by 27 publications

References 51 publications

Improving Encapsulation of Hydrophilic Chloroquine Diphosphate into Biodegradable Nanoparticles: A Promising Approach against Herpes Virus Simplex-1 Infection

Improving Encapsulation of Hydrophilic Chloroquine Diphosphate into Biodegradable Nanoparticles: A Promising Approach against Herpes Virus Simplex-1 Infection

Phytol-Loaded Solid Lipid Nanoparticles as a Novel Anticandidal Nanobiotechnological Approach

Self-Assembled Benznidazole-Loaded Cationic Nanoparticles Containing Cholesterol/Sialic Acid: Physicochemical Properties, In Vitro Drug Release and In Vitro Anticancer Efficacy

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