Antimonial drugs entrapped into phosphatidylserine liposomes: physicochemical evaluation and antileishmanial activity

Borborema, Samanta Etel Treiger; Osso, João Alberto; Andrade, Heitor Franco de; Nascimento, N.

doi:10.1590/0037-8682-0041-2016

Cited by 13 publications

(4 citation statements)

References 33 publications

(38 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…In other words, the small unilamellar vesicles appear to increase partitioning to the bone marrow. Also, they increase the longevity of vesicles in circulation (Borborema et al., 2016 ). It was reported that nanocarriers smaller than 500 nm can penetrate the bloodstream efficiently (Priya & Iyer, 2020 ).…”

Section: Resultsmentioning

confidence: 99%

Development and optimization of curcumin analog nano-bilosomes using 2¹.3¹full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

et al. 2022

View full text Add to dashboard Cite

Curcumin (CU) is a natural polyphenolic phytoingredient. CU has anti-inflammatory, anti-oxidant, and anticancer activities. The poor solubility, bioavailability, and stability of CU diminish its clinical application. Hence, structural modification of CU is highly recommended. The CU analog; 3,5-bis(4-bromobenzylidene)-1-propanoylpiperidin-4-one (PIP) exhibited high stability, safety, and more potent antiproliferative activity against hepatocellular carcinoma. In the present study, nano-bilosomes (BLs) were formulated to augment PIP delivery and enhance its solubility. A 2 1 .3 1 full factorial design was adopted to prepare the synthesized PIP-loaded BLs. Optimized F4 showed a biphasic release pattern extended over 24 h, with EE%, ZP, and PS of 90.21 ± 1.0%, −27.05 ± 1.08 mV, and 111.68 ± 1.4 nm. PIP-loaded BLs were tested for safety against a non-cancerous cell line (Wi-38) and for anticancer activity against the Huh-7 human hepatocellular carcinoma cells and compared to the standard anticancer drug doxorubicin (Dox). The anticancer selectivity index of PIP-loaded BLs recorded 420.55 against Huh-7 liver cancer cells, markedly higher than a CU suspension (18.959) or the Dox (20.82). The antiproliferative activity of nano-encapsulated PIP was roughly equivalent to Dox. PIP-loaded BLs, showed enhanced drug solubility, and enhanced anticancer effect, with lower toxicity and higher selectivity against Huh-7 liver cancer cells, compared to the parent CU.

show abstract

Section: Resultsmentioning

confidence: 99%

Development and optimization of curcumin analog nano-bilosomes using 2¹.3¹full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

et al. 2022

View full text Add to dashboard Cite

show abstract

“…Studying the biodistribution of MA is easier when the drug is radioactive, but there are no antimony radioisotopes commercially available. As we previously described, irradiating the MA was the best choice by which to support this goal in in vivo studies [21,22,24,25]. The advantage of this procedure is that neutron irradiation of the stable antimony isotopes present in the MA formulation enables the detection and quantification of total antimony, but without distinguishing between the pentavalent and trivalent antimony species.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of neutron-irradiated meglumine antimoniate in Leishmania amazonensis-infected BALB/c mice

Borborema

Osso

Andrade

et al. 2019

J. Venom. Anim. Toxins incl. Trop. Dis

Self Cite

View full text Add to dashboard Cite

Background: Cutaneous leishmaniasis (CL) is a parasitic disease caused by the protozoan Leishmania spp. Pentavalent antimonial agents have been used as an effective therapy, despite their side effects and resistant cases. Their pharmacokinetics remain largely unexplored. This study aimed to investigate the pharmacokinetic profile of meglumine antimoniate in a murine model of cutaneous leishmaniasis using a radiotracer approach. Methods: Meglumine antimoniate was neutron-irradiated inside a nuclear reactor and was administered once intraperitoneally to uninfected and L . amazonensis -infected BALB/c mice. Different organs and tissues were collected and the total antimony was measured. Results: Higher antimony levels were found in infected than uninfected footpad (0.29% IA vs. 0.14% IA, p = 0.0057) and maintained the concentration. The animals accumulated and retained antimony in the liver, which cleared slowly. The kidney and intestinal uptake data support the hypothesis that antimony has two elimination pathways, first through renal excretion, followed by biliary excretion. Both processes demonstrated a biphasic elimination profile classified as fast and slow. In the blood, antimony followed a biexponential open model. Infected mice showed a lower maximum concentration (6.2% IA/mL vs. 11.8% IA/mL, p = 0.0001), a 2.5-fold smaller area under the curve, a 2.7-fold reduction in the mean residence time, and a 2.5-fold higher clearance rate when compared to the uninfected mice. Conclusions: neutron-irradiated meglumine antimoniate concentrates in infected footpad, while the infection affects antimony pharmacokinetics.

show abstract

“…In recent years, the tools offered by nanotechnology techniques have been applied to the development of new medicines through the handling of materials and/or nanocomposites due to their electrical, optical, magnetic and physicochemical properties, making them beneficial for medical, physical, optical and electronic applications [ 7 ]. With the advent of nanodrug technology, delivery systems based on liposomes, nanoemulsions, micelles and dendrimers conjugated to polymeric nanoparticles, solid lipid nanoparticles, metal nanoparticles, carbon nanotubes and drugs of interest (meglumine antimoniate, amphotericin and miltefosine, among others) [ 8 , 9 ] have shown excellent potential, with antileishmanial activity against Leishmania major [ 10 ], Leishmania infantum [ 11 ], Leishmania tropica [ 12 ], and Leishmania amazonensis [ 13 ].…”

Section: Introductionmentioning

confidence: 99%

AgNP-PVP-meglumine antimoniate nanocomposite reduces Leishmania amazonensis infection in macrophages

et al. 2021

View full text Add to dashboard Cite

Background Leishmaniasis is an infectious disease caused by parasites of the genus Leishmania and presents different clinical manifestations. The adverse effects, immunosuppression and resistant strains associated with this disease necessitate the development of new drugs. Nanoparticles have shown potential as alternative antileishmanial drugs. We showed in a previous study the biosynthesis, characterization and ideal concentration of a nanocomposite that promoted leishmanicidal activity. In the present study, we conducted a specific analysis to show the mechanism of action of AgNP-PVP-MA (silver nanoparticle–polyvinylpyrrolidone-[meglumine antimoniate (Glucantime®)]) nanocomposite during Leishmania amazonensis infection in vitro. Results Through ultrastructural analysis, we observed significant alterations, such as the presence of small vesicles in the flagellar pocket and in the extracellular membrane, myelin-like structure formation in the Golgi complex and mitochondria, flagellum and plasma membrane rupture, and electrodense material deposition at the edges of the parasite nucleus in both evolutive forms. Furthermore, the Leishmania parasite infection index in macrophages decreased significantly after treatment, and nitric oxide and reactive oxygen species production levels were determined. Additionally, inflammatory, and pro-inflammatory cytokine and chemokine production levels were evaluated. The IL-4, TNF-α and MIP-1α levels increased significantly, while the IL-17 A level decreased significantly after treatment. Conclusions Thus, we demonstrate in this study that the AgNP-PVP-MA nanocomposite has leishmanial potential, and the mechanism of action was demonstrated for the first time, showing that this bioproduct seems to be a potential alternative treatment for leishmaniasis.

show abstract

Antimonial drugs entrapped into phosphatidylserine liposomes: physicochemical evaluation and antileishmanial activity

Cited by 13 publications

References 33 publications

Development and optimization of curcumin analog nano-bilosomes using 2¹.3¹full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

Development and optimization of curcumin analog nano-bilosomes using 2¹.3¹full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

Pharmacokinetics of neutron-irradiated meglumine antimoniate in Leishmania amazonensis-infected BALB/c mice

AgNP-PVP-meglumine antimoniate nanocomposite reduces Leishmania amazonensis infection in macrophages

Contact Info

Product

Resources

About

Antimonial drugs entrapped into phosphatidylserine liposomes: physicochemical evaluation and antileishmanial activity

Cited by 13 publications

References 33 publications

Development and optimization of curcumin analog nano-bilosomes using 21.31full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

Development and optimization of curcumin analog nano-bilosomes using 21.31full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

Pharmacokinetics of neutron-irradiated meglumine antimoniate in Leishmania amazonensis-infected BALB/c mice

AgNP-PVP-meglumine antimoniate nanocomposite reduces Leishmania amazonensis infection in macrophages

Contact Info

Product

Resources

About

Development and optimization of curcumin analog nano-bilosomes using 2¹.3¹full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay

Development and optimization of curcumin analog nano-bilosomes using 2¹.3¹full factorial design for anti-tumor profiles improvement in human hepatocellular carcinoma:in-vitroevaluation,in-vivosafety assay