Formulation of lipid core nanocapsules

Venturini, Cristina G.; Jäger, Eliézer; Oliveira, Catiúscia Padilha de; Bernardi, Andressa; Battastini, Ana Maria Oliveira; Guterres, Sílvia Stanisçuaski; Pohlmann, Adriana Raffin

doi:10.1016/j.colsurfa.2010.12.011

Cited by 156 publications

(122 citation statements)

References 42 publications

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“…This physical stability of formulations was also explained by the efficient particle size control, and the qualitative and quantitative optimization of the formulation components. 26 The absence of physical instability of the RH-loaded formulations reinforces our previous suggestion about the absence of drug crystals in these formulations.…”

supporting

confidence: 75%

“…Each formulation (20 mL) was scanned from the bottom to the top of the glass cell (25 mm diameter, 55 mm height) at time intervals of 5 minutes over 60 minutes at 25°C. 26 In vitro drug release study…”

Section: Physical Stabilitymentioning

confidence: 99%

“…34 However, recently, Jäger et al 35 and Venturini et al 26 showed that excessive oil may lead to simultaneous formation of polymeric nanocapsules and nanoemulsion. Furthermore, in order to reject the hypothesis that the higher numbers of particles in the nanocapsule suspensions of Eudragit ® RS100 were related to the formation of nanocrystals due to the presence of excessive raloxifene, scattering intensity and size distribution between NC-RS and RH-NC-RS were correlated.…”

mentioning

confidence: 99%

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Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells

Fontana

Beckenkamp

Buffon

et al. 2014

IJN

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Raloxifene hydrochloride (RH) is considered to be an antiproliferative agent of mammary tissue. The aim of this study was to investigate the effect of the encapsulation of RH in polymeric nanocapsules with anionic or cationic surface on its release profile and antiproliferative activity. They were prepared by interfacial deposition of preformed polymer, followed by wide physicochemical characterization. The in vitro RH release was assessed by the dialysis membrane method and the data analyzed by mathematical modeling. The antiproliferative effect on MCF-7 cell viability was investigated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay as well as by counting viable cells. They had high encapsulation efficiency, low polydispersity, and nanometric mean size. Nanocapsules prepared with Eudragit ® RS100 and Eudragit ® S100 presented positive and negative zeta potentials, respectively. Drug release studies demonstrated controlled release of RH from anionic nanocapsules, which could be explained due to a stronger interaction of the drug to these nanocapsules and the larger amount of entrapped drug. On the other hand, this control was not observed from cationic nanocapsules due to the larger amount of drug adsorbed onto their surface. MCF-7 cell viability studies and cell counting showed that RH-loaded Eudragit ® RS100 nanocapsules promote the best antiproliferative activity after 24 hours of treatment, whereas the best activity was observed for RH-loaded Eudragit ® S100 nanocapsules after 72 hours. Furthermore, the combined treatment of these formulations improved the antiproliferative effect during the entire treatment.

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supporting

confidence: 75%

Section: Physical Stabilitymentioning

confidence: 99%

mentioning

confidence: 99%

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Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells

Fontana

Beckenkamp

Buffon

et al. 2014

IJN

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“…The concentration of ingredients used to prepare the LNC was based on previous preformulation studies, which showed that the exclusive formation of LNC structures dispersed in water (without nanoemulsion or nanosphere contaminants) is reached at the mass proportions of SM:CCT:PCL of 1.0:4.0:2.6. 38,45 The process yielded colloidal dispersions without any phase separation after preparation. In this way, no centrifugation or filtration was needed to perform the physicochemical characterization of formulations.…”

Section: Results and Discussion Synthesis And Characterization Of Pclmentioning

confidence: 99%

Novel therapeutic mechanisms determine the effectiveness of lipid-core nanocapsules on melanoma models

Drewes¹,

Fiel²,

Bexiga³

et al. 2016

IJN

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Melanoma is a severe metastatic skin cancer with poor prognosis and no effective treatment. Therefore, novel therapeutic approaches using nanotechnology have been proposed to improve therapeutic effectiveness. Lipid-core nanocapsules (LNCs), prepared with poly(ε-caprolactone), capric/caprylic triglyceride, and sorbitan monostearate and stabilized by polysorbate 80, are efficient as drug delivery systems. Here, we investigated the effects of acetyleugenol-loaded LNC (AcE-LNC) on human SK-Mel-28 melanoma cells and its therapeutic efficacies on melanoma induced by B16F10 in C57B6 mice. LNC and AcE-LNC had z -average diameters and zeta potential close to 210 nm and -10.0 mV, respectively. CytoViva ® microscopy images showed that LNC and AcE-LNC penetrated into SK-Mel-28 cells, and remained in the cytoplasm. AcE-LNC in vitro treatment (18–90×10 9 particles/mL; 1 hour) induced late apoptosis and necrosis; LNC and AcE-LNC (3–18×10 9 particles/mL; 48 hours) treatments reduced cell proliferation and delayed the cell cycle. Elevated levels of nitric oxide were found in supernatant of LNC and AcE-LNC, which were not dependent on nitric oxide synthase expressions. Daily intraperitoneal or oral treatment (days 3–10 after tumor injection) with LNC or AcE-LNC (1×10 12 particles/day), but not with AcE (50 mg/kg/day, same dose as AcE-LNC), reduced the volume of the tumor; nevertheless, intraperitoneal treatment caused toxicity. Oral LNC treatment was more efficient than AcE-LNC treatment. Moreover, oral treatment with nonencapsulated capric/caprylic triglyceride did not inhibit tumor development, implying that nanocapsule supramolecular structure is important to the therapeutic effects. Together, data herein presented highlight the relevance of the supramolecular structure of LNCs to toxicity on SK-Mel-28 cells and to the therapeutic efficacy on melanoma development in mice, conferring novel therapeutic mechanisms to LNC further than a drug delivery system.

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“…[18][19][20][21] This new nanoparticulate system is referred to as lipid-core nanocapsules (LNC), and it has proved an interesting nanocarrier for indomethacin for the therapy of glioblastomas and the inflammation process, 22,23 as well as for methotrexate diethyl ester and tretinoin, which have been implicated in the reversion of tumor resistance. 24,25 Based on the promising properties of LNC as a new drug-delivery system, the aims of our investigations were to evaluate whether methotrexateloaded lipid-core nanocapsules (MTX-LNC) prepared in a liquid-dose form reduce proinflammatory and T-cell-derived cytokines on activated mononuclear cells derived from RA patients, even in functional MTX-resistant conditions, and whether the MTX-LNC are able to reduce inflammation at lower doses than an MTX solution in an experimental model of inflammatory arthritis. )…”

Section: Introductionmentioning

confidence: 99%

Methotrexate-loaded lipid-core nanocapsules are highly effective in the control of inflammation in synovial cells and a chronic arthritis model

Boechat¹,

Oliveira

Tarragô³

et al. 2015

IJN

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Background Rheumatoid arthritis (RA) is the most common autoimmune disease in the word, affecting 1% of the population. Long-term prognosis in RA was greatly improved following the introduction of highly effective medications such as methotrexate (MTX). Despite the importance of this drug in RA, 8%–16% of patients must discontinue the treatment because of adverse effects. Last decade, we developed a promising new nanocarrier as a drug-delivery system, lipid-core nanocapsules. Objective The aim of the investigation reported here was to evaluate if methotrexate-loaded lipid-core nanocapsules (MTX-LNC) reduce proinflammatory and T-cell-derived cytokines in activated mononuclear cells derived from RA patients and even in functional MTX-resistant conditions. We also aimed to find out if MTX-LNC would reduce inflammation in experimentally inflammatory arthritis at lower doses than MTX solution. Methods Formulations were prepared by self-assembling methodology. The adjuvant arthritis was induced in Lewis rats (AIA) and the effect on edema formation, TNF-α levels, and interleukin-1 beta levels after treatment was evaluated. Mononuclear cells obtained from the synovial fluid of RA patients during articular infiltration procedures were treated with MTX solution and MTX-LNC. For in vitro experiments, the same dose of MTX was used in comparing MTX and MTX-LNC, while the dose of MTX in the MTX-LNC was 75% lower than the drug in solution in in vivo experiments. Results Formulations presented nanometric and unimodal size distribution profiles, with D[4.3] of 175±17 nm and span of 1.6±0.2. Experimental results showed that MTX-LNC had the same effect as MTX on arthritis inhibition on day 28 of the experiment ( P <0.0001); however, this effect was achieved earlier, on day 21 ( P <0.0001), by MTX-LNC, and this formulation had reduced both TNF-α ( P =0.001) and IL-1α ( P =0.0002) serum levels by the last day of the experiment. Further, the MTX-LNC were more effective at reducing the cytokine production from mononuclear synovial cells than MTX. Conclusion The MTX-LNC were better than the MTX solution at reducing proinflammatory cytokines and T-cell-derived cytokines such as interferon-gamma and interleukin-17A. This result, combined with the reduction in the dose required for therapy, shows that MTX-LNC are a very promising system for the treatment of RA.

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Formulation of lipid core nanocapsules

Cited by 156 publications

References 42 publications

Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells

Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells

Novel therapeutic mechanisms determine the effectiveness of lipid-core nanocapsules on melanoma models

Methotrexate-loaded lipid-core nanocapsules are highly effective in the control of inflammation in synovial cells and a chronic arthritis model

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Formulation of lipid core nanocapsules

Cited by 156 publications

References 42 publications

Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells

Controlled release of raloxifene by nanoencapsulation: effect on in vitro antiproliferative activity of human breast cancer cells

Novel therapeutic mechanisms determine the effectiveness of lipid-core nanocapsules on melanoma models

Methotrexate-loaded lipid-core nanocapsules are highly effective in the control of inflammation in&nbsp;synovial cells and a chronic arthritis model

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Methotrexate-loaded lipid-core nanocapsules are highly effective in the control of inflammation in synovial cells and a chronic arthritis model