Nimesulide-loaded nanoparticles for the potential coadjuvant treatment of prostate cancer

Huerta, Concepción; Aberturas, M.R.; Molpeceres, Jesús

doi:10.1016/j.ijpharm.2015.07.027

Cited by 18 publications

(16 citation statements)

References 34 publications

(31 reference statements)

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“…The increase in SLM permeation when formulated into the nanomicelles is attributable to the increased lipophilicity of the extract [56]. Mass balance was higher than 80% for all the experiments, indicating that the calculated Pe is useful for in vitro prediction [57].…”

Section: Resultsmentioning

confidence: 99%

Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

et al. 2019

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Two novel nanomicellar formulations were developed to improve the poor aqueous solubility and the oral absorption of silymarin. Polymeric nanomicelles made of Soluplus and mixed nanomicelles combining Soluplus with d-α-tocopherol polyethylene glycol 1000 succinate (vitamin E TPGS) were prepared using the thin film method. Physicochemical parameters were investigated, in particular the average diameter, the homogeneity (expressed as polydispersity index), the zeta potential, the morphology, the encapsulation efficiency, the drug loading, the critical micellar concentration and the cloud point. The sizes of ~60 nm, the narrow size distribution (polydispersity index ≤0.1) and the encapsulation efficiency >92% indicated the high affinity between silymarin and the core of the nanomicelles. Solubility studies demonstrated that the solubility of silymarin increased by ~6-fold when loaded into nanomicelles. Furthermore, the physical and chemical parameters of SLM-loaded formulations stored at room temperature and in refrigerated conditions (4 °C) were monitored over three months. In vitro stability and release studies in media miming the physiological conditions were also performed. In addition, both formulations did not alter the antioxidant properties of silymarin as evidenced by the 1,1-Diphenyl-2-picrylhydrazyl radical (DPPH) assay. The potential of the nanomicelles to increase the intestinal absorption of silymarin was firstly investigated by the parallel artificial membrane permeability assay. Subsequently, transport studies employing Caco-2 cell line demonstrated that mixed nanomicelles statistically enhanced the permeability of silymarin compared to polymeric nanomicelles and unformulated extract. Finally, the uptake studies indicated that both nanomicellar formulations entered into Caco-2 cells via energy-dependent mechanisms.

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Section: Resultsmentioning

confidence: 99%

Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

et al. 2019

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“…Nimesulide (4-nitro-2-phenoxymethanesulfonamide) (NiM) is a non-steroidal anti-inflammatory drug (NSAID), widely used to ameliorate acute pain [1,2]. Its mechanism of action is associated with the inhibition of the ciclo-oxigenase-2 (COX-2) isoform [3]. Like most of the NSAIDs, NiM shows low solubility in water, which limits its bioavailability in vivo [2].…”

Section: Introductionmentioning

confidence: 99%

Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

Campos

Fernandes

Sousa

et al. 2019

Pharmaceutical Development and Technology

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The aim of this work has been the development of a non-toxic, long-term stable solid lipid nanoparticles (SLN) formulation for the loading of Nimsulide (NiM) by a 2 2 factorial design. The optimized formulation was composed of 10 wt% of glyceryl behenate and 2.5 wt% of poloxamer 188. Immediately after production, Z-Ave of NiM-SLN was 166.1±0.114 nm, with a polydispersity index (PI) of 0.171±0051 and zeta potential nearly neutral (-3.10±0.166 mV). A slight increase of Z-Ave was recorded for NiM-SLN stored at 25ºC for a period of 15 days, whereas at 4ºC particles kept size within similar range. Long-term stability was monitored using TurbiscanLab®, showing a high stability of the nanoparticles with variations in the backscattering profiles below 10%. The release profile of NiM-SLN followed a sustained pattern with ca. 30% of drug released up to 24 h. Empty-SLN and NiM-SLN were non-toxic after exposing Caco-2 cells to the highest concentration (100 μg/mL) up to 48 hours (cell viability higher than 80%). NiM-SLN were lyophilized using different cryoprotectants, producing particles of 463.1±36.63 nm (PI 0.491±0.027) with 5% trehalose. Solid character of NiM-SLN was confirmed by DSC, recording a recrystallization index of 83% for NiM-SLN and of 74% for lyophilized SLN.

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“…Further preclinical examples include the development of PLGA nanoparticles loaded with nimesulide, a cyclooxygenase‐2 (COX‐2) inhibitor that generally presents with poor solubility, [ 127 ] and the encapsulation of EGCG in chitosan polysaccharide nanoparticle, which exhibited enhanced anti‐tumoral activity and the significant inhibition of PSA secretion when compared to free EGCG [ 128 ] ( Table 2 ).…”

Section: Nanomedicines For Advanced Prostate Cancer Treatmentmentioning

confidence: 99%

Nanomedicine for the Treatment of Advanced Prostate Cancer

Vicente‐Ruiz

Serrano‐Martí

Armiñán

et al. 2020

Advanced Therapeutics

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Current prostate cancer (PCa) treatment options include hormonal therapy, chemotherapy, immunotherapy, and radiotherapy; however, a lack of targeting and overall efficiency has failed to improve survival rates or reduce unwanted side‐effects in advanced stage PCa patients. The modification of existing therapeutics, including their reformulation as nanomedicines, can increase stability in plasma, enhance tumor targeting, and improve pharmacokinetics to foster improvements in patient outcomes. This review now describes those nanomedicinal approaches to advanced PCa treatment under evaluation in both preclinical and clinical studies. Despite the current advantages provided by nanomedicine in PCa treatment, there exists the opportunity to improve the design of novel therapeutic approaches. Therefore, this review also highlights the importance of identifying novel functional biomarkers to stratify patients and guide nanomedicinal design. Finally, the authors describe strategies employed to enhance the passive accumulation of nanomedicines in tumors and discuss the enormous potential of combination therapies that target tumor cells and the all‐important tumor microenvironment to reduce tumor growth and overcome therapeutic resistance.

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Nimesulide-loaded nanoparticles for the potential coadjuvant treatment of prostate cancer

Cited by 18 publications

References 34 publications

Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

Formulation of Nanomicelles to Improve the Solubility and the Oral Absorption of Silymarin

Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

Nanomedicine for the Treatment of Advanced Prostate Cancer

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