Diclofenac Loaded Biodegradable Nanoparticles as Antitumoral and Antiangiogenic Therapy

Souto, Eliana B.; Espina, Marta; García, María L.; Świtalska, Marta; Wietrzyk, Joanna; Gliszczyńska, Anna

doi:10.3390/pharmaceutics15010102

Cited by 6 publications

(4 citation statements)

References 51 publications

(72 reference statements)

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“…These values may be explained by an initial rapid release caused by the free Ca(OH) 2 located in the outer part of the NPs causing that K d value. Once the free Ca(OH) 2 is released, the release of Ca(OH) 2 from the inside of the NPs starts, allowing a prolonged and slow profile until the maximum release is reached (Esteruelas et al., 2023). Conversely, Ca(OH) 2 ‐NPs‐gel best fit was the Korsmeyer‐Peppas equation.…”

Section: Resultsmentioning

confidence: 99%

Calcium hydroxide‐loaded nanoparticles dispersed in thermosensitive gel as a novel intracanal medicament

Roig,

Halbaut,

Elmsmari

et al. 2024

Int Endodontic J

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AimDesign, produce and assess the viability of a novel nanotechnological antibacterial thermo‐sensible intracanal medicament This involves encapsulating calcium hydroxide (Ca(OH)2) within polylactic‐co‐glycolic acid (PLGA) nanoparticles (NPs) and dispersing them in a thermosensitive gel (Ca(OH)2‐NPs‐gel). In addition, perform in vitro and ex vivo assessments to evaluate tissue irritation and penetration capacity into dentinal tubules in comparison to free Ca(OH)2.MethodologyReproducibility of Ca(OH)₂‐NPs was confirmed by obtaining the average size of the NPs, their polydispersity index, zeta potential and entrapment efficiency. Moreover, rheological studies of Ca(OH)2‐NPs‐gel were carried out with a rheometer, studying the oscillatory stress sweep, the mean viscosity value, frequency and temperature sweeps. Tolerance was assessed using the membrane of an embryonated chicken egg. In vitro Ca(OH)2 release was studied by direct dialysis in an aqueous media monitoring the amount of Ca(OH)2 released. Six extracted human teeth were used to study the depth of penetration of fluorescently labelled Ca(OH)2‐NPs‐gel into the dentinal tubules and significant differences against free Ca(OH)2 were calculated using one‐way anova.ResultsCa(OH)2‐NPs‐gel demonstrated to be highly reproducible with an average size below 200 nm, a homogeneous NPs population, negative surface charge and high entrapment efficiency. The analysis of the thermosensitive gel allowed us to determine its rheological characteristics, showing that at 10°C gels owned a fluid‐like behaviour meanwhile at 37°C they owned an elastic‐like behaviour. Ca(OH)2‐NPs‐gel showed a prolonged drug release and the depth of penetration inside the dentinal tubules increased in the most apical areas. In addition, it was found that this drug did not produce irritation when applied to tissues such as eggs' chorialantoidonic membrane.ConclusionCalcium hydroxide‐loaded PLGA NPs dispersed in a thermosensitive gel may constitute a suitable alternative as an intracanal antibacterial medicament.

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Section: Resultsmentioning

confidence: 99%

Calcium hydroxide‐loaded nanoparticles dispersed in thermosensitive gel as a novel intracanal medicament

Roig,

Halbaut,

Elmsmari

et al. 2024

Int Endodontic J

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“…The dissociation constant (K d ) of APG-NLC was higher in both the slow and fast phases than in free APG (0.07 and 0.27 vs 0.02 h), thus indicating a prolonged release. 37 Moreover, the half-life results (t 1/2 ) showed that there was a burst release at the beginning during the fast phase of the formulation, but during the slow phase, it had a sustained release, with a t 1/2 value of 160.5 h. 50…”

Section: Biopharmaceutical Behaviourmentioning

confidence: 98%

“…To determine the antiangiogenic effects of APG-NLC, a modified chorioallantoic membrane (CAM) test was used. 37 It was carried out using fertilised chicken eggs incubated at 37 °C and 85 % humidity. A lateral window was opened on the eggshell on the third day of incubation, and after 24 h of stabilization, 40 µL of the sample were inoculated to the CAM.…”

Section: Antiangiogenic Capacitymentioning

confidence: 99%

Dually Active Apigenin-Loaded Nanostructured Lipid Carriers for Cancer Treatment

Bonilla-Vidal,

Świtalska,

Espina

et al. 2023

IJN

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Cancer is one of the major causes of death worldwide affecting more than 19 million people. Traditional cancer therapies have many adverse effects and often result in unsatisfactory outcomes. Natural flavones, such as apigenin (APG), have demonstrated excellent antitumoral properties. However, they have a low aqueous solubility. To overcome this drawback, APG can be encapsulated in nanostructured lipid carriers (NLC). Therefore, we developed dual NLC encapsulating APG (APG-NLC) with a lipid matrix containing rosehip oil, which is known for its anti-inflammatory and antioxidant properties. Methods: Optimisation, physicochemical characterisation, biopharmaceutical behaviour, and therapeutic efficacy of this novel nanostructured system were assessed. Results: APG-NLC were optimized obtaining an average particle size below 200 nm, a surface charge of −20 mV, and an encapsulation efficiency over 99%. The APG-NLC released APG in a sustained manner, and the results showed that the formulation was stable for more than 10 months. In vitro studies showed that APG-NLC possess significant antiangiogenic activity in ovo and selective antiproliferative activity in several cancer cell lines without exhibiting toxicity in healthy cells. Conclusion: APG-NLC containing rosehip oil were optimised. They exhibit suitable physicochemical parameters, storage stability for more than 10 months, and prolonged APG release. Moreover, APG-NLC were internalised inside tumour cells, showing the capacity to cause cytotoxicity in cancer cells without damaging healthy cells.

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“…Because the mechanism of the anti-inflammatory action of diclofenac and GCs is due to COX-2 and NF-kB inhibition, this could be one of the reasons for their cytotoxic effect on cancerous cells. Diclofenac has also antiangiogenic activity [ 25 ]. Similarly, glucocorticoids have both anti-inflammatory and antitumor activities [ 17 ].…”

Section: Introductionmentioning

confidence: 99%

Possible Participation of Adenine Nucleotide Translocase ANT1 in the Cytotoxic Action of Progestins, Glucocorticoids, and Diclofenac on Tumor Cells

Ulchenko,

Miloykovich,

Zemlyanaya

et al. 2023

Pharmaceutics

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A comparative analysis of the cytostatic effects of progestins (gestobutanoyl, megestrol acetate, amol, dienogest, and medroxyprogesterone acetate), glucocorticoids (hydrocortisone, dexamethasone), and diclofenac on tumor cells was carried out in order to confirm their in silico predicted probabilities experimentally. The results showed the different sensitivity of HeLa, MCF-7, Hep-2, K-562, and Wi-38 cell lines to progestins, glucocorticoids, and diclofenac. The minimum IC50 was found for progestin gestobutanoyl (GB) as 18 µM for HeLa cells, and varied from 31 to 38 µM for MCF-7, Hep-2, and K-562. Glucocorticoids and diclofenac were much less cytotoxic in the HeLa, MCF-7, and Hep-2 cell lines than progestins, with IC50 values in the range of 150–3000 μM. Myelogenous leukemia K-562 cells were the least sensitive to the action of progestins and glucocorticoids but the most sensitive to diclofenac, which showed a pronounced cytotoxic effect with an IC50 of 31 μM. As we have shown earlier, progestins can uniquely modulate MPTP opening via the binding of adenine nucleotide translocase. On this basis, we evaluated the expression of adenylate nucleotide translocase ANT1 (SLC25 A4) as a possible participant in cytotoxic action in these cell lines after 48 h incubation with drugs. The results showed that progestins differently regulated ANT1 expression in different cell lines. Gestobutanoyl had the opposite effect on ANT1 expression in the HeLa, K562, and Wi-38 cells compared with the other progestins. It increased the ANT1 expression more than twofold in the HeLa and K562 cells but had no influence on the Wi-38 cells. Glucocorticoids and diclofenac increased ANT1 expression in the Wi-38 cells and decreased it in the K562, MCF-7, and Hep-2 cells. The modulation of ANT1 expression discovered in our study can be a new explanation of the cytotoxic and cytoprotective effects of hormones, which can vary depending on the cell type. ANT isoforms in normal and cancerous cells could be a new target for steroid hormone and anti-inflammatory drug action.

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Diclofenac Loaded Biodegradable Nanoparticles as Antitumoral and Antiangiogenic Therapy

Cited by 6 publications

References 51 publications

Calcium hydroxide‐loaded nanoparticles dispersed in thermosensitive gel as a novel intracanal medicament

Calcium hydroxide‐loaded nanoparticles dispersed in thermosensitive gel as a novel intracanal medicament

Dually Active Apigenin-Loaded Nanostructured Lipid Carriers for Cancer Treatment

Possible Participation of Adenine Nucleotide Translocase ANT1 in the Cytotoxic Action of Progestins, Glucocorticoids, and Diclofenac on Tumor Cells

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