Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line

Nocca, Giuseppina; D’Avenio, Giuseppe; Amalfitano, Adriana; Chronopoulou, Laura; Mordente, Alvaro; Palocci, Cleofe; Grigioni, Mauro

doi:10.3390/ma14143893

Cited by 6 publications

(6 citation statements)

References 23 publications

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“…18β-glycyrrhetinic acid (GA) is a pentacyclic triterpene with promising hepatoprotective and anti-hepatocellular carcinoma effects. In reference [78], GA was encapsulated in core-shell NPs in order to overcome its low water solubility, which lowers its biodistribution and bioavailability, limiting its applications in biomedicine. The core-shell NPs were made of PolyD-L-lactide-co-glycolide (PLGA) coated with chitosan (CS), prepared through an osmosis-based methodology, to efficiently entrap GA.…”

Section: Drug/protein Delivery Systemsmentioning

confidence: 99%

Nanostructured Medical Devices: Regulatory Perspective and Current Applications

D’Avenio,

Daniele,

Grigioni

2024

Materials

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Nanomaterials (NMs) are having a huge impact in several domains, including the fabrication of medical devices (MDs). Hence, nanostructured MDs are becoming quite common; nevertheless, the associated risks must be carefully considered in order to demonstrate safety prior to their immission on the market. The biological effect of NMs requires the consideration of methodological issues since already established methods for, e.g., cytotoxicity can be subject to a loss of accuracy in the presence of certain NMs. The need for oversight of MDs containing NMs is reflected by the European Regulation 2017/745 on MDs, which states that MDs incorporating or consisting of NMs are in class III, at highest risk, unless the NM is encapsulated or bound in such a manner that the potential for its internal exposure is low or negligible (Rule 19). This study addresses the role of NMs in medical devices, highlighting the current applications and considering the regulatory requirements of such products.

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Section: Drug/protein Delivery Systemsmentioning

confidence: 99%

Nanostructured Medical Devices: Regulatory Perspective and Current Applications

D’Avenio,

Daniele,

Grigioni

2024

Materials

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“…However, at the same RZ concentration, NPR led to higher cell viability than free RZ. Since the cytotoxic effect of any active compound depends largely on its form of administration, we can infer that the encapsulation of RZ; thus, its controlled release decreases its cytotoxicity (56).…”

Section: Cell Viability Assessment and In Vitro Evaluation Of Antiher...mentioning

confidence: 99%

Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity

Solís-Cruz,

Alvarez-Roman,

Rivas-Galindo

et al. 2023

Acta Pharmaceutica

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Riolozatrione (RZ) is a diterpenoid compound isolated from a dichloromethane extract of the Jatropha dioica root. This compound has been shown to possess moderate antiherpetic activity in vitro. However, because of the poor solubility of this compound in aqueous vehicles, generating a stable formulation for potential use in the treatment of infection is challenging. The aim of this work was to optimize and physio-chemically characterize Eudragit® L100-55-based polymeric nanoparticles (NPs) loaded with RZ (NPR) for in vitro antiherpetic application. The NPs formulation was initially optimized using the dichloromethane extract of J. dioica, the major component of which was RZ. The optimized NPR formulation was stable, with a size of 263 nm, polydispersity index < 0.2, the zeta potential of –37 mV, and RZ encapsulation efficiency of 89 %. The NPR showed sustained release of RZ for 48 h with release percentages of 95 and 97 % at neutral and slightly acidic pH, respectively. Regarding in vitro antiherpetic activity, the optimized NPR showed a selectivity index for HSV-1 of ≈16 and for HSV-2 of 13.

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“…An advantage of the CS backbone is that it can be modified by many functional groups. Toward this aim, Nocca and coworkers tested the in vitro cytotoxic effect of GA-loaded PLGA-CS NPs (2:1 polymer:drug ratio) on human HCC HepG2 cells [ 44 ]. NPs were able to transport a higher amount of GA inside the cells than simple diffusion through the cell membrane.…”

Section: Ga-functionalized Polymer-based Ddssmentioning

confidence: 99%

“…However, not all of the GA carried by the NPs was immediately bioavailable since about 5% (after 2 h of incubation) of the GA was released into the cytoplasm. However, even if GA (500 µM) was unable to reach the cellular compartments in the encapsulated form with the same efficacy as the free form, its concentration was high enough to affect cellular viability to the same extent as free GA [ 44 ].…”

Section: Ga-functionalized Polymer-based Ddssmentioning

confidence: 99%

Recent Advances in Glycyrrhetinic Acid-Functionalized Biomaterials for Liver Cancer-Targeting Therapy

et al. 2022

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Liver cancer is one of the most common causes of cancer mortality worldwide. Chemotherapy and radiotherapy are the conventional therapies generally employed in patients with liver tumors. The major issue associated with the administration of chemotherapeutics is their high toxicity and lack of selectivity, leading to systemic toxicity that can be detrimental to the patient’s quality of life. An important approach to the development of original liver-targeted therapeutic products takes advantage of the employment of biologically active ligands able to bind specific receptors on the cytoplasmatic membranes of liver cells. In this perspective, glycyrrhetinic acid (GA), a pentacyclic triterpenoid present in roots and rhizomes of licorice, has been used as a ligand for targeting the liver due to the expression of GA receptors on the sinusoidal surface of mammalian hepatocytes, so it may be employed to modify drug delivery systems (DDSs) and obtain better liver or hepatocyte drug uptake and efficacy. In the current review, we focus on the most recent and interesting research advances in the development of GA-based hybrid compounds and DDSs developed for potential employment as efficacious therapeutic options for the treatment of hepatic cancer.

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Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line

Cited by 6 publications

References 23 publications

Nanostructured Medical Devices: Regulatory Perspective and Current Applications

Nanostructured Medical Devices: Regulatory Perspective and Current Applications

Formulation and optimization of polymeric nanoparticles loaded with riolozatrione: a promising nanoformulation with potential antiherpetic activity

Recent Advances in Glycyrrhetinic Acid-Functionalized Biomaterials for Liver Cancer-Targeting Therapy

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