by Keyword: Peg-modified liposomes
Caddeo, C, Nigro, I, Chiummiento, L, Funicello, M, Lupattelli, P, Santarsiere, A, Fernàndez-Busquets, X, Valenti, D, Rosa, E, Miglionico, R, Armentano, MF, Vassallo, A, (2025). A novel aminohydroxy sulfonamide formulated in PEGylated liposomes with potential antitumor activity Journal Of Drug Delivery Science And Technology 106, 106739 
Cancer ranks as a leading cause of death worldwide, with liver cancer being one of the most commonly diagnosed. Currently, several molecules are being studied in order to find new therapeutic options that can reduce cancer recurrence rate and increase patient survival. This study proposes PEGylated liposomes for the delivery of a newly synthesized aminohydroxy sulfonamide, BupM-NH2, which has shown dose-dependent cytotoxicity towards hepatic tumor cells. The prepared PEG-liposomes were nanosized, spherical, and unilamellar, as shown by light scattering data and cryo-TEM micrographs. The physical stability of the PEG-liposomes was preserved when tested in simulated body fluids. Similar results were found for the storage stability evaluation. Furthermore, the PEG-liposomes efficiently entrapped BupM-NH2 and modulated its release. The antitumor activity of BupM-NH2 in PEG-liposomes was assessed in vitro in hepatocarcinoma cells. The viability assay showed that PEG-liposomes were able to control the release of BupM-NH2 over time and induce the death of HepG2 cells at a concentration about two-times lower than that required by free BupM-NH2 (IC50: 33.31 vs. 57.05 mu M). Furthermore, the liposomal formulation showed a less cytotoxic effect against non-cancerous cell line (IHH) compared to the free molecule (IC50 > 200 vs. 106.9 mu M), encouraging further investigation to confirm its effective and safe use.
JTD Keywords: Aminohydroxy sulfonamide, Anticancer formulation, Cancer, Delivery-systems, Drug-delivery, Hepatic cancer cells, Parenteral delivery, Peg-modified liposomes, Pegylated liposomes, Stability
Caddeo, Carla, Pucci, Laura, Gabriele, Morena, Carbone, Claudia, Fernàndez-Busquets, Xavier, Valenti, Donatella, Pons, Ramon, Vassallo, Antonio, Fadda, Anna Maria, Manconi, Maria, (2018). Stability, biocompatibility and antioxidant activity of PEG-modified liposomes containing resveratrol International Journal of Pharmaceutics 538, (1), 40-47
The present investigation reports the development of PEG-modified liposomes for the delivery of naturally occurring resveratrol. PEG-modified liposomes were prepared by direct sonication of the phospholipid aqueous dispersion, in the presence of two PEG-surfactants. Small, spherical, unilamellar vesicles were produced, as demonstrated by light scattering, cryo-TEM, and SAXS. The aging of the vesicles was assessed by using the Turbiscan® technology, and their physical stability was evaluated in vitro in simulated body fluids, results showing that the key features of the liposomes were preserved. The biocompatibility of the formulations was demonstrated in an ex vivo model of hemolysis in human erythrocytes. Further, the incorporation of resveratrol in PEG-modified liposomes did not affect its intrinsic antioxidant activity, as DPPH radical was almost completely inhibited, and the vesicles were also able to ensure an optimal protection against oxidative stress in an ex vivo human erythrocytes-based model. Therefore, the proposed PEG-modified liposomes, which were prepared by a simple and reliable method, represent an interesting approach to safely deliver resveratrol, ensuring the preservation of the carrier structural integrity in the biological fluids, and the antioxidant efficacy of the polyphenol to be exploited against oxidative stress associated with cancer.
JTD Keywords: Resveratrol, Antioxidant, PEG-surfactants, PEG-modified liposomes, Human erythrocytes
