Bioresponsive nanostructured systems for sustained naltrexone release and treatment of alcohol use disorder: Development and biological evaluation

Santos, Rogério Alexandre Scripnic Xavier dos; Rae, Mariana; Dartora, Vanessa Franco Carvalho; Matos, Jenyffer K.R. de; Camarini, Rosana; Lopes, Luciana B.

doi:10.1016/j.ijpharm.2020.119474

Cited by 11 publications

(11 citation statements)

References 83 publications

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“…This has been attributed to fluorochrome adsorption in the animal skin, which turned blue as shown in Figure . This retention was previously observed . Although in whole animal fluorescence images it was not possible to distinguish the fluorescence in the breast tissue from that on the skin, administration of the Alexa-loaded ME did not result in blue stains in the skin (Figure ).…”

Section: Resultssupporting

confidence: 78%

“…Percentages of water taken up by the formulation were fitted with three different kinetic models, and the results suggest that swelling can be better described by second-order kinetics ( R 2 = 0.9995), which is similar to the results with liquid-crystalline-based systems ,, and indicates that swelling speed decreases proportionally to its uptake capacity and to the area that did not interact with the aqueous component…”

Section: Resultssupporting

confidence: 62%

“…The experiments described in this section had three main objectives: to assess the rate of uptake of aqueous fluids, how fast the liquid-crystalline phase would be formed upon contact with these fluids, and if the selected ME would spread on the tissue immediately after administration or would be contained due to its fast transformation in the semi-solid system. , …”

Section: Methodsmentioning

confidence: 99%

“…This experiment aimed at assessing whether the selected ME formed a local depot that prolonged the release of a fluorescent marker. Alexa Fluor 647 was selected as the fluorescent marker because its emission wavelength is above 650 nm and thus is not subjected to interference of hair follicle autofluorescence . The Alexa Fluor-loaded ME (0.05%, w/w) was obtained by diluting the marker in the polar phase of the formulation.…”

Section: Methodsmentioning

confidence: 99%

“…Second, replacing water with propylene glycol (PG) and obtaining a non-aqueous ME improve fenretinide (a very lipophilic compound) solubilization . MEs, generally described as isotropic dispersions of two non-miscible liquids in combination with a surfactant blend, have other advantages, including low cost, thermodynamic stability, and easy obtainment. , Third, due to the low viscosity, parenteral administration of MEs is less problematic compared to gels …”

Section: Introductionmentioning

confidence: 99%

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Microemulsion for Prolonged Release of Fenretinide in the Mammary Tissue and Prevention of Breast Cancer Development

et al. 2021

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The need of pharmacological strategies to preclude breast cancer development motivated us to develop a non-aqueous microemulsion (ME) capable of forming a depot after administration in the mammary tissue and uptake of interstitial fluids for prolonged release of the retinoid fenretinide. The selected ME was composed of phosphatidylcholine/tricaprylin/propylene glycol (45:5:50, w/w/w) and presented a droplet diameter of 175.3 ± 8.9 nm. Upon water uptake, the ME transformed successively into a lamellar phase, gel, and a lamellar phase-containing emulsion in vitro as the water content increased and released 30% of fenretinide in vitro after 9 days. Consistent with the slow release, the ME formed a depot in cell cultures and increased fenretinide IC50 values by 68.3- and 13.2-fold in MCF-7 and T-47D cells compared to a solution, respectively. At non-cytotoxic concentrations, the ME reduced T-47D cell migration by 75.9% and spheroid growth, resulting in ∼30% smaller structures. The depot formed in vivo prolonged a fluorochrome release for 30 days without producing any sings of local irritation. In a preclinical model of chemically induced carcinogenesis, ME administration every 3 weeks for 3 months significantly reduced (4.7-fold) the incidence of breast tumors and increased type II collagen expression, which might contribute to limit spreading. These promising results support the potential ME applicability as a preventive therapy of breast cancer.

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Section: Resultssupporting

confidence: 78%