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Biosurfactants as stabilizers of niclosamide nanocrystals: Enhancing stability, solubility, and cytotoxicity profiling

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Mol Pereira, Erika A. ; Santos, M. Soledade C. S. ; Minas da Piedade, Manuel E. ; Faria, Rafael de Oliveira ; de Souza, Gabriel Batista ; Lameu, Claudiana ; Barbosa, Eduardo Jose ; Bou-Chacra, Nadia A. ; Lourenco, Felipe Rebello ; Nonato Bezzon, Vinicius Danilo ; Carvalho, Flavio M. S. ; de Araujo, Gabriel L. B.
Número total de Autores: 12
Tipo de documento: Artigo Científico
Fonte: JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY; v. 100, p. 11-pg., 2024-08-27.
Resumo

Biosurfactants are surface-active compounds of biological origin, stable over a wide range of temperature, pH, and salinity. In this work, the ability of the biosurfactants rhamnolipid (RAM), sophorolipid (SOFO) and surfactin (SURF) to stabilize a nanocrystal suspension of niclosamide (NCL) in water, and to enhance the drug solubility were evaluated. The performances were compared with those of the synthetic surfactants tween 80 (TW) and soluplus (SOLU). Overall, RAM, SOFO, and SURF proved to be as effective as TW and SOFO in terms of NCL nanocrystal suspension stabilization. Formulations containing 3 % (w/w) surfactant exhibited the best stability at 4 degrees C and 25 degrees C. The three biosurfactants also led to an improvement of aqueous NCL solubility, even when a slurry of the micronized drug was used without nanocrystal formulation. The best performance was observed for the SURF 3 % (w/w) nanocrystal formulation (1157.48 mu g/mL), which released more than twice the amount of NCL compared to the best synthetic surfactant formulation (TW 3 % (w/w), 542.57 mu g/mL), and 622 times more than the pure solid drug (1.86 mu g/mL). Cell viability was not compromised by the surfactants alone, indicating that the formulation cytotoxic effect is related to the enhanced solubilization of NCL. Consistently, the NCL/ SURF formulation was the most effective, achieving a maximum cytotoxicity effect of 80 % at a concentration of 1000 nM, while the other formulations reached a maximum effect of 71 % at concentrations starting from 1500 nM. Nevertheless, when the balance between formulation stability, drug release enhancement, and cytotoxicity is considered the three biosurfactants studied in this work showed significant potential advantages relative to synthetic analogues that can be explored in pharmaceutical development. (AU)

Processo FAPESP: 22/11093-9 - Sinalização purinérgica na transição fenotípica de macrófagos associados a tumor (TAMs) e Células Tumorais Circulantes (CTCs) para metástase cerebral de Câncer de Mama
Beneficiário:Claudiana Lameu
Modalidade de apoio: Auxílio à Pesquisa - Regular
Processo FAPESP: 21/04769-3 - Sinalização purinérgica mediada por exossomos na plasticidade do microambiente tumoral e quimiorresistência do Neuroblastoma
Beneficiário:Rafael de Oliveira Faria
Modalidade de apoio: Bolsas no Brasil - Doutorado Direto
Processo FAPESP: 19/04998-2 - Formulações nanocristalinas e dispersões sólidas amorfas para a melhoria de terapias antitumorais
Beneficiário:Gabriel Lima Barros de Araujo
Modalidade de apoio: Auxílio à Pesquisa - Regular