The present work aimed to investigate the suitability of polymeric nanoparticles (NPs) loaded with resveratrol (RES) for drug delivery to cochlear cells. RES-loaded NPs were prepared by a solvent-diffusion method without surfactant. The Box–Behnken design was used to study the effect of the formulation variables on the particle mean diameter (PMD), polydispersity index (PDI), zeta-potential (ζ), percent drug encapsulation efficiency (EE%), and ratio between NP size before and after freeze-drying (Sf/Si). The physicochemical stability of the RES-loaded NPs during freeze-drying was investigated using four well-known cryoprotectants (i.e., lactose, mannitol, sucrose, and trehalose) at different concentrations. The RES-loaded NPs were also characterized by powder X-ray diffraction (PXRD) and in vitro drug release studies. Finally, the in vitro toxicity of the synthesized NPs was evaluated on two cochlear cell lines: HEI-OC1 and SVK-1 cells. The optimal formulation (desirability: 0.86) had 135.5 ± 37.3 nm as PMD, 0.126 ± 0.080 as PDI, −26.84 ± 3.31 mV as ζ, 99.83 ± 17.59% as EE%, and 3.30 ± 0.92 as Sf/Si ratio. The PMD and PDI of the RES-loaded NPs were maintained within the model space only when trehalose was used at concentrations higher than 15% (w/v). Results from the in vitro cytotoxicity studies showed that blank NPs did not alter the viability of both cells lines, except for concentrations higher than 600 μg/mL. However, the cell viability was significantly decreased at high concentrations of native RES (>50 μM, p < 0.05) in both cell lines. Overall, the results suggested that the RES-loaded polymeric NPs could be a suitable template for cochlea antioxidant delivery and otoproctection.

Resveratrol-loaded nanocarriers: formulation, optimization, characterization and in vitro toxicity on cochlear cells / U.M. Musazzi, I. Youm, J.B. Murowchick, M.J. Ezoulin, B.C. Youan. - In: COLLOIDS AND SURFACES. B, BIOINTERFACES. - ISSN 0927-7765. - 118(2014), pp. 234-242. [10.1016/j.colsurfb.2014.03.054]

Resveratrol-loaded nanocarriers: formulation, optimization, characterization and in vitro toxicity on cochlear cells

U.M. Musazzi
Primo
;
2014

Abstract

The present work aimed to investigate the suitability of polymeric nanoparticles (NPs) loaded with resveratrol (RES) for drug delivery to cochlear cells. RES-loaded NPs were prepared by a solvent-diffusion method without surfactant. The Box–Behnken design was used to study the effect of the formulation variables on the particle mean diameter (PMD), polydispersity index (PDI), zeta-potential (ζ), percent drug encapsulation efficiency (EE%), and ratio between NP size before and after freeze-drying (Sf/Si). The physicochemical stability of the RES-loaded NPs during freeze-drying was investigated using four well-known cryoprotectants (i.e., lactose, mannitol, sucrose, and trehalose) at different concentrations. The RES-loaded NPs were also characterized by powder X-ray diffraction (PXRD) and in vitro drug release studies. Finally, the in vitro toxicity of the synthesized NPs was evaluated on two cochlear cell lines: HEI-OC1 and SVK-1 cells. The optimal formulation (desirability: 0.86) had 135.5 ± 37.3 nm as PMD, 0.126 ± 0.080 as PDI, −26.84 ± 3.31 mV as ζ, 99.83 ± 17.59% as EE%, and 3.30 ± 0.92 as Sf/Si ratio. The PMD and PDI of the RES-loaded NPs were maintained within the model space only when trehalose was used at concentrations higher than 15% (w/v). Results from the in vitro cytotoxicity studies showed that blank NPs did not alter the viability of both cells lines, except for concentrations higher than 600 μg/mL. However, the cell viability was significantly decreased at high concentrations of native RES (>50 μM, p < 0.05) in both cell lines. Overall, the results suggested that the RES-loaded polymeric NPs could be a suitable template for cochlea antioxidant delivery and otoproctection.
Resveratrol; Polymeric nanoparticles; Box-Behnken design; Trehalose; Ototoxicity
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
Article (author)
File in questo prodotto:
File Dimensione Formato  
1-s2.0-S0927776514001866-main.pdf

accesso riservato

Tipologia: Publisher's version/PDF
Dimensione 2.01 MB
Formato Adobe PDF
2.01 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/235708
Citazioni
  • ???jsp.display-item.citation.pmc??? 9
  • Scopus 31
  • ???jsp.display-item.citation.isi??? 29
social impact