Publication:
FUNCTIONAL PROPERTIES AND STABILITY OF RESVERATROL LOADED SPAN 60 / TWEEN 60 BASED NIOSOMES WITH VITAMIN D AS VESICULAR STABILISER

Date
2024
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IMU University
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Abstract
Resveratrol (RSV) is an essential non-flavonoid polyphenolic compound that is frequently present in numerous botanical species. RSV exhibits properties that are associated with anticancer, antioxidant, anti-inflammatory, and cardioprotective effects. Nevertheless, the systemic absorption of the substance is constrained as a result of its lowered water solubility, which consequently reduces its oral bioavailability and its natural chemical instability. Using resveratrol as a model drug, resveratrol-loaded niosomes with two levels of RSV loading concentration (2 mg/mL and 4 mg/mL) were prepared by the thin-film hydration method with different molar ratios of Span 60 (SP 60) / Tween 60 (TW 60) mixed non-ionic surfactants to vitamin D3 (VD3) and to cholesterol (CHL) as vesicular stabiliser, respectively. Their physicochemical properties including shape, vesicle size, polydispersity index (PDI), zeta potential, and stability study, were characterized by zeta sizer and scanning electron microscopy (SEM), while encapsulation efficiency and drug release profile were measured by RP-HPLC and UV-vis spectrophotometer, respectively. It was found that the ratio of stabiliser-to-the mixed non-ionic surfactant and the RSV loading concentration affected particle sizes (125.5 nm to 934.2 nm), PDI (0.492 to 0.794), and zeta potential (-29.9 mV to -42.1 mV) to various extent, with niosomes prepared from resveratrol solution loading concentration of 2 mg/mL having more significant impact. Specifically, VD3-stablised resveratrol-loaded niosomes had a smaller mean particle size and a lower negative zeta potential value than CHL-stabilised ones, suggesting that the type of stabiliser and drug concentration affect the zeta potential but not the stability of the niosomes. The SEM images of selected VD3- stabilised niosomes (Formulation F3; 4 mg/mL RSV) exhibited a quasispherical surface shape, while the CHL-stabilised niosome (Formulation F3; 4 mg/mL RSV) showed a spherical shape. Although the RSV entrapment efficiency (%EE) of the VD3-stabilised niosomes were significantly lower compared with those of CHL-stabilised niosomes prepared at both RSV loading concentrations, the VD3-stabilised niosomes had significantly faster RSV release rate (64.1%) than CHL-stabilised niosomes (56.7%) at 12 hours (F2, RSV = 4 mg/mL loading conc). In the niosomal stability study, the VD3- stabilised niosomes have shown better stability when kept at 4°C than at 25°C over 90 days. Therefore, it can be concluded that VD3 performed better in enhancing favorable characteristics with regard to particle size, stability, and in vitro drug release rate, making it an appropriate replacement for CHL as a stabiliser.
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Resveratrol, Vitamin D, Biological Availability, Liposomes, Surface-Active Agents
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