Title : Self-assembled synthesis of food-grade vitamin D3-loaded mixed T60/QS nanomicelles with enhanced delivery capability: Physico-chemical characterization, gastrointestinal digestion and release kinetics
Abstract:
Within contemporary nutrition trends, there is a growing focus on enhancing the stability and bioavailability of key bioactives compounds through the development of nanoencapsulation systems. One noteworthy approach is the synthesis of nanomicelles.
In this work, our objective relies on incorporating vitamin D3 (VD3) into nanomicelles. VD3 plays a crucial role in bone health, as deficiency (≤ 29 ng · mL-1) makes individuals susceptible to diseases such as cancer, type 2 diabetes, sarcopenia, etc [1]. To synthesize nanomicelles, we opted for Tween 60/quillaja saponin (T60/QS) as emulsifiers after evaluating them alongside other potential food-grade surfactants (Tween 80, 40 and 20 as synthetic surfactant and soy lecithin as natural one), considering parameters relative to size, zeta-potentical, polydispersity index and encapsulation efficiency (EE). The resulting amphiphilic surfactants self-assembled into nanomicelles that were satisfactorily monodispersed and spherical, with a particle size of 49.6 nm, polydispersity index: 0.34, zeta-potential of -32.6 mV and EE of 90%.
A comparative analysis was conducted between the synthesized nanocarrier and existing commercial nanomicelles and liposomes containing equivalent VD3 concentrations. These samples were exposed to UV light (365 nm) and heating at 80º for up to 30 hours. All nanocarriers demonstrated enhanced stability compared to free VD3, with liposomes exhibiting the highest stability, while the synthesized nanomicelles showed superior stability at 80º (cumulative degradation rate, CDR, 35%) compare to commercial nanomicelles (CDR 65 %).
Understanding the release pattern of bioactives from formulations is crucial, especially for modified and immediate release dosage forms. Various mathematical models were employed to analyze experiment data, including zero order, first order, Korsmeyer-Peppas, Higuchi, Weibull, Hixon Crowell and Beaker-Lonsdale models, enabling effective formulation design. Moreover, in vitro studies indicated that VD3NMs exhibit superior stability in simulated gastric fluid, with subsequent controlled release primarily occurring in simulated intestinal fluid [2]. T60/QS mixed micelles can effectively shield VD3 in acidic environments while facilitating sustained release, presenting practical advantages for VD3 protection an delivery in the food industry.
