Institut of Biosciences, Coastal Campus of São Vicente, Paulista State University-UNESP, São Vicente, São Paulo, Brazil.
Department of Pharmacy, Federal University of Piauí, Teresina, Brazil.
AAPS PharmSciTech. 2023 Oct 17;24(8):212. doi: 10.1208/s12249-023-02655-z.
Fridericia platyphylla (Cham.) L.G. Lohmann is a species native to the Brazilian cerrado, with promising bioactivity. The organic fraction of the roots is rich in unusual dimeric flavonoids, reported as potential candidates for cancer treatment. The exploration of these flavonoids is very important, considering their diverse biological activities and the need for innovative therapeutic options. This work aimed to develop and characterize a microemulsion loaded with a non-polar fraction (DCM). The constituents were chosen, and the pseudo-ternary diagram was constructed to determine the region of microemulsion formation. The microemulsions blank (ME), with 3% (ME3) and 5% (ME5) of fraction DCM, were characterized in terms of droplet size, zeta potential, and polydispersity index. Both MEs showed particle sizes <100 nm; only ME3 exhibited better values for polydispersity index and zeta potential and was therefore selected for further study. The organoleptic and physicochemical characteristics were evaluated, revealing limpidity and transparency typical of these microstructures, physiologically acceptable pH, refractive index of 1.42±0.01, and density of 1.017 g/cm±0.01. The stability tests showed good stability profiles even after exposure to extreme thermal conditions, with minimal changes in pH and the content of the incorporated fraction. The in vitro release study demonstrated that ME3 enabled the controlled release of the fraction, with a cumulative amount released over 60% within 6 h. Furthermore, fraction DCM and ME3 exhibited no toxicity in Tenebrio molitor larvae. The developed microemulsion exhibited excellent properties, so this study represents the first successful attempt to develop a formulation that incorporates the dimeric flavonoid fraction.
宽叶金锦香(Fridericia platyphylla (Cham.) L.G. Lohmann)是一种原产于巴西塞拉多的物种,具有有前景的生物活性。其根的有机部分富含不寻常的二聚类黄酮,被报道为癌症治疗的潜在候选药物。探索这些类黄酮非常重要,因为它们具有多样化的生物活性,并且需要创新的治疗选择。本工作旨在开发和表征一种负载非极性部分(DCM)的微乳液。选择了成分,并构建了伪三元相图以确定微乳液形成区域。微乳液空白(ME),含有 3%(ME3)和 5%(ME5)的 DCM 部分,从粒径、ζ 电势和多分散指数方面进行了表征。两种 ME 均表现出粒径 <100nm;只有 ME3 表现出更好的多分散指数和 ζ 电势值,因此被选为进一步研究。评估了感官和物理化学特性,显示出这些微结构的典型的清澈和透明、生理上可接受的 pH 值、折射率为 1.42±0.01 和密度为 1.017 g/cm±0.01。稳定性测试显示,即使在暴露于极端热条件下,也具有良好的稳定性,pH 值和所包含部分的含量变化最小。体外释放研究表明,ME3 能够实现部分的控制释放,在 6 小时内累积释放量超过 60%。此外,DCM 部分和 ME3 对黄粉虫幼虫均无毒性。所开发的微乳液表现出优异的性能,因此,本研究代表了首次成功尝试开发一种包含二聚类黄酮部分的配方。