Barbosa Raquel de Melo, Leite Aliana Monteiro, García-Villén Fátima, Sánchez-Espejo Rita, Cerezo Pilar, Viseras César, Faccendini Angela, Sandri Giuseppina, Raffin Fernanda Nervo, Moura Túlio Flávio Accioly de Lima E
Laboratory of Drug Development, Department of Pharmacy, Federal University of Rio Grande do Norte, Natal 59012-570, Brazil.
Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Campus of Cartuja s/n, 18071 Granada, Spain.
Pharmaceutics. 2022 May 17;14(5):1067. doi: 10.3390/pharmaceutics14051067.
Nanocomposites formed by clay and lipid carriers (NLCs) show a high potential for providing controlled release and specific delivery of bioactive molecules and have recently gained attention in the pharmaceutical sector due to their ability to transport hydrophilic and hydrophobic drugs. Recent studies have recognized the biological activity of the oil of Bixa orellana L. (AO) with regards to its healing, antioxidant, antibacterial, and anti-leishmanial properties. Therefore, the purpose of this study is the preparation and characterization of hybrid systems based on lipid nanocarriers and laponite for the delivery of AO. NLCs were prepared by the fusion-emulsification method, using cetyl palmitate (CP) or myristyl myristate (MM), AO, and Poloxamer 188. The morphology, hydrodynamic diameters, zeta potential (ZP), polydispersity index (PDI), thermal analysis, X-ray diffraction analysis (XRD), viscosity behavior, and cytotoxicity testing of the hybrid systems were performed. The thermal study and X-ray diffraction analyses (XRD) revealed polymorphic structural changes compatible with the amorphization of the material. Rheological assays highlighted a typical pseudoplastic behavior in all systems (MM and CP with LAP). The hybrid systems’ morphology, size diameters, and PDIs were similar, preset spherical and monodisperse structures (≈200 nm; <0.3), without significant change up to sixty days. The ZP values differed from each other, becoming higher with increasing AO concentration. XEDS spectra and elemental X-ray maps show peaks of lipids (organic components, C and O) and inorganic components O, Mg, and Si. All samples showed cell viability above 60%. The results indicated a stable, biocompatible hybrid system that can be an alternative for topical application.
由粘土和脂质载体形成的纳米复合材料（NLCs）在提供生物活性分子的控释和特定递送方面具有很高的潜力，并且由于其能够运输亲水性和疏水性药物，最近在制药领域受到关注。最近的研究已经认识到红木（Bixa orellana L.）油（AO）在愈合、抗氧化、抗菌和抗利什曼原虫特性方面的生物活性。因此，本研究的目的是制备和表征基于脂质纳米载体和锂皂石的用于AO递送的混合系统。通过融合乳化法制备NLCs，使用棕榈酸十六酯（CP）或肉豆蔻酸肉豆蔻酯（MM）、AO和泊洛沙姆188。对混合系统进行了形态学、流体动力学直径、zeta电位（ZP）、多分散指数（PDI）、热分析、X射线衍射分析（XRD）、粘度行为和细胞毒性测试。热研究和X射线衍射分析（XRD）揭示了与材料非晶化相容的多晶结构变化。流变学分析突出了所有系统（MM和CP与LAP）中典型的假塑性行为。混合系统的形态、尺寸直径和PDI相似，呈现预设的球形和单分散结构（≈200nm；<0.3），长达60天无显著变化。ZP值彼此不同，随着AO浓度的增加而升高。XEDS光谱和元素X射线图显示了脂质（有机成分，C和O）以及无机成分O、Mg和Si的峰。所有样品的细胞活力均高于60%。结果表明该混合系统稳定且具有生物相容性，可作为局部应用的替代物。
