利用刚果五种植物的粗皂甙制备胶束纳米粒子并确定其特性

Pathy B. Lokole , Nadège K. Ngombe , Dave I. Motomba , Justin B. Safari , Michel K. Mpuza , Rui W.M. Krause , Paulin K. Mutwale , Christian I. Nkanga
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引用次数: 0

摘要

纳米粒子(NPs)在药物输送、免疫疗法、疫苗和诊断等医疗应用领域具有显著的先进性。这种多功能性部分归功于从多种来源定制 NPs 的潜力。值得注意的是,皂苷这种两亲性植物代谢产物在 NP 制剂中显示出巨大的前景。本研究利用从五种刚果植物中提取的皂苷粗馏分(SCFs)探索了胶束 NPs 的开发:这五种刚果植物分别是:Millettia laurentii、Penthaclethra eetveldeana、Schwenckia americana、Musa paradisiaca 和 Musa sapientum。通过光学显微镜对植物材料进行了组织学检查,而通过薄层色谱法进行的植物化学分析证实了 SCFs 中皂甙的存在和主要成分。我们使用酞菁-异噻嗪混合物(Pc-INH)作为疏水探针来确定 SCFs 的临界胶束浓度,并探索开发具有成本效益的皂基胶束(SBMs)的可行性。植物化学筛选表明,提取的 SCF 中含有皂苷和其他代谢物,如类黄酮、酚酸和花青素。动态光散射和透射电子显微镜分析表明形成了纳米尺寸的颗粒,特别是 P. eetveldeana 的 SBMs 具有显著的尺寸(157 nm,PDI 为 0.27,ZP 为 -4.01 mV)和球形。与纯皂苷配制的对照胶束(33%)相比,月桂树皂苷胶束对 Pc-INH 的封装效率更高(55%)。体外测试表明,月见草皂苷胶束对红细胞的安全性最好,溶血率为 10%,而散装 SCF 的溶血率为 150%。不过,SCFs 和 SBMs 之间存在显著差异(p < 0.0001)。仙人掌果 SBM 的释放曲线显示出与 pH 值相关的关系,这表明它具有刺激响应式给药的潜力。这项工作为在纳米技术中利用植物提取的粗皂甙奠定了基础,强调了它们的封装效率、控释潜力和生物相容性,为经济高效地生产高价值的生物医学 NPs 铺平了道路。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preparation and characterization of micellar nanoparticles using crude saponins from five Congolese plant species

Preparation and characterization of micellar nanoparticles using crude saponins from five Congolese plant species
Nanoparticles (NPs) have significantly advanced medical applications, including drug delivery, immunotherapy, vaccines, and diagnostics. This versatility is partly due to the potential of tailoring NPs from multiple sources. Notably, saponins, amphiphilic plant metabolites, have shown great promise in NP formulation. This study explored the development of micellar NPs using saponin crude fractions (SCFs) extracted from five Congolese plant species: Millettia laurentii, Penthaclethra eetveldeana, Schwenckia americana, Musa paradisiaca, and Musa sapientum. Plant materials were subjected to histological examination through optical microscopy, while phytochemical analyses by thin-layer chromatography confirmed the presence and predominance of saponins in the SCFs. We used a phthalocyanine-isoniazid hybrid (Pc-INH) as a hydrophobic probe to determine the critical micellar concentrations of SCFs and explore the feasibility of developing cost-effective saponin-based micelles (SBMs). Phytochemical screenings indicated saponins in the extracted SCF and other metabolites like flavonoids, phenolic acids, and anthocyanins. Dynamic light scattering and transmission electron microscopy analyses revealed the formation of nano-sized particles, particularly noting SBMs from P. eetveldeana with notable dimensions (157 ​nm, PDI of 0.27, and ZP of −4.01 ​mV) and spherical shape. The micelles from M. laurentii exhibited superior encapsulation efficiency for Pc-INH (55%) compared to control micelles formulated from pure saponin (33%). In vitro tests showed that M. paradisiaca SBMs have the best safety profile for red blood cells, with a 10% hemolysis rate compared to a 150% rate for bulk SCFs. However, there is a significant difference between SCFs and SBMs (p ​< ​0.0001). The release profiles of M. paradisiaca SBMs show a pH-dependent relationship, suggesting potential for stimuli-responsive drug delivery. This work lays the foundation for leveraging plant-derived crude saponins in nanotechnology, emphazising their encapsulation efficiency, controlled release potential, and biocompatibility, paving the way for the cost-effective production of high-value biomedical NPs.
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