Koleva Iskra Z, Kamenova Katya, Petrov Petar D, Tzachev Christo T
Faculty of Chemistry and Pharmacy, Sofia University "St. Kliment Ohridski", 1 J. Bourchier Blvd., 1164 Sofia, Bulgaria.
Institute of Polymers, Bulgarian Academy of Sciences, "Akad. G. Bonchev" Street, Bl. 103A, 1113 Sofia, Bulgaria.
Pharmaceuticals (Basel). 2025 Jun 23;18(7):944. doi: 10.3390/ph18070944.
: In this study, we present a green, scalable platform for the production of water-dispersible powders co-encapsulating the lipophilic bioactives curcumin (Cur) and eugenol (Eug) within the amphiphilic polymer Soluplus (SP) via low-temperature spray drying. : The amount of Cur (1%, 5%, and 10%) and Eug (5%, 10%, 15%, and 20%) was varied to achieve single- and double-loaded water-soluble powders with the maximum amount of active substances. The powders containing a higher loading of Cur, 5% and 10% (and Eug), were obtained from water/ethanol mixtures (2:1 and 5:1 / ratio), while the formulation with 1% of Cur was spray-dried by using water as a solvent. : By leveraging aqueous or aqueous-ethanolic feed systems, we achieved high loading of the bioactive substances-up to 10% Cur and 20% Eug (/)-while minimizing organic solvent use. Myo-inositol was incorporated as a stabilizing excipient to modulate particle morphology, improve powder flowability, and enhance redispersibility. Physicochemical characterization revealed nanoscale micellization (53-127 nm), amorphization of both actives as confirmed by XRD and DSC, and the absence of crystalline residue. Encapsulation efficiencies exceeded 95% for Cur and 93% for Eug. Dissolution tests demonstrated a rapid release from the 5% Cur/5% Eug formulation (>85% in 5 min), while higher-loaded single-formulations showed progressively slower release (up to 45 min). : This work demonstrates a robust and environmentally responsible encapsulation strategy, suitable for delivering poorly water-soluble phytochemicals with potential applications in oral nutraceuticals and pharmaceutical dosage forms.
在本研究中，我们展示了一个绿色、可扩展的平台，用于通过低温喷雾干燥在两亲性聚合物Soluplus（SP）中共同封装亲脂性生物活性成分姜黄素（Cur）和丁香酚（Eug）来生产水分散性粉末。改变Cur（1%、5%和10%）和Eug（5%、10%、15%和20%）的用量，以获得含有最大量活性物质的单负载和双负载水溶性粉末。含有较高Cur负载量（5%和10%，以及Eug）的粉末是从水/乙醇混合物（2:1和5:1/比例）中获得的，而含有1%Cur的制剂则以水为溶剂进行喷雾干燥。通过利用水性或水-乙醇进料系统，我们实现了生物活性物质的高负载量——高达10%的Cur和20%的Eug（/），同时将有机溶剂的使用降至最低。引入肌醇作为稳定赋形剂，以调节颗粒形态、改善粉末流动性并增强再分散性。物理化学表征显示形成了纳米级胶束（53-127nm），XRD和DSC证实两种活性成分均为非晶态，且无结晶残留。Cur的包封率超过95%，Eug的包封率超过93%。溶出试验表明，5%Cur/5%Eug制剂的释放速度很快（5分钟内>85%），而高负载的单制剂释放速度逐渐减慢（长达45分钟）。这项工作展示了一种稳健且对环境负责的封装策略，适用于递送水溶性差的植物化学物质，在口服营养保健品和药物剂型中具有潜在应用。
