Boškov Ivana A, Savić Ivan M, Grozdanić Stanisavljević Nađa Đ, Kundaković-Vasović Tatjana D, Radović Selgrad Jelena S, Savić Gajić Ivana M
Faculty of Technology in Leskovac, University of Nis, Bulevar oslobodjenja 124, 16000 Leskovac, Serbia.
Institute for Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia.
Polymers (Basel). 2024 Mar 2;16(5):688. doi: 10.3390/polym16050688.
Black locust flower extract contains various polyphenols and their glucosides contribute to the potential health benefits. After intake of these bioactive compounds and passage through the gastrointestinal tract, their degradation can occur and lead to a loss of biological activity. To overcome this problem, the bioactive compounds should be protected from environmental conditions. This study aimed to encapsulate the black flower extract in the microparticles based on biodegradable polysaccharides, alginate, and chitosan. In the extract, the total antioxidant content was found to be 3.18 ± 0.01 g gallic acid equivalent per 100 g of dry weight. Also, the presence of lipids (16), phenolics (27), organic acids (4), L-aspartic acid derivative, questinol, gibberellic acid, sterol, and saponins (2) was confirmed using the UHPLC-ESI-MS analysis. In vitro assays showed that the extract has weak anti--glucosidase activity and moderate antioxidant and cytotoxic activity against the HeLa cell line. The extrusion method with secondary air flow enabled the preparation of microparticles (about 270 μm) encapsulated with extract. An encapsulation efficiency of over 92% was achieved in the alginate and alginate-chitosan microparticles. The swelling study confirmed a lower permeability of alginate-chitosan microparticles compared with alginate microparticles. For both types of microparticles, the release profile of antioxidants in the simulated gastrointestinal fluids at 37 °C followed the Korsmeyer-Peppas model. A lower diffusion coefficient than 0.5 indicated the simple Fick diffusion of antioxidants. The alginate-chitosan microparticles enabled a more sustained release of antioxidants from extract compared to the alginate microparticles. The obtained results indicated an improvement in the antioxidant activity of bioactive compounds from the extract and their protection from degradation in the simulated gastric conditions via encapsulation in the polymer matrixes. Alginate-chitosan showed slightly slower cumulative antioxidant release from microparticles and better antioxidant activity of the extract compared to the alginate system. According to these results, alginate-chitosan microparticles are more suitable for further application in the encapsulation of black locust flower extract. Also, the proposed polymer matrix as a drug delivery system is safe for human use due to its biodegradability and non-toxicity.
刺槐花花提取物含有多种多酚类物质，其糖苷对潜在的健康益处有贡献。摄入这些生物活性化合物并通过胃肠道后，它们可能会发生降解并导致生物活性丧失。为克服这一问题，生物活性化合物应受到环境保护。本研究旨在基于可生物降解的多糖、海藻酸盐和壳聚糖，将刺槐花花提取物包封在微粒中。在提取物中，发现总抗氧化剂含量为每100克干重3.18±0.01克没食子酸当量。此外，使用超高效液相色谱-电喷雾电离质谱分析确认了脂质（16种）、酚类（27种）、有机酸（4种）、L-天冬氨酸衍生物、喹诺酮、赤霉素、甾醇和皂苷（2种）的存在。体外试验表明，该提取物对HeLa细胞系具有较弱的抗葡萄糖苷酶活性、中等的抗氧化和细胞毒性活性。采用二次气流挤压法可制备包封有提取物的微粒（约270μm）。海藻酸盐和海藻酸盐-壳聚糖微粒的包封效率超过92%。溶胀研究证实，与海藻酸盐微粒相比，海藻酸盐-壳聚糖微粒的渗透性较低。对于这两种类型的微粒，37℃下模拟胃肠液中抗氧化剂的释放曲线遵循Korsmeyer-Peppas模型。低于0.5的扩散系数表明抗氧化剂的简单菲克扩散。与海藻酸盐微粒相比，海藻酸盐-壳聚糖微粒能使提取物中的抗氧化剂更持续地释放。所得结果表明，提取物中生物活性化合物的抗氧化活性有所提高，并且通过包封在聚合物基质中，它们在模拟胃液条件下能免受降解。与海藻酸盐体系相比，海藻酸盐-壳聚糖显示出从微粒中累积抗氧化剂释放略慢，且提取物的抗氧化活性更好。根据这些结果，海藻酸盐-壳聚糖微粒更适合进一步应用于刺槐花花提取物的包封。此外，所提出的聚合物基质作为药物递送系统，因其可生物降解性和无毒性，对人体使用是安全的。
