Department of Pharmacy - Pharmaceutical Sciences, University of Bari "Aldo Moro", Via E. Orabona, 4, I-70125 Bari, Italy.
Department of Pharmacy - Pharmaceutical Sciences, University of Bari "Aldo Moro", Via E. Orabona, 4, I-70125 Bari, Italy.
Int J Pharm. 2021 Apr 15;599:120412. doi: 10.1016/j.ijpharm.2021.120412. Epub 2021 Mar 1.
Natural oils that are rich in biologically active polyunsaturated fatty acids have many health benefits but have insufficient bioavailability and may oxidize in the gastrointestinal tract. For these reasons and to improve the handling as well, the possibility of incorporating a natural oil, extracted from Serenoa Repens fruits (SR-oil), in alginate-based beads was investigated. SR-oil has been used from centuries in both traditional and modern medicine for various nutraceutical or therapeutic purposes such as, in both sexes, as a general tonic, for genitourinary problems, to increase sexual vigor, as a diuretic or to treat in male lower urinary tract symptoms and benign prostatic hyperplasia. In this study, alginate-based beads prepared by vibration technology, also known as prilling technique, were explored as SR-oil delivery systems. Twenty-seven different formulations (F1-F27) were produced starting from stable emulsions for the period of the production. The formulations having spheroid shape (sfericity factor <0.07), high formulation yield (>90%) and high encapsulation efficiency (EE% > 80) were selected for further characterizations. Gas chromatographic analysis revealed a high loading of lauric acid as principal component of SR-oil allowing to calculate the content of total fatty acids (>50%) into the beads. Swelling behavior and release features were also studied at different pH values. The swelling of the beads and their SR-oil release were negligible for the first 2 h in simulated gastric fluid (pH 1.2), and appreciable in simulated intestinal fluid (pH 6.8). The release data were fitted by various equations to define the release kinetic mechanism. In addition, the selected formulation (F16) was stable to the oxidation not only during the formulation process, but also after 3 months of storage at room temperature. In summary, these polynucleate alginate beads, produced by prilling technique, are promising systems for improving the intestinal specific delivery and bioavailability of health-promoting bioactive SR-oil.
天然油富含生物活性多不饱和脂肪酸，对健康有很多益处，但生物利用度不足，并且可能在胃肠道中氧化。出于这些原因，为了提高处理效果，研究了将天然油（从 Serenoa Repens 果实中提取的油，简称 SR 油）纳入藻酸盐珠中的可能性。几个世纪以来，SR 油一直被用于传统和现代医学，用于各种营养或治疗目的，例如，在两性中，作为一般补品，用于治疗泌尿生殖问题，提高性活力，作为利尿剂或治疗男性下尿路症状和良性前列腺增生。在这项研究中，通过振动技术（也称为制粒技术）制备的藻酸盐珠被探索作为 SR 油的递送系统。从生产期间的稳定乳液开始，制备了 27 种不同的配方（F1-F27）。选择具有球形形状（球形度因子 <0.07）、高配方产率（>90%）和高包封效率（EE%>80%）的制剂进行进一步的特性研究。气相色谱分析显示，SR 油的主要成分月桂酸的负载量很高，允许计算珠内总脂肪酸（>50%）的含量。还研究了在不同 pH 值下的溶胀行为和释放特征。在模拟胃液（pH 1.2）中，珠子的溶胀及其 SR 油的释放在前 2 小时内可以忽略不计，而在模拟肠液（pH 6.8）中则明显。通过各种方程拟合释放数据，以确定释放动力学机制。此外，所选配方（F16）不仅在配方过程中而且在室温下储存 3 个月后也稳定，不会发生氧化。总之，这些多核藻酸盐珠通过制粒技术生产，是改善健康促进生物活性 SR 油的肠道特异性递送和生物利用度的有前途的系统。
