Mohammadi Misagh, Karimi Mehrnaz, Raofie Farhad
Department of Analytical Chemistry and Pollutants, Shahid Beheshti University, Tehran, 1983969411, Iran.
Sci Rep. 2025 May 2;15(1):15386. doi: 10.1038/s41598-024-82018-1.
Sertraline is one of the drugs whose transport from the blood circulation to the brain is severely limited by the blood-brain barrier and it shows low bioavailability (44%). Liposomes can be an effective carrier for this drug and increase bioavailability. In this study, the synthesis of nanometer-sized liposomes containing sertraline hydrochloride is proposed using a technique called supercritical fluid expansion into aqueous solution (ESSAS). In this technique, phospholipid precipitation rates are controlled, and homogeneous liposomes with nanometer-sized dimensions can be created. The operational parameters were optimized using the response surface methodology (pressure drop: 29.9 MPa, collection time: 13.6 min, temperature: 40 °C), which showed that the optimal values for the encapsulation efficiency, mean size, and number of liposomes were 78.4%, 89.5 nm, and 85, respectively. Also, the drug release test showed that it takes 27 h for sertraline to be completely released from the liposomal suspension.
舍曲林是一种从血液循环转运至大脑会受到血脑屏障严重限制的药物，其生物利用度较低（44%）。脂质体可以成为这种药物的有效载体并提高生物利用度。在本研究中，建议使用一种名为超临界流体膨胀法（ESSAS）的技术来合成含有盐酸舍曲林的纳米级脂质体。在该技术中，磷脂沉淀速率受到控制，并且可以制备出尺寸为纳米级的均匀脂质体。使用响应面法对操作参数进行了优化（压降：29.9MPa，收集时间：13.6分钟，温度：40°C），结果表明，脂质体的包封率、平均粒径和数量的最佳值分别为78.4%、89.5nm和85。此外，药物释放试验表明，舍曲林从脂质体悬浮液中完全释放需要27小时。
