Rushmi Zerin T, Akter Nasrin, Mow Rabeya J, Afroz Merina, Kazi Mohsin, de Matas Marcel, Rahman Mahbubur, Shariare Mohammad H
Department of Pharmaceutical Sciences, North South University, Dhaka, Bangladesh.
Department of Pharmaceutics, King Saud University, Riyadh, Saudi Arabia.
Saudi Pharm J. 2017 Mar;25(3):404-412. doi: 10.1016/j.jsps.2016.09.011. Epub 2016 Oct 1.
This study aimed to formulate black seed oil () loaded liposomes using the ethanol injection method to enhance oral bioavailability and improve therapeutic activity in small animal studies of analgesia. The impact of formulation attributes and process parameters on the liposomal system was evaluated with key quality attributes being particle size, morphology, and entrapment efficiency. The particle size and entrapment efficiency of the liposome preparation were found to be between the range of 50-900 nm and 34-87% respectively. Particle size distribution data suggested that increasing the percentage of oil, up to a certain concentration, reduced the size of the liposomes significantly from 520 ± 81.2 nm to 51.48 ± 1.31 nm. Stirring and injection rate were shown to have marked impact on the average particle size of liposome. It was observed that entrapment efficiency of liposomes was greatly influenced by the amount of cholesterol and type of cryoprotectant used during formulation. The stability study indicated that the liposomal preparation was stable at ambient conditions for one month. studies showed that the liposomal preparation demonstrated significant analgesic activity in mice.
本研究旨在采用乙醇注入法制备载有黑种草子油的脂质体，以提高口服生物利用度，并在小动物镇痛研究中改善治疗活性。通过关键质量属性（粒径、形态和包封率）评估制剂属性和工艺参数对脂质体系统的影响。发现脂质体制剂的粒径和包封率分别在50 - 900 nm和34 - 87%的范围内。粒径分布数据表明，在一定浓度范围内增加油的百分比，可使脂质体的尺寸从520±81.2 nm显著减小至51.48±1.31 nm。搅拌和注入速率对脂质体的平均粒径有显著影响。观察到脂质体的包封率受配方中胆固醇用量和所用冷冻保护剂类型的极大影响。稳定性研究表明，脂质体制剂在环境条件下可稳定保存一个月。研究表明，该脂质体制剂在小鼠中表现出显著的镇痛活性。
