Department of Pharmacy, Banasthali Vidyapith, Rajasthan, India.
Department of Pharmacy, SMS Medical College, Rajasthan, India.
J Microbiol Methods. 2019 Jun;161:18-27. doi: 10.1016/j.mimet.2019.04.001. Epub 2019 Apr 3.
Present study deals with the preparation, characterization and in-vivo evaluation of flurbiprofen loaded ethanolic liposome which provides predetermined and controlled release of drug through a transdermal drug delivery system. Ethanolic liposomes were prepared by using flurbiprofen, phospholipon 90-G, and ethanol in varied concentration ratio. The prepared ethanolic liposomes were optimized and characterized for particle size, zeta potential, polydispersive index and % entrapment efficiency. FTIR study was performed to analyze the interaction between drug and excipient. To study the thermal behavior of the formulation DSC and TGA were carried out. The surface morphology of ethanolic liposome was performed with the help of SEM, TEM, and AFM. In-vitro drug permeation study of the optimized formulation was carried out using the albino rat skin model and peripheral nociceptive activity was evaluated by writhing assay. In addition, formulations were also inspected for stability study for three months at a different temperature. The optimized formulation EF5 exhibited a particle size of 167.2 ± 3.7 nm with a zeta potential of -51.6 ± 0.2 mV and PDI of 0.209. The optimized formulation showed an ideal surface morphology with a maximum % entrapment efficiency i.e. 93.51 ± 2.1. In-vitro permeation study shows a release of 70.23% in 24 h and transdermal flux was found as 238.2 μg/cm/h. Writhing assay demonstrate that the optimized formulation decreases the number of writhes and thus shows the peripheral analgesic activity. In stability study, optimized formulation showed maximum stability at 4 °C. These results suggest that transdermal system mediated application of flurbiprofen loaded ethanolic liposome can be considered as an effective way to afford consistent and predictable release of flurbiprofen which could provide beneficial effects in the management of various inflammatory diseases.
本研究涉及制备、表征和体内评价氟比洛芬醇质体，通过透皮给药系统提供药物的预定和控制释放。乙醇脂质体通过使用氟比洛芬、磷脂 90-G 和不同浓度比的乙醇制备。对制备的乙醇脂质体进行了优化和粒径、Zeta 电位、多分散指数和%包封效率的表征。傅里叶变换红外光谱（FTIR）研究用于分析药物与赋形剂之间的相互作用。为了研究制剂的热行为，进行了差示扫描量热法（DSC）和热重分析（TGA）。使用 SEM、TEM 和 AFM 对乙醇脂质体的表面形态进行了研究。通过白化大鼠皮肤模型进行了优化制剂的体外药物渗透研究，并通过扭体试验评估了周围伤害感受活性。此外，还在不同温度下对制剂进行了三个月的稳定性研究。优化后的 EF5 制剂粒径为 167.2±3.7nm，Zeta 电位为-51.6±0.2mV，PDI 为 0.209。优化后的制剂具有理想的表面形态，最大包封效率为 93.51±2.1%。体外渗透研究显示，24 小时内释放 70.23%，透皮通量为 238.2μg/cm/h。扭体试验表明，优化后的制剂减少了扭体的数量，从而表现出外周镇痛活性。在稳定性研究中，优化后的制剂在 4°C 时表现出最大的稳定性。这些结果表明，氟比洛芬醇质体经皮给药系统可以作为一种有效的方法，提供氟比洛芬的持续和可预测释放，从而为各种炎症性疾病的治疗提供有益效果。
