Department of Pharmaceutics, Sinhgad Technical Education Society's, Smt. Kashibai Navale College of Pharmacy, Pune, Maharashtra, India.
School of Pharmacy and Biomedical Sciences, The University of Newcastle, Newcastle, NSW 2308, Australia.
Drug Deliv Transl Res. 2016 Oct;6(5):511-8. doi: 10.1007/s13346-016-0296-9.
Proniosomes are the new generation provesicular drug delivery system of non-ionic surfactant, lecithin and cholesterol which upon reconstitution get converted into niosomes. The objective of current study was to develop stable and sustain transdermal delivery system for lornoxicam. Lornoxicam-loaded topically applied proniosomal gel was formulated, optimized, and evaluated with the aim to deliver drug transdermally. Lornoxicam-loaded proniosomal gels were prepared that contained Lutrol F68 and lecithin as surfactants, cholesterol as a stabilizer, and minimal amount of ethanol and trace water. The resultant lornoxicam-loaded proniosomal gel were assessed for stability and the proniosomes-derived niosomes were characterized for morphology, size, zeta potential, and entrapment efficiency, which revealed that they were suitable for skin application. The coacervation phase separation technique was used in formulation of lornoxicam proniosomal gel and the gel was further assessed for in vitro permeation of lornoxicam through the freshly excised rat skin and the cumulative permeation amount of lornoxicam from proniosome, all exhibited significant increase as compared to 1.0 % lornoxicam-loaded pure gel. The optimized F5 batch had shown maximum entrapment efficiency up to 66.98 %. It has shown sustained drug release for more than 24 h. The skin permeability of proniosomal gel was found to be 59.73 %. The SEM and zeta potential studies showed formation of good and stable vesicles. Thus, proniosomes proved to have better potential for transdermal delivery of lornoxicam over conventional gel formulations.
前体脂质体是新一代证明的非离子表面活性剂、卵磷脂和胆固醇的囊泡药物传递系统,在重新构成后转化为脂质体。本研究的目的是开发洛索洛芬的稳定和持续的透皮传递系统。制备了洛索洛芬经皮给药的前体脂质体凝胶,并对其进行了优化和评价,目的是经皮给药。洛索洛芬前体脂质体凝胶含有 Lutrol F68 和卵磷脂作为表面活性剂、胆固醇作为稳定剂以及少量乙醇和痕量水。评估了洛索洛芬前体脂质体凝胶的稳定性,并对前体脂质体衍生的脂质体进行了形态、粒径、Zeta 电位和包封效率的特征分析,结果表明它们适合皮肤应用。采用凝聚相分离技术制备洛索洛芬前体脂质体凝胶,并进一步评估洛索洛芬通过新鲜离体大鼠皮肤的体外渗透和前体脂质体中洛索洛芬的累积渗透量,与 1.0%洛索洛芬负载的纯凝胶相比均显著增加。优化的 F5 批显示最大包封效率高达 66.98%。它表现出超过 24 小时的持续药物释放。前体脂质体凝胶的皮肤渗透性为 59.73%。SEM 和 Zeta 电位研究表明形成了良好和稳定的囊泡。因此,前体脂质体在经皮传递洛索洛芬方面比传统的凝胶制剂具有更好的潜力。