Jain Sanjay K, Gupta Yashwant, Jain Anekant, Amin Sadia
Pharmaceutics Research Projects Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour Vishwavidyalaya, Sagar [M. P.] 470003, India.
Curr Drug Deliv. 2008 Jul;5(3):207-14. doi: 10.2174/156720108784911677.
The ultra-flexible lipid vesicles, the elastic liposomes bearing meloxicam-beta-cyclodextrin complex were prepared for its topical administration with the aim of simultaneously exploiting the favorable properties of both the carriers. The prepared meloxicam-beta-cyclodextrin complex was evaluated using DSC, XRD and FT-IR, which indicates the formation of inclusion complex in a molar ratio of 1:2 of meloxicam and beta-cyclodextrin (beta-CD). The elastic liposomes were prepared by conventional rotary evaporation method and characterized for various parameters such as vesicle shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, stability and in-vitro release pattern. Permeability studies of meloxicam and meloxicam-beta-cyclodextrin complex, as such or incorporated in elastic liposomes performed both across artificial membranes and rat skin highlighted a favorable effect of cyclodextrin on drug permeation rate, due to its solubilizing action. Moreover skin-permeation enhancer property of elastic liposomes has been evidenced. Skin permeation potential of the developed formulation was assessed using confocal laser scanning microscopy (CLSM), which revealed an enhanced permeation of the formulation to the deeper layers of the skin (up to 160 microm) following channel like pathways. Skin permeation profile of elastic liposomal formulation bearing meloxicam-beta-cyclodextrin complex was observed and the investigations revealed an enhanced transdermal flux (12.48+/-0.9 microg/cm(2)/h) and decreased lag time (0.7 h) for meloxicam. The obtained flux was nearly 1.4 and 9.1 times higher than elastic liposomal formulation bearing meloxicam and plain drug solution, respectively (P<0.005). The results indicate that the elastic liposomes may be promising vehicles for the transdermal delivery of meloxicam.
制备了超柔性脂质囊泡，即负载美洛昔康-β-环糊精复合物的弹性脂质体，用于局部给药，目的是同时利用两种载体的有利特性。使用差示扫描量热法（DSC）、X射线衍射法（XRD）和傅里叶变换红外光谱法（FT-IR）对制备的美洛昔康-β-环糊精复合物进行了评估，结果表明美洛昔康与β-环糊精（β-CD）以1:2的摩尔比形成了包合物。通过常规旋转蒸发法制备了弹性脂质体，并对其各种参数进行了表征，如囊泡形状和表面形态、大小和大小分布、包封率、弹性、稳定性和体外释放模式。对美洛昔康和美洛昔康-β-环糊精复合物（原样或掺入弹性脂质体中）在人工膜和大鼠皮肤上进行的渗透性研究表明，由于环糊精的增溶作用，其对药物渗透速率有有利影响。此外，还证明了弹性脂质体具有皮肤渗透促进剂的特性。使用共聚焦激光扫描显微镜（CLSM）评估了所开发制剂的皮肤渗透潜力，结果显示该制剂通过类似通道的途径增强了向皮肤深层（达160微米）的渗透。观察了负载美洛昔康-β-环糊精复合物的弹性脂质体制剂的皮肤渗透情况，研究表明美洛昔康的经皮通量增加（12.48±0.9微克/平方厘米/小时），滞后时间缩短（0.7小时）。所获得的通量分别比负载美洛昔康的弹性脂质体制剂和普通药物溶液高出近1.4倍和9.1倍（P<0.005）。结果表明，弹性脂质体可能是美洛昔康经皮给药的有前途的载体。
