Fetih Gihan, Fathalla Dina, El-Badry Mahmoud
Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, 71526, Egypt.
Drug Dev Res. 2014 Jun;75(4):257-66. doi: 10.1002/ddr.21179. Epub 2014 Jun 3.
The objective of this work was to evaluate liposome-containing gel formulations for the sustained, site-specific delivery of celecoxib (CXB). Liposomes composed of phosphadtidylcholine (and various amounts of cholesterol (Ch) were prepared using thin film hydration and characterized for encapsulation efficiency, vesicle size, and drug-excipient interaction using differential scanning calorimetry and Fourier-transform infrared spectroscopy. The selected liposome formulation was incorporated in different gel formulations: the Ch ratio affected the encapsulation efficiency of the drug, by increasing Ch ratio up until 1:1 the encapsulation efficiency increased. Further increasing the Ch ratio resulted in decreasing encapsulation efficiency. In vitro drug release and skin permeation studies showed sustained release and enhanced permeation compared with gel formulations containing free drug. In the rat paw edema test, the anti-inflammatory activity of the selected liposomal gel formulation was higher and more sustained compared with that of the nonliposomal gel formulation containing free drug. These results suggest that the liposome-containing gels are promising formulations for sustained, site-specific delivery of CXB.
这项工作的目的是评估含脂质体的凝胶制剂用于塞来昔布（CXB）的持续、位点特异性递送的效果。使用薄膜水化法制备了由磷脂酰胆碱和不同量胆固醇（Ch）组成的脂质体，并通过差示扫描量热法和傅里叶变换红外光谱法对其包封效率、囊泡大小和药物-辅料相互作用进行了表征。将选定的脂质体制剂掺入不同的凝胶制剂中：Ch比例影响药物的包封效率，直到Ch比例达到1:1时包封效率增加。进一步增加Ch比例会导致包封效率降低。体外药物释放和皮肤渗透研究表明，与含游离药物的凝胶制剂相比，其具有持续释放和增强渗透的效果。在大鼠足肿胀试验中，与含游离药物的非脂质体凝胶制剂相比，选定的脂质体凝胶制剂的抗炎活性更高且更持久。这些结果表明，含脂质体的凝胶是用于CXB持续、位点特异性递送的有前景的制剂。
