Gaur Praveen Kumar, Mishra Shikha, Purohit Suresh, Kumar Yatendra, Bhandari Anil
Department of Pharmaceutics, I.T.S. Paramedical (Pharmacy) College , Muradnagar, Ghaziabad, U.P. , India.
Artif Cells Nanomed Biotechnol. 2014 Oct;42(5):323-30. doi: 10.3109/21691401.2013.827119. Epub 2013 Aug 15.
Ibuprofen is an important NSAID, however, it can cause GI disturbances when given orally, and employment of transdermal route will require permeation enhancer causing skin injury.
Drug-loaded nanovesicles of ceramide-2, cholesterol, palmitic acid, and cholesteryl sulfate (ICVG) were formulated and analyzed for physicochemical and permeation properties.
Vesicles were formulated using film hydration method and physicochemical parameters, in vitro drug release, and stability were assessed. Further, nanovesicle gels were evaluated against plain gel containing drug (CG) for ex vivo/in vivo drug permeation and anti-inflammatory activity.
The developed formulations showed optimal physicochemical profile and ICV-1 gave 97.24% drug release. Drug permeation was between 17.32 and 33.12 μg/cm(2) for ICVG formulations and 0.27 μg/cm(2) for CG. ICVG-1 and CG showed Cmax of 9.6 and 0.7 μg/ml at 8 and 4 h. ICVG-1 showed 19.9 times higher AUC than CG. Edema inhibition was 57.98% during initial hours by ICVG-1.
Ratio of ceramide 2 and palmitic acid plays a critical role in drug permeation through stratum corneum. The stability and protective effect of the formulations were due to ceramide content.
The composition has an important role in physicochemical properties and drug permeation thereby generating an optimum formulation.
布洛芬是一种重要的非甾体抗炎药，然而，口服时它会引起胃肠道不适，而采用透皮途径则需要渗透促进剂，这会导致皮肤损伤。
制备并分析由神经酰胺 -2、胆固醇、棕榈酸和硫酸胆固醇组成的载药纳米囊泡（ICVG）的物理化学性质和渗透特性。
采用薄膜水化法制备囊泡，并评估其物理化学参数、体外药物释放和稳定性。此外，针对含药普通凝胶（CG），评估纳米囊泡凝胶的离体/体内药物渗透和抗炎活性。
所开发的制剂呈现出最佳的物理化学特性，ICV -1的药物释放率为97.24%。ICVG制剂的药物渗透率在17.32至33.12μg/cm²之间，而CG的药物渗透率为0.27μg/cm²。ICVG -1和CG在8小时和4小时时的Cmax分别为9.6和0.7μg/ml。ICVG -1的AUC比CG高19.9倍。ICVG -1在最初几小时内对水肿的抑制率为57.98%。
神经酰胺2和棕榈酸的比例在药物透过角质层的过程中起关键作用。制剂的稳定性和保护作用归因于神经酰胺含量。
该组合物在物理化学性质和药物渗透方面具有重要作用，从而产生了一种最佳制剂。
