Abstract：
Our study aimed to explore the potential of using nanostructured lipid carriers (NLCs) to enhance the topical administration of β-sitosterol, a bioactive that is poorly soluble in water. Here, we have taken advantage of the unique characteristics that cubosomes have to provide as a drug delivery system. These characteristics include a large surface area, thermal stability, and the capacity to encapsulate molecules that are hydrophobic, amphiphilic, and hydrophilic. The cubosomal formulation was optimized by building a central composite design. The optimum dispersion exhibited a particle size of 88.3 nm, a zeta potential of -43, a polydispersity index of 0.358, and drug entrapment of 95.6%. It was composed of 15% w/w oleic acid and 5% w/w pluronic F127. The optimized cubosome dispersion was incorporated into a sponge formulation. The optimized cubosome sponge achieved a higher drug release compared with the cubosome dispersion. The SEM micrograph of the selected sponge showed that it has an interwoven irregular fibrous lamellar structure with low density and high porosity. The in-vivo data revealed that topical application of the β-sitosterol cubosomal sponge showed significant higher wound closure percentage relative to the β-sitosterol product (Mebo)®.
摘要：
我们的研究旨在探索使用纳米结构脂质载体（NLCs）来增强β-谷甾醇的局部给药的潜力，难溶于水的生物活性物质。这里,我们利用了立方体作为药物递送系统所具有的独特特性。这些特征包括大的表面积，热稳定性，以及封装疏水分子的能力，两亲性,和亲水性。通过构建中心复合材料设计来优化立方体制剂。最佳分散体的粒径为88.3nm，zeta电位为-43，多分散指数为0.358，药物包封率为95.6%。它由15%w/w的油酸和5%w/w的pluronicF127组成。将优化的立方体分散体掺入海绵制剂中。与长方体分散体相比，优化的长方体海绵实现了更高的药物释放。所选海绵的SEM显微照片表明，它具有低密度和高孔隙率的交织不规则纤维层状结构。体内数据显示,相对于β-谷甾醇产品(Mebo)®,局部施用β-谷甾醇立方体海绵显示出显著更高的伤口闭合百分比。
