The purpose of this research was to formulate nanocomposites comprising of celecoxib with shellac and eudragit S100 for solubility enhancement and targeting drug delivery to the colon. Celecoxib belongs to the class NSAIDs and it shows anticancer activity as well, by COX-II dependent and independent mechanisms. The nanocomposites were prepared by the microwave-assisted method. The prepared nanocomposites were evaluated by techniques such as FTIR, DSC, XRD, solubility determination studies, dissolution studies, SEM and TEM. The effect of the drug and polymer ratio on the solubility and the release of celecoxib at colonic pH were evaluated. The solubility of the drug increases up to a certain level when the polymer concentration increases, after which it was found to be decreased. The solubility studies revealed that as the concentration of the polymer increases up to the optimum level, the solubility of the drug increases. Enhancement of solubility for optimum batches was found to be 26.22 and 8.58 μg/ml for a 1:3 ratio of celecoxib-shellac nanocomposite (CSNC) and 1:4 for celecoxib-eudragit nanocomposite (CENC), respectively, as compared to pure celecoxib. SEM and TEM analysis showed the surface texture of the composite and the size of nanoparticles embedded in the polymeric matrix. Needle-shaped nanoparticles were observed with a size of about 50 nm in the polymeric matrix. The optimum ratio of drug to polymer showed the release of drug by 92.72 ± 1.7% and 79.66 ± 2.4% for CSNC and CENC, respectively, at the end of 8 h at colonic pH.

中文翻译：

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微波辅助合成塞来昔布纳米复合材料以增强溶解度和结肠癌靶向

本研究的目的是配制由塞来昔布、虫胶和 eudragit S100 组成的纳米复合材料，以增强溶解度并将药物靶向递送至结肠。塞来昔布属于 NSAID 类，它还通过 COX-II 依赖和独立机制表现出抗癌活性。采用微波辅助方法制备了纳米复合材料。通过 FTIR、DSC、XRD、溶解度测定研究、溶出研究、SEM 和 TEM 等技术对制备的纳米复合材料进行了评估。评估了药物和聚合物的比例对塞来考昔在结肠pH值下的溶解度和释放的影响。当聚合物浓度增加时，药物的溶解度增加到一定水平，之后发现溶解度降低。溶解度研究表明，随着聚合物浓度增加到最佳水平，药物的溶解度增加。与纯塞来昔布相比，最佳批次的溶解度增加，对于 1:3 比例的塞来昔布-虫胶纳米复合材料 (CSNC) 和 1:4 比例的塞来昔布-尤特奇纳米复合材料 (CENC)，溶解度分别提高了 26.22 和 8.58 μg/ml 。SEM 和 TEM 分析显示了复合材料的表面纹理和嵌入聚合物基质中的纳米颗粒的尺寸。在聚合物基质中观察到尺寸约为 50 nm 的针状纳米颗粒。药物与聚合物的最佳比例显示，在结肠 pH 值下 8 小时后，CSNC 和 CENC 的药物释放量分别为 92.72 ± 1.7% 和 79.66 ± 2.4%。