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Novel multiparticulate pH triggered delayed release chronotherapeutic drug delivery of celecoxib-β-cyclodextrin inclusion complexes by using Box-Behnken design.
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-02 , DOI: 10.1016/j.ejps.2020.105254 Irsah Maqbool 1 , Muhammad Akhtar 1 , Rabbiya Ahmad 1 , Hadia Sadaquat 1 , Sobia Noreen 1 , Amna Batool 1 , Sajid Ullah Khan 2
European Journal of Pharmaceutical Sciences ( IF 4.3 ) Pub Date : 2020-02-02 , DOI: 10.1016/j.ejps.2020.105254 Irsah Maqbool 1 , Muhammad Akhtar 1 , Rabbiya Ahmad 1 , Hadia Sadaquat 1 , Sobia Noreen 1 , Amna Batool 1 , Sajid Ullah Khan 2
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This study aimed to prepare novel colon targeted celecoxib-β-cyclodextrin (CXB-β-CD) inclusion complex loaded eudragit S 100 (ES100) microparticles for chronotherapy of rheumatoid arthritis (RA) which is an innovative approach, never reported before, for the fabrication of CXB-β-CD complex in the form of microparticles and its colon targeting. CXB was complexed with β-cyclodextrin by kneading technique and we evaluated the effect of β-CD on saturation solubility of CXB. Microparticles were developed by oil-in-oil emulsion solvent evaporation technique and formulation variables (polymer conc, surfactant conc and stirring speed) were optimized by using three-factor three-level Box-Behnken design (BBD). SEM imaging revealed smooth, uniform and spherical shape microparticles. There was 7.3 fold increases in saturation solubility of CXB-β-CD inclusion complex in distilled water as compared to pure CXB. Particle size was in the range of 50.42 µm to 238.38 µm with entrapment efficiency of 68.47% to 91.65%. Biphasic drug release pattern was found i.e initially delayed release in stomach and small intestine followed by fast release at colonic pH. Response variable results achieved from optimized formulation were very close to the response values suggested by BBD signifying the actual reliability and robustness of BBD in the fabrication of colon targeted CXB-β-CD microparticles. The comparison of CXB-β-CD optimized formulation with optimized formulation containing pure CXB showed increase in drug release due to enhancement of water solubility of CXB-β-CD inclusion complex. So, it can be concluded that CXB-β-CD loaded ES100 microparticles can be successfully fabricated with enhanced solubility for the chronotherapy of rheumatoid arthritis.
中文翻译：
新型多颗粒pH通过Box-Behnken设计触发了塞来昔布-β-环糊精包合物的延迟释放计时治疗药物传递。
这项研究旨在制备新型的结肠靶向塞来昔布-β-环糊精（CXB-β-CD）包合物负载的eudragit S 100（ES100）微粒，用于风湿性关节炎（RA）的时间疗法，这是一种从未有过报道的创新方法。形式的CXB-β-CD复合物的制备及其结肠靶向性。通过捏合技术将CXB与β-环糊精复合，我们评估了β-CD对CXB饱和溶解度的影响。通过油包油乳液溶剂蒸发技术开发了微粒，并使用三因素三级Box-Behnken设计（BBD）优化了配方变量（聚合物浓，表面活性剂浓和搅拌速度）。SEM成像显示出光滑，均匀和球形的微粒。有7。与纯CXB相比，CXB-β-CD包合物在蒸馏水中的饱和溶解度增加了3倍。粒度在50.42μm至238.38μm的范围内，包封率为68.47％至91.65％。发现双相药物释放模式，即最初在胃和小肠中延迟释放，然后在结肠pH下快速释放。通过优化配方获得的响应变量结果非常接近BBD建议的响应值，这表明BBD在结肠靶向CXB-β-CD微粒的制造中的实际可靠性和耐用性。将CXB-β-CD优化制剂与包含纯CXB的优化制剂进行比较表明，由于CXB-β-CD包合物的水溶性增加，药物释放增加。所以，
更新日期：2020-02-03
中文翻译：
新型多颗粒pH通过Box-Behnken设计触发了塞来昔布-β-环糊精包合物的延迟释放计时治疗药物传递。
这项研究旨在制备新型的结肠靶向塞来昔布-β-环糊精（CXB-β-CD）包合物负载的eudragit S 100（ES100）微粒，用于风湿性关节炎（RA）的时间疗法，这是一种从未有过报道的创新方法。形式的CXB-β-CD复合物的制备及其结肠靶向性。通过捏合技术将CXB与β-环糊精复合，我们评估了β-CD对CXB饱和溶解度的影响。通过油包油乳液溶剂蒸发技术开发了微粒，并使用三因素三级Box-Behnken设计（BBD）优化了配方变量（聚合物浓，表面活性剂浓和搅拌速度）。SEM成像显示出光滑，均匀和球形的微粒。有7。与纯CXB相比，CXB-β-CD包合物在蒸馏水中的饱和溶解度增加了3倍。粒度在50.42μm至238.38μm的范围内，包封率为68.47％至91.65％。发现双相药物释放模式，即最初在胃和小肠中延迟释放，然后在结肠pH下快速释放。通过优化配方获得的响应变量结果非常接近BBD建议的响应值，这表明BBD在结肠靶向CXB-β-CD微粒的制造中的实际可靠性和耐用性。将CXB-β-CD优化制剂与包含纯CXB的优化制剂进行比较表明，由于CXB-β-CD包合物的水溶性增加，药物释放增加。所以，
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