Faculdade de Farmácia, Laboratório de Pesquisa e Desenvolvimento Farmacotécnico, Departamento de Medicamentos, Universidade Federal do Rio de Janeiro, Brazil.
AAPS PharmSciTech. 2012 Mar;13(1):101-11. doi: 10.1208/s12249-011-9725-8. Epub 2011 Dec 9.
Celecoxib (Cx) shows high efficacy in the treatment of osteoarthritis and rheumatoid arthritis as a result of its high specificity for COX-2, without gastrolesivity or interference with platelet function at therapeutic concentrations. Besides of anti-inflammatory effects, Cx also has a potential role for oral cancer chemoprevention. For these conditions, oral administration in long-term treatment is a concern due to its systemic side effects. However, local application at the site of injury (e.g., buccal inflammation conditions or chemoprevention of oral cancer) is a promising way to reduce its toxicity. In this study, the in vitro characterization of mucoadhesive chitosan (CHT) gels associated to Azone® was assessed to explore the potential buccal mucosal administration of Cx in this tissue. Rheological properties of gels were analyzed by a rheometer with cone-plate geometry. In vitro Cx release and permeability studies used artificial membranes and pig cheek mucosa, respectively. Mucoadhesion were measured with a universal test machine. CHT gels (3.0%) containing 2.0% or 3.0% Az showed more appropriate characteristics compared to the others: pH values, rheology, higher amount of Cx retained in the mucosa, and minimal permeation through mucosa, besides the highest mucoadhesion values, ideal for buccal application. Moreover, the flux (J) and amounts of drug released decreased with increased CHT and Az concentrations. CHT gels (3.0%) associated with 2.0% or 3.0% Az may be considered potential delivery systems for buccal administration of Cx.
塞来昔布（Cx）作为 COX-2 的高特异性药物，在治疗骨关节炎和类风湿性关节炎方面显示出高效，在治疗浓度下没有胃刺激性或干扰血小板功能。除了抗炎作用外，Cx 还具有口腔癌化学预防的潜在作用。对于这些疾病，由于其全身副作用，长期口服治疗是一个问题。然而，在损伤部位进行局部应用（例如，颊部炎症情况或口腔癌的化学预防）是减少其毒性的一种有前途的方法。在这项研究中，评估了与氮酮（Azone®）相关的粘弹性壳聚糖（CHT）凝胶的体外特性，以探索在这种组织中局部给予 Cx 的可能性。使用具有锥板几何形状的流变仪分析凝胶的流变特性。通过人工膜和猪颊黏膜分别进行体外 Cx 释放和渗透性研究。使用万能试验机测量粘膜粘附性。与其他制剂相比，含 2.0%或 3.0%Azone®的 3.0%CHT 凝胶具有更合适的特性：pH 值、流变学、更多的 Cx 保留在粘膜中、最小的粘膜透过率，以及最高的粘膜粘附性，非常适合颊部应用。此外，通量（J）和释放的药物量随着 CHT 和 Az 浓度的增加而减少。含 2.0%或 3.0%Azone®的 3.0%CHT 凝胶可被认为是 Cx 颊部给药的潜在递送系统。
