Patlolla V G R, Holbrook W P, Gizurarson S, Kristmundsdottir P
Pharmazie. 2020 Jan 2;75(1):7-12. doi: 10.1691/ph.2020.9122.
Delivery of active ingredients to the oral mucosa from topically applied formulations reduces side effects from systemic administration and enhances the treatment efficiency. The challenge however, is to maintain the formulation at the administration site due to rapid salivary flow and mechanical movements of the mouth. Therefore, addition of mucoadhesive polymers could aid in enhancing the formulation residence time by increasing the mucoadhesion capacity but this effect is negligible especially if low ratio of mucoadhesive polymers are added to the formulation. Different mucoadhesive polymers at 0.5% w/w (either single or combination of two polymers) were added to the hydrogels and tested for mucoadhesion capacity, tensile strengths, adhesiveness, cohesiveness, compressibility and hardness. 0.5% povidone showed significantly highest work of mucoadhesion, 0.5% Carbopol formulation showed least cohesiveness and 0.5% HPMC showed highest adhesiveness, but a formulation containing a combination of 0.25% HPMC and 0.25% povidone showed the ideal parameters among all the mucoadhesive polymers tested. The effect of increase in concentration of HPMC (0.5, 1, 1.5, 2%) showed linear relationship for work of mucoadhesion and tensile strengths whereas for TPA the values were non-linear. The drug release from the optimized polymer matrices was found to follow zero-order release profile and the mechanism was found to be super case-II transport relaxation release. The results of this study indicate the mucoadhesive polymers do not impact the tensile strengths ( =0.05), but the texture properties and work of mucoadhesion of the formulations can be significantly ( <0.05) altered by the choice of mucoadhesive component at 0.5%w/w, though not for all the polymers tested. The study provides scope to predict performance and helps optimize for localized delivery.
通过局部应用制剂将活性成分递送至口腔黏膜可减少全身给药的副作用并提高治疗效率。然而,由于唾液快速流动和口腔的机械运动,将制剂维持在给药部位是一项挑战。因此,添加黏膜黏附聚合物可通过增加黏膜黏附能力来帮助延长制剂停留时间,但这种效果可忽略不计,特别是当向制剂中添加低比例的黏膜黏附聚合物时。将不同的黏膜黏附聚合物以0.5% w/w(单一聚合物或两种聚合物的组合)添加到水凝胶中,并测试其黏膜黏附能力、拉伸强度、黏附性、内聚性、可压缩性和硬度。0.5%聚维酮显示出显著最高的黏膜黏附功,0.5%卡波姆制剂显示出最低的内聚性,0.5%羟丙基甲基纤维素显示出最高的黏附性,但含有0.25%羟丙基甲基纤维素和0.25%聚维酮组合的制剂在所有测试的黏膜黏附聚合物中显示出理想的参数。羟丙基甲基纤维素浓度增加(0.5%、1%、1.5%、2%)对黏膜黏附功和拉伸强度呈线性关系,而对于组织蛋白酶A,其值呈非线性。从优化的聚合物基质中释放药物遵循零级释放曲线,其机制为超Ⅱ型转运松弛释放。本研究结果表明,黏膜黏附聚合物不会影响拉伸强度(P = 0.05),但通过选择0.5%w/w的黏膜黏附成分,制剂的质地特性和黏膜黏附功可能会显著改变(P < 0.05),尽管并非所有测试的聚合物都是如此。该研究为预测性能提供了空间,并有助于优化局部给药。