Solomonidou D, Cremer K, Krumme M, Kreuter J
Institut für Pharmazeutische Technologie, Johann Wolfgang Goethe-Universität, Frankfurt am Main, Germany.
J Biomater Sci Polym Ed. 2001;12(11):1191-205. doi: 10.1163/156856201753395743.
Mucoadhesive drug delivery systems may enable a prolonged and localized drug release at various sites of the gastrointestinal tract. In the present study, the mucoadhesive properties of flexible polymeric films based on PVP or PVA as film-forming polymers were assessed by measuring the detachment force from excised porcine duodenal mucosa using a tensile strength tester. The mucoadhesive films were comprised of an impermeable backing layer of cellulose acetate butyrate. Carbopol 934P, Carbopol 974NF, and Noveon AA1 were incorporated as mucoadhesive excipients in concentrations of 0-22 wt% relative to the dry mass of the mucoadhesive layer and with various degrees of neutralization corresponding to pH 4.8, 5.5, 6.8, or 7.5. Films based on PVP were generally more mucoadhesive than corresponding formulations based on PVA. Maximum adhesion of PVP-films was observed at pH 5.5 and 6.8 depending on the type of the mucoadhesive polymer and its concentration. An optimal mucoadhesive polymer concentration range was found to be between 2 and 10 wt%. Higher polymer concentrations did not further enhance the mucoadhesive properties, and in some cases even decreased mucoadhesion. Film formulations based on PVA demonstrated no satisfactory mucoadhesive strength.
粘膜粘附给药系统可使药物在胃肠道的不同部位实现延长的局部释放。在本研究中，通过使用拉伸强度测试仪测量从切除的猪十二指肠粘膜上的分离力，评估了以聚乙烯吡咯烷酮（PVP）或聚乙烯醇（PVA）作为成膜聚合物的柔性聚合物膜的粘膜粘附特性。粘膜粘附膜由醋酸丁酸纤维素的不透性背衬层组成。卡波姆934P、卡波姆974NF和诺维昂AA1作为粘膜粘附辅料，相对于粘膜粘附层的干质量，其浓度为0-22 wt%，并具有对应于pH 4.8、5.5、6.8或7.5的不同中和度。基于PVP的膜通常比基于PVA的相应制剂具有更强的粘膜粘附性。根据粘膜粘附聚合物的类型及其浓度，在pH 5.5和6.8时观察到PVP膜的最大粘附力。发现最佳的粘膜粘附聚合物浓度范围为2至10 wt%。较高的聚合物浓度并未进一步增强粘膜粘附性能，在某些情况下甚至降低了粘膜粘附性。基于PVA的膜制剂未表现出令人满意的粘膜粘附强度。
