Shin Baek-Ki, Baek Eun Jung, Choi Soon Gil, Davaa Enkhzaya, Nho Young-Chang, Lim Youn-Mook, Park Jong-Seok, Huh Kang Moo, Park Jeong-Sook
College of Pharmacy, Chungnam National University , Daejeon , Korea.
Drug Dev Ind Pharm. 2013 Dec;39(12):1874-80. doi: 10.3109/03639045.2012.665925. Epub 2012 Mar 12.
To improve physical properties and modulate the mucoadhesive hydrogel formulation via cross-linking by radiation, hydrogels were prepared using thermoreversible polymer Pluronic F127 (PF127) and mucoadhesive polymer carbopol 934P (C934P). As a model drug, naproxen was loaded in the hydrogel formulation. Sol-gel transition temperatures of hydrogels were measured by the tube-inversion method. The mucoadhesive potential of each formulation was determined by measuring the force required to detach the formulation from oral mucosal tissue. To strengthen the mechanical properties, the formulations were irradiated using an electronic beam. Drug release from the hydrogels and the cytotoxicity of each formulation were investigated. Sol-gel transition temperatures of the formulations were decreased by the addition of carbopol and were close to body temperature. The mucoadhesive force of the PF127 formulation was increased by addition of carbopol. In vitro release was sustained and the release rate was reduced by the addition of carbopol. After irradiation, the mucoadhesive force was increased about five-fold especially in the case of PF127 23% (9.7 kPa) and in vitro release was not sustained further. In conclusion, the use of a PF127 formulation incorporating a mucoadhesive polymer could effectively and safely improve oral residence time and absorption of naproxen. Irradiated formulations showed permanent cross-linking and improved properties.
为了通过辐射交联改善物理性能并调节粘膜粘附水凝胶制剂,使用热可逆聚合物普朗尼克F127(PF127)和粘膜粘附聚合物卡波姆934P(C934P)制备水凝胶。作为模型药物,将萘普生载入水凝胶制剂中。通过试管倒置法测量水凝胶的溶胶-凝胶转变温度。通过测量将制剂从口腔粘膜组织分离所需的力来确定每种制剂的粘膜粘附潜力。为了增强机械性能,使用电子束对制剂进行辐照。研究了水凝胶中的药物释放和每种制剂的细胞毒性。通过添加卡波姆降低了制剂的溶胶-凝胶转变温度,使其接近体温。通过添加卡波姆提高了PF127制剂的粘膜粘附力。体外释放是持续的,并且通过添加卡波姆降低了释放速率。辐照后,粘膜粘附力增加了约五倍,特别是在PF127 23%(9.7 kPa)的情况下,并且体外释放不再持续。总之,使用包含粘膜粘附聚合物的PF127制剂可以有效且安全地改善萘普生的口腔滞留时间和吸收。辐照后的制剂显示出永久交联并改善了性能。