College of Pharmacy and Allied Health Professions, St John's University, Jamaica, NY, USA.
Pharm Dev Technol. 2010 Mar-Apr;15(2):192-208. doi: 10.1080/10837450903085442.
Insulin-loaded buccal Pluronic F-127 (PF-127) gel formulations were fabricated to study the effect of PF-127 concentration, insulin concentration, presence of salt, addition of polymer, and permeation enhancer on their gelation time, mucoadhesion force, release and permeation characteristics of insulin from the gels. Thereafter, the principle of statistical optimization to prepare a gel formulation having the potential for buccal delivery of basal insulin in diabetic patients was employed. The gelation time decreased as the concentration of PF-127 increased. Presence of salts as well as addition of polymer, such as methyl cellulose (MC) and hydroxypropylmethyl cellulose (HPMC) decreased the gelation time. An increase in PF-127 concentration and addition of MC and HPMC increased the mucoadhesion force of the gel formulations. Release and permeation of insulin from the gel formulations decreased with increased concentration of PF-127, presence of salts, and addition of MC and HPMC. Permeation of insulin from the optimized gel formulation was 93.17 (+/- 0.058, n = 3) microg/cm(2) which was not only found in close agreement with predicted results from the model equations used for the formulation optimization but also considered comparable to clinical setting. Therefore, the development of optimized buccal insulin-loaded Pluronic F-127 gels using a statistical experimental design is feasible.
胰岛素负载颊用 Pluronic F-127（PF-127）凝胶制剂被制备来研究 PF-127 浓度、胰岛素浓度、盐的存在、聚合物的添加和渗透促进剂对其胶凝时间、粘膜粘附力、胰岛素从凝胶中的释放和渗透特性的影响。此后，采用统计优化原理来制备具有在糖尿病患者中颊部递送基础胰岛素潜力的凝胶制剂配方。随着 PF-127 浓度的增加，胶凝时间缩短。盐的存在以及聚合物如甲基纤维素（MC）和羟丙基甲基纤维素（HPMC）的添加均降低了胶凝时间。PF-127 浓度的增加以及 MC 和 HPMC 的添加增加了凝胶制剂的粘膜粘附力。胰岛素从凝胶制剂中的释放和渗透随着 PF-127 浓度的增加、盐的存在以及 MC 和 HPMC 的添加而降低。从优化的凝胶制剂中释放的胰岛素为 93.17（+/-0.058，n=3）μg/cm²，不仅与用于制剂优化的模型方程的预测结果非常吻合，而且与临床情况相当。因此，使用统计实验设计开发优化的颊用胰岛素负载 Pluronic F-127 凝胶是可行的。
