Former Student at International University, Ho Chi Minh City, Vietnam.
Deakin University, School of Medicine, IMPACT, Institute for Innovation in Physical and Mental Health and Clinical Translation, Geelong, Australia.
Anticancer Agents Med Chem. 2021;21(14):1894-1900. doi: 10.2174/1871520621666201207091827.
Mucoadhesive polymers play a critical role in controlled-release tablets for buccal drug delivery.
This research aimed to investigate the characterization and mechanisms of solid lipid particle-based tablets with different mucoadhesive polymers for buccal delivery.
Prednisolone (PSL)-loaded Solid Lipid Particles (SLPs) were conventionally prepared by ultrasonication. The freeze-drying method was used to convert the SLP suspension into a solid dosage form for buccal delivery by using mucoadhesive polymers.
All formulations showed over 80% drug release after 6h, which followed immediate and sustained release patterns depending on the SLP type. However, the different polymers in the formulations resulted in different mucoadhesion times and drug release and drug permeability profiles. HPMC 4000 showed higher drug permeation (3327 μg vs. 2589 μg after 6h) but a shorter mucoadhesion time than Carbopol (197 min vs. 361 min). In addition, surface morphology, swelling and erosion, particle size and zeta potential were also noted for the different mechanisms for buccal tablet design with different controlled release profiles.
The results of this work indicate a good strategy for the selection of mucoadhesive polymers for SLP-based tablets in improving the bioavailability of poorly water-soluble drugs.
黏膜黏附聚合物在口腔药物传递的控释片剂中起着至关重要的作用。
本研究旨在探讨不同黏膜黏附聚合物的基于固体脂质粒子的片剂的特性和机制，用于口腔给药。
采用超声法常规制备负载泼尼松龙（PSL）的固体脂质粒子（SLP）。通过冷冻干燥方法，使用黏膜黏附聚合物将 SLP 混悬液转化为用于口腔给药的固体剂型。
所有配方在 6 小时后均显示出超过 80%的药物释放，其释放模式取决于 SLP 类型，表现为即刻和持续释放。然而，配方中不同的聚合物导致不同的黏膜黏附时间、药物释放和药物渗透特性。HPMC 4000 显示出更高的药物渗透（6 小时后为 3327μg 比 2589μg），但黏膜黏附时间比 Carbopol 短（197 分钟比 361 分钟）。此外，还注意到不同的控制释放曲线的口腔片剂设计的不同机制的表面形态、溶胀和侵蚀、粒径和 Zeta 电位。
这项工作的结果表明，对于基于 SLP 的片剂选择黏膜黏附聚合物是一种提高难溶性药物生物利用度的良好策略。
