Wanasathop Apipa, Patel Priya B, Choi Hyojin A, Li S Kevin
Division of Pharmaceutical Sciences, College of Pharmacy, University of Cincinnati, 231 Albert Sabin Way, MSB # 3005, Cincinnati, OH 45267, USA.
Pharmaceutics. 2021 Oct 31;13(11):1814. doi: 10.3390/pharmaceutics13111814.
The buccal mucosa provides an alternative route of drug delivery that can be more beneficial compared to other administration routes. Although numerous studies and reviews have been published on buccal drug delivery, an extensive review of the permeability data is not available. Understanding the buccal mucosa barrier could provide insights into the approaches to effective drug delivery and optimization of dosage forms. This paper provides a review on the permeability of the buccal mucosa. The intrinsic permeability coefficients of porcine buccal mucosa were collected. Large variability was observed among the published permeability data. The permeability coefficients were then analyzed using a model involving parallel lipoidal and polar transport pathways. For the lipoidal pathway, a correlation was observed between the permeability coefficients and permeant octanol/water partition coefficients () and molecular weight (MW) in a subset of the permeability data under specific conditions. The permeability analysis suggested that the buccal permeation barrier was less lipophilic than octanol. For the polar pathway and macromolecules, a correlation was observed between the permeability coefficients and permeant MW. The hindered transport analysis suggested an effective pore radius of 1.5 to 3 nm for the buccal membrane barrier.
颊黏膜提供了一种药物递送的替代途径，与其他给药途径相比可能更具优势。尽管已经发表了许多关于颊部药物递送的研究和综述，但尚无对渗透性数据的全面综述。了解颊黏膜屏障有助于深入了解有效药物递送的方法和剂型优化。本文对颊黏膜的渗透性进行了综述。收集了猪颊黏膜的固有渗透系数。已发表的渗透性数据存在很大差异。然后使用一个涉及平行类脂和极性转运途径的模型对渗透系数进行分析。对于类脂途径，在特定条件下的一部分渗透性数据中，观察到渗透系数与渗透剂正辛醇/水分配系数（）和分子量（MW）之间存在相关性。渗透性分析表明，颊部渗透屏障的亲脂性低于正辛醇。对于极性途径和大分子，观察到渗透系数与渗透剂MW之间存在相关性。受阻转运分析表明，颊膜屏障的有效孔径为1.5至3纳米。
