De Caro Viviana, Giandalia Giulia, Siragusa Maria Gabriella, Paderni Carlo, Campisi Giuseppina, Giannola Libero Italo
Dipartimento di Chimica e Tecnologie Farmaceutiche, Università degli study di Palermo, Italy.
Eur J Pharm Biopharm. 2008 Nov;70(3):869-73. doi: 10.1016/j.ejpb.2008.06.025. Epub 2008 Jul 4.
Over the last decade, interest in delivering drugs through buccal mucosa has increased. As a major limitation in buccal drug delivery could be the low permeability of the epithelium, the aim of this study was to evaluate the aptitude of galantamine, useful in Alzheimer's disease, to penetrate the buccal mucosa. The evaluation of the ability of galantamine to permeate through the buccal epithelium was investigated using two permeation models. Firstly, in vitro permeation experiments were carried out using reconstituted human oral non-keratinised epithelium and Transwell diffusion cells system. Results were validated by ex vivo experiments using porcine buccal mucosa as membrane and Franz type diffusion cells as permeation model. The entity of buccal permeation was expressed in terms of drug flux (J(s)) and permeability coefficients (K(p)). Data collected by in vitro and ex vivo experiments were in agreement and suggested that buccal mucosa does not block diffusion of galantamine. The effects of drug application on histology of tissue specimens used in every experiment were also studied: no sign of flogosis and no significant cytological or architectural changes were highlighted.
在过去十年中，通过颊黏膜给药的关注度有所增加。由于颊部药物递送的一个主要限制可能是上皮的低渗透性，本研究的目的是评估对阿尔茨海默病有用的加兰他敏穿透颊黏膜的能力。使用两种渗透模型研究了加兰他敏透过颊上皮能力的评估。首先，使用重组人口腔非角化上皮和Transwell扩散池系统进行体外渗透实验。结果通过使用猪颊黏膜作为膜和Franz型扩散池作为渗透模型的离体实验进行验证。颊部渗透的程度以药物通量（J(s)）和渗透系数（K(p)）表示。体外和离体实验收集的数据一致，并表明颊黏膜不会阻碍加兰他敏的扩散。还研究了药物应用对每个实验中使用的组织标本组织学的影响：未发现炎症迹象，也未突出显示明显的细胞学或结构变化。
