Ceschel G C, Maffei P, Sforzini A, Lombardi Borgia S, Yasin A, Ronchi C
Dipartimento di Scienze Farmaceutiche, Università di Bologna, Via San Donato 19/2, 4100, Bologna, Italy.
Fitoterapia. 2002 Nov;73 Suppl 1:S44-52. doi: 10.1016/s0367-326x(02)00190-9.
Recent studies have shown that propolis has on the oral cavity appreciable antibacterial, antifungal and antiviral actions, as well as anti-inflammatory, anaesthetic and cytostatic properties. In light of these studies, an assessment of the diffusion and permeation of caffeic acid phenetyl ester (CAPE) through porcine buccal mucosa was considered useful as a possible application in the stomatological field. To do so, a mucoadhesive topical gel was prepared to apply to the buccal mucosa. The gel was formulated in such a way as to improve the solubility of the propolis, conducting to an increase of the flux. The mucosal permeation of CAPE from the formulation was evaluated using Franz cells, with porcine buccal mucosa as septum between the formulation (donor compartment) and the receptor phase chamber. The diffusion through the membrane was determined by evaluating the amount of CAPE present in the receiving solution, the flux and the permeation coefficient (at the steady state) in the different formulations at set intervals. Qualitative and quantitative determinations were done by HPLC analysis. From the results, CAPE allowed a high permeability coefficient in comparison to the coefficient of other molecules, as expected from its physical-chemical structure. Moreover, the developed gel improved the CAPE flux approximately 35 times more with respect to an ethanol solution formulated at the same gel concentration. The developed gel was also tested in order to evaluate the mucoadhesive behaviour and comfort in vivo on 10 volunteers in a period of 8 h. The in vivo evaluation of mucoadhesive gel revealed adequate comfort and non-irritancy during the period of study and it was well accepted by the volunteers.
最近的研究表明，蜂胶对口腔具有明显的抗菌、抗真菌和抗病毒作用，以及抗炎、麻醉和抑制细胞生长的特性。鉴于这些研究，评估咖啡酸苯乙酯（CAPE）通过猪颊黏膜的扩散和渗透情况，对于其在口腔医学领域的可能应用具有重要意义。为此，制备了一种用于颊黏膜的黏膜黏附性局部凝胶。该凝胶的配方旨在提高蜂胶的溶解度，从而增加通量。使用Franz扩散池评估CAPE从该制剂中的黏膜渗透情况，以猪颊黏膜作为制剂（供体室）和受体相室之间的隔膜。通过在设定的时间间隔内评估接收溶液中CAPE的含量、通量和渗透系数（稳态时）来确定其通过膜的扩散情况。通过高效液相色谱分析进行定性和定量测定。结果表明，与其他分子的系数相比，CAPE具有较高的渗透系数，这与其物理化学结构相符。此外，所制备的凝胶相对于相同凝胶浓度的乙醇溶液，使CAPE通量提高了约35倍。还对所制备的凝胶进行了测试，以评估其在10名志愿者体内8小时内的黏膜黏附行为和舒适度。对黏膜黏附凝胶的体内评估显示，在研究期间具有足够的舒适度且无刺激性，志愿者对其接受度良好。
