Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, Damanhour University, Damanhour, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Int J Pharm. 2015 Jul 5;488(1-2):78-85. doi: 10.1016/j.ijpharm.2015.04.052. Epub 2015 Apr 18.
This study aims at improving the buccal delivery of vitamin B6 (VB6) as a model highly water-soluble, low permeable vitamin. Two main strategies were combined; first VB6 was entrapped in liposomes, which were then formulated as mucoadhesive film. Both plain and VB6-loaded liposomes (LPs) containing Lipoid S100 and propylene glycol (∼ 200 nm) were then incorporated into mucoadhesive film composed of SCMC and HPMC. Results showed prolonged release of VB6 (72.65%, T50% diss 105 min) after 6h from LP-film compared to control film containing free VB6 (96.37%, T50% diss 30 min). Mucoadhesion was assessed both ex vivo on chicken pouch and in vivo in human. Mucoadhesive force of 0.2N and residence time of 4.4h were recorded. Ex vivo permeation of VB6, across chicken pouch mucosa indicated increased permeation from LP-systems compared to corresponding controls. Interestingly, incorporation of the vesicles in mucoadhesive film reduced the flux by 36.89% relative to LP-dispersion. Meanwhile, both films provided faster initial permeation than the liquid forms. Correlating the cumulative percent permeated ex vivo with the cumulative percent released in vitro indicated that LPs retarded VB6 release but improved permeation. These promising results represent a step forward in the field of buccal delivery of water-soluble vitamins.
本研究旨在改善维生素 B6（VB6）的颊部递送，作为一种高度水溶性、低渗透性的维生素模型。采用了两种主要策略；首先将 VB6 包封于脂质体中，然后将其制成粘膜粘附性薄膜。然后将含有 Lipoid S100 和丙二醇的普通和 VB6 负载脂质体（LPs）（约 200nm）纳入由 SCMC 和 HPMC 组成的粘膜粘附性薄膜中。结果表明，与含有游离 VB6 的对照薄膜（96.37%，T50%溶解 30 分钟）相比，LP 薄膜在 6 小时后释放 VB6 时间延长（72.65%，T50%溶解 105 分钟）。在鸡袋上进行了体外评估，并在人体中进行了体内评估。记录了 0.2N 的粘膜粘附力和 4.4 小时的停留时间。VB6 经鸡袋粘膜的体外渗透表明，与相应的对照相比，LP 系统的渗透增加。有趣的是，将囊泡纳入粘膜粘附性薄膜会使通量减少 36.89%，相对于 LP 分散体。同时，两种薄膜的初始渗透速度均快于液体形式。将体外累积渗透百分率与体外累积释放百分率相关表明，LPs 可延缓 VB6 的释放，但可改善渗透。这些有前途的结果代表了水溶性维生素颊部递送领域的一个进步。
