Adamczak Małgorzata I, Hagesaether Ellen, Smistad Gro, Hiorth Marianne
Department of Pharmacy, School of Pharmacy, University of Oslo, P.O. Box 1068 Blindern, 0316 Oslo, Norway.
Faculty of Health Sciences, Oslo and Akershus University College of Applied Sciences, Pilestredet 50, 0130 Oslo, Norway.
Int J Pharm. 2016 Feb 10;498(1-2):225-33. doi: 10.1016/j.ijpharm.2015.12.030. Epub 2015 Dec 17.
Drug delivery to the oral cavity poses a significant challenge due to the short residence time of the formulations at the site of action. From this point of view, nanoparticulate drug delivery systems with ability to adhere to the oral mucosa are advantageous as they could increase the effectiveness of the therapy. Positively, negatively and neutrally charged liposomes were coated with four different types of polymers: alginate, low-ester pectin, chitosan and hydrophobically modified ethyl hydroxyethyl cellulose. The mucoadhesion was studied using a novel in vitro method allowing the liposomes to interact with a mucus-producing confluent HT29-MTX cell-line without applying any external force. MTT viability and paracellular permeability tests were conducted on the same cell-line. The alginate-coated liposomes achieved a high specific (genuine) mucin interaction, with a low potential of cell-irritation. The positively charged uncoated liposomes achieved the highest initial mucoadhesion, but also displayed a higher probability of cell-irritation. The chitosan-coated liposomes displayed the highest potential for long lasting mucoadhesion, but with the drawback of a higher general adhesion (tack) and a higher potential for irritating the cells.
由于制剂在作用部位的停留时间较短,向口腔给药面临重大挑战。从这一角度来看,具有粘附于口腔粘膜能力的纳米颗粒药物递送系统具有优势,因为它们可以提高治疗效果。分别用四种不同类型的聚合物(藻酸盐、低酯果胶、壳聚糖和疏水改性乙基羟乙基纤维素)对带正电、带负电和中性的脂质体进行包衣。使用一种新颖的体外方法研究粘膜粘附性,该方法允许脂质体在不施加任何外力的情况下与产生粘液的汇合HT29-MTX细胞系相互作用。对同一细胞系进行MTT活力和细胞旁通透性测试。藻酸盐包衣的脂质体实现了高特异性(真正的)粘蛋白相互作用,且细胞刺激潜力较低。带正电的未包衣脂质体实现了最高的初始粘膜粘附,但也显示出较高的细胞刺激可能性。壳聚糖包衣的脂质体显示出持久粘膜粘附的最高潜力,但缺点是一般粘附性(粘性)较高且刺激细胞的可能性较大。