School of Pharmacy, Queen's University Belfast, 97 Lisburn Road, Belfast BT9 7BL, UK.
Eur J Pharm Sci. 2013 Nov 20;50(3-4):312-22. doi: 10.1016/j.ejps.2013.07.006. Epub 2013 Jul 19.
This work describes the development of spray dried polymer coated liposomes composed of soy phosphatidylcholine (SPC) and phospholipid dimyristoyl phosphatidylglycerol (DMPG) coated with alginate, chitosan or trimethyl chitosan (TMC), that are able to penetrate through the nasal mucosa and offer enhanced penetration over uncoated liposomes when delivered as a dry powder. All the liposome formulations, loaded with BSA as model antigen, were spray-dried to obtain powder size and liposome size in a suitable range for nasal delivery. Although coating resulted in some reduction in encapsulation efficiency, levels were still maintained between 60% and 69% and the structural integrity of the entrapped protein and its release characteristics were maintained. Coating with TMC gave the best product characteristics in terms of entrapment efficiency, glass transition (T(g)) and mucoadhesive strength, while penetration of nasal mucosal tissue was very encouraging when these liposomes were administered as dispersions although improved results were observed for the dry powders.
这项工作描述了喷雾干燥聚合物包被的脂质体的开发,该脂质体由大豆卵磷脂(SPC)和磷脂二肉豆蔻酰磷脂酰甘油(DMPG)组成,用藻酸盐、壳聚糖或三甲基壳聚糖(TMC)包被,能够穿透鼻黏膜,并在作为干粉给药时提供比未包被的脂质体更好的穿透性。所有载有 BSA 作为模型抗原的脂质体制剂均经喷雾干燥以获得适合鼻内给药的粉末粒径和脂质体粒径。尽管包被导致包封效率略有降低,但仍保持在 60%至 69%之间,并且包封的蛋白质的结构完整性及其释放特性得以保持。就包封效率、玻璃化转变温度(T(g))和粘膜粘附强度而言,用 TMC 包被可获得最佳的产品特性,而当这些脂质体作为分散体给药时,对鼻黏膜组织的穿透性非常令人鼓舞,尽管干粉的结果有所改善。