Lai Francesco, Valenti Donatella, Sinico Chiara, Manconi Maria, Mendez José Blanco, Fadda Anna Maria
Dipartimento Farmaco Chimico Tecnologico, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.
Curr Drug Deliv. 2004 Apr;1(2):145-52. doi: 10.2174/1567201043479957.
The aim of this work is to study liposomes as carriers of nutrients and therapeutic agents in aquaculture with Venerupis decussatus and Venerupis pullastra larvae. Multilamellar (MLVs) and large unilamellar (LUVs) vesicles were prepared from a commercial mixture of soy phosphatidylcholine, rich in unsaturated and polyunsaturated fatty acids, cholesterol, and hydrated with a solution of vitamin B1 both in distilled and sea water. Carboxyfluorescein-loaded liposomes were also prepared in order to test the uptake of vesicles by larvae. The stability of formulations was checked by monitoring the size of vesicles and their drug leakage. In order to limit the vitamin loss, liposome freeze-drying was studied. Dried formulations were also prepared by using different amounts of trehalose as cryoprotectant. We found that freeze-dried vesicles, rehydrated after two weeks, had a vitamin retention (R%) equal to 95%, while their diameter significantly increased. By contrast, liposomes freeze-dried in the presence of trehalose displayed a lower R%, but higher bilayer stability. Finally, when CF-loaded vesicles were added to Venerupis decussatus and Venerupis pullastra larvae incubated in filtered sea water, a bright and diffused fluorescence was present in most of the larvae, a fact which can be regarded as evidence of liposome uptake by Venerupis larvae.
这项工作的目的是研究脂质体作为水产养殖中皱纹盘鲍和翡翠贻贝幼虫营养物质及治疗剂载体的情况。由富含不饱和脂肪酸和多不饱和脂肪酸的大豆磷脂酰胆碱商业混合物、胆固醇制备多层囊泡（MLVs）和大单层囊泡（LUVs），并用维生素B1溶液在蒸馏水和海水中进行水合。还制备了负载羧基荧光素的脂质体，以测试幼虫对囊泡的摄取。通过监测囊泡大小及其药物泄漏来检查制剂的稳定性。为了限制维生素损失，研究了脂质体冻干。还使用不同量的海藻糖作为冷冻保护剂制备了干燥制剂。我们发现，两周后复水的冻干囊泡的维生素保留率（R%）等于95%，而其直径显著增加。相比之下，在海藻糖存在下冻干的脂质体显示出较低的R%，但双层稳定性更高。最后，当将负载CF的囊泡添加到在过滤海水中孵育的皱纹盘鲍和翡翠贻贝幼虫中时，大多数幼虫中都出现了明亮且弥散的荧光，这一事实可被视为翡翠贻贝幼虫摄取脂质体的证据。
