Abstract
Abstract CDP-choline (CDPc) was encapsulated in unilamellar long circulating liposomes to improve biological effectiveness. The liposomal colloidal suspension was prepared by extrusion of multilamellar vesicles through polycarbonate filters. Unilamellar liposomes with a mean size of 50 nm and a polydispersity index of 0.01 were obtained. CDPc encapsulation capacity was 28 ml/mmol. Unilamellar liposome suspension presented a certain stability both in phosphate buffer and in serum, 25% of CDPc was released after 24 h. The colloidal properties and the presence of ganglioside G MI in liposome composition ensured a long-circulation of the carrier after i.v. administration. The therapeutic effects of CDPc-loaded unilamellar liposomes compared to the free drug were evaluated by an experimental model of ischemia and reperfusion, performed with Wistar rats (320–350 g). The liposomal formulation improved the survival rate of rats subjected to ischemia and reperfusion by approximately 66%, compared to free CDPc. A clinical application may be proposed.
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