Abstract— Citicoline is a therapeutic agent widely used in the treatment of brain injury, for example in cerebrovascular disease or traumatic accidents. Unfortunately, the strong polar nature of this drug prevents it crossing the blood‐brain barrier. In this paper, the possibility of efficiently trapping citicoline in liposomes to improve its therapeutic effects is reported. The citicoline‐encapsulation efficiency, drug leakage and size analysis of various liposome systems were studied. The real therapeutic effectiveness of these citicoline liposome formulations was evaluated by biological assay. The effects of free and liposome encapsulated citicoline on survival rate of ischaemic reperfused male Wistar rats (80–100 g) were investigated. Of the phospholipid mixtures used in citicoline liposome formulation the best in terms of delivery and therapeutic effects was 1,2‐dipalmitoyl‐sn‐glycero‐phosphocholine:dipalmitoyl‐dl‐α‐phosphatidyl‐l‐serine: cholesterol (7:4:7 molar ratio). This phospholipid mixture was also assayed for brain conjugated diene levels in rats, since this parameter is an index of lipid peroxidation in rat cerebral cortex during post‐ischaemic reperfusion. A citicoline‐loaded phospholipid mixture has produced an increase in rat survival rate of about 24% and a reduction in diene levels of 60%, compared to the free drug. 1994 Royal Pharmaceutical Society of Great Britain

Liposomes as In‐vivo Carriers for Citicoline: Effects on Rat Cerebral Post‐ischaemic Reperfusion

FRESTA M.;
1994-01-01

Abstract

Abstract— Citicoline is a therapeutic agent widely used in the treatment of brain injury, for example in cerebrovascular disease or traumatic accidents. Unfortunately, the strong polar nature of this drug prevents it crossing the blood‐brain barrier. In this paper, the possibility of efficiently trapping citicoline in liposomes to improve its therapeutic effects is reported. The citicoline‐encapsulation efficiency, drug leakage and size analysis of various liposome systems were studied. The real therapeutic effectiveness of these citicoline liposome formulations was evaluated by biological assay. The effects of free and liposome encapsulated citicoline on survival rate of ischaemic reperfused male Wistar rats (80–100 g) were investigated. Of the phospholipid mixtures used in citicoline liposome formulation the best in terms of delivery and therapeutic effects was 1,2‐dipalmitoyl‐sn‐glycero‐phosphocholine:dipalmitoyl‐dl‐α‐phosphatidyl‐l‐serine: cholesterol (7:4:7 molar ratio). This phospholipid mixture was also assayed for brain conjugated diene levels in rats, since this parameter is an index of lipid peroxidation in rat cerebral cortex during post‐ischaemic reperfusion. A citicoline‐loaded phospholipid mixture has produced an increase in rat survival rate of about 24% and a reduction in diene levels of 60%, compared to the free drug. 1994 Royal Pharmaceutical Society of Great Britain
1994
1,2-Dipalmitoylphosphatidylcholine
Animals
Blood-Brain Barrier
Brain Ischemia
Cerebral Cortex
Cholesterol
Chromatography, High Pressure Liquid
Cytidine Diphosphate Choline
Disease Models, Animal
Drug Carriers
Drug Compounding
Drug Evaluation
Lactates
Lactic Acid
Lipid Peroxidation
Liposomes
Male
Phosphatidylserines
Rats
Rats, Wistar
Reperfusion Injury
Survival Rate
Drug Delivery Systems
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.12317/63717
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 72
  • ???jsp.display-item.citation.isi??? ND
social impact