Uptake of liposomally entrapped adenosine-3′-5′-cyclic monophosphate in mouse brain

[H-3] Adenosine-3', 5'-cyclic monophosphate (cAMP) could be entrapped efficiently into small unilamellar vesicles when bound to cAMP-dependent protein kinase. The leakage of [H-3] cAMP protein kinase complex from liposomes was reduced by more than 60% as compared to free [H-3] cAMP. Hyperosmolar mannitol increased the delivery of liposomally entrapped [H-3] cAMP protein kinase to the brain with maximum uptake occurring at 10 min after mannitol administration. Optimal delivery to the brain was observed when vesicles composed of total brain lipids or phosphatidylcholine: cholesterol: sulfatides ( 7: 2: 1) were used. A slower clearance of liposomally entrapped material from brain tissue was seen under hyperosmolar conditions.