The preparation and acute antihypertensive effects of a nanocapsular form of darodipine, a dihydropyridine calcium entry blocker.
We have addressed two problems associated with the use of dihydropyridine calcium entry blockers in antihypertensive therapy, namely, potent vasodilation and short half-lives, by incorporating the representative blocker, darodipine, into a nanocapsular vehicle. In awake, renovascular hypertensive rats, darodipine nanocapsules lowered blood pressure when given orally or intramuscularly, and the initial fall in blood pressure was less marked than that observed with the same dose of darodipine dissolved in polyethylene glycol 400 (PEG). Intramuscular administration of the nanocapsular form of darodipine had an antihypertensive effect which lasted for at least 24 hr.
Hubert
B
B
Laboratory de Pharmacie Galénique, Faculté des Sciences Pharmaceutiques Biologiques, Nancy, France.
Atkinson
J
J
Guerret
M
M
Hoffman
M
M
Devissaguet
J P
JP
Maincent
P
P
D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000494:pharmacology; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000494:pharmacology; D002214:Capsules; D006978:Hypertension, Renovascular / Q000188:drug therapy; D008297:Male; D009543:Nifedipine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013535:Suspensions
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; D002214:Capsules; D013535:Suspensions; D009543:Nifedipine; C034600:darodipine