Poly(epsilon-caprolactone) nanocapsules in carteolol ophthalmic delivery.
In order to increase the ocular absorption of carteolol, this antiglaucomatous drug was incorporated into either nanoparticles (NP) or nanocapsules (NC). The polymer used was poly(epsilon-caprolactone) (PCL). The dosage forms were tested on intraocular hypertensive-induced rabbits. Results are presented as the chronological variations of the intraocular pressure (IOP) in comparison with the commercial aqueous solution (Carteol eye drops). The therapeutic results (decrease in IOP) were much more pronounced with carteolol incorporated into the colloidal carriers than with the commercial eye drops. Further, NC displayed a better effect than NP because the drug was entrapped in the oily core of the carrier, thus more readily available to the eye. The incorporation of the drug into nanocapsules produced a decline in the cardiovascular side effects in comparison with aqueous eye drops, thus showing that the undesired noncorneal absorption was reduced. In conclusion, colloidal suspension made of poly(epsilon-caprolactone) could offer a good opportunity for ophthalmic delivery of drugs.
Marchal-Heussler
L
L
Laboratoire de Pharmacie Galénique, Biopharmacie et Pharmacie Hospitalière, Faculté de Pharmacie, Nancy, France.
Sirbat
D
D
Hoffman
M
M
Maincent
P
P
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002214:Capsules; D002354:Carteolol / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects; D007429:Intraocular Pressure / Q000187:drug effects; D007545:Isoproterenol / Q000494:pharmacology; D009798:Ocular Hypertension / Q000503:physiopathology; D009883:Ophthalmic Solutions; D011091:Polyesters; D011817:Rabbits
D002214:Capsules; D009883:Ophthalmic Solutions; D011091:Polyesters; C016240:polycaprolactone; D002354:Carteolol; D007545:Isoproterenol