Comparative in vitro evaluation of several colloidal systems, nanoparticles, nanocapsules, and nanoemulsions, as ocular drug carriers.
Three different colloidal carriers, namely, nanoparticles and nanocapsules made of poly-epsilon-caprolactone and submicron emulsions, were designed, and their capacity for increasing the comeal penetration of drugs was investigated. The three systems differed in their inner structure and composition, but they had a similar size (200-250 nm) and a negative superficial charge (-16 to -42 mV). Indomethacin, which was used as a model drug, was dispersed at a molecular level within the colloidal systems, no chemical interaction between the polymer and the drug being detected. Release of the encapsulated indomethacin occurred very rapidly upon high dilution in a buffered medium and was independent of the composition of the system. The in vitro comeal penetration of the encapsulated indomethacin was more than 3-fold that of the commercial eye drops. This increased penetration was similar for the three formulations investigated, which therefore excludes the influence of the inner structure or chemical composition of the colloidal systems on the comeal penetration of indomethacin. Thus, it could be stated that the main factor responsible for the favorable comeal transport of indomethacin is the colloidal nature of these carriers rather than their inner structure or composition.
Calvo
P
P
Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Santiago de Compostela, Spain.
Vila-Jato
J L
JL
Alonso
M J
MJ
D000818:Animals; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D003102:Colloids / Q000008:administration & dosage* / Q000737:chemistry; D003315:Cornea / Q000378:metabolism*; D004337:Drug Carriers; D004355:Drug Stability; D004655:Emulsions; D005069:Evaluation Studies as Topic; D007213:Indomethacin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D009883:Ophthalmic Solutions; D010316:Particle Size; D011091:Polyesters / Q000008:administration & dosage* / Q000737:chemistry; D011817:Rabbits
D002214:Capsules; D003102:Colloids; D004337:Drug Carriers; D004655:Emulsions; D009883:Ophthalmic Solutions; D011091:Polyesters; C016240:polycaprolactone; D007213:Indomethacin