Prednisolone-loaded nanocapsules as ocular drug delivery system: development, in vitro drug release and eye toxicity.
OBJECTIVE
To develop non-toxic aqueous ocular drug delivery systems containing prednisolone by means of its nanoencapsulation.


METHODS
Nanocapsules were prepared by interfacial deposition of preformed polymer [poly(ε-caprolactone) or Eudragit® RS100]. Particle size distribution was determined by laser diffractometry, photon correlation spectroscopy and nanoparticle tracking analysis. Ocular irritation and cytotoxicity were evaluated in vitro on the chorioallantoic membrane (CAM) and rabbit corneal epithelial cell line, respectively.


CONCLUSIONS
Nanocapsules showed mean particle sizes between 100 and 300 nm and prednisolone encapsulation efficiency of around 50%. Controlled release of prednisolone occurred for 5 h for both formulations according to the biexponential model. Both formulations were found to be non-irritant in the CAM test and non-cytotoxic toward rabbit corneal epithelial cells.


CONCLUSIONS
Encapsulation of prednisolone in nanocapsules was reported for the first time, being suitable for producing eye drops for the treatment of ocular inflammatory and no eye toxicity was indicated.
Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul (UFRGS) , Porto Alegre, RS , Brazil .
Tatiele
T
Katzer
Paula
P
Chaves
Andressa
A
Bernardi
Adriana
A
Pohlmann
Silvia S
SS
Guterres
Ruy Carlos
RC
Ruver Beck
D000180:Acrylic Resins / Q000737:chemistry; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology; D002460:Cell Line; D002642:Chick Embryo; D003231:Conjunctivitis / Q000188:drug therapy* / Q000473:pathology; D016503:Drug Delivery Systems; D004353:Drug Evaluation, Preclinical; D053769:Nanocapsules / Q000737:chemistry*; D009883:Ophthalmic Solutions / Q000737:chemistry / Q000494:pharmacology; D011091:Polyesters / Q000737:chemistry; D011239:Prednisolone / Q000737:chemistry / Q000494:pharmacology; D011817:Rabbits
D000180:Acrylic Resins; D000893:Anti-Inflammatory Agents; D053769:Nanocapsules; D009883:Ophthalmic Solutions; D011091:Polyesters; C016240:polycaprolactone; C050528:Eudragit RS; D011239:Prednisolone
Chorioallantoic membrane; cytotoxicity; eye drops; eye toxicity; nanoparticles; ocular