ABSTRACT
OBJECTIVE: To develop non-toxic aqueous ocular drug delivery systems containing prednisolone by means of its nanoencapsulation. MATERIALS AND 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. RESULTS AND DISCUSSION: 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.
Subject(s)
Anti-Inflammatory Agents , Conjunctivitis/drug therapy , Drug Delivery Systems , Nanocapsules/chemistry , Ophthalmic Solutions , Prednisolone , Acrylic Resins/chemistry , Animals , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Cell Line , Chick Embryo , Conjunctivitis/pathology , Drug Evaluation, Preclinical , Ophthalmic Solutions/chemistry , Ophthalmic Solutions/pharmacology , Polyesters/chemistry , Prednisolone/chemistry , Prednisolone/pharmacology , RabbitsABSTRACT
AIMS: The influence of nanoencapsulation of mometasone furoate (MF) in poly(ε-caprolactone) lipid-core nanocapsules (LNC) on its in vitro human skin permeation and penetration was evaluated. METHODS: Semisolid formulations were prepared by increasing the viscosity of LNC using a carbomer (Carbopol(®) Ultrez at 0.5% w/v). Two complementary techniques (the static Franz diffusion cell model and the Saarbrücken penetration model) were used to evaluate skin permeation/penetration. RESULTS: The drug release rate was decreased by nanoencapsulation. The skin permeability of MF was controlled by the nanoencapsulation as well as by increasing the viscosity. Furthermore, the formulation containing the nanoencapsulated MF controlled the amount of drug reaching the deeper skin layers without changing its accumulation in the stratum corneum. CONCLUSION: This formulation is suitable for prolonged treatment of skin disorders which should avoid systemic absorption.
