title: Nanoencapsulation of olanzapine increases its efficacy in antipsychotic treatment and reduces adverse effects.
abstract: Olanzapine is an atypical antipsychotic drug, whose chronic use has been associated with the development of potential adverse effects such as weight gain and cardio-metabolic disorders like hypercholesterolemia and diabetes. To circumvent these side effects, the controlled release of olanzapine is a promising approach to improve adhesion of schizophrenic patients to the treatment. An innovative strategy to prolong drug release consists of loading the drug into biodegradable polymeric lipid-core nanocapsules. In this study, particle size, polydispersity, pH, zeta potential and drug loading of olanzapine-loaded lipid-core nanocapsules were analyzed. Weight gain, biochemical parameters and antipsychotic activity were evaluated in male Wistar rats. The lipid-core nanocapsules had a mean diameter of 156 +/- 13 nm, a polydispersity index lower than 0.1, a pH value of 6.12 +/- 0.14, zeta potential of -17 +/- 2.40 mV and encapsulation efficiency close to 100%. The animals treated with olanzapine-loaded lipid-core nanocapsules showed significantly lower weight gain (63.4 +/- 19.6 g) and total cholesterol levels (66.2 +/- 3.5 g x dl(-1)), compared to those administered with free olanzapine (112.6 +/- 10.3 g and 90.4 +/- 2.4 g x dl(-1)), respectively. Additionally, a more prolonged antipsychotic action was observed in the stereotyped behavior animal model induced by D,L-amphetamine, which affords to conclude that nanoencapsulation is a promising alternative to treat schizophrenic patients.
authors.forename: Frantiescoli A
authors.initials: FA
authors.lastname: Dimer
authors.forename: Manoel
authors.initials: M
authors.lastname: Ortiz
authors.forename: Camila S
authors.initials: CS
authors.lastname: Pase
authors.forename: Katiane
authors.initials: K
authors.lastname: Roversi
authors.forename: Rossana B
authors.initials: RB
authors.lastname: Friedrich
authors.forename: Adriana R
authors.initials: AR
authors.lastname: Pohlmann
authors.forename: Marilise E
authors.initials: ME
authors.lastname: Burger
authors.forename: Silvia S
authors.initials: SS
authors.lastname: Guterres
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry; D001569:Benzodiazepines / Q000008:administration & dosage* / Q000009:adverse effects* / Q000737:chemistry; D004058:Diffusion; D004357:Drug Synergism; D008297:Male; D001523:Mental Disorders / Q000139:chemically induced* / Q000517:prevention & control*; D053769:Nanocapsules / Q000008:administration & dosage* / Q000009:adverse effects / Q000737:chemistry* / Q000648:ultrastructure; D000077152:Olanzapine; D010316:Particle Size; D011618:Psychotic Disorders / Q000175:diagnosis / Q000188:drug therapy*; D051381:Rats; D017208:Rats, Wistar; D013499:Surface Properties; D016896:Treatment Outcome
chemical_list: D014150:Antipsychotic Agents; D053769:Nanocapsules; D001569:Benzodiazepines; D000077152:Olanzapine