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Int J Biol Macromol ; 110: 269-275, 2018 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-29402457

RESUMO

Olanzapine is an atypical antipsychotic, undergoes extensive first pass metabolism, also has poor aqueous solubility and belongs to BCS (Biopharmaceutical Classification System) Class II drug) exhibit low oral bioavailability. To overcome this and to enhance the bioavailability, intestinal lymphatic transport of drugs can be exploited through Nano structured lipid carriers (NLCs). The NLCs were formulated by solvent diffusion method using solid lipid (glyceryl tripalmitate), liquid lipid (castor oil) and surfactants (Pluronic F-68, Soylecithin). The formulated NLCs were characterized for physico-chemical properties, in-vitro release studies and in-vivo oral bioavailability. F6 has shown average particle size of 158.5 nm with PI of 0.115 indicating narrow particle size distribution and follows uni modal distribution. It was found that the batch with stearyl amine has a zeta potential of 28.39 mV which confers stability to the dispersion. Bioavailability studies indicate that there was more than 5½-fold increase in oral bioavailability in case of NLCs (F6) compared to olanzapine suspension which indicates that NLCs provided sustained release of the drugs, and these systems can be the preferred as drug carriers for lipophilic drugs in long term disease conditions such as schizophrenia for enhanced bioavailability.


Assuntos
Antipsicóticos , Benzodiazepinas , Portadores de Fármacos , Nanopartículas , Administração Oral , Animais , Antipsicóticos/química , Antipsicóticos/farmacocinética , Antipsicóticos/farmacologia , Benzodiazepinas/química , Benzodiazepinas/farmacocinética , Benzodiazepinas/farmacologia , Disponibilidade Biológica , Óleo de Rícino/química , Óleo de Rícino/farmacocinética , Óleo de Rícino/farmacologia , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacologia , Lecitinas/química , Lecitinas/farmacocinética , Lecitinas/farmacologia , Masculino , Nanopartículas/química , Nanopartículas/uso terapêutico , Olanzapina , Poloxâmero/química , Poloxâmero/farmacocinética , Poloxâmero/farmacologia , Ratos , Ratos Wistar , Triglicerídeos/química , Triglicerídeos/farmacocinética , Triglicerídeos/farmacologia
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