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Enhanced oral bioavailability of an antipsychotic drug through nanostructured lipid carriers.
- Source :
-
International journal of biological macromolecules [Int J Biol Macromol] 2018 Apr 15; Vol. 110, pp. 269-275. Date of Electronic Publication: 2018 Jan 31. - Publication Year :
- 2018
-
Abstract
- 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.<br /> (Copyright © 2018 Elsevier B.V. All rights reserved.)
- Subjects :
- Administration, Oral
Animals
Biological Availability
Castor Oil chemistry
Castor Oil pharmacokinetics
Castor Oil pharmacology
Lecithins chemistry
Lecithins pharmacokinetics
Lecithins pharmacology
Male
Olanzapine
Poloxamer chemistry
Poloxamer pharmacokinetics
Poloxamer pharmacology
Rats
Rats, Wistar
Triglycerides chemistry
Triglycerides pharmacokinetics
Triglycerides pharmacology
Antipsychotic Agents chemistry
Antipsychotic Agents pharmacokinetics
Antipsychotic Agents pharmacology
Benzodiazepines chemistry
Benzodiazepines pharmacokinetics
Benzodiazepines pharmacology
Drug Carriers chemistry
Drug Carriers pharmacokinetics
Drug Carriers pharmacology
Nanoparticles chemistry
Nanoparticles therapeutic use
Subjects
Details
- Language :
- English
- ISSN :
- 1879-0003
- Volume :
- 110
- Database :
- MEDLINE
- Journal :
- International journal of biological macromolecules
- Publication Type :
- Academic Journal
- Accession number :
- 29402457
- Full Text :
- https://doi.org/10.1016/j.ijbiomac.2018.01.121