title: Modification of solid lipid nanoparticles loaded with nebivolol hydrochloride for improvement of oral bioavailability in treatment of hypertension: polyethylene glycol versus chitosan oligosaccharide lactate.
abstract: Nebivolol (NB)-loaded solid lipid nanoparticles (SLNs) were prepared and modified with chitosan oligosaccharide lactate (COL) and polyethylene glycol (PEG) stearate for improvement of its oral bioavailability. Compritol, poloxamer and lecithin were used for the preparation of SLNs by homogenisation method. After in vitro characterisation effect of lipase, pepsin, or pancreatin on degradation and release rate were investigated. Cytotoxicity and permeation were studied on Caco-2 cells. As COL concentration increased in SLNs, size and zeta potential increased. PEG concentration was reversely proportional to particle size with no change in zeta potential. Encapsulation efficiencies (EEs) were determined as 84-98%. DSC confirmed solubilisation of NB in lipid matrix. A sustained release with no burst effect was determined. The presence of enzymes affected the release. SLNs did not reveal cytotoxicity and highest permeability was obtained with PEG modification. PEG-modified SLNs could be offered as a promising strategy for oral delivery of NB.
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, University of Ege , Bornova , Izmir , Turkey and.
authors.forename: Neslihan
authors.initials: N
authors.lastname: Üstündağ-Okur
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, University of Ege , Bornova , Izmir , Turkey and.
authors.forename: Aysu
authors.initials: A
authors.lastname: Yurdasiper
authors.affiliation: b Department of Radiopharmacy , Faculty of Pharmacy, University of Ege , Bornova , Izmir , Turkey.
authors.forename: Evren
authors.initials: E
authors.lastname: Gündoğdu
authors.affiliation: a Department of Pharmaceutical Technology , Faculty of Pharmacy, University of Ege , Bornova , Izmir , Turkey and.
authors.forename: Evren Homan
authors.initials: EH
authors.lastname: Gökçe
mesh_terms: D000284:Administration, Oral; D018938:Caco-2 Cells; D048271:Chitosan / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D053758:Nanoparticles / Q000737:chemistry*; D000068577:Nebivolol / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D009844:Oligosaccharides / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: D009844:Oligosaccharides; D000068577:Nebivolol; D011092:Polyethylene Glycols; D048271:Chitosan; C000595209:polyethylene glycol 1000
keywords: Encapsulation; cell culture; permeation