Modification of solid lipid nanoparticles loaded with nebivolol hydrochloride for improvement of oral bioavailability in treatment of hypertension: polyethylene glycol versus chitosan oligosaccharide lactate

• Published in: Journal of microencapsulation Vol. 33; no. 1; pp. 30 - 42
• Main Authors: Üstündağ-Okur, Neslihan, Yurdasiper, Aysu, Gündoğdu, Evren, Homan Gökçe, Evren
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 02-01-2016
• Subjects: Administration, Oral; Caco-2 Cells; cell culture; Chitosan - chemistry; Chitosan - pharmacokinetics; Chitosan - pharmacology; Encapsulation; Humans; Hypertension - drug therapy; Nanoparticles - chemistry; Nebivolol - chemistry; Nebivolol - pharmacokinetics; Nebivolol - pharmacology; Oligosaccharides - chemistry; Oligosaccharides - pharmacokinetics; Oligosaccharides - pharmacology; permeation; Polyethylene Glycols - chemistry; Polyethylene Glycols - pharmacokinetics; Polyethylene Glycols - pharmacology; Encapsulation; cell culture; permeation
• ISSN: 0265-2048; 1464-5246
• DOI: 10.3109/02652048.2015.1094532

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.