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Biodegradable Solid Lipid Nanoparticle Flocculates for Pulmonary Delivery of Insulin

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The aim of our study was to prepare and characterize biodegradable insulin-loaded solid lipid nanoparticles (Ins-SLNs) flocculates for the pulmonary delivery of Ins. The cationic Ins-SLNs and anionic Ins-SLNs were prepared by W/O/W emulsion technique, respectively. Then anionic Ins-SLNs were self-assembled into flocculates via electrostatic interactions with the oppositely surface charged cationic Ins-SLNs followed by lyophilized into dry powders. The maximal entrapment efficiency of cationic Ins-SLNs and anionic Ins-SLNs were 56.32±1.01% and 66.02±1.58%, respectively. Freeze-drying the Ins-SLNs flocculates yielded dry powders with desirable aerodynamic diameter of 2.04±0.17 μm and low bulk density of 0.06146±0.0045 g/cm3, suitable for inhalation. In addition, the flocculates showed high aerosolization efficiency (emitted fraction of 92.54±0.77% and respirable fraction of 66.89±3.02%). The in vivo study showed that Ins-SLNs flocculates could prolong hypoglycemic effect and a relative pharmacological bioavailability of 35.62±1.34% could be achieved after intratracheal instillation to diabetic rats at the dose of 8 IU/kg dosage. Therefore, the biodegradable SLN flocculates fabricated via charge interaction may provide a useful strategy to fabricate dry powder for pulmonary administration of protein therapeutics or antigens.
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Keywords: CHARGE INTERACTION; HYPOGLYCEMIC EFFECT; INSULIN; PULMONARY DELIVERY; RELATIVE PHARMACOLOGICAL BIOAVAILABILITY; SOLID LIPID NANOPARTICLE

Document Type: Research Article

Publication date: October 1, 2012

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  • Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
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