title: Solid lipid nanoparticles for encapsulation of hydrophilic drugs by an organic solvent free double emulsion technique.
abstract: Encapsulation of hydrophilic compounds for drug delivery systems with high loading efficiency is not easily feasible and remains a challenge, mainly due to the leaking of the drug to the outer aqueous phase during nanoparticle production. Usually, encapsulation of hydrophilic drugs is achieved by using double emulsion or inverse miniemulsion systems that often require the use of organic solvents, which may generate toxicological issues arising from solvent residues. Herein, we present the preparation of solid lipid nanoparticles loaded with a hydrophilic compound by a novel organic solvent free double emulsion/melt dispersion technique. The main objective of this study was to investigate the influence of important process and formulation variables, such as lipid composition, surfactant type, sonication parameters and lipid solidification conditions over physicochemical characteristics of SLN dispersion. Particle size and dispersity, as well as dispersion stability were used as responses. SLN dispersions with average size ranging from 277 to 550 nm were obtained, showing stability for over 60 days at 4 °C depending on the chosen emulsifying system. Entrapment efficiency of fluorescent dyes used as model markers was assessed by fluorescence microscopy and UV-vis spectrophotometry and results suggest that the obtained lipid based nanoparticles could be potentially applied as a delivery system of water soluble drugs.
authors.affiliation: Chemical Engineering Department, Federal University of Santa Catarina-UFSC, P.O. Box 476, 88040-900 Florianópolis, SC, Brazil. Electronic address: lu.beckerperes@gmail.com.
authors.forename: Luana
authors.initials: L
authors.lastname: Becker Peres
authors.affiliation: Chemical Engineering Department, Federal University of Santa Catarina-UFSC, P.O. Box 476, 88040-900 Florianópolis, SC, Brazil. Electronic address: lahbecker@gmail.com.
authors.forename: Laize
authors.initials: L
authors.lastname: Becker Peres
authors.affiliation: Chemical Engineering Department, Federal University of Santa Catarina-UFSC, P.O. Box 476, 88040-900 Florianópolis, SC, Brazil. Electronic address: pedro.h.araujo@ufsc.br.
authors.forename: Pedro Henrique Hermes
authors.initials: PHH
authors.lastname: de Araújo
authors.affiliation: Chemical Engineering Department, Federal University of Santa Catarina-UFSC, P.O. Box 476, 88040-900 Florianópolis, SC, Brazil. Electronic address: claudia.sayer@ufsc.br.
authors.forename: Claudia
authors.initials: C
authors.lastname: Sayer
mesh_terms: D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D004655:Emulsions / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D008055:Lipids / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D008856:Microscopy, Fluorescence; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013010:Sonication; D013501:Surface-Active Agents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors; D014867:Water / Q000737:chemistry
chemical_list: D004655:Emulsions; D008055:Lipids; D004364:Pharmaceutical Preparations; D012997:Solvents; D013501:Surface-Active Agents; D014867:Water
keywords: Delivery systems; Encapsulation efficiency; Hydrophilic compounds; Organic solvent free double emulsion; Solid lipid nanoparticles