title: Sonication-Assisted Layer-by-Layer Assembly for Low Solubility Drug Nanoformulation.
abstract: Sonication-assisted layer-by-layer (LbL) self-assembly is a nanoencapsulation technique based on the alternate adsorption of oppositely charged polyelectrolytes, enabling the encapsulation of low solubility drugs. In this work, a top-down LbL technique was performed using a washless approach and ibuprofen (IBF) as a model class II drug. For each saturated layer deposition, polyelectrolyte concentration was determined by titration curves. The first layer was constituted by cationic poly(allylamine hydrochloride) (PAH), given the IBF negative surface charge, followed by anionic polystyrenesulfonate (PSS). This polyelectrolyte sequence was made up with 2.5, 5.5, and 7.5 bilayer nanoshells. IBF nanoparticles (NPs) coated with 7.5 bilayers of PAH/PSS showed 127.5 ± 38.0 nm of particle size, a PDI of 0.24, and a high zeta potential (+32.7 ± 0.6 mV), allowing for a stable aqueous nanocolloid of the drug. IBF entrapment efficiency of 72.1 ± 5.8% was determined by HPLC quantification. In vitro MTT assay showed that LbL NPs were biocompatible. According to the number of coating layers, a controlled release of IBF from LbL NPs was achieved under simulated intestinal conditions (from 5 h up to 7 days). PAH/PSS-LbL NPs constitute a potential delivery system to improve biopharmaceutical parameters of water low solubility drugs.
authors.affiliation: †Center for Neuroscience and Cell Biology, University of Coimbra, Rua Larga, Faculty of Medicine, Pólo I, First Floor, 3000-504 Coimbra, Portugal.|‡Faculty of Pharmacy, University of Coimbra, Azinhaga Sta. Comba, 3000-548 Coimbra, Portugal.
authors.forename: Ana C
authors.initials: AC
authors.lastname: Santos
authors.affiliation: §Institute for Micromanufacturing, Louisiana Tech University, P.O. Box 10137, Ruston 71272, Louisiana, United States.
authors.forename: Pravin
authors.initials: P
authors.lastname: Pattekari
authors.affiliation: †Center for Neuroscience and Cell Biology, University of Coimbra, Rua Larga, Faculty of Medicine, Pólo I, First Floor, 3000-504 Coimbra, Portugal.|‡Faculty of Pharmacy, University of Coimbra, Azinhaga Sta. Comba, 3000-548 Coimbra, Portugal.
authors.forename: Sandra
authors.initials: S
authors.lastname: Jesus
authors.affiliation: †Center for Neuroscience and Cell Biology, University of Coimbra, Rua Larga, Faculty of Medicine, Pólo I, First Floor, 3000-504 Coimbra, Portugal.|‡Faculty of Pharmacy, University of Coimbra, Azinhaga Sta. Comba, 3000-548 Coimbra, Portugal.
authors.forename: Francisco
authors.initials: F
authors.lastname: Veiga
authors.affiliation: §Institute for Micromanufacturing, Louisiana Tech University, P.O. Box 10137, Ruston 71272, Louisiana, United States.
authors.forename: Yuri
authors.initials: Y
authors.lastname: Lvov
authors.affiliation: ‡Faculty of Pharmacy, University of Coimbra, Azinhaga Sta. Comba, 3000-548 Coimbra, Portugal.|∥Institute For Innovation And Health Research, Group Genetics of Cognitive Dysfunction, Institute for Molecular and Cell Biology, Rua do Campo Alegre, 823, 4150-180 Porto, Portugal.
authors.forename: António J
authors.initials: AJ
authors.lastname: Ribeiro
mesh_terms: D000327:Adsorption / Q000187:drug effects; D000499:Allylamine / Q000737:chemistry; D004339:Drug Compounding; D004573:Electrolytes / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007052:Ibuprofen / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011137:Polystyrenes / Q000737:chemistry* / Q000494:pharmacology; D012995:Solubility / Q000187:drug effects; D013010:Sonication
chemical_list: D004573:Electrolytes; D011137:Polystyrenes; D000499:Allylamine; C003321:polystyrene sulfonic acid; D007052:Ibuprofen
keywords: colloid; controlled release; electrostatic interactions; layer-by-layer self-assembly; oral delivery; washless