6533b7d0fe1ef96bd125ae7b
RESEARCH PRODUCT
Core-Shell Arginine-Containing Chitosan Microparticles for Enhanced Transcorneal Permeation of Drugs
Paola VarvaràGaetano GiammonaNicolò MauroMariano LicciardiGennara CavallaroGiulia Di Primasubject
Drug3003congenital hereditary and neonatal diseases and abnormalitiesArginineSwinemedia_common.quotation_subjectamphiphilic copolymerPharmaceutical ScienceL-arginineAdministration Ophthalmic02 engineering and technologyArginine030226 pharmacology & pharmacyCorneaChitosan03 medical and health scienceschemistry.chemical_compoundDrug Delivery Systems0302 clinical medicineMucoadhesionSide chainAnimalsskin and connective tissue diseasesProtein Kinase Inhibitorsmedia_commonMucin-3microparticlesDrug CarriersMucinnutritional and metabolic diseasesSorafenibPermeation021001 nanoscience & nanotechnologyCombinatorial chemistryBioavailabilityDrug LiberationmicroparticlechemistrySettore CHIM/09 - Farmaceutico Tecnologico Applicativoocular administrationchitosan0210 nano-technologymucoadhesiondescription
Chitosan oligosaccharide (C) was functionalized with L-arginine (A) and short hydrocarbon chains (C-8) to design an amphiphilic copolymer, henceforth CAC(8), leading to microparticles (MPs) consisting of an arginine-decorated hydrophilic shell and inner hydrophobic domains allowing the encapsulation of high amount hydrophobic drugs such as sorafenib tosylate (>10% w/w). L-arginine side chains were selected in order to impart the final MPs enhanced transcorneal penetration properties, thus overcoming the typical biological barriers which hamper the absorption of drugs upon topical ocular administration. The mucoadhesive properties and drug release profile of the CAC(8) MPs (CAC(8)-MPs) were studied, showing that CAC(8)-MPs can strongly interact with mucin, and thus gradually release their payload in situ to potentially improve the bioavailability of the drug after topical administration. In vitro transcorneal studies also showed that CAC(8)-MPs are endowed with effective permeation enhancer ability combined with negligible toxicity. (c) 2019 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2019-01-01 |