Polymer coated liposomes for use in the oral cavity - a study of the in vitro toxicity, effect on cell permeability and interaction with mucin.
In this study we investigated the in vitro toxicity, impact on cell permeability and mucoadhesive potential of polymer-coated liposomes intended for use in the oral cavity. A TR146 cell line was used as a model. The overall aim was to end up with a selection of safe polymer coated liposomes with promising mucoadhesive properties for drug delivery to the oral cavity. The following polymers were tested: chitosan, low-methoxylated pectin (LM-pectin), high-methoxylated pectin (HM-pectin), amidated pectin (AM-pectin), Eudragit, poly(N-isopropylacrylamide-co-methacrylic acid) (p(NIPAAM-co-MAA)), hydrophobically modified hydroxyethyl cellulose (HM-HEC), and hydrophobically modified ethyl hydroxyethyl cellulose (HM-EHEC). With chitosan as an exception, all the systems exhibited no significant effect on cell viability and permeability at the considered concentrations. Additionally, all the formulations showed to a varying degree an interaction with mucin (BSM type I-S); the positively charged formulations exhibited the strongest interaction, while the negatively and neutrally charged formulations displayed a moderate or low interaction. The ability to interact with mucin makes all the liposomal formulations promising for oromucosal administration. Although the chitosan-coated liposomes affected the cell viability, this formulation also influenced the cell permeability, which makes it an interesting candidate for systemic drug delivery from the oral cavity.
a Department of Pharmacy , School of Pharmacy, University of Oslo , Blindern , Oslo , Norway.
Therese
http://orcid.org/0000-0001-9654-6697
T
Klemetsrud
b Faculty of Engineering , Østfold University College , Halden , Norway , and.
Anna-Lena
AL
Kjøniksen
a Department of Pharmacy , School of Pharmacy, University of Oslo , Blindern , Oslo , Norway.
Marianne
M
Hiorth
c Section for Pharmaceutical Design and Drug Delivery, Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen , Universitetsparken 2, Copenhagen , Denmark.
Jette
J
Jacobsen
a Department of Pharmacy , School of Pharmacy, University of Oslo , Blindern , Oslo , Norway.
Gro
G
Smistad
D002460:Cell Line; D002470:Cell Survival; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D065546:Drug Liberation; D006801:Humans; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D008081:Liposomes / Q000737:chemistry* / Q000494:pharmacology; D009055:Mouth / Q000378:metabolism*; D009077:Mucins / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D010368:Pectins / Q000737:chemistry*; D010539:Permeability; D013499:Surface Properties
D008081:Liposomes; D009077:Mucins; C462399:ethyl(hydroxyethyl)cellulose; D010368:Pectins; D002482:Cellulose; C002283:hydroxyethylcellulose; D048271:Chitosan
Liposome; mucoadhesion; nanotechnology; polymer coating; toxicity