title: The influence of liposomal formulation factors on the interactions between liposomes and hydroxyapatite.
abstract: Liposomes may have potentials as a drug delivery system in the oral cavity; hence, the adsorption to, oral tissues may be of importance. The aim of this study was to find an optimal liposomal formulation with appropriate in vitro stability and which liposomal formulation parameters may be of importance for the interaction to tooth enamel surfaces. Charged liposomes were adsorbed in vitro onto hydroxyapatite (HA), used as a model substance for human dental enamel. For a systematic approach of lipid selection, statistical experimental design and multivariate analysis were conducted to interpret the data. The factors investigated were the type of charge (positive, negative), type of main phospholipid (egg-PC, DPPC, DMPC), type of charged lipid (diacyl-TAP, -ethylPC, -PA, -PG, -PS), the amount of charged component (2.5, 10mol%) and the inclusion of cholesterol in the lipid bilayer. The results indicated that positively charged liposomes expressed significantly higher adsorption levels than the negatively charged ones. The effect of incorporating cholesterol did not turn out to be significant. Both positive egg-PC and DPPC liposomes exhibited high adsorption levels; however egg-PC liposomes were unstable during storage. For positively charged liposomes, the factor "type of main lipid" was found to be of significance for the adsorption, whereas, for negatively charged liposomes, no such important factors were found. Based on the adsorption profile to HA and the in vitro stability in phosphate buffer, the most promising liposomal formulation to target for human enamel in this study was the positively charged DPPC liposomes with 10mol% charged lipid included. However, more experiments are needed to determine the optimum mol% of positively charged lipid for the adsorption onto HA.
authors.affiliation: Department of Pharmacy, School of Pharmacy, University of Oslo, Oslo, Norway. s.h.nguyen@farmasi.uio.no
authors.forename: Sanko
authors.initials: S
authors.lastname: Nguyen
authors.forename: Lee
authors.initials: L
authors.lastname: Solheim
authors.forename: Ragnar
authors.initials: R
authors.lastname: Bye
authors.forename: Morten
authors.initials: M
authors.lastname: Rykke
authors.forename: Marianne
authors.initials: M
authors.lastname: Hiorth
authors.forename: Gro
authors.initials: G
authors.lastname: Smistad
mesh_terms: D000284:Administration, Oral; D000327:Adsorption; D001672:Biocompatible Materials / Q000494:pharmacology; D002851:Chromatography, High Pressure Liquid; D016503:Drug Delivery Systems; D004355:Drug Stability; D017886:Durapatite / Q000494:pharmacology*; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage / Q000494:pharmacology*
chemical_list: D001672:Biocompatible Materials; D008081:Liposomes; D017886:Durapatite