title: Bioadhesive lipid compositions: self-assembly structures, functionality, and medical applications.
abstract: Lipid-based liquid crystalline compositions of phospholipids and diglycerides have unique bioadhesive properties with several medical applications, as exemplified by a lipid-based medical device indicated for management and relief of intraoral pain. The present paper describes the relation between self-assembly properties of phosphatidyl choline (PC) and glycerol dioleate (GDO) mixtures in the presence of aqueous fluids and functional attributes of the system, including: film formation and bioadhesion, intraoral coverage, acceptance by patients, and potential as a drug delivery system. The phase behavior of PC/GDO was characterized using synchrotron small-angle X-ray scattering. Functional properties, including the presence of study formulations at intraoral surfaces, ease of attachment, taste, and degree of and intraoral pain, were assessed in a crossover clinical pilot study in head and neck cancer patients. An optimum in functional properties was indicated for formulations with a PC/GDO weight ratio of about 35/65, where the lipids form a reversed cubic liquid crystalline micellar phase structure (Fd3m space group) over the relevant temperature range (25-40 °C).
authors.affiliation: Biomedical Science, Faculty of Health and Society, Malmö University , SE-20506 Malmö, Sweden.
authors.forename: Justas
authors.initials: J
authors.lastname: Barauskas
authors.forename: Lars
authors.initials: L
authors.lastname: Christerson
authors.forename: Maria
authors.initials: M
authors.lastname: Wadsäter
authors.forename: Fredrick
authors.initials: F
authors.lastname: Lindström
authors.forename: Anna-Karin
authors.initials: AK
authors.lastname: Lindqvist
authors.forename: Fredrik
authors.initials: F
authors.lastname: Tiberg
mesh_terms: D000818:Animals; D002448:Cell Adhesion; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D004075:Diglycerides / Q000737:chemistry / Q000378:metabolism; D004311:Double-Blind Method; D016503:Drug Delivery Systems; D005260:Female; D006258:Head and Neck Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology*; D006801:Humans; D008055:Lipids / Q000008:administration & dosage / Q000737:chemistry*; D050866:Liquid Crystals / Q000737:chemistry*; D008297:Male; D008647:Mesocricetus; D008823:Micelles; D009055:Mouth / Q000187:drug effects / Q000378:metabolism / Q000473:pathology*; D053758:Nanoparticles / Q000008:administration & dosage*; D019226:Oral Ulcer / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology*; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D044367:Phase Transition; D010713:Phosphatidylcholines / Q000737:chemistry / Q000378:metabolism; D010865:Pilot Projects; D011136:Polysorbates; D053838:Scattering, Small Angle; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry; D017356:Synchrotrons; D014867:Water / Q000737:chemistry
chemical_list: D004075:Diglycerides; D008055:Lipids; D008823:Micelles; D004364:Pharmaceutical Preparations; D010713:Phosphatidylcholines; D011136:Polysorbates; D013501:Surface-Active Agents; D014867:Water; C013965:diolein
keywords: bioadhesive; diglyceride; glycerol dioleate; lipid; liquid crystalline; oral mucositis; pain; phosphatidyl choline