Bioadhesive drug delivery systems. I. Characterisation of mucoadhesive properties of systems based on glyceryl mono-oleate and glyceryl monolinoleate.
A group of fatty acid esters capable of forming liquid crystals has been identified as a new class of potential bioadhesive substances. The liquid crystals may act as a controlled release system. The experimental work was focused on the monoglycerides, glyceryl mono-oleate (GMO) and glyceryl monolinoleate (GML). The mucoadhesive properties of GMO and GML were demonstrated in vitro by a 'flushing' bioadhesion test system and a tensiometric method. The flushing system was validated with GMO. Mucoadhesion is influenced by the drug and excipient added, their concentrations, and the ability to form especially the cubic phase. It has been shown that the cubic phase is mucoadhesive when formed on wet mucosa, such as rabbit jejunum, and that drug added to the precursor formulation is incorporated in the cubic phase formed. Tensiometric measurements have shown that the unswollen monoglycerides have the greatest mucoadhesion, followed by the partly swollen lamellar phase and the fully swollen cubic phase. The values found for the work of adhesion were in the range 0.007-0.048 mJcm-2. The mechanism of mucoadhesion is unspecific and probably involves dehydration of the mucosa. The cubic phase of GMO and GML may be an interesting candidate for a bioadhesive drug delivery system.
Nielsen
L S
LS
DUMEX-ALPHARMA A/S, International Pharmaceuticals Division, Pharmaceutical Development, Dalslandsgade 11, DK-2300 Copenhagen S, Denmark. lise-sylvest.nielsen@alpharma.no
Schubert
L
L
Hansen
J
J
D000268:Adhesiveness; D000818:Animals; D016503:Drug Delivery Systems; D005989:Glycerides / Q000737:chemistry* / Q000378:metabolism; D008297:Male; D009092:Mucous Membrane / Q000378:metabolism; D011817:Rabbits; D013552:Swine
D005989:Glycerides; C005953:monoolein