Lipid particle forming matrix, preparation and use thereof
AssigneePharmacia & Upjohn Aktiebolag
InventorsBengt Herslof, Alf Gunnar Martin Nicklasson
Life of this patent
Estimating the term…
Abstract
The invention relates to a lipid particle forming matrix, characterized by, that from a defined system of at least two lipid components chosen from classes of different polarity, in which at least one of the lipid components is bilayer forming, discrete lipid particles are formed spontaneously when interacting with aqueous systems. Preferably at least one of the lipid components is amphiphatic and polar and one is nonpolar. These discrete particles are formed spontaneously from the matrix without any chemical or physical treatment or initiation. The invention also relates to a process for producing the matrix and use thereof.
Claims40
An essentially water-free, liquid or semi-solid, lipid particle forming matrix comprising a bioactive material and a system of analytically pure lipids comprising at least two lipids of different polarity, wherein
- i) at least one lipid is phosphatidylcholine, which is a polar and amphiphilic bilayer forming phospholipid in an amount of 5 to 50% (w/w) of the lipids, and, the remainder of said system is,
- ii) at least one lipid that is a nonpolar lipid and comprises a mixture of monoacyl glycerols wherein the acyl group of each is selected from the group consisting of caprylate (C:8) and caprate (C:10), and
- wherein the said composition forms discrete lipid particles spontaneously at the interface between aqueous and lipid phase after contact with external water of an aqueous medium by budding.
A process for forming lipid carrier particles from an essentially water-free, liquid or semi-solid matrix consisting essentially of mixing, in arbitrary order,
- i) analytically pure phospholipid selected from the group consisting of phosphatidylcholine, phosphatidylglycerol, phosphatidylinositol, phosphatidylserine, phosphatidyl ethanolamine, phosphatidic acid, and derivatives and mixtures thereof which is a polar and amphiphilic bilayer forming phospholipid in an amount of 5 to 50% (w/w) of the lipids,
- ii) at least one analytically pure nonpolar lipid and comprises a mixture of monoacyl glycerols wherein the acyl group of each is selected from the group consisting of caprylate (C:8) and caprate (C:10), as the remainder of the lipid, and
- iii) a bioactive material, whereupon external water or an aqueous medium is added at which discrete lipid particles are formed spontaneously at the interface between the aqueous and lipid phase by budding.
Dependencies are inferred from the claim text.