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US 4,911,928 AGranted
Paucilamellar lipid vesicles
AssigneeMicro-Pak, Inc.
InventorDonald F. H. Wallach
Life of this patent
Estimating the term…
Abstract
A new method of producing paucilamellar lipid vesicles has been developed. The vesicles are made of non-phospholipid surfactants. The paucilamellar lipid vesicles have 2-8 lipid bilayers surrounding a central cavity which may be filled with either an aqueous-based solution or an oil or wax.
Claims12
A method of making paucilamellar lipid vesicles having a water immiscible oily material filling a substantial portion of the amorphous central cavity comprising the steps of:
- A. forming a lipid phase of a surfactant and any lipid soluble materials to be incorporated into said lipid vesicles, said surfactant being selected from a group consisting of
- polyoxyethylene fatty esters having the formula
- R.sub.1 --COO(C.sub.2 H.sub.4 O).sub.n H
- where R.sub.1 is lauric, myristic, cetyl, stearic, or oleic acid, or their derivatives and n=2-10;
- polyoxyethylene fatty acid ethers, having the formula
- R.sub.2 --CO(C.sub.2 H.sub.4)).sub.m H
- where R.sub.2 is lauric, myristic, or cetyl acids or their derivatives, single or double unsaturated octadecyl acids or their derivative, or double unsaturated eicodienoic acids or their derivatives and m ranges from 2-4;
- diethanolamides, having the formula
- (HOCH.sub.2 --CH.sub.2).sub.2 NCO--R.sub.3
- where R.sub.3 is caprylic, lauric, myristic or linoleic acids or their derivatives;
- long chain acyl hexosamides having the formula
- R.sub.4 --NHCO--(CH.sub.2).sub.3 --CH.sub.3
- where b ranges from 10-18 and R.sub.4 is a sugar molecule selected from a group consisting of glucosamine, glactosmaine, and N-methylglucamine;
- long chain acyl amino acid amides having the formula
- R.sub.5 --CH(COOH)--NHCO--(CH.sub.2).sub.c --CH.sub.3
- where c ranges from 10-18 and R.sub.5 is an amino acid side chain;
- long chain acyl amides having the formula
- HOOC--(CH.sub.2).sub.d --N(CH.sub.3)--(CH.sub.2).sub.3 --NHCO--R.sub.6
- where R.sub.6 is an acyl chain having 12-20 carbons and not more than two unsaturations, and d ranges from 1-3;
- polyoxyethylene (20) sorbitan mono- or trioletate;
- polyoxyethylene glyceryl monosterate with 1-10 polyoxyethylene groups;
- and glycerol monosterate;
- B. forming an oily phase of water immiscible oily material and an oil-suspendable or oil-soluble material to be incorporated;
- C. forming a lipophilic phase by dispersing said oily phase in said lipid phase;
- D. forming an aqueous phase of an aqueous solution and any aqueous soluble material to be incorporated into said lipid vesicles;
- E. blending said lipophilic phase and said aqueous phase under shear mixing conditions
- thereby forming said paucilamellar lipid vesicles having about 2-8 exterior lipid bilayers surrounding a substantially amorphous center with said water immiscible oily material substantially filling said amorphous central cavity.
24 more elements
Oil filled paucilamellar lipid vesicles consisting of about 2-8 lipid bilayers in the form of substantially spherical shells separated by aqueous layers, said lipid bilayers surrounding a large, substantially oil filled amorphous central cavity, said lipid bilayers comprising
- a surfactant selected from a group consisting of polyoxyethylene fatty esters having the formula
- R.sub.1 --COO(C.sub.2 H.sub.4 O).sub.n H
- where R.sub.1 is lauric, myristic, cetyl, stearic, or oleic acid, or their derivatives and n=2-10;
- polyoxyethylene fatty acid ethers, having the formula
- R.sub.2 --CO(C.sub.2 H.sub.4 O).sub.m H
- where R.sub.2 is lauric, myristic, or cetyl acids of their derivatives, single or double unsaturated octadecyl acids or their derivative, or double unsaturated eicodienoic acids or their derivatives and m ranges from 2-4;
- diethanolamides, having the formula
- (HOCH.sub.2 --CH.sub.2).sub.2 NCO--R.sub.3
- where R.sub.3 is caprylic, lauric, myristic or linoleic acids or their derivatives;
- long chain acyl hexosamides having the formula
- R.sub.4 --NHCO--(CH.sub.2).sub.3 --CH.sub.3
- where b ranges from 10-18 and R.sub.4 is a sugar molecule selected from a group consisting of glucosamine, galactomsamine, and N-methylglucamine;
- long chain acyl amino acid amides having the formula
- R.sub.5 --CH(COOH)--NHCO--(CH.sub.2).sub.c --CH.sub.3
- where c ranges from 10-18 and R.sub.5 is an amino acid side chain;
- long chain acyl amides having the formula
- HOOC--(CH.sub.2).sub.d --N--(CH.sub.3)--(CH.sub.2).sub.3 --NHCO--R.sub.6
- where R.sub.6 is an acyl chain having 12-20 carbons and not more than two unsaturations, and d ranges from 1-3;
- polyoxyethylene (20) sorbitan mono- or trioleate;
- polyoxyethylene glyceryl monosterate with 1-10 polyoxyethylene groups;
- and glycerol monostearate;
- said amorphous central cavity being substantially filled with a water immiscible oily solution.
19 more elements
Dependencies are inferred from the claim text.