Method for drug loading in liposomes
First Claim
1. A method of preparing liposomes, comprising forming liposomes having an internal compartment and a bilayer lipid membrane, said liposomes having a concentration gradient of ammonium glucuronate across their bilayer lipid membranes;
- and contacting the liposomes with an ionizable therapeutic agent to achieve transport of the agent into the internal compartment.
0 Assignments
0 Petitions
Accused Products
Abstract
A liposome composition having a protonatable therapeutic agent entrapped in the form of a salt with a glucuronate anion is disclosed. Methods for preparing the composition using an ammonium ion transmembrane gradient having glucuronate as the counterion are also disclosed. In one embodiment where the protonatable agent is doxorubicin, the method of the invention has comparable loading efficiency, faster release rate, without compromising the therapeutic efficacy compared to loading with an ammonium ion gradient having sulfate as the counterion.
20 Citations
9 Claims
-
1. A method of preparing liposomes, comprising forming liposomes having an internal compartment and a bilayer lipid membrane, said liposomes having a concentration gradient of ammonium glucuronate across their bilayer lipid membranes;
- and contacting the liposomes with an ionizable therapeutic agent to achieve transport of the agent into the internal compartment.
- View Dependent Claims (2, 3, 4, 5)
-
6. A method for loading a protonatable compound into pre-formed liposomes, comprising:
- preparing a suspension of liposomes having a greater concentration of ammonium glucuronate inside the liposomes than outside the liposomes thereby establishing an ammonium ion concentration gradient from the inside to outside of the liposomes;
wherein said gradient is capable of active transport of said protonatable compound towards the inside of the liposomes, adding an amount of protonatable compound to the suspension, and allowing said protonatable compound to transport into said liposomes to achieve a content of said protonatable compound inside the liposomes to be greater than that outside of the liposomes. - View Dependent Claims (7, 8, 9)
- preparing a suspension of liposomes having a greater concentration of ammonium glucuronate inside the liposomes than outside the liposomes thereby establishing an ammonium ion concentration gradient from the inside to outside of the liposomes;
Specification