Vesicle formulation for the controlled release of therapeutic agents

• US 5,186,941 A
• Filed: 11/18/1991
• Issued: 02/16/1993
• Est. Priority Date: 05/06/1983
• Status: Expired due to Term

• Current Assignee: NeXstar Pharmaceuticals, Inc. (Gilead Sciences Inc.)
• Original Assignee: Vestar, Inc. (Advanced Micro Devices, Inc.)
• Inventors: Callahan, Richard A., Tin, George W.
• Primary Examiner(s): Lovering, Richard D.
• Application Number:
  US07/794,777
• Time in Patent Office: 456 Days
• Field of Search: 264/4.1, 264/4.3, 424/1.1, 424/450, 428/402.2, 436/829, 514/823, 514/963
• US Class Current: 424/450
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: Y10T 428/2984 Microcapsule with fluid core [includes liposome]

Abstract

Disclosed herein are vesicle compositions for controlled sustained release of an encapsulated therapeutic agent after parenteral administration. By adjusting the osmolarity between the suspending solution and the solution within the vesicles by adjusting the concentration of the suspending solution, the rate of release of the therapeutic agent after parenteral administration can be varied. The compositions can be effectively administered by intramuscular, subcutaneous injection or other means.

Claims

1. A composition comprising a solution of a therapeutic agent encapsulated in vesicles, the vesicles being suspended in a solution containing sufficient solute selected from the group consisting of sugars and polypeptides to provide an osmolarity of the suspending solution which is hypertonic, with respect to the solution within the vesicles and which is of greater osmolarity than physiological saline, said composition being capable of controlling the release in vivo of said therapeutic agent and capable of subcutaneous and intramuscular administration to a host.

2. A composition according to claim 1 wherein said solute is a hexose.

3. A composition according to claim 1 wherein the solute is glucose.

4. A process for administration to a host of a therapeutic agent encapsulated in vesicles, comprising administering to the host a suspension of the agent in vesicles, the vesicles being suspended in a solution containing sufficient solute selected from the group consisting of sugars and polypeptides to provide an osmolarity which is at least about 25% of the osmolarity of the solution within the vesicles and which is of greater osmolarity than physiological saline to control the release in vivo of said therapeutic agent.

5. A process according to claim 4 wherein the osmolarity of the suspending solution is at least about 40 to about 50% of the osmolarity of the solution within the vesicles.

6. A process according to claim 4 wherein the osmolarity of the suspending solution is at least about 75 to about 90% of the osmolarity of the solution within the vesicles.

7. A process according to claim 4 wherein the suspending solution is hypertonic with respect to the solution within the vesicles.

8. A process according to claim 4, wherein said solute is hexose.

9. A process according to claim 4, 5, 6 or 7 wherein the solute is glucose.