Delivery of biologically active material in a liposomal formulation for administration into the mouth

• US 5,891,465 A
• Filed: 05/14/1996
• Issued: 04/06/1999
• Est. Priority Date: 05/14/1996
• Status: Expired due to Term

• Current Assignee: BioZone Laboratories, Incorporated (Ceba-Tech Specialty Solutions, Inc.)
• Original Assignee: BioZone Laboratories, Incorporated (Ceba-Tech Specialty Solutions, Inc.)
• Inventors: Kiss, Steven, Keller, Brian C., Fisher, Daniel L.
• Primary Examiner(s): Kishore, Gollamudi S.
• Application Number:
  US08/645,894
• Time in Patent Office: 1,057 Days
• Field of Search: 424/450, 424/43, 424/45, 424/195.1
• US Class Current: 424/450
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61K 9/1277 Processes for preparing; Proliposomes

Abstract

The present invention provides compositions and methods of administering nutritional supplements. The compositions and methods of the present invention are based on nutritional supplements that are encapsulated in lipid vesicles for administration as an aerosol or liquid droplet spray.

Claims

1. A liposomal composition suitable for the aerosol or spray delivery of melatonin to a subject, said composition comprising melatonin and optionally an additional supplement in phospholipid liposomes and a carrier wherein the liposomes have between about 20 nm and 10 microns in diameter and results in absorption into the blood stream, when administered, wherein the phospholipid liposome comprises one or more bilayer forming lipids, wherein said composition provides an increase in bioavailability of said supplement or drug of approximately 20 % or more when compared to an orally administered solid form, and wherein said composition comprises by weight percent, from about 0.25 to 20% lecithin, from about 0.025 to 2% cholesterol or zoosterol or phytosterol, from about 0.01 to 3% antioxidant, from about 0.05 to 0.4% melatonin, from about 0.1 to 20% glycerin, propylene glycol or butylene glycol, from about 0.1% to 10% ethanol, from about 0.015 to 4% anti microbial agent and from about 2 to 99.9% water.

2. The composition of claim 1 wherein said composition further comprises one or more additional supplements selected from the group consisting of Ginkgo biloba extract, Kava Kava extract, Ginseng extract, Saw Palmetto extract, glucosamine sulfate, chromium picolinate, Milk thistle extract, Grape seed extract, Ma Huang extract, Echinecia, Co-Q10 supplement, water soluble vitamins, and fat soluble vitamins.

3. The composition of claim 1, wherein said composition provides an increase in bioavailability from about 20% to 50% when compared to an orally administered solid form of said agent.

4. The composition of claim 3, wherein said composition provides an increase in bioavailability of approximately 30% when compared to an orally administered solid form of said agent.

5. A method for the systemic administration of a drug or supplement to a subject, said method comprising the steps of:

orally administering an aerosol or spray comprising the composition of claim 1 or 2 which results in

said composition being sublingually absorbed into the blood stream, wherein the phospholipid vesicles comprising one or more bilayer forming lipids and said method provides an increase in bioavailability of approximately 20% or more when compared to an orally administered solid form of said supplement or drug.

6. The method of claim 5 wherein said aerosol or spray is provided by a mechanical pump delivery device.

7. The method of claim 5, wherein said method provides an increase in bioavailability from about 20% to 50% when compared to an orally administered solid form of said agent.

8. The method of claim 7, wherein said method provides an increase in bioavailability of approximately 30% when compared to an orally administered solid form of said agent.

9. A mechanical pump delivery device containing the composition of claim 1.