Micellar nanoparticles

• US 5,629,021 A
• Filed: 01/31/1995
• Issued: 05/13/1997
• Est. Priority Date: 01/31/1995
• Status: Expired due to Term

• Current Assignee: Graceway Pharmaceuticals LLC (Bausch Health Cos., Inc.)
• Original Assignee: Novavax Inc.
• Inventors: Wright, D. Craig
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Benston, Jr., William E.
• Application Number:
  US08/380,942
• Time in Patent Office: 833 Days
• Field of Search: 514/3, 424/489, 424/470, 424/450, 252/312
• US Class Current: 424/489
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: Y10S 977/773 Nanoparticle, i.e. structure having three dimensions of 100 nm or less
• CPC Class Codes: Y10S 977/915 Therapeutic or pharmaceutical composition
• CPC Class Codes: Y10S 977/926 Topical chemical, e.g. cosmetic or sunscreen

Abstract

The present invention relates to micellar nanoparticles and methods of their production. Micellar nanoparticles are made by hydrating a mixture of an oil, a stabilizer/surfactant, and an alcoholic initiator with an aqueous solution. These micellar nanoparticles are normally less than 100 nanometers in diameter. The micellar nanoparticles are particularly advantageous in delivering materials such as estradiol topically through the skin because their small size allows easy penetration.

Claims

1. A micellar nanoparticle having a diameter of between about 25 and 1000 nm, said micellar nanoparticle comprising a lipophilic phase which includes an oil, a stabilizer and an alcohol-based initiator, hydrated with a suitable aqueous solution

wherein said stabilizer is selected from the group consisting of Tween 60, Tween 80, nonylphenol polyethylene glycol ethers, and mixtures thereof.

2. The micellar nanoparticle of claim 1 wherein said initiator is selected from the group consisting of alcoholic materials containing methanol, ethanol and mixtures thereof.

3. The micellar nanoparticle of claim 2 wherein said initiator is selected from the group consisting of alcoholic materials containing 50% or higher ethanol, methanol, and mixtures thereof.

4. The micellar nanoparticle of claim 1 wherein said oil is selected from the group consisting vegetable oils, nut oils, fish oils, lard oil, mineral oils, squalane, tricaprylin, and mixtures thereof.

5. The micellar nanoparticle of claim 1 wherein said aqueous solution comprises a physiologically compatible solution.

6. The micellar nanoparticle of claim 1 wherein said aqueous solution is selected from the group consisting of water, and phosphate buffered saline.

7. The micellar nanoparticle of claim 1 wherein said aqueous phase has an active material dissolved or suspended therein.

8. The micellar nanoparticle of claim 1 wherein said oil has an active material dissolved or suspended therein.

9. The micellar nanoparticle of claim 1 wherein said initiator has an active material dissolved or suspended therein.

10. The micellar nanoparticle of claim 9 wherein said active material comprises estradiol.

11. The micellar nanoparticle of claim 1 wherein said micellar nanoparticle is dispersible in aqueous solution.

12. The micellar nanoparticle of claim 1 wherein the diameter of said micellar nanoparticle allows passage through a 0.2 mm filter.