Microcapsules in the nanometric range and a method for their production

• US 4,021,364 A
• Filed: 12/04/1973
• Issued: 05/03/1977
• Est. Priority Date: 12/04/1972
• Status: Expired due to Term

• Current Assignee: Speiser; Prof. Dr. Peter
• Original Assignee: Speiser; Prof. Dr. Peter
• Inventors: Speiser, Peter, Birrenbach, Gerd
• Primary Examiner(s): Lovering, Richard D.
• Application Number:
  US05/421,604
• Time in Patent Office: 1,246 Days
• Field of Search: 252/316, 424/33, 424/1, 424/85, 424/89, 117/161 UN, 260/80.3 N, 427/5, 427/36
• US Class Current: 424/1.25
• 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: A61K 9/5138 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5192 Processes
• CPC Class Codes: B01J 13/14 Polymerisation; cross-linking
• CPC Class Codes: Y10T 428/2987 Addition polymer from unsaturated monomers only
• CPC Class Codes: Y10T 428/2989 Microcapsule with solid core [includes liposome]

Abstract

The present invention is concerned with novel synthetic capsules which are colloid soluble in water or suspendible or colloid soluble in hydrophobic media and consist of compatible polymeric material, more especially of acrylamide and N,N'"'"'-methylene-bis-acrylamide gel or of acrylic acid and acrylic acid methyl ester gel, which are submicroscopic and mainly micellar in size, and which contain biologically or pharmacodynamically active material, more especially proteins, antigens, pharmacologically or therapeutically active substances or pesticides, fertilizers, dyes, color forming agents, adhesives and catalysts or other technically active substances in an incorporated and/or adsorbed form, together with the method for their production and their application.

Claims

1. Microcapsules of encapsulated active material, said microcapsules being colloidally soluble in water, said capsules comprising a gel of polymerized acrylamide, polymerized N,N'"'"'-methylene-bis acrylamide, polymerized acrylic acid, or methyl acrylate, said microcapsules having a diameter in a micellar order of magnitude of 20-200 nanometers.

2. The microcapsules as in claim 1, characterized in that the mean diameter of the capsules is below 80 nanometers and the polymeric material is polymerized N,N'"'"' -methylene-bis-acrylamide.

3. A process for the production of microcapsules of polymeric material having encapsulated active materials, said microcapsules being colloidally soluble in water and having a diameter in a micellar order of magnitude of 20-200 nanometers, said process comprising:

(a) dissolving boundary surface-active auxiliary emulsifying substances in a hydrophobic liquid to form micellar reaction spaces in said hydrophobic liquids;

(b) adding to said hydrophobic liquid while stirring, an aqueous solution of an active material to be encapsulated and an encapsulating monomer from the group consisting of acrylamide, N,N'"'"'-methylene-bis-acrylamide, acrylic acid, and methyl acrylate, said aqueous solution substantially assuming a presence in said micellar spaces;

(c) polymerizing the micellarly dissolved monomers to form microcapsules having said active material absorbed and/or encapsulated in said microcapsules, said polymerization taking place in said micellar spaces in said hydrophobic liquid to produce microcapsules having a diameter of a micellar order of magnitude of 20-200 nanometers; and

(d) isolating the resulting microcapsules from the hydrophobic liquid.

4. The process of claim 3 wherein the monomer is first dissolved in water and a solution of the active substance is added to said monomer solution prior to mixing with the hydrophobic liquid.

5. The process of claim 3, in which n-lower alkane, having a boiling point below 0°

C. under vacuum is used as hydrophobic liquid.

6. The process of claim 5 in which the n-lower alkane is n-hexane or n-heptane.

7. The process of claim 3, in which paraffin, ethyl oleate, castor oil or other vegetable oils are used as the hydrophobic liquid.