Active/passive immunization of the internal female reproductive organs

• US 4,732,763 A
• Filed: 09/28/1984
• Issued: 03/22/1988
• Est. Priority Date: 10/17/1978
• Status: Expired due to Fees

• Current Assignee: Alkermes Controlled Therapeutics Inc. II (Alkermes plc)
• Original Assignee: Stolle Research & Development Corporation
• Inventors: Tanquary, Albert C., Flowers, Charles F., Cowsar, Donald R., Beck, Lee R.
• Primary Examiner(s): GRIFFIN, RONALD
• Application Number:
  US06/655,989
• Time in Patent Office: 1,271 Days
• Field of Search: 424/14-22, 424/78, 424/85-92, 424/433, 514/931, 514/932, 514/963
• US Class Current: 424/433
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61K 39/00 Medicinal preparations containing antigens or antibodies materials for immunoassay G01N33/53
• CPC Class Codes: A61K 9/0036 Devices retained in the vagina or cervix for a prolonged period, e.g. intravaginal rings, medicated tampons, medicated diaphragms
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/1647 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: C07K 16/00 Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies antibodies with enzymatic activity, e.g. abzymes C12N9/0002
• CPC Class Codes: C12N 11/04 entrapped within the carrier, e.g. gel or hollow fibres
• CPC Class Codes: Y10S 424/811 involving sex selection or contraception

Abstract

Antibody or antigen containing microparticles for the active or passive immunization of the internal female reproductive organs, comprising: microparticles of an antigen or antibody incorporated in a matrix material which is biocompatible and biologically degradable, said microparticles capable of being transported after deposition in the vagina by the natural transport mechanism of the internal female reproductive organs across the cervix into the uterus.

Claims

1. Anti-B-HCG containing microparticles for the immunization of the internal female reproductive organs, said microparticles containing a biologically effective amount of anti-B-HCG incorporated in a matrix material which is biocompatible and biologically degradable, said microcapsules being capable of being transported after deposition in the vagina by the natural transport mechanism of the internal female reproductive organs across the cervix into the uterus wherein immunization is effected within said internal female organs, said microparticles having a diameter of from 10 to 100 μ

m.

2. The anti-B-HCG containing microparticles of claim 1, wherein the said microparticles have a diameter of from 20 to 70 μ

m.

3. The anti-B-HCG containing microparticles of claim 1, wherein the said microparticles have a diameter of from 20 to 60 μ

m.

4. The anti-B-HCG containing microparticles of claim 1, wherein the said microparticles comprise a central anti-B-HCG containing core surrounded by an outer shell of matrix material free of anti-B-HCG.

5. The anti-B-HCG containing microparticles of claim 4, wherein said outer shell of the microparticles is resistant to the acidic pH environment of the vagina and susceptible to breakdown when exposed to the neutral pH of the cervix.

6. The anti-B-HCG containing microparticles of claim 4, said microparticles having a configuration comprising alternate layers of anti-B-HCG containing layers and anti-B-HCG free matrix material.

7. The anti-B-HCG containing microparticles of claim 1, said microparticles containing from 10 weight % to 60 weight % of anti-B-HCG.

8. The anti-B-HCG containing microparticles of claim 1, said microparticles containing from 10 weight % to 50 weight % of anti-B-HCG.

9. The anti-B-HCG containing microparticles of claim 1, said microparticles containing from 10 weight % to 25 weight % of anti-B-HCG.

10. The anti-B-HCG containing microparticles of claim 4, said microparticles containing from 10 weight % to 60 weight % of anti-B-HCG.

11. The anti-B-HCG containing microparticles of claim 4, said microparticles containing from 10 weight % to 50 weight % of anti-B-HCG.

12. The anti-B-HCG containing microparticles of claim 4, said microparticles containing from 10 weight % to 25 weight % of anti-B-HCG.

13. Anti-B-HCG containing microparticles for the immunization of the internal female reproductive organs, which comprise microparticles having a size of from 10 to 100 μ

m and containing a biologically effective amount of anti-B-HCG incorporated in a matrix material which is biocompatible and biologically degradable, said microparticles being capable of being transported after deposition in the vagina by the natural transport mechanism of the internal female reproductive organs across the cervix into the uterus wherein immunization is effected within said internal female reproductive organs.

14. The microparticles of claim 13, wherein said microparticles further contain a menstrual cycle regulatory hormone which stimulates said natural transport mechanism.

15. The microcapsules of claim 14, wherein said hormone is estradiol or progesterone.

16. The microparticles of claim 13, wherein said microparticles are of a size ranging from 20 to 70 μ

m.

17. The microparticles of claim 13, wherein said matrix material is polylactic acid, polyglycolic acid, or copolymers of glycolic and lactic acids.

18. The microparticles of claim 13, wherein said microparticles are of a monolithic structure in which said antibody is dispersed throughout the matrix material.

19. The microparticles of claim 13, wherein said microparticles contain from 10 wt.% to 60 wt.% of said antibody.