Entrapment of bioactives in sol-gel alumina materials

Patent metadata

Field	Value
Publication number	US-9463245-B2
Application number	US-201414267425-A
Country	US
Kind code	B2
Filing date	May 1, 2014
Priority date	May 2, 2013
Publication date	Oct 11, 2016
Grant date	Oct 11, 2016

Abstract

Provided is a platform for entrapment within alumina sol-gel carriers of labile biologically active materials such as proteins, therapeutic enzymes, enzymes of industrial relevance, antigens, and small molecules for achieving successful and efficient protective storage, protection from harsh environmental conditions such as heat, pH and chemicals, delivery to site and subsequent treatment and/or vaccination against diseases against which the active agents are targeted.

First claim

The invention claimed is:

1. A pharmaceutical material comprising of a plurality of alumina sol-gel particles, each particle comprising at least one labile bioactive agent.

2. The pharmaceutical material according to claim 1 , wherein said bioactive agent is contained, entrapped or enclosed by said alumina sol-gel particles.

3. The pharmaceutical material according to claim 1 , wherein the alumina sol gel is in a form selected from the group consisting of an amorphous material and randomly sized and shaped particles.

4. The pharmaceutical material according to claim 1 , being an injectable material.

5. The pharmaceutical material according to claim 1 , wherein the particles average size is from 0.1 to 50 micron.

6. The pharmaceutical material according to claim 1 , wherein the labile bioactive agent is selected from the group consisting of proteins, enzymes, peptides, antibodies, nucleic acids, growth factors, cells, viruses, and carriers.

7. The pharmaceutical material according to claim 6 , wherein the labile bioactive agent is selected from the group consisting of peptides, proteins, hormones, enzymes, antibodies, receptor binding proteins, antibody fragments, antibody conjugates, aptamers, iRNA, siRNA, microRNA, DNA, RNA, antisense nucleic acid, VEGF inhibitors, macrocyclic lactones, dopamine agonists, dopamine antagonists, low-molecular weight compounds, high-molecular-weight compounds, and conjugated bioactive agents.

8. The pharmaceutical material according to claim 6 , wherein the labile bioactive agent is selected from the group consisting of androgen inhibitors, polysaccharides, growth factors, hormones, anti-angiogenesis factors, peptides, polypeptides, proteins, amino acids, hormones, interferons, and cytokines.

9. The pharmaceutical material according to claim 6 , wherein the labile bioactive agent is one or more immunomodulators selected from a cytokine, an interleukin, interferon, colony stimulating factor, and tumor necrosis factor.

10. The pharmaceutical material according to claim 1 , wherein the labile bioactive agent is selected from the group consisting of heat-sensitive, acid-sensitive, and base-sensitive bioactive agents.

11. The pharmaceutical material according to claim 10 , wherein the labile bioactive agent is an enzyme, a peptide, a polypeptide, a protein, or an amino acid.

12. A pharmaceutical composition comprising a pharmaceutical material according to claim 1 .

13. The composition according to claim 12 , configured as a slow-release formulation, a fast-release formulation, or a sustained-release formulation.

14. The composition according to claim 12 , wherein the pharmaceutical material is entrapped without spontaneous short-term or long-term release of a bioactive agent contained in the material, for maintaining or increasing the stability of a bioactive.

15. The composition according to claim 14 , for prolonging shelf-life of a bioactive during storage, delivery or use, by arresting bioactive decomposition, decreasing or diminishing bioactive sensitivity, increasing or maintaining stability of a bioactive, protecting a bioactive from increased sensitivity or lability, or for achieving enhanced functionality of a bioactive.

16. A hybrid material comprising alumina sol-gel and at least one heat-sensitive bioactive material, wherein the at least one heat sensitive bioactive material is entrapped within the alumina sol-gel material and having a deactivation temperature at least 10° C. higher as compared to the same heat sensitive bioactive material when free.

Assignees

• Yissum Res Dev Co

Inventors

• Avnir David
• Rutenberg Abraham
• Vinogradov Vladimir V

Classifications

• A61K9/143

  with inorganic compounds · CPC title

• A61K9/1611

  Inorganic compounds · CPC title

• A61K9/0019

  Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title

• A61K38/00

  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 title

• A61K38/465

  acting on ester bonds (3.1), e.g. lipases, ribonucleases · CPC title