# US 9,872,859 B2 · Materials and methods for targeting therapeutic compositions to gut-associated lymphoid tissue (GALT) > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,872,859 B2 - Document ID: US9872859B2 - Status: Granted - Kind: B2 - Application number: 15/437,878 - Filed: 2017-02-21 - Published: 2017-08-24 - Granted: 2018-01-23 - Earliest claimed: 2016-02-20 - Assignees: The Florida International University Board of Trustees - Applicants: Upal Roy; Hong Ding; Madhavan Nair - Inventors: Upal Roy; Hong Ding; Madhavan Nair - Web page: https://patentgrep.com/patent/US9872859B2 ## CPC - A61K 31/536: ortho- or peri-condensed with carbocyclic ring systems - A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol - A61K 47/68: the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment - A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant} - A61K 47/6907: {the form being a microemulsion, nanoemulsion or micelle} - C07K 16/30: from tumour cells - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) ## Abstract The present invention provides novel, long-acting nanoformulated drugs and targeted drug delivery methods, and uses thereof. In one embodiment, the nanoformulated drug is a retroviral drug. In one embodiment, the nanoformulated composition comprises a nanocarrier with one or more incorporated drugs. In an exemplary embodiment, the drug is efavirenz (EFV). In a further embodiment, the nanocarrier is associated with an agent for targeting microfold cells (M-cells). In a specific embodiment, the targeting agent binds to an M-cell marker known as glycoprotein 2 (GP2). Via this mechanism, the nanodrug is targeted toward GALT. ## Claims ### Claim 1 A pharmaceutical composition comprising a nanodrug that comprises an active agent, a poloxamer, and an antibody to glycoprotein-2 (GP2) or antibody fragment to GP2 that targets microfold cells (M-cells) and facilitates the uptake of the nanodrug by M-cells. ### Claim 2 (depends on 1) The pharmaceutical composition, according to claim 1, in which the poloxamer is F127COOH. ### Claim 3 (depends on 2) The pharmaceutical composition, according to claim 2, having F127COOH conjugated to GP2. ### Claim 4 (depends on 1) The pharmaceutical composition, according to claim 1, comprising a retroviral agent as the active agent. ### Claim 5 (depends on 4) The pharmaceutical composition, according to claim 4, wherein the retroviral agent is efavirenz. ### Claim 6 (depends on 1) The pharmaceutical composition, according to claim 1, comprising a latency activating drug. ### Claim 7 (depends on 1) The pharmaceutical composition, according to claim 1, wherein the nanodrug is encapsulated in an enteric coating that resists degradation at pHs below 5.0 and releases the nanodrug at a pH above 5.0. ### Claim 8 A method of delivering an active agent to gut-associated lymphoid tissue (GALT) comprising administering, to a subject, a pharmaceutical composition comprising a nanodrug that comprises an active agent, a poloxamer, and an antibody to GP2 or antibody fragment to GP2 that targets M-cells and facilitates the uptake of the nanodrug by M-cells. ### Claim 9 (depends on 8) The method, according to claim 8, used to deliver a retroviral drug directly to GALT and beyond. ### Claim 10 (depends on 8) The method, according to claim 8, wherein a sustained release of the active agent occurs. ### Claim 11 (depends on 8) The method, according to claim 8, used to treat HIV in the subject. ### Claim 12 (depends on 8) The method, according to claim 8, in which the poloxamer is F127COOH. ### Claim 13 (depends on 8) The method, according to claim 8, wherein the subject is a human or mouse and the composition is administered intravenously, intraperitoneally, or subcutaneously. ### Claim 14 (depends on 9) The method, according to claim 9, wherein the retroviral drug is efavirenz. ### Claim 15 (depends on 8) The method, according to claim 8, wherein the pharmaceutical composition comprises a latency activating drug. ### Claim 16 (depends on 8) The method, according to claim 8, wherein the nanodrug is encapsulated in an enteric coating that resists degradation at pHs below 5.0 and releases the nanodrug at a pH above 5.0. ### Claim 17 A pharmaceutical composition comprising a nanodrug comprising efavirenz and F127COOH conjugated to anti-GP2 antibody that facilitates the uptake of the nanodrug by M-cells, and wherein the nanodrug is coated with an enteric coating that degrades only at a pH above 5.0. ### Claim 18 A method of delivering an active agent to gut-associated lymphoid tissue (GALT) comprising administering, to a subject, a pharmaceutical composition comprising a nanodrug comprising a F127COOH micelle conjugated to anti-GP2 antibody that facilitates the uptake of the F127COOH micelle by M-cells, and further comprising efavirenz encapsulated in the F127COOH micelle, characterized in that the nanodrug is coated with an enteric coating that degrades only at a pH above 5.0. ### Claim 19 (depends on 18) The method, according to claim 18, in which the F127COOH micelle has a size of 120-140 nm.