Two-phase, water-absorbent bioadhesive composition for delivery of an active agent to a patient
An adhesive composition is provided that contains both a hydrophobic phase and a hydrophilic phase, wherein the hydrophobic phase is composed of a crosslinked hydrophobic polymer composition and the hydrophilic phase is a water-absorbent blend of a hydrophilic polymer and a complementary oligomer capable of crosslinking the hydrophilic polymer through hydrogen bonding, ionic bonding, and/or covalent bonding. The composition is useful as a bioadhesive, for affixing drug delivery systems, wound dressings, bandages, cushions, or the like to a body surface such as skin or mucosal tissue.
1 . A composition for delivery of an active agent to a human patient, comprising an effective amount of an active agent loaded into a bioadhesive composition comprising a hydrophobic phase and a hydrophilic phase, wherein the hydrophobic phase comprises a crosslinked hydrophobic polymer composition and the hydrophilic phase comprises a mixture of a hydrophilic polymer and a complementary oligomer capable of crosslinking the hydrophilic polymer through hydrogen bonding, ionic bonding, or covalent bonding.
2 . The composition of claim 1 , wherein the active agent is a locally acting, topically administrable agent.
3 . The composition of claim 2 , wherein the active agent is selected from bacteriostatic agents, bacteriocidal agents, antibiotic agents, pain-relieving agents, antifungal agents, keratolytic agents, vesicants, and anti-acne agents.
4 . A topical pharmaceutical formulation comprising the composition of claim 2 and a pharmaceutically acceptable topical carrier.
5 . The composition of claim 1 , wherein the active agent is a systemically active agent.
6 . The composition of claim 5 , wherein the active agent is selected from: analeptic agents; analgesic agents; anesthetic agents; antiarthritic agents; respiratory drugs; anticancer agents; anticholinergics; anticonvulsants; antidepressants; antidiabetic agents; antidiarrheals; antihelminthics; antihistamines; antihyperlipidemic agents; antihypertensive agents; anti-infective agents; antinflammatory agents; antimigraine preparations; antinauseants; antiparkinsonism drugs; antipruritics; antipsychotics; antipyretics; antitubercular agents; antiulcer agents; antiviral agents; anxiolytics; appetite suppressants; attention deficit disorder (ADD) and attention deficit hyperactivity disorder (ADHD) drugs; calcium channel blockers; antianginal agents; central nervous system (CNS) agents; beta-blockers; antiarrhythmic agents; cough and cold preparations; diuretics; genetic materials; herbal remedies; hormonolytics; hypnotics; hypoglycemic agents; immunosuppressive agents; leukotriene inhibitors; mitotic inhibitors; muscle relaxants; narcotic antagonists; nicotine; nutritional agents; ophthalmic drugs; parasympatholytics; peptide drugs; psychostimulants; sedatives; steroids; smoking cessation agents; tranquilizers; and vasodilators.
7 . An improved delivery system composed of an active agent reservoir, a backing layer laminated thereto, and an integral means for affixing the system to the body surface, wherein the improvement comprises formulating the active agent reservoir from the composition of claim 1 .
8 . The composition of claim 1 , wherein the crosslinked hydrophobic polymer composition is a crosslinked butyl rubber.
9 . The composition of claim 2 , wherein the crosslinked hydrophobic polymer composition is butyl rubber crosslinked with polyisobutylene.
10 . The composition of claim 1 , wherein the hydrophilic polymer and the complementary oligomer are covalently crosslinked.
11 . The composition of claim 1 , wherein the hydrophilic polymer is selected from the group consisting of poly(N-vinyl lactams), poly(N-vinyl amides), poly(N-alkylacrylamides), polyacrylic acid, polymethacrylic acid, polyvinyl alcohol, polyvinylamine, and copolymers and blends thereof.
12 . The composition of claim 1 1 , wherein the hydrophilic polymer is selected from the group consisting of poly(N-vinyl lactams), poly(N-vinyl amides), poly(N-alkylacrylamides), and copolymers and blends thereof.
13 . The composition of claim 12 , wherein the hydrophilic polymer is a poly(N-vinyl lactam).
14 . The composition of claim 13 , wherein the hydrophilic polymer is a poly(N-vinyl lactam) homopolymer.
15 . The composition of claim 14 , wherein the poly(N-vinyl lactam) is selected from the group consisting of polyvinyl pyrrolidone, polyvinyl caprolactam, and blends thereof.
16 . The composition of claim 15 , wherein the poly(N-vinyl lactam) is polyvinyl pyrrolidone.
17 . The composition of claim 15 , wherein the poly(N-vinyl lactam) is polyvinyl caprolactam.
18 . The composition of claim 1 , wherein the hydrophilic polymer has a number average molecular weight in the range of approximately 20,000 to 2,000,000.
19 . The composition of claim 18 , wherein the hydrophilic polymer has a number average molecular weight in the range of approximately 200,000 to 1,000,000.
20 . The composition of claim 1 , wherein the complementary oligomer has a molecular weight in the range of about 45 to 800.
21 . The composition of claim 20 , wherein the complementary oligomer has a molecular weight in the range of about 45 to 600.
22 . The composition of claim 21 , wherein the complementary oligomer has a molecular weight in the range of about 300 to 600.
23 . The composition of claim 1 , wherein the complementary oligomer is selected from the group consisting of polyalcohols, monomeric and oligomeric alkylene glycols, polyalkylene glycols, carboxyl-terminated polyalkylene glycols, amino-terminated polyalkylene glycols, ether alcohols, alkane diols and carbonic diacids.
24 . The composition of claim 23 , wherein the complementary oligomer is selected from the group consisting of polyalkylene glycols and carboxyl-terminated polyalkylene glycols.
25 . The composition of claim 24 , wherein the complementary oligomer is selected from the group consisting of polyethylene glycol and carboxyl-terminated polyethylene glycol.
26 . The composition of claim 25 , wherein the complementary oligomer is polyethylene glycol.
27 . The composition of claim 26 , wherein the complementary oligomer is polyethylene glycol 400.
28 . An implantable dosage form comprising the composition of claim 1 .
29 . An oral dosage form comprising the composition of claim 1 .
30 . A transmucosal dosage form comprising the composition of claim 1 .
31 . A method for delivering an active agent comprising applying the composition of claim 1 to an individual's body surface.