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Targeted formulations of GLP -1 for Type 1 diabetes

Award Information

Department of Health and Human Services
Award ID:
Program Year/Program:
2004 / SBIR
Agency Tracking Number:
Solicitation Year:
Solicitation Topic Code:
Solicitation Number:
Small Business Information
19805 N. Creek Pkwy, Suite 200 Bothell, WA -
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Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
Phase 1
Fiscal Year: 2004
Title: Targeted formulations of GLP -1 for Type 1 diabetes
Agency: HHS
Contract: 1R43DK069727-01
Award Amount: $1,000,599.00


DESCRIPTION (provided by applicant): New therapies are desperately needed for patients with Type 1 diabetes. Recent reports that the insulin-stimulating hormone Glucagon-Like Peptide (GLP-1), can increase pancreatic beta cell mass, offers the exciting prospect that beta cells can be regenerated in Type 1 diabetes, avoiding the need for islet transplantation. A number of modified analogues of GLP-1 are in development that are resistant to the peptidase DPP-IV that rapidly inactivates GLP-1 in the bloodstream. Our company proposes to apply a novel drug delivery nanotechnology Protected Graft Copolymers (PGC) coupled with Pharmaln's Reversible Binding (PRB) to reversibly associate native GLP-1 with the carrier. Since GLP-I in the carrier would be encased in a polymer; we anticipate protection of the peptide from cleavage by DPP-IV and thus an extended half-life. Importantly, since this carrier has been demonstrated to accumulate in sites of inflammation, the envisioned formulation would result in increased delivery to the pancreas, thus potentially minimizing gastrointestinal side effects. -to demonstrate the feasibility of the approach we propose to 1) formulate PGC/PRB:GLP-1 and measure the complex formation efficiency, binding constant and stability in serum; 2) determine the in vitro potency of PGC/PRB:GLP-1 receptor binding and sensitivity to degradation by DPP-IV ; 3) demonstrate the effect of PGC/PRB:GLP-1 on beta cell insulin secretion and glucose responsiveness as well as ability to induce neogenesis of new beta cells from ductal cells in vitro; 4) determine the PK, accumulation of the complex in the pancreas and its stability and 5) demonstrate efficacy in vivo in regeneration of beta cell mass in a rat model of streptozotocin-induced diabetes. The Phase II studies will involve the validation and optimization of the treatment to extended animal groups, including models of Type 1 diabetes in combination with immunosuppressants. The envisioned product, GLP-1 in an optimal pancreas-directed delivery system, should be of commercial interest not only for the treatment of Type 1 diabetes, but also for other applications being investigated for this peptide, including obesity, Alzheimer's and Type 2 diabetes.

Principal Investigator:

Elijah M. Bolotin

Business Contact:

Small Business Information at Submission:


EIN/Tax ID: 364357862
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No