Methods and compositions for enhanced transmucosal delivery of peptides and proteins
View Patent ↗Provided are methods and compositions for enhancing the transmucosal absorption of bioactive peptides and proteins. More particularly, the invention provides compositions for enhancing the transmucosal absorption of bioactive peptides and proteins, such as exendin-4, PYY, PYY 3-36 , and GLP-1 and their analogs and derivatives, wherein the compositions comprise an absorption enhancing mixture of a cationic polyamino acid and a buffer that is compatible with the polyamino acid. Also provided are methods for enhancing the transmucosal absorption and bioavailability of bioactive peptides and proteins using such compositions.
1. A pharmaceutical composition for transmucosal administration comprising about 0.5% (w/v) of exendin-4; about 0.5% (w/v) of poly-arginine having an average molecular weight of about 141 kDa; and about 0.56% monosodium glutamate monohydrate (w/v), at a pH of about 4.5 and wherein the exendin-4 has the same net charge as the poly-arginine at the pH of the composition.
2. The composition of claim 1 , wherein said poly-arginine is poly-L-arginine.
3. The composition of claim 1 , wherein said composition further comprises a tonicifying agent, a viscosity-increasing agent, a bioadhesive agent, a preservative, or any combination thereof.
4. The composition of claim 1 , further comprising about 0.72% sodium chloride (w/v).
5. A pharmaceutical composition for transmucosal administration comprising about 0.5% (w/v) of exendin-4; about 1.0% (w/v) of poly-arginine having an average molecular weight of about 141 kDa; and about 0.56% monosodium glutamate monohydrate (w/v), at a pH of about 4.5 and wherein the exendin-4 has the same net charge as the poly-arginine at the pH of the composition.
6. The composition of claim 5 , wherein said poly-arginine is poly-L-arginine.
7. The composition of claim 5 , wherein said composition further comprises a tonicifying agent, a viscosity-increasing agent, a bioadhesive agent, a preservative, or any combination thereof.
8. The composition of claim 5 , further comprising about 0.72% sodium chloride (w/v).