Gelated microparticle suitable for oral delivery of therapeutic peptides to the lower intestine
A gelated microparticle suitable for delivery intact to the mammalian lower intestine via an oral route comprises a monodispersed matrix formed of at least partially hydrolyzed casein, chitosan, and an active agent, and includes a minor amount of at least one permeation enhancer dispersed throughout the matrix.
1. A gelated microparticle suitable for delivery intact to the mammalian lower intestine via an oral route and comprising a monodispersed matrix formed of at least partially hydrolysed casein, chitosan, and an active agent, and including a minor amount of at least one permeation enhancer dispersed throughout the matrix.
2. A gelated microparticle according to claim 1 in which the at least one permeation enhancer is selected from taurochloric acid and Vitamin B12.
3. A gelated microparticle according to claim 1 in which the at least one permeation enhancer is taurochloric acid.
4. A gelated microparticle according to claim 1 in which the at least one permeation enhancer is Vitamin B12.
5. A gelated microparticle according to claim 1 in which the active agent has a molecular weight of less than 20 KDa.
6. A gelated microparticle according to claim 1 in which the active agent is a therapeutic peptide.
7. A gelated microparticle according to claim 1 in which the microparticle comprises 50-80% casein (w/w).
8. A gelated microparticle according to claim 1 in which the microparticle comprises 1-5% chitosan (w/w).
9. A gelated microparticle according to claim 1 in which the microparticle comprises 20-40% active agent (w/w).
10. A gelated microparticle according to claim 1 in which the microparticle comprises 0.001-0.1% permeation enhancer (w/w).
11. A gelated microparticle according to claim 1 in which the microparticle comprises 0.005-0.02% taurochloric acid (w/w).
12. A gelated microparticle according to claim 1 in which the microparticle comprises 0.02-0.06% Vitamin B12 (w/w).
13. A gelated microparticle according to claim 1 and comprising:
50-80% casein (w/w);
at least 3% chitosan (w/w); and
20-40% active agent (w/w).
14. A gelated microparticle according to claim 1 and comprising:
68-75% casein (w/w);
5-8% chitosan (w/w); and
24-35% active agent (w/w).
15. A gelated microparticle according to claim 1 and comprising:
68-75% casein (w/w);
5-8% chitosan (w/w);
24-35% active agent (w/w);
0.005-0.02% TCA (w/w); and
0.02-0.06% Vitamin B12 (w/w).
16. A gelated microparticle according to claim 1 in a dried format.
17. A pharmaceutical composition comprising a gelated microparticle according to claim 1 in combination with a suitable pharmaceutical excipient.
18. A pharmaceutical composition comprising a gelated microparticle according to claim 1 in combination with a suitable pharmaceutical excipient and in which the active agent is insulin or an insulin analog, and in which the at least one permeation enhancer is taurochloric acid, Vitamin B12, or a mixture of taurochloric acid and Vitamin B12.