The majority of peptide and protein pharmaceuticals are
currently administered via sub-cutaneous injection, often requiring
considerable patient education, pain and discomfort, and sometimes leading
to undesirable side-effects. In contrast, oral delivery
of peptides and proteins is a much more attractive route of delivery
due to the ease of administration, increased patient comfort and is seen
as more socially acceptable, thus leading to increased patient compliance
and ultimately more effective disease treatment. Until recently, oral
delivery of peptides and proteins has generally been limited to only one
or two proteins because the majority of peptides and proteins, are rapidly
cleaved into non-functional fragments by the intestinal proteases. Those
peptide or proteins that survive digestion are unable to cross the single
cell barrier that comprises the intestinal wall.
Early studies using natural transporters, such as vitamin
B12, have shown that it is possible to orally administer pharmaceutically
relevant quantities of peptides and proteins, either alone, attached to
polymers or entrapped within nanoparticles. Transported molecules included
LHRH analogues, insulin, EPO, G-CSF and others. These studies have been
integral in the identification of many different transport molecules,
which could be used for oral delivery of peptides and proteins and such as insulin,
Monoclonal antibodies and many other recombinant proteins.
of targeting agent to
in the Mesenteric LN
Oral delivery of IgG and IgG-Fc fusion proteins
Mentor has identified a novel mode of oral delivery of IgG1
and IgG1-fusion proteins. Using this method an oral
bioavailability of biologically active anti-TNF molecules such as Humira
of above 20% has been demonstrated. This mode of delivery should be
applicable to the vast majority of antibody and antibody fusion molecules.
Oral delivery of insulin
Mentor has identified several novel methods to increase the
oral bioavailability of insulin. These methods include novel nanocarriers,
novel targeting agents (apart from vitamin B12), and novel
methods of promoting RMT of insulin using the natural insulin RMT process
resident in the gut
Mentor can provide technical advice on
The identification of targeting molecules.
The synthesis of conjugates.
Methods to enhance the oral delivery of IgG and IgG-Fc fusion proteins
Oral delivery of insulin
Oral delivery of nanoparticles
Preparation of protein-loaded nanolattices suitable for
The preparation of targeted nanoparticles containing the
Appropriate in vitro and in vivo models.