Mentor  Pharmaceutical Consulting


Oral Delivery of Proteins

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.

Binding of targeting agent to GIT epithelium

Uptake of targeted nanoparticles

Targeted nanoparticles 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 oral delivery

  • The preparation of targeted nanoparticles containing the pharmaceuticals.

  • Appropriate in vitro and in vivo models.