Prefilled Syringes or Peptide Pills? - Pharmaceutical Technology

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Prefilled Syringes or Peptide Pills?
The impact of new delivery technologies in designing peptide therapies.

Pharmaceutical Technology
Volume 37, Issue 5, pp. 46-49


Nanoparticulate technologies are receiving interest for their ability to enable oral peptide delivery to the brain. The pharmaceutical industry, driven by the medical and clinical success of intravenously administered biologics, is increasingly accepting more complex brain and peptide drug-delivery systems to enter niche treatment markets and address the growing need for brain therapeutics. The translation of a technology for oral peptide delivery to the brain can provide an answer to a therapeutic field with unmet needs.

For oral to brain peptide delivery, the focus has been on delivering endogenous opioid peptides and their analogs for the treatment of neuropathic and chronic pain. The first reported strategy able to deliver peptides orally involved a leucine-enkephalin synthetic analogue (dalargin) encapsulated in polybutylcyanoacrylate nanoparticles overcoated with polysorbate 80 (32), and in some cases, overcoated with polysorbate 80 and polyethylene glycol (20 kDa) (33). However, the technology has not yet progressed into Phase I studies.

On the other hand, Nanomerics has announced that its nanotechnology-enabled peptide pill (METDoloron) involving the molecular-envelope technology (MET) will be moving into Phase I clinical trials within the next two years (34). The technology is based on an engineered amphiphilic chitosan polymer (i.e., quaternary ammonium palmitoyl glycol chitosan) tailored to form nanoscale polymeric aggregates that are able to package or specifically interact (covalently and noncovalently) with peptides (13).

Preclinical studies showed successful delivery of leucine-enkephalin across the BBB with significantly higher pharmaco-kinetic amounts (i.e., a 67% increase in plasma levels [AUC0–24] and a 57% increase in brain maximum concentration [Cmax]). Moreover, significant enhancement of pharmacodynamic activity in a pain animal model was observed (13). Combining the molecular-envelope technology with a prodrug lipidization strategy of leucine-enkephalin potentiated the oral antinociceptive effect, leading to analgesia lasting more than eight hours after oral administration, accompanied with significant enhancements in brain bioavailability (13).

The commercialization of peptides as oral therapies is still deemed risky by the biopharmaceutical industry. However, the reward of niche treatment market areas will fuel the development of a peptide pill enabled by nanotechnology either alone, or combined with chemical modification (lipidization, cyclization) or other formulation strategies (controlled-release polymer coating, permeation enhancers, protease inhibitors).


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