Flamel, Connetics collaborate on novel delivery of recombinant protein

Can relaxin be administered through microspheres?

Flamel Technologies S.A. (Lyons, France) and Connetics Corp. (Palo Alto, CA) have teamed up to determine if Flamel's Medusa drug delivery technology can deliver therapeutic levels of Connetics' recombinant human relaxin protein. Medusa consists of polyaminoacid nanoparticles that trap and release large-molecule drugs. Porcine relaxin has been used since the 1950s to treat scleroderma, a connective tissue disease. Connetics, whose recombinant relaxin is identical to natural human relaxin, believes the protein could also benefit patients with cardiovascular disease and infertility.

Another non-injectible delivery system?
Medusa is entering a crowded marketplace of development-stage delivery systems for large molecules. The principal drawback of therapeutic proteins is they must be administered by injection, which is expensive and fraught with compliance problems. Medusa, along with pulmonary and transdermal alternatives, might allow needle-less—and in some cases controlled release—delivery of products valued in the tens of billions of dollars per year. The market for non-injected insulin alone has been estimated at $2.3 billion.

How it works
Medusa is made from two, alternating amino acids: one lipophilic, the other hydrophilic, making the Medusa scaffold amphiphilic. In water, Medusa particles show a fairly regular (50 nm to 200 nm) particle distribution range, which remains constant over wide pH values. Composed of 95% water and 5% polymer, Medusa is more like a gel than a solid and may be stored in either liquid or dry form.

Medusa traps protein drugs and releases them from a self-assembled amphiphilic polymer network.

When proteins are added to a solution of Medusa particles, the lipophilic regions in "host" (drug) and "guest" (Medusa) align, forming a self-assembled structure. Release is controlled by altering the proportions of amino acid building blocks, or by toying with the protein/Medusa ratio.

In addition to Medusa, Flamel also markets Micropump, an oral delivery platform for controlled release and taste masking, and Agsome, a controlled-release product for agricultural applications. Flamel's Basulin, a controlled-release insulin using Medusa technology, is undergoing Phase I testing with Novo Nordisk.

For more information: Gerard Soula at Flamel Technologies. Tel: +33 4-72-78-34-34. Fax: +33 4-72-78-34-35. Email: soula@flamel.com.

By Angelo DePalma
Managing Editor, Pharmaceutical Online and Drug Discovery Online
Email: adepalma@vertical.net