Bioprogress Future2

How far ahead or behind might bprg be with DITM films

Oral drug delivery constitutes the maximum share among drug delivery systems, estimated to have a 32% share of the $75.3 billion drug delivery market in 20043, and is considered the most traditional among drug delivery systems. Some new developments taking place in this area include delivering medication through quick-dissolving tablets or strips and designing drugs to deliver macromolecules such as proteins and peptides.
Earlier this year, MonoSol LLC, a water-soluble film company, acquired Kosmos Pharma, a drug delivery company, to form MonosolRx LLC. Using films as a fast-dissolve oral drug delivery platform, Portage-IN based MonoSolRx’s FDTAB® film oral dosage form looks like a postage stamp and dissolves instantly on the tongue to deliver medicines, replacing the use of conventional tablets and capsules. Such a dosage form presents many advantages for pediatric and geriatric patients, who have difficulty swallowing or chewing other oral dosage forms.
Pradeep Sanghvi, PhD, Vice President of Pharmaceutical Development, lists the advantages of solid oral film technology: “The films are flat and thin, dissolve rapidly and provide several unique packaging configurations. Ingestion of the films does not require water. The films are inconspicuous and easy to consume and taste good due to added flavors. This improves patient compliance tremendously. This technology is a new frontier in drug delivery that overlaps the solid-liquid boundary. Film drug delivery systems can improve bioavailability and efficacy of certain drugs.”

Overcoming the challenges of this technology, according to Sanghvi, will require a strong knowledge base of polymer chemistry, wet chemistry, drug-excipient interactions, flavor systems and solution physical chemistry. “The film is restricted by its size and hence puts an imposition on the drug loading in the films,” says Sanghvi, who hails film technology as the future of drug delivery systems. For the quick-dissolve films, size is not specific and depends on marketing and dose. Dissolution of these films is almost instantaneous to few seconds depending on end use.
Another area of increasing importance in oral drug delivery is the delivery of proteins. “The biggest challenge of protein delivery via the oral route is getting past the digestive system,” says Richard Soltero, PhD, president of Cary, NC-based PharmaDirections Inc. “The digestive system is designed to break down the proteins, and so we have to design the drug in such a way that it can go past the stomach without getting digested.”

The protein is protected through various mechanisms such as providing the drug with an enteric or polymeric coating or chemically modifying the protein in such a manner that it is saved from enzymatic action. Present developments include packing the liquid protein drug within an oil coating or micelle.
Soletero points out that presently there are no commercially available oral protein drugs though this technology has been in development for nearly 70-80 years. “Protecting the protein from enzyme digestion and ensuring its absorption through the intestinal epithelium have been challenges that we will soon overcome, but it is hard to predict when. Insulin and hormones, presently delivered via injections, can soon be delivered via the oral route once technologies aid optimum absorption of such large protein molecules. It will also depend on what price the market is willing to pay for an oral protein drug alternative,” says Soltero.