ISOCHEM highlights innovative drug delivery model for Tocophersolan TPGS
Press Release | ISOCHEM S.A.S.
JUNE 03, 2015
Vert-Le-Petit, France: – A senior scientist for specialist fine chemicals and API manufacturer ISOCHEM has called attention to the natural vitamin E derivative Tocophersolan (TPGS) as an innovative excipient in drug delivery.
Dr. Yves Robin, ISOCHEM Vice President for R&D, reports that TPGS has surfactant properties that mean it can dramatically increase the concentration of an active substance in an aqueous matrix.
Dr. Robin’s findings are contained in the article “A natural vitamin E derivative is an innovative excipient,” published in the journal Pharmaceutical Technology, Volume 39, Issue 1; Pages: 48-52.
Tocophersolan or d-α-tocopheryl polyethylene glycol succinate (TPGS) was developed 60 years ago as a water-soluble form of vitamin E. Its surfactant properties triggered the interest of drug formulation developers, steadily moving it into the toolbox of pharmaceutical drug-delivery innovators. In particular, Tocophersolan was involved in the commercialization of the HIV protease inhibitor, amprenavir (Agenerase).
Since 1999, TPGS has been approved for several specialty products, including an active ingredient in Vedrop as a source of supplemental vitamin E.
Second wave excipient
Dr. Robin finds it ‘likely’ that could play a key role in enhancing the efficacy of a second wave of launched drugs in coming years. He also identifies a potential new role for Tocophersolan in enhancing the efficacy and bioavailability of nutraceuticals, as it has already done for pharmaceuticals.
“TPGS is now clearly established as a solid option for drug delivery innovation as a result of its non-ionic surfactant characteristics; its solubilizing, emulsifying, and stabilizing properties; and even its permeation- and absorption-enhancement effects,” says Dr. Robin.
New life for old molecule
“This is an ‘old molecule’ with a long history. However, the strong demand of innovation in pharmaceutical drug delivery is offering it a greater life. The patent and scientific publication activity regarding TPGS in addition to its track records in marketed products allows the scientific community to think about a promising future for this multifaceted molecule,” he says.
“TPGS can also be used in other fields of application, such as nutrition, food, or even cosmetics. Indeed, these markets need innovative solutions as well and they could possibly benefit from TPGS’s unique properties,” he concludes.
“Not least of the advantages of TPGS are its ubiquity and versatility,” Dr. Robin points out.
“At ISOCHEM, we can offer Tocophersolan ‘off the shelf’ in finished bulk or research forms in a wide variety of formats. This makes it highly applicable in R&D in a range of delivery models, including oral, intravenous and topical,” Dr. Robin points out.
Talking about the starting point for his research, he says:
“ISOCHEM is unique; not just for its experience and knowhow but also because of the way it is always prepared to do a ‘back to basics’ review of the properties of its compounds to re-examine their potential.”
“We can also offer many different PEG chain length analogues to enhance the standard TPGS,“ said Dr. Robin.
Yves ROBIN, VP R&D – Industrialization, ISOCHEM S.A.S
Tel: +33 1 64 99 05 49
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