Positive trial results for transdermal Lidocaine system

Dec 8 2008

Phosphagenics Limited has announced the successful completion of a phase 1 clinical trial that examined the ability of its patented drug delivery system, TPM, to topically deliver the pain relief drug, lidocaine, safely into humans.

The trial demonstrated that the patented lidocaine formulation was able to deliver a significantly greater amount of lidocaine into the localised area of the skin compared to a leading commercial product.

Lidocaine is a well known topical anaesthetic, sales of which exceeded US $1.2 billion in 2007. It is used for a wide variety of ailments, including temporary relief of rashes, stings, sprains, strains, bites, and burns. This clinical trial compared the dermal penetration and measured the systemic exposure of lidocaine between one of the leading marketed products, Xylocaine (5% lidocaine), and Phosphagenics' TPM/lidocaine (5% lidocaine).

One hour after application, TPM/lidocaine delivered 500 percent more (p<0.001) lidocaine into the stratum corneum, the outer layer of the skin, than the commercial product, Xylocaine. Phosphagenics' TPM/lidocaine also augmented the depth of penetration, with 450 percent (p<0.01) more lidocaine found in the deepest layers of the skin sampled.

TPM/lidocaine significantly increased the amount, rate, and depth of lidocaine penetration into the skin compared to Xylocaine, parameters that are normally expected to produce a local analgesic effect. Despite the increase in dermal drug delivery, TPM/lidocaine did not increase the plasma lidocaine concentration compared to Xylocaine after 6 hours.

Dr. Esra Ogru, Executive Vice President of Research and Development at Phosphagenics said; "While we have previously demonstrated the penetrative power of our TPM technology, the success of this trial validates the versatility and precision of Phosphagenics' drug delivery platform in humans. We view this as a major achievement for our company and look forward to moving ahead with further clinical trials."

The open label, single centre study was conducted at the Centre for Pharmaceutical Research, University of South Australia, under the guidance of Principal Investigator Dr. David Foster. 11 healthy adult volunteers enrolled in the bioavailability trial of dermal and systemic pharmacokinetics, which incorporated secondary endpoints of safety and tolerability.