Indaflex™ Cream is a semi-solid formulation for topical administration, containing the active ingredient Indomethacin, at a concentration of 2.5%. Indaflex™ Cream is an innovative oil-in-water emulsion formulation. There are three main features of this product which contribute to its improved efficacy as a topical analgesic: drug loading/concentration, a nanoparticulate oil-in-water emulsion formulation and an improved partitioning of lipophilic drug from nanoparticles into the lipid matrix of the absorbing tissue. Indaflex™ Cream is composed of a highly dispersed colloidal suspension of nano-sized oil droplets, loaded with active drug and suspended in an aqueous phase.
The Indaflex™ Cream formulation, containing solubilized Indomethacin with an enhanced proprietary delivery system, is designed to improve on the normally poor penetration of Indomethacin through the human epidermis while bypassing systemic delivery and associated systemic side effects. Indaflex™ Cream formulation, has demonstrated a quantifiable improvement in the anti-inflammatory activity of Indomethacin in preclinical models, due to it’s increased solubility in an oil phase, combined with an enhanced skin penetration, due to drug-delivery vehicle components.
The combination of nanoparticle size, oil-in-water emulsion for a hydrophobic drug, enhanced thermodynamic activity, increased surface area of nanoparticles, and increased partition of hydrophobic drugs from the oil phase into lipid matrices of the skin/tissues (stratum corneum in human skin, cell membranes, subcutaneous adipose tissue) facilitate penetration of Indomethacin into the deep tissues surrounding joints where the drug is needed. The Company believes that the physical/chemical principles outlined above may contribute to the superior efficacy of Indaflex™ Cream and thus, its clinical potential as an efficacious topical product in the treatment of the signs and symptoms of Osteo-arthritis (OA).
At this time, Indaflex™ Cream is being developed for:
Indication: Treatment of the signs and symptoms of OA.
Dosage: 2 grams of Indaflex™ Cream (50 mg indomethacin) applied to knee 3 times/day.
After topical application, the maximal indomethacin blood concentration would normally be <5-10% of a comparable oral or parenteral dose of the same drug. The systemic side effects from topically applied transdermal Indaflex™ Cream would be expected to be minimal.