Pertinax acts as a slow release material for CHX when in contact with water or aqueous solution. The material is supplied as a fine, white powder and can be prepared with specific particle size ranges if required for particular applications such as spray delivery.
The mechanism of CHX environment maintenance is one of slow leaching of soluble CHX ions from the powder, whether applied directly in a topical formulation or embedded within a material. Thus, Pertinax is stable as a dry solid and only releases the active agent when exposed to aqueous solutions. As such, Pertinax must be formulated in materials and products as a solid powder; it cannot be dissolved for formulation purposes as this negates its mechanism of action. Pertinax is not soluble in most solvents (including alcohols, acetone and most organic solvents) and only dissolves slowly in water, hence its sustained efficacy. Pertinax is stable at moderate temperatures and thus it may be possible to incorporate it within certain injection moulding applications.
Pertinax can be used as a component for direct topical application to skin or wounds, as a spray or cream for example. It can be used as a component of a coating for materials including glass, metals and various polymers, and can also be used as a dopant for composite materials, for example wound care materials, dental impression materials and biomedical cements.
Pertinax has been shown to be efficacious against a wide range of microorganisms including methicillin-resistant Staphylococcus aureus (MRSA), Pseudomonas aeruginosa, Escherichia coli, Candida albicans, Streptococcus mutans, Streptococcus gordonii and Porphyromonas gingivalis.
CHX digluconate has been investigated extensively with respect to cytotoxicity. Like many drugs, adverse effects on cells are observed when the concentration is sufficiently high. However, CHX causes fewer adverse events than other antimicrobials or strategies. In hand hygiene for medical professionals, CHX digluconate caused less hand skin problems than non-medicated soap or soap containing different antimicrobial agents.
Comparing a range of dilutions of a 5mM solution of CHX digluconate with a Pertinax suspension containing the equivalent concentration of 5 mM CHX, using cell viability assays with a human cell line, the Pertinax formulation has significantly lower cytotoxicity than the equivalent concentration of aqueous CHX. Furthermore, substrates coated with Pertinax display lower cytotoxicity than commercial CHX digluconate-containing wound dressings. The reason for this lower comparative cytotoxicity is that Pertinax only releases its CHX ‘payload’ gradually and controllably at the site of infection unlike CHX digluconate, most of which is lost to the environment immediately on contact.
CHX digluconate has been licensed for use in a wide variety of human and veterinary clinical and general healthcare applications for over 50 years. Its biocompatibility is well understood and at therapeutic concentrations adverse reactions are rare. With so many extant medical and healthcare applications of CHX there is no shortage of predicates for new products containing Pertinax.
Pertinax materials will be regulated under the EU Medicines Directive as a new active pharmaceutical ingredient (API) or under the EU Biocide Regulations as a biocide depending on its intended use.
Pertinax technology has two intrinsic attributes which will very likely appeal to the regulatory authorities.
The company is in the process of implementing its regulatory plans with the objective of submitting an Active Substance Master File for an API and Biocide in early 2019.
CHX is a broad-spectrum biocide. Its mechanism of action is non-specific, disrupting the microbial cell membrane, meaning that it is effective against Gram-positive bacteria, Gram-negative bacteria and fungi. CHX inactivates microorganisms with a broader spectrum than antibiotics, and operates rapidly, with a faster kill rate than some other antimicrobials such as povidone-iodine. It is either bacteriostatic (inhibits bacterial growth) or bactericidal (kills bacteria) depending on its concentration.