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Pertinax technology

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. 

Pertinax Technology

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.

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Biocompatibility of Pertinax compared with CHX digluconate

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.

 

 

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Regulatory environment

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.

  • Pertinax remains localized at the site of application, it means less total CHX is required to treat a given condition. With CHXdg, most of it will be lost to the environment meaning a higher application concentration and a higher frequency of application is required. With Pertinax, less total CHX and fewer applications can be used to provide continuous antimicrobial function with a reduced environmental impact.
  • Pertinax exhibits less cytotoxicity than equivalent concentrations of CHX.

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.

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Chlorhexidine mechanism of action

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.

  • BacteriaBacteria
  • Fungi and yeastsFungi and yeasts
  • BiofilmBiofilms
CHX carries positive charge, and it binds to negatively-charged sites on the bacterial cell wall, destabilising the wall and increasing its permeability. The process is rapid, taking under a minute. At low concentration, this reduction in cell wall integrity allows the components of the cell to leach out, leading to cell death; at higher concentrations, the entry of the CHX into the cell causes the cytoplasm to solidify.

CHX’s mechanism of action against fungi is very similar to that for bacteria. The CHX impairs the integrity of the fungal cell, entering the cytoplasm resulting in leakage of cell contents and cell death. CHX is highly effective against species including Candida and Aspergillus.

Biofilms are complex, diverse and heterogeneous aggregations of microorganisms growing on a solid substrate and surrounded by a matrix of a sticky, polymer substance produced by the microorganisms. A common example is dental plaque. CHX can prevent the initial formation of biofilms and under some circumstances can disrupt established biofilms

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