Transcutol® V, A Must-Have, Safe and Versatile Excipient for Optimised Veterinary Medicines

Gattefossé is a leading supplier of functional excipients for veterinary industries worldwide, enabling to formulate any dosage form for any animal species. Our acknowledged technical and regulatory support makes Gattefossé a unique partner for developing safe and efficient veterinary medicines, from conventional dosage forms to innovative drug delivery systems. A recent in-depth review highlights Gattefossé’s excipients functionalities in veterinary dosage forms, show cases their history of use across species and provides insights to tackle modern veterinary challenges.

Transcutol® V is Gattefossé’s tradename for diethylene glycol monoethyl ether (DEGEE), also named ethoxydiglycol. Chemically it belongs to the class of solvents and functionally it is a powerful drug solubiliser and skin permeation enhancer, widely used in human and veterinary medicines worldwide in oral, skin and injectable drug delivery.2

Transcutol® V, Efficacy Without Compromise on Safety

When selecting a solvent for veterinary medicine formulation, technical, quality and safety considerations should be taken into account.

The solubilising capacity is the primary criterion as drug solubilisation is the first step for absorption and bioavailability. Transcutol® V has been used for decades in human and veterinary formulations for its exceptional solubilising capacity, as highlighted in Figure 1, providing drug solubility data compared to propylene glycol.

Main advantages of Transcutol® V compared to other solvents, are:

• Suitable for both lipophilic and hydrophilic APIs.
• Lower volumes of solvents are required for drug solubilisation, contributing to lower volume of injections and hence pain.

The quality of the excipient is also critical to minimise the risk of adverse reactions. Transcutol® is the highest purity diethylene glycol monoethyl ether available on the markets.3 Gattefossé is renowned worldwide for its high-quality pharmaceutical-grade excipients, aligned with the high level of safety needed in human and veterinary medicines.

The safety of the excipient for the target species and for the caregiver is also determinant when developing a formulation. DEGEE has been used in drug products approved by health authorities worldwide. The European Commission adopted a Regulation in 2015 establishing that no MRL (Maximum Residue Limits) is required for diethylene glycol monoethyl ether in all food producing species.4

Moreover, Gattefossé has carried out an extensive review and analysis of the safety of Transcutol® V in veterinary medicinal products and issued a certificate of toxicological assessment. Given the physicochemical and toxicological data available for Transcutol®, its bioavailability as well as the purity degree of Transcutol® V, a daily dose of Transcutol® V up to the Permitted Daily Exposure multiplied by the body weight of the target animal species should not present any reasonably foreseeable risk in case of its incorporation into a veterinary product without undergoing any chemical modification, whatever the route of administration of the product considered.5

The safety profile of Transcutol® V constitutes a tremendous advantage compared to other solvents used in veterinary medicines and enables to formulate medicines with minimum risk for the target animal and the caregiver. For instance, propylene glycol can provoke adverse reactions to cats and horses and should be used cautiously in these species. Another example is the use of N-methyl pyrrolidone which is classified as teratogen in Europe.7 Using this excipient is controverted both for the breed and the female caregivers. Formulating veterinary medicines with Transcutol® V offers greater safety and wider possibilities. The safety of use of Transcutol® V in veterinary applications is clearly established and well documented in Gattefossé regulatory documentation, as well as by its history of use in numerous veterinary medicines worldwide (Table 1).

Use of Transcutol® V in Oral Dosage Forms

Drug solubility is often the limiting factor for oral absorption and Transcutol® V can be used as solvent in the formulation to overcome this issue. To ensure that the drug remains in solubilised state in the formulation and upon digestion, lipid based formulation (LBF) is a frequently used strategy. Lipid based formulations consist in mixtures of oils, surfactants and solvents in different proportions. Depending on the nature of the components, they bring the following advantages: drug solubilisation throughout the gastro-intestinal tract, intestinal permeation enhancement, lymphatic absorption and mitigation of the food effect.9

LBF has been used in human and veterinary medicines wordwide for decades. The first historical commercial application is a ciclosporin formulation, which has been successfully transferred to veterinary use. An oral solution of ciclosporin for cats and dogs is commercially available and consists in the mixture of solvents (ethanol and diethylene glycol monoethyl ether, e.g. Transcutol® V), oleoyl macrogolglycerides (e.g. Labrafil® M 1944 CS) as self emulsifying excipient, i.e. oil and surfactant. For companion animals this medicine is easily dispensed with a dosing syringe calibrated upon animal weight.

For poultry, it is more convenient to disperse the solution via the drinking water. In that case the solution needs to be stable in the concentrate form and when diluted in the drinking water. In our Technical Centre of Excellence, we showed that a combination of Transcutol® V and Tween® 80 enables the production of stable concentrates and dilutions of ivermectin, ponazuril, fluralaner or essential oils used in drinking water medication.11 For instance, a 0.56% ponazuril solution was stable in concentrate at 40°C and upon dilution in water at a ratio 1:1000. A lice treatment for chicken with fluralaner is commercially available and consists of similar formulation based on diethylene glycol monoethyl ether, e.g. Transcutol® V and polysorbate 80, eg Tween® 80.12

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Source: IAHS – International Animal Health Journal, Gattefossé, Transcutol® V, A Must-Have, Safe and Versatile Excipient for Optimised Veterinary Medicines, https://international-animalhealth.com/transcutol-v-a-must-have-safe-and-versatile-excipient-for-optimised-veterinary-medicines/

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