Background Patients with tuberous sclerosis often develop facial angiofibromas that can be successfully treated with topical 1% sirolimus ointments. Nevertheless, this ointment’s greasy nature can produce acne, causing patients to refuse the treatment.
Purpose To devise a non-oily formula for topical sirolimus for patients with tuberous sclerosis and facial angiofibromas who develop acne due this ointment.
Material and methods We reviewed the literature searching for standard procedures for making alternative topical formulations of sirolimus. In addition, the physicochemical properties of sirolimus were considered in order to find the most suitable formulation for this particular case.
Results No standard ways were found of producing oil-free formulations of sirolimus. We decided to compound a 0.2% sirolimus gel with the following procedure. First, prepare a 2% carmellose gel. For this, heat aqua conservans (Nipagin 0.25 g + Nipasol 0.11 g + distilled water 500 mL) to 50°C. In a mortar, mix 2 g of sodium carboxymethylcellulose and 10 g of glycerol. Then, add the content of the mortar to 88 g of heated aqua conservans and stir the mixture until room temperature is reached. Once the carmellose gel has been prepared, weigh 0.2 g of sirolimus and add a few drops of glycerol to it. Slowly, pour the carmellose gel onto the sirolimus, mixing them by stirring, until 100 g has been added. Let it stand for 12 h until the gel is homogeneous. We give it an expiry date of 2 months, stored in an opaque container and at room temperature (below 25°C). Mask and gloves must be used throughout the procedure.
Conclusion We found a way to formulate sirolimus in non-oily excipients in order to diminish the development of acne with its use. Further studies will be needed to determine the efficacy of this formula in the treatment of facial angiofibromas of patients with tuberous sclerosis and the improvement of the acne presented by these patients.
References and/or acknowledgements No conflict of interest.
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