RESEARCH OF SOFT DOSAGE FORMS CONTAINING RETINOIDS
DOI:
https://doi.org/10.32782/health-2024.1.20Keywords:
retinoids, adapalene, tretinoin, solubility, soft dosage forms, gel, substances, nanoemulsionsAbstract
Acne is a common skin disease, which is accompanied by a significant skin and psychological burden. Topical therapy is the first choice for the treatment of mild to moderate acne, and in severe cases it can provide additional support to other traditional forms of acne vulgaris treatment. The use of topical retinoids, such as adapalene and tretinoin, can present significant challenges due to their proven instability, low bioavailability and penetration, and potential for skin irritation. The purpose of our work was to study the method of introducing active substances into soft medicinal products (gels) containing adapalene and tretinoine (by the type of emulsion, suspension, solution) and to study the solubility of these active substances. The objects of the study were soft medicines (gels) containing adapalene and tretinoin, both mono- and combined. Determination of optical indicators of soft dosage forms was carried out according to the methodology of the State Pharmacopoeia of Ukraine; in dissolution studies, adapalene and tretinoin substances purchased from the Sigma-Aldrich RTC company (Germany) were used. Based on the results of photomicrography of samples with adapalene and tretinoin, it was concluded that in the soft dosage form the substances are insoluble and are administered as a suspension. At the same time, the presence of insoluble crystals in the composition of the soft dosage form is the main cause of side effects of medicinal and cosmetic products with retinoids. We determined the solubility of adapalene and tretinoin in non-aqueous solvents. According to the obtained data, tretinoin has better solubility in the proposed non-aqueous solvents. Its solubility in polysorbates and tea tree essential oil makes it possible to use these solvents in the preparation of emulsion systems. Adapalene dissolved in dimexide and a mixture of dimexide with tea tree essential oil when heated above 50 oC. Based on the results of the analysis of commercial soft drugs with adapalene and tretinoin, it was determined that these substances were included in the composition as a suspension. The technology for obtaining the presented gels does not involve the use of methods of improving the bioavailability of active substances due to nanoencapsulation. The micronization method (application of microsphere technology) proposed by the manufacturers («Adapalene 3 gel» and «Tretinoin 1 gel») does not significantly reduce the size of the particles of the substance.
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