Solubilizer choice justification of the antiviral ointment composition

Abstract

Introduction. Modern pharmacy aims to create highly effective dosage forms with an improved safety profile. The rise in mixed viral-bacterial infections, particularly herpesvirus lesions, necessitates the development of combination drugs with synergistic effects. Optimization of the solubility of hydrophobic APIs is a critical stage in the pharmaceutical development of soft dosage forms. Increasing the degree of dispersion and solubility of active substances in an ointment base ensures the formation of a thermodynamically stable system, thereby guaranteeing dosage uniformity, improving release kinetics, and increasing the drug's bioavailability. The use of solubilizers, optimization of viscoelastic properties, and control of temperature parameters in the technological process provide a significant increase in the efficiency of the transport of active substances into the skin and in their pharmacological activity. The aim: experimental justification of the choice of solubilizer and its concentration to ensure optimal dispersion of acyclovir in the composition of a combined ointment with antiviral and antimicrobial action. Materials and methods. The work used APIs of acyclovir and miramistin. Cetyl stearyl alcohol and glycerol monostearate, at concentrations of 1.0% to 5.0%, were studied as solubilizers. The study of the dispersion of acyclovir particles was conducted using optical microscopy with a Granum R-40 microscope and morphometric analysis software. Results and discussion. It was established that the introduction of solubilizers significantly affects the size of acyclovir particles in the ointment base. The best results were demonstrated by cetyl stearyl alcohol at a concentration of 3.0%. It was shown that increasing the preparation temperature from 65 °C to 75 °C does not significantly affect particle dissolution, allowing the 65 °C mode to be chosen as energy-efficient and safe for component stability. Conclusions. To ensure a high degree of dispersion of acyclovir in the composition of the ointment, the use of the solubilizer SCS at a concentration of 3.0% at a manufacturing temperature of 65 °C is justified.