Abstract

FORMULATION & DEVELOPMENT OF POSACONAZOLE TOPICAL GEL: THE IMPACT OF POLYMER VARIABILITY ON ANTIFUNGAL EFFICACY: A REVIEW

Harshit Gautam*, Dr Abhishek Nagar

ABSTRACT

Posaconazole, a triazole antifungal agent, has emerged as a critical therapeutic option for the prevention and treatment of invasive fungal infections, particularly in immunocompromised patients. Its broad-spectrum activity encompasses most Candida and Aspergillus species, as well as a range of uncommon but clinically significant molds such as Mucorales. Posaconazole inhibits the enzyme lanosterol 14α-demethylase, a crucial component of the fungal cell membrane biosynthesis pathway, leading to disruption of cell membrane integrity and fungal death. The pharmacokinetic profile of posaconazole is influenced by its formulation. Initially available as an oral suspension, its bioavailability was limited and variable, dependent on food intake and gastric acidity. The introduction of delayed-release tablets and intravenous formulations significantly improved its pharmacokineticconsistency and overall efficacy. Posaconazole demonstrates a favorable safety profile, with the most common adverse effects being gastrointestinal disturbances and mild hepatotoxicity. Drug-drug interactions are notable due to its inhibition of the cytochrome P450 3A4 enzyme system, necessitating careful consideration in polypharmacy scenarios.

Keywords: Posaconazole, triazole antifungal, invasive fungal infections, Candida, Aspergillus, Mucorales, lanosterol 14?-demethylase.