Design, Development, and Characterization of Lyophilized Posaconazole-Loaded Mixed Micelles for Improved Fungal Treatment and Stability

Authors : Adesh Kurane, Rutuja Chougale, Vibhuti Thakur, Kiran Patil, Shalaka Patki, John D'souza, Ashok Hajare

Pages : 143-162

Doi:10.55262/fabadeczacilik.1331702

View : 39 | Download : 59

Publication Date : 2024-03-26

Article Type : Research Paper

Abstract :Posaconazole, a BCS class II drug with poor solubility, hampers its absorption in the body, leading to suboptimal drug levels and reduced treatment effectiveness. To address this issue, this research aimed to develop a lyophilized powder of posaconazole-loaded mixed micelles (POS-MMs) using pluronic F68 and soluplus to enhance fungal treatment and stability. A 32 factorial design optimized the POS-MMs formulation by varying PF68 and soluplus concentrations. Various characterization techniques were employed, including particle size analysis, zeta potential measurement, FTIR, DSC, and XRPD. In vitro drug release studies indicated sustained release with 79.4% released within 24 hrs, while in vitro hemolysis studies confirmed biocompatibility. Lyophilization with lactose as a cryoprotectant was successful, yielding a stable formulation over three months. The optimized POS-MMs exhibited a particle size of 66.30 ± 2.10 nm, a high % entrapment efficiency of 94.88 ± 2.4%, and a desirable zeta potential of -25.3±2.8 mV. These findings highlight the potential of POS-MMs to enhance the therapeutic outcomes of posaconazole in the treatment of fungal infections. In addition, lyophilized powder is a promising technique for improving the stability of POS-MMs.
Keywords : posaconazole, mixed micelles, lyophilization, stability, fungal infections