Abstract

DEVELOPMENT AND EVALUATION OF ITRACONAZOLE-LOADED LIPID-POLYMER HYBRID NANOPARTICLES FOR ENHANCED ORAL BIOAVAILABILITY

Sadhna Shrivastava, Dr. Santosh Kumar Mishra*, Archana Tomar

Abstract

Itraconazole is a broad-spectrum triazole antifungal agent widely used for the treatment of superficial and systemic fungal infections. However, its clinical effectiveness is significantly limited by poor aqueous solubility, pH-dependent dissolution, extensive first-pass metabolism, and variable gastrointestinal absorption, resulting in low and inconsistent oral bioavailability. Recent advances in nanotechnology have provided innovative approaches to overcome these biopharmaceutical challenges. Among various nanocarrier systems, lipid–polymer hybrid nanoparticles (LPHNs) have emerged as a promising oral drug delivery platform due to their ability to combine the structural advantages of polymeric nanoparticles with the biocompatibility and absorptionenhancing properties of lipid-based systems. This review comprehensively discusses the physicochemical and pharmacokinetic limitations of itraconazole and highlights the potential of LPHNs in improving its oral delivery. The review covers the composition, structure, preparation methods, formulation strategies, characterization techniques, and mechanisms responsible for enhanced bioavailability of itraconazole-loaded LPHNs. Particular emphasis is placed on particle size optimization, drug loading, entrapment efficiency, morphological characterization, thermal analysis, in vitro drug release, stability studies, and pharmacokinetic evaluation. Furthermore, the review summarizes recent findings on dissolution enhancement, intestinal permeation, antifungal efficacy, and safety assessment of hybrid nanoparticulate systems. Current research trends, scale-up challenges, regulatory considerations, and future opportunities in oral antifungal drug delivery are also discussed. Overall, itraconazole-loaded LPHNs represent a highly promising strategy for improving oral bioavailability, enhancing therapeutic efficacy, reducing dose-related toxicity, and advancing the clinical management of fungal infections.

Keywords: Itraconazole; Lipid–Polymer Hybrid Nanoparticles (LPHNs); Oral Bioavailability; Antifungal Drug Delivery; Nanotechnology; Controlled Release; Lipid-Based Nanocarriers; Polymeric Nanoparticles.