Design, Optimization, and Evaluation of a Macrophage-Targeted Nanoformulation for Enhanced Delivery and Therapeutic Efficacy of Antitubercular Drugs
Keywords:
Macrophage targeting, nanoformulation, antitubercular drug delivery, optimization, sustained release, tuberculosis, pharmacokinetics, Box–Behnken designAbstract
The present study focuses on the design, optimization, and evaluation of a macrophage-targeted nanoformulation to enhance the therapeutic efficacy of antitubercular drugs. Using a Box–Behnken statistical design, key formulation variables were optimized to achieve desirable particle size, high entrapment efficiency, and sustained drug release. The optimized formulation demonstrated strong agreement between predicted and experimental values, confirming model accuracy. In-vitro studies revealed controlled release kinetics following diffusion-based mechanisms, while cytotoxicity and uptake studies confirmed excellent biocompatibility and enhanced macrophage internalization. In-vivo evaluations showed improved pharmacokinetic performance, higher bioavailability, and reduced hepatotoxicity compared to the pure drug. Mechanistic insights supported the strong drug–polymer interactions and effective macrophage targeting. Overall, the nanoformulation shows significant potential for improving tuberculosis treatment outcomes through targeted delivery, sustained release, and enhanced safety.
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