ナノメディシンとナノテクノロジーのジャーナル

概要

Formulation Development & Characterization of Nintedanib loaded Micellar Drug Delivery System for improved therapy of Idiopathic Pulmonary Fibrosis

Rajesh Palva*, Ahmedraza R. Memon, Rajnikant Suthar and Musaratafrin Saiyed

Aim: The study aims to create a formulation of Nintedanib Esylate loaded Polymeric Micelles for treating Idiopathic pulmonary fibrosis (IPF) by administering the drug via the pulmonary route, preventing adverse side effects from oral administration. Experimental work: The study aimed to optimize polymeric micelles preparation using various polymers and drugs. The optimal polymer ratio was selected using a Central composite design, and the impact of polymer concentration on drug entry efficiency was evaluated. The optimized batch was used for drug release and Dry Powder Inhaler (DPI) preparation. Result and Discussion: Solvent emulsification yielded polymeric micelles with high encapsulation efficiency (%EE) increasing with polymer concentration. Particle size (10-100 nm) was confirmed. Central composite design optimized Solutol-HS 15 (400 mg): Soluplus (300 mg) ratio for maximum %EE (85.36%) and desired particle size (78.1 nm). TEM confirmed spherical micelles with core-shell structure. Micelles showed significantly higher drug release than pure drug, indicating improved dissolution. They were stable at lower temperatures (2-8°C) with minimal changes in %EE, size, and zeta potential over four weeks. The DPI formulation achieved high drug content (94.1%) with spherical micelles and showed greater lung binding affinity compared to pure API. Conclusion: The present study reports the development of Nintedanib Esylate-loaded DPI Polymeric Micelles may be a promising alternative to overcome the problem of conventional oral delivery of Nintedanib Esylate.