Formulation and Evaluation of Eudragit RL-100 Nanoparticles Loaded In-Situ Forming Gel for Intranasal Delivery of Rivastigmine

Abstract

Purpose: Rivastigmine hydrogen tartrate (RHT) is commonly used for the treatment of mild to moderate Alzheimer’s disease (AD). The aim of this work was to formulate in-situ pluronic F-127 (PF-127) hydrogels containing Eudragit RL-100 (EU-RL) nanoparticles (NPs) in order to improve the therapeutic efficacy of RHT through the nasal route. Methods: The NPs were prepared using different polymer to drug ratios and evaluated for their physicochemical characteristics, cellular uptake and in vitro cytotoxicity against lung adenocarcinoma cells (A459). PF-127 nanoformulations were prepared via cold method and analyzed in terms of physicochemical properties and drug release profiles. The nanoformulations and plain drug gel were then assessed by ex vivo permeation studies across the sheep nasal mucosa. Results: The EU-RL NPs exhibited a particle size within the range of 118 to 154 nm and positive zeta potential values of 22.5 to 30 mV with an approximately spherical shape. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD) suggested no drug to polymer interaction through the preparation of nanoformulations. The RHT-loaded NPs exhibited an acceptable cytocompatibility with a time- and dose-dependent cellular internalization. Conclusion: Our results clearly indicated the potential of nanoformulations as controlled release systems to improve the therapeutic efficacy of RHT through the intranasal administration

Emerging Nanotechnology for Treatment of Alzheimer’s and Parkinson’s Disease

“…Salatin et al use a surfactant (F-127) hydrogel to embed NPs made from Eudragit RL-100 polymer. The hydrogel acts as a thermoreversible delivery system that enables controlled, intranasal delivery of the AD drug, Rivastigmine ( Salatin et al, 2020 ).…”

Formulation and Evaluation of Baclofen Polymeric Nanoparticles for Transdermal Delivery In-vitro and Ex-vivo Optimization

“…This method depends on adding water-miscible solvents like acetone and methanol which diffuse rapidly in the water giving a chance for ERL to precipitate as NPs carrying the drug particles 9,19 . The addition of PVA is important for the stabilization of the NPs and the prevention of their agglomeration by reducing the surface tension between water and solvents 20 . By applying this technique, the NPs of ERL loading Baclofen were successfully formed.…”

Development of Nitazoxanide Loaded Polymeric Nanocarriers: Box Behnken Experimental Design Based Optimisation and Characterisation

“…-79225). The concept behind the selection criteria of polymer is that the Eudragit RL 100 is a positively charge polymer to synthesise nanoparticles which rises the interface between mucin and nanoparticles thus increases the drug bioavailability [8]. Due to biodegradable, aqueous solubility, minimal cell adhesion produces non -toxic effect, stability towards temperature variation and easy entanglement with nanoparticles surface PVA is selected as an another polymer [5,8].…”

“…The drug payload can be transported through the process of diffusion. Eudragit RL 100 polymer is also used as a film former agent for solid dosage form and for the preparations of time-controlled drug delivery formulations [8]. Polymeric nanoparticles utilized Eudragit RL100 as a polymer and polyvinyl alcohol (PVA) as cross linking agent using NTZ as a model drug.…”