Amino‐Decorated Mesoporous Silica Nanoparticles: An Innovative Approach for Controlled Release and Enhanced Oral Bioavailability of Nebivolol

This study was designed to fabricate amino‐decorated mesoporous silica nanoparticles (AMS‐NPs) for sustained release, enhancing permeation, and improving the oral bioavailability of nebivolol (NEB), a model BCS Class II drug. First, mesoporous silica nanoparticles (MS‐NPs) were synthesized by a sol–gel technique, followed by surface functionalization via amino groups using (3‐aminopropyl)triethoxysilane (APTES). Newly synthesized AMS‐NPs were characterized by FT‐IR, scanning electron microscopy (SEM), transmission electron microscopy (TEM), nitrogen adsorption, X‐ray diffraction (XRD), thermal analysis (DSC and TGA), size, and zeta potential measurements. Moreover, drug loading, entrapment, in vitro release, safety, cell permeation, and pharmacokinetic studies were performed. Characterization studies showed successful synthesis of spherical, amino‐decorated MS‐NPs with a size of 380 nm and 62% entrapment efficiency. Thermal analysis studies confirmed the stability of NEB‐loaded AMS‐NPs. Newly synthesized NPs showed no signs of toxicity and exhibited sustained drug release behavior for almost 16 h. The drug permeation enhancement ratio (R) due to AMS‐NPs was 6‐fold higher in comparison to the control across Caco‐2 cell monolayers. The NEB‐loaded AMS‐NPs showed enhanced C max, and AUC compared to free and drug‐loaded MS‐NPs. Moreover, the relative bioavailability of NEB‐loaded AMS‐NPs was 4.5‐ and 1.6‐fold higher than that of free and drug‐loaded MS‐NPs, respectively. Based on all these findings, it can be concluded that newly designed NEB‐loaded amino‐decorated MS‐NPs can be an ideal tool for augmenting the solubility, permeability, and bioavailability of poorly soluble drugs.