Formulation and Optimization of Alogliptin-Loaded Polymeric Nanoparticles: In Vitro to In Vivo Assessment

Abstract

The nano-drug delivery system has gained greater acceptability for poorly soluble drugs. Alogliptin (ALG) is a FDA-approved oral anti-hyperglycemic drug that inhibits dipeptidyl peptidase-4. The present study is designed to prepare polymeric ALG nanoparticles (NPs) for the management of diabetes. ALG-NPs were prepared using the nanoprecipitation method and further optimized by Box–Behnken experimental design (BBD). The formulation was optimized by varying the independent variables Eudragit RSPO (A), Tween 20 (B), and sonication time (C), and the effects on the hydrodynamic diameter (Y1) and entrapment efficiency (Y2) were evaluated. The optimized ALG-NPs were further evaluated for in vitro release, intestinal permeation, and pharmacokinetic and anti-diabetic activity. The prepared ALG-NPs show a hydrodynamic diameter of between 272.34 nm and 482.87 nm, and an entrapment efficiency of between 64.43 and 95.21%. The in vitro release data of ALG-NPs reveals a prolonged release pattern (84.52 ± 4.1%) in 24 h. The permeation study results show a 2.35-fold higher permeation flux than pure ALG. ALG-NPs exhibit a significantly (p < 0.05) higher pharmacokinetic profile than pure ALG. They also significantly (p < 0.05) reduce the blood sugar levels as compared to pure ALG. The findings of the study support the application of ALG-entrapped Eudragit RSPO nanoparticles as an alternative carrier for the improvement of therapeutic activity.

Polymer based dual drug delivery system for targeted treatment of fluoroquinolone resistant Staphylococcus aureus mediated infections

“…Similar results have been demonstrated by Eudragit RSPO polymeric nanoparticles loaded with an oral anti-hyperglycemic agent Alogliptin, wherein the prepared nanoparticles exhibited an average particle size of 272 nm, the highest entrapment of 95% and prolonged release profile reaching 84% at the end of 24 h 49 . In another study, dual controlled release nanoparticles of Betaxolol hydrochloride was developed using montmorillonite mineral and Eudragit PO polymer, wherein an initial burst release of surface-bound drug was observed, followed by a slow release due to slow erosion, and maximum drug release of 80% by the complete breakdown of particles after 10 h 50 .…”

Polymer-based dual drug delivery system for targeted treatment of fluoroquinolone-resistant Staphylococcus aureus mediated infections

“…Similar results have been demonstrated by Eudragit RSPO polymeric nanoparticles loaded with an oral anti-hyperglycemic agent Alogliptin, wherein the prepared nanoparticles exhibited an average particle size of 272 nm, the highest entrapment of 95% and prolonged release pro le reaching 84% at the end of 24 h. 50 . In another study, dual controlled release nanoparticles of Betaxolol hydrochloride was developed using montmorillonite mineral and Eudragit PO polymer, wherein an initial burst release of surface-bound drug was observed, followed by a slow release due to slow erosion, and maximum drug release of 80% by the complete breakdown of particles after 10 h 51 .…”

A Study on the Formulation and Evaluation of Herbal Hair Oils

“…The evaluation parameters and the values determined were found to be under limit, which indicates fit for using. 21 Table 2: Evaluation parameters and values…”