Core-Shell Structured PLGA Particles Having Highly Controllable Ketoprofen Drug Release

Pharmaceutics. 2023 Apr 28;15(5):1355. doi: 10.3390/pharmaceutics15051355.

Abstract

The non-steroid anti-inflammatory drug ketoprofen (KP) as a model molecule is encapsulated in different poly(lactide-co-glycolide) (PLGA) nanostructured particles, using Tween20 (TWEEN) and Pluronic F127 (PLUR) as stabilizers to demonstrate the design of a biocompatible colloidal carrier particles with highly controllable drug release feature. Based on TEM images the formation of well-defined core-shell structure is highly favorable using nanoprecipitation method. Stabile polymer-based colloids with ~200-210 nm hydrodynamic diameter can be formed by successful optimization of the KP concentration with the right choice of stabilizer. Encapsulation efficiency (EE%) of 14-18% can be achieved. We clearly confirmed that the molecular weight of the stabilizer thus its structure greatly controls the drug release from the PLGA carrier particles. It can be determined that ~20% and ~70% retention is available with the use of PLUR and TWEEN, respectively. This measurable difference can be explained by the fact that the non-ionic PLUR polymer provides a steric stabilization of the carrier particles in the form of a loose shell, while the adsorption of the non-ionic biocompatible TWEEN surfactant results in a more compact and well-ordered shell around the PLGA particles. In addition, the release property can be further tuned by decreasing the hydrophilicity of PLGA by changing the monomer ratio in the range of ~20-60% (PLUR) and 70-90% (TWEEN).

Keywords: PLGA; controlled release; core-shell nanocarrier; ketoprofen.

Grants and funding

TKP2021-EGA-32 has been implemented with the support provided by the Ministry of Innovation and Technology of Hungary from the National Research, Development and Innovation Fund. This research was supported by the NRDIH through FK131446, PD146152 project. Norbert Varga is grateful for financial support from the János Bolyai Research Scholarship of the Hungarian Academy of Sciences. E. Csapó thanks the financial support of the “Momentum” Program of the Hungarian Academy of Sciences (Project no. LP2021-5).