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

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).

2.1. Materials

The poly(lactide-co-glycolide) copolymers with different lactide to glycolide ratio (PLGA50: 50/50, M_w = 30,000–50,000 Da; PLGA65: 65/35, M_w = 40,000–75,000 Da; PLGA75: 75/25, M_w = 66,000–107,000 Da) were purchased from Sigma-Aldrich (Budapest, Hungary). Sodium phosphate dibasic dodecahydrate (Na₂HPO₄ × 12H₂O; ≥99%), sodium phosphate monobasic dihydrate (NaH₂PO₄ × 2H₂O; ≥99%), sodium chloride (NaCl; ≥99%), acetone (C₃H₆O; ≥99%) and dimethyl-sulfoxide (DMSO; C₂H₆OS; ≥99%) were obtained from Molar Chemicals (Budapest, Hungary). The ketoprofen (KP, C₁₆H₁₄O₃, ≥98%), Pluronic F127 (PLUR, (C₃H₆O·C₂H₄O)x, M_w = ~12,600 Da) and Tween20 (TWEEN, C₅₈H₁₁₄O₂₆, M_w = 1228 Da) were obtained from Sigma-Aldrich. Highly purified water was obtained with a Millipore Direct-Q 3 UV purification apparatus (18.2 MΩ·cm at 25 °C). The components and solvents were analytical grade and further purifications were not used.

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Varga, N.; Bélteki, R.; Juhász, Á.; Csapó, E. Core-Shell Structured PLGA Particles Having Highly Controllable Ketoprofen Drug Release. Pharmaceutics 2023, 15, 1355. https://doi.org/10.3390/pharmaceutics15051355

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