Encapsulating darunavir nanocrystals within Eudragit L100 using coaxial electrospraying

Published in European Journal of Pharmaceutics and Biopharmaceutics, vol. 113, pp. 50–59 (2017) · Elsevier
DOI: 10.1016/j.ejpb.2016.12.002

Summary

Darunavir is a poorly water-soluble antiretroviral drug whose delivery benefits from being formulated as fine particles and protected from the acidic stomach. This study uses coaxial electrospraying — a single-step technique based on concentric (co-axial) nozzles — to build core–shell nanoparticles in which a core of darunavir nanocrystals is encapsulated within a shell of the enteric polymer Eudragit L100. Feeding separate core and shell solutions through the coaxial nozzle, the authors produced particles that were characterised for morphology, physical state, encapsulation efficiency and in-vitro dissolution. The Eudragit L100 shell acted as a gastro-resistant (enteric) coating, sharply limiting drug release in acidic medium so that release occurs later, at intestinal pH. The work demonstrates coaxial electrospraying as a versatile one-step route to enteric-coated nanoparticulate drug formulations.

Authors & Affiliations

  • Duong Nhat Nguyen
    Drug Delivery and Disposition, Dept. of Pharmaceutical and Pharmacological Sciences, KU Leuven, Belgium
  • Christian Clasen
    Dept. of Chemical Engineering, KU Leuven, Belgium
  • Guy Van den Mooter Corresponding
    Drug Delivery and Disposition, Dept. of Pharmaceutical and Pharmacological Sciences, KU Leuven, Belgium

Topics

Coaxial Electrospraying Drug Encapsulation Enteric Coating Core-Shell Nanoparticles

Materials

Darunavir Eudragit L100 Hydroxypropyl Methylcellulose (HPMC)

Linari Electrospinning Systems

Coaxial electrospinning needles by Linari Nanotech
Coaxial electrospraying and electrospinning rely on concentric core–shell nozzles. Linari Nanotech supplies coaxial needles for producing core–shell fibres and particles.
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