One‐step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying

Summary

Darunavir (DRV) is a poorly water-soluble anti-HIV drug, so improving its dissolution while protecting it from the acidic stomach is valuable for oral delivery. This study tests whether both goals can be met in a single manufacturing step using coaxial electrospraying to make core–shell nanoparticles. The core was a solution of darunavir with hydroxypropyl methylcellulose (HPMC) — forming a solid dispersion that keeps the drug in a fast-dissolving amorphous state — while the shell was an enteric polymer (Eudragit L100) that resists dissolution at low pH and releases in the intestine. The resulting particles were characterised for morphology, physical (amorphous) state, encapsulation efficiency and in-vitro dissolution, demonstrating that coaxial electrospraying can produce enteric-coated amorphous solid-dispersion nanoparticles of darunavir in one step.

Authors & Affiliations

• Duong Nhat Nguyen

  Drug Delivery and Disposition, Dept. of Pharmaceutical & Pharmacological Sciences, KU Leuven, Belgium
• Ljiljana Palangetic

  Dept. of Chemical Engineering, KU Leuven, Belgium
• Christian Clasen

  Dept. of Chemical Engineering, KU Leuven, Belgium
• Guy Van den Mooter Corresponding

  Drug Delivery and Disposition, Dept. of Pharmaceutical & Pharmacological Sciences, KU Leuven, Belgium

Topics

Materials

Linari Electrospinning Systems