One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying.
OBJECTIVE
The aim of this work was to investigate the feasibility of producing darunavir (DRV) solid dispersion nanoparticles coated with an enteric polymer in one single step using electrospraying.


METHODS
The core-shell nanoparticles were made using coaxial electrospraying. A solution of DRV with hydroxypropyl methylcellulose in a mixture of organic solvents formed the core, while the shell was produced from an enteric polymer (Eudragit L100) dissolved in an organic solvent. The final particles were evaluated in terms of morphology, physical state, encapsulation efficiency and in-vitro dissolution.


RESULTS
Nanoparticles of encapsulated DRV solid dispersions within Eudragit L100 were successfully prepared with high encapsulation efficiency (90%). The enteric coating layer reduced the percentage of DRV release in acidic medium in the in-vitro dissolution test to less than 20%.


CONCLUSIONS
This study showed the potential of coaxial electrospraying for encapsulating solid dispersions within core-shell structured nanoparticles.
Department of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven - University of Leuven, Leuven, Belgium.
Duong Nhat
DN
Nguyen
Department of Chemical Engineering, KU Leuven - University of Leuven, Leuven, Belgium.
Ljiljana
L
Palangetic
Department of Chemical Engineering, KU Leuven - University of Leuven, Leuven, Belgium.
Christian
C
Clasen
Department of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven - University of Leuven, Leuven, Belgium.
Guy
G
Van den Mooter
D000336:Aerosols; D018360:Crystallography, X-Ray; D000069454:Darunavir / Q000737:chemistry*; D004337:Drug Carriers; D004339:Drug Compounding; D005240:Feasibility Studies; D017320:HIV Protease Inhibitors / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives / Q000737:chemistry*; D007700:Kinetics; D053758:Nanoparticles; D036103:Nanotechnology; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry*; D033362:Powder Diffraction; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013057:Spectrum Analysis; D013499:Surface Properties; D013678:Technology, Pharmaceutical / Q000379:methods*
D000336:Aerosols; D004337:Drug Carriers; D017320:HIV Protease Inhibitors; D011109:Polymethacrylic Acids; D012997:Solvents; C038300:methylmethacrylate-methacrylic acid copolymer; D065347:Hypromellose Derivatives; D000069454:Darunavir
darunavir; electrospraying; enteric coating; solid dispersion