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

Objectives 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...

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Veröffentlicht in:Journal of pharmacy and pharmacology 2016-05, Vol.68 (5), p.625-633
Hauptverfasser: Nguyen, Duong Nhat, Palangetic, Ljiljana, Clasen, Christian, Van den Mooter, Guy
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container_end_page 633
container_issue 5
container_start_page 625
container_title Journal of pharmacy and pharmacology
container_volume 68
creator Nguyen, Duong Nhat
Palangetic, Ljiljana
Clasen, Christian
Van den Mooter, Guy
description Objectives 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. Key findings 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.
doi_str_mv 10.1111/jphp.12459
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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. Key findings 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%. 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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. Key findings 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%. 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source MEDLINE; Oxford University Press Journals Current; Wiley Online Library Journals Frontfile Complete
subjects Aerosols
Crystallography, X-Ray
darunavir
Darunavir - chemistry
Drug Carriers
Drug Compounding
electrospraying
enteric coating
Feasibility Studies
HIV Protease Inhibitors - chemistry
Hydrogen-Ion Concentration
Hypromellose Derivatives - chemistry
Kinetics
Nanoparticles
Nanotechnology
Particle Size
Polymers
Polymethacrylic Acids - chemistry
Powder Diffraction
solid dispersion
Solubility
Solvents - chemistry
Spectrum Analysis
Surface Properties
Technology, Pharmaceutical - methods
title One-step production of darunavir solid dispersion nanoparticles coated with enteric polymers using electrospraying
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