Spray drying Eudragit® E-PO with acetaminophen using 2- and 3-fluid nozzles for taste masking

Conventional spray drying using a 2-fluid nozzle forms matrix microparticles, where drug is distributed throughout the particle and may not effectively mask taste. In contrast, spray drying using a 3-fluid nozzle has been reported to encapsulate material. The objective of this study was to spray dry Eudragit® E-PO (EE) with acetaminophen (APAP), a water-soluble model drug with a bitter taste, using 2- and 3-fluid nozzles for taste masking. Spray drying EE with APAP, however, resulted in yields of ≤ 13 %, irrespective of nozzle configuration. Yields improved when Eudragit® L 100–55 (EL) or Methocel® E6 (HPMC) was used in the inner fluid stream of the 3-fluid nozzle or in place of EE for the 2-fluid nozzle.

Highlights

Eudragit E was spray dried using 2- and 3-fluid nozzles for taste masking.

Slower drug release occurred from microparticles prepared using the 3-fluid nozzle.

Low yields resulted when drug/Eudragit E were spray dried, irrespective of nozzle.

Yields improved with high glass transition temperature polymer in the inner stream

Polymers with similar solubility parameters mixed during 3-fluid spray drying.

Drug release from microparticles prepared with the 2-fluid nozzle was relatively rapid. Using EE in the outer fluid stream of the 3-fluid nozzle resulted in comparatively slower drug release, although drug release was observed, indicating that encapsulation was incomplete. Results from these studies also show that miscible polymers used in the two fluid streams mix during the spray drying process. In addition, findings from this study indicate that the polymer used in the inner fluid stream can impact drug release.

Materials

Acetaminophen (APAP) was purchased from Alfa Aesar (Ward Hill, MA). The methacrylate polymers Eudragit® E-PO (EE) and Eudragit® L 100–55 (EL) were donated by Evonik (Darmstadt, Germany) and Methocel® E6 Premium LV hydroxypropyl methylcellulose (HPMC) was donated by IFF Pharma Solutions (Wilmington, DE). The fluorescent markers Rhodamine B and 5-fluorescein isothiocyanate (FITC) were purchased from Sigma (St. Louis, MO) and Acros Organics (Geel, Belgium), respectively.

Linda A. Felton, Gülşilan Binzet, Cody Wiley, David McChesney, Jason McConville, Metin Ҫelik, Pavan Muttil,
Spray drying Eudragit® E-PO with acetaminophen using 2- and 3-fluid nozzles for taste masking, International Journal of Pharmaceutics, 2024, 124191, ISSN 0378-5173, https://doi.org/10.1016/j.ijpharm.2024.124191.

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