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Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems

Hot melt coating (HMC) of an active pharmaceutical ingredient (API) powder with lipid-based excipients is an innovative method for manufacturing patient-convenient dosage forms. However, drug release instability is still its main industrial challenge. The correlation between the unstable pharmaceuti...

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Autores principales: Schertel, Sonja, Salar-Behzadi, Sharareh, Zimmer, Andreas
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001618/
https://www.ncbi.nlm.nih.gov/pubmed/33802098
http://dx.doi.org/10.3390/pharmaceutics13030366
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author Schertel, Sonja
Salar-Behzadi, Sharareh
Zimmer, Andreas
author_facet Schertel, Sonja
Salar-Behzadi, Sharareh
Zimmer, Andreas
author_sort Schertel, Sonja
collection PubMed
description Hot melt coating (HMC) of an active pharmaceutical ingredient (API) powder with lipid-based excipients is an innovative method for manufacturing patient-convenient dosage forms. However, drug release instability is still its main industrial challenge. The correlation between the unstable pharmaceutical product performance with the solid-state alteration of lipids is currently well-investigated. The remaining problem is the inconsistent release alteration of different APIs coated with the same lipid after storage, such as faster release in some cases and slower release in others. The interaction between API surface and lipid-based coating and its alteration during storage were investigated in this work. The surface properties of five different APIs and the coating composition of tripalmitin and polysorbate 65 were screened via Washburn and pendant drop methods, respectively. Metformin hydrochloride and hydrochlorothiazide particles were each coated with the coating composition. The water sorption alteration of coated particles and the crystal growth of tripalmitin in the coating after storage were measured via tensiometry and X-ray diffraction. The cleavage work necessary to overcome the adhesion of coating composition on the core surface was calculated for each API. The accelerated release of the polar core (metformin) after storage was correlated with a low cleavage work and a distinctive phase separation. In contrast, a decelerated release of the hydrophobic core (hydrochlorothiazide) was favored by the crystal growth of the lipid-based coating. The gained knowledge can be used to design the product stability during the formulation development.
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spelling pubmed-80016182021-03-28 Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems Schertel, Sonja Salar-Behzadi, Sharareh Zimmer, Andreas Pharmaceutics Article Hot melt coating (HMC) of an active pharmaceutical ingredient (API) powder with lipid-based excipients is an innovative method for manufacturing patient-convenient dosage forms. However, drug release instability is still its main industrial challenge. The correlation between the unstable pharmaceutical product performance with the solid-state alteration of lipids is currently well-investigated. The remaining problem is the inconsistent release alteration of different APIs coated with the same lipid after storage, such as faster release in some cases and slower release in others. The interaction between API surface and lipid-based coating and its alteration during storage were investigated in this work. The surface properties of five different APIs and the coating composition of tripalmitin and polysorbate 65 were screened via Washburn and pendant drop methods, respectively. Metformin hydrochloride and hydrochlorothiazide particles were each coated with the coating composition. The water sorption alteration of coated particles and the crystal growth of tripalmitin in the coating after storage were measured via tensiometry and X-ray diffraction. The cleavage work necessary to overcome the adhesion of coating composition on the core surface was calculated for each API. The accelerated release of the polar core (metformin) after storage was correlated with a low cleavage work and a distinctive phase separation. In contrast, a decelerated release of the hydrophobic core (hydrochlorothiazide) was favored by the crystal growth of the lipid-based coating. The gained knowledge can be used to design the product stability during the formulation development. MDPI 2021-03-10 /pmc/articles/PMC8001618/ /pubmed/33802098 http://dx.doi.org/10.3390/pharmaceutics13030366 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Article
Schertel, Sonja
Salar-Behzadi, Sharareh
Zimmer, Andreas
Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems
title Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems
title_full Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems
title_fullStr Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems
title_full_unstemmed Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems
title_short Impact of Surface Properties of Core Material on the Stability of Hot Melt-Coated Multiparticulate Systems
title_sort impact of surface properties of core material on the stability of hot melt-coated multiparticulate systems
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001618/
https://www.ncbi.nlm.nih.gov/pubmed/33802098
http://dx.doi.org/10.3390/pharmaceutics13030366
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