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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...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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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. |
format | Online Article Text |
id | pubmed-8001618 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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