Molecular 3D Characterisation of Drug Distribution and Mg‐Stearate Coating on Lactose Carrier Particles by ToF‐SIMS and XPS.
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| Title: | Molecular 3D Characterisation of Drug Distribution and Mg‐Stearate Coating on Lactose Carrier Particles by ToF‐SIMS and XPS. |
|---|---|
| Authors: | Sjövall, Peter1 (AUTHOR) peter.sjovall@ri.se, Ernstsson, Marie2 (AUTHOR), Mahlin, Denny3 (AUTHOR), Thalberg, Kyrre4,5 (AUTHOR) |
| Source: | Surface & Interface Analysis: SIA. May2025, Vol. 57 Issue 5, p334-342. 9p. |
| Subjects: | Particulate matter, Depth profiling, Drug efficacy, Lactose, Budesonide |
| Abstract: | A common type of inhalation medicine uses a dry powder formulation where the active pharmaceutical ingredient (API) is attached on the surface of carrier particles, often in combination with additional components. The spatial distribution of the API on the carrier particle is critical for the release into the lungs and thus for the efficacy of the drug. In this work, we use ToF‐SIMS imaging in combination with argon gas cluster sputtering to determine the 3D distributions of budesonide (the API) and magnesium stearate (Mg‐stearate) on the surface of lactose carrier particles in a so‐called adhesive mixture formulation. The results show that the carrier particles are largely covered by Mg‐stearate, with only small spots showing exposed lactose or budesonide. Upon sputtering, Mg‐stearate is rapidly removed to expose flat regions of lactose as well as discrete budesonide particles distributed over the lactose surface. Depth profiles also indicate some smearing of budesonide on the lactose surface. These results provide clear evidence that budesonide, as well as lactose, is largely covered with Mg‐stearate on the drug particle surface. Subsequent SEM analyses of the sample areas provide detailed microstructural information, including identification of budesonide and lactose fine particles attached on the lactose surface. Furthermore, the thickness of the Mg‐stearate overlayer was estimated by XPS to be approximately 5 nm. The detailed information obtained about the 3D distribution of Mg‐stearate serves to clarify the mechanisms behind its performance‐enhancing effect in adhesive mixtures and also to improve formulation optimization with regard to Mg‐stearate load and application process. [ABSTRACT FROM AUTHOR] |
| Copyright of Surface & Interface Analysis: SIA is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) | |
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| Header | DbId: egs DbLabel: Engineering Source An: 184200058 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Molecular 3D Characterisation of Drug Distribution and Mg‐Stearate Coating on Lactose Carrier Particles by ToF‐SIMS and XPS. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Sjövall%2C+Peter%22">Sjövall, Peter</searchLink><relatesTo>1</relatesTo> (AUTHOR)<i> peter.sjovall@ri.se</i><br /><searchLink fieldCode="AR" term="%22Ernstsson%2C+Marie%22">Ernstsson, Marie</searchLink><relatesTo>2</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Mahlin%2C+Denny%22">Mahlin, Denny</searchLink><relatesTo>3</relatesTo> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Thalberg%2C+Kyrre%22">Thalberg, Kyrre</searchLink><relatesTo>4,5</relatesTo> (AUTHOR) – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22Surface+%26+Interface+Analysis%3A+SIA%22">Surface & Interface Analysis: SIA</searchLink>. May2025, Vol. 57 Issue 5, p334-342. 9p. – Name: Subject Label: Subjects Group: Su Data: <searchLink fieldCode="DE" term="%22Particulate+matter%22">Particulate matter</searchLink><br /><searchLink fieldCode="DE" term="%22Depth+profiling%22">Depth profiling</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+efficacy%22">Drug efficacy</searchLink><br /><searchLink fieldCode="DE" term="%22Lactose%22">Lactose</searchLink><br /><searchLink fieldCode="DE" term="%22Budesonide%22">Budesonide</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: A common type of inhalation medicine uses a dry powder formulation where the active pharmaceutical ingredient (API) is attached on the surface of carrier particles, often in combination with additional components. The spatial distribution of the API on the carrier particle is critical for the release into the lungs and thus for the efficacy of the drug. In this work, we use ToF‐SIMS imaging in combination with argon gas cluster sputtering to determine the 3D distributions of budesonide (the API) and magnesium stearate (Mg‐stearate) on the surface of lactose carrier particles in a so‐called adhesive mixture formulation. The results show that the carrier particles are largely covered by Mg‐stearate, with only small spots showing exposed lactose or budesonide. Upon sputtering, Mg‐stearate is rapidly removed to expose flat regions of lactose as well as discrete budesonide particles distributed over the lactose surface. Depth profiles also indicate some smearing of budesonide on the lactose surface. These results provide clear evidence that budesonide, as well as lactose, is largely covered with Mg‐stearate on the drug particle surface. Subsequent SEM analyses of the sample areas provide detailed microstructural information, including identification of budesonide and lactose fine particles attached on the lactose surface. Furthermore, the thickness of the Mg‐stearate overlayer was estimated by XPS to be approximately 5 nm. The detailed information obtained about the 3D distribution of Mg‐stearate serves to clarify the mechanisms behind its performance‐enhancing effect in adhesive mixtures and also to improve formulation optimization with regard to Mg‐stearate load and application process. [ABSTRACT FROM AUTHOR] – Name: AbstractSuppliedCopyright Label: Group: Ab Data: <i>Copyright of Surface & Interface Analysis: SIA is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1002/sia.7385 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 9 StartPage: 334 Subjects: – SubjectFull: Particulate matter Type: general – SubjectFull: Depth profiling Type: general – SubjectFull: Drug efficacy Type: general – SubjectFull: Lactose Type: general – SubjectFull: Budesonide Type: general Titles: – TitleFull: Molecular 3D Characterisation of Drug Distribution and Mg‐Stearate Coating on Lactose Carrier Particles by ToF‐SIMS and XPS. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Sjövall, Peter – PersonEntity: Name: NameFull: Ernstsson, Marie – PersonEntity: Name: NameFull: Mahlin, Denny – PersonEntity: Name: NameFull: Thalberg, Kyrre IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 05 Text: May2025 Type: published Y: 2025 Identifiers: – Type: issn-print Value: 01422421 Numbering: – Type: volume Value: 57 – Type: issue Value: 5 Titles: – TitleFull: Surface & Interface Analysis: SIA Type: main |
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