Mohamad Anas Al Tahan, Ali Al-Khattawi, Craig Russell
{"title":"硬脂酸包覆介孔二氧化硅微颗粒作为新型针状结构药物递送载体。","authors":"Mohamad Anas Al Tahan, Ali Al-Khattawi, Craig Russell","doi":"10.1016/j.ejpb.2024.114619","DOIUrl":null,"url":null,"abstract":"<p><p>Mesoporous silica are widely utilised as drug carriers due to their large pore volume and surface area, which facilitate effective loading. Additionally, they can be used to enhance drugs stability and protect against enzymatic degradation due to their silica framework. However, without the addition of a capping material, the loaded cargo may be prematurely released before reaching the target site. This work reports the functionalisation of a commercially available silica microparticle (SYLOID XDP 3050) with stearic acid at various stearic acid loading concentrations (20-120 % w/w). Scanning electron microscopy (SEM) analysis revealed that the pores were capped with stearic acid, with the filling ratio increasing proportionally to the loading concentration. Notably, needle-like structures appeared when the stearic acid amount exceeded 80 % w/w, surpassing the calculated theoretical maximum pore filling ratio (64.32 %). The molecular interactions were highlighted using Fourier-transform infrared spectroscopy (FTIR), as the intensity of the CH<sub>3</sub> increased with increased stearic acid loading concentrations. The needle-structures phenomenon was corroborated by 3D confocal imaging. It utilised the autofluorescence properties of stearic acid to demonstrate its presence within the carrier, with fluorescence intensity increasing alongside the stearic acid concentration. Differential scanning calorimetry (DSC) indicated the crystalline nature of these needle structures, which was further confirmed by X-ray diffraction (XRD) analysis, validating the crystallisation of the stearic acid needles. Moreover, nitrogen porosimetry was employed to assess the pore volume and surface area, where the formulation containing 120 % stearic acid exhibited the lowest pore volume (0.59 cc). This value was smaller than unloaded SYLOID (2.1 cc), indicating near-complete filling of the carrier. This newly developed SYLOID-stearic acid carrier will now be used to enhance formulation development as a platform to enhance protein oral drug delivery.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114619"},"PeriodicalIF":4.4000,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Stearic acid-capped mesoporous silica microparticles as novel needle-like-structured drug delivery carriers.\",\"authors\":\"Mohamad Anas Al Tahan, Ali Al-Khattawi, Craig Russell\",\"doi\":\"10.1016/j.ejpb.2024.114619\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Mesoporous silica are widely utilised as drug carriers due to their large pore volume and surface area, which facilitate effective loading. Additionally, they can be used to enhance drugs stability and protect against enzymatic degradation due to their silica framework. However, without the addition of a capping material, the loaded cargo may be prematurely released before reaching the target site. This work reports the functionalisation of a commercially available silica microparticle (SYLOID XDP 3050) with stearic acid at various stearic acid loading concentrations (20-120 % w/w). Scanning electron microscopy (SEM) analysis revealed that the pores were capped with stearic acid, with the filling ratio increasing proportionally to the loading concentration. Notably, needle-like structures appeared when the stearic acid amount exceeded 80 % w/w, surpassing the calculated theoretical maximum pore filling ratio (64.32 %). The molecular interactions were highlighted using Fourier-transform infrared spectroscopy (FTIR), as the intensity of the CH<sub>3</sub> increased with increased stearic acid loading concentrations. The needle-structures phenomenon was corroborated by 3D confocal imaging. It utilised the autofluorescence properties of stearic acid to demonstrate its presence within the carrier, with fluorescence intensity increasing alongside the stearic acid concentration. Differential scanning calorimetry (DSC) indicated the crystalline nature of these needle structures, which was further confirmed by X-ray diffraction (XRD) analysis, validating the crystallisation of the stearic acid needles. Moreover, nitrogen porosimetry was employed to assess the pore volume and surface area, where the formulation containing 120 % stearic acid exhibited the lowest pore volume (0.59 cc). This value was smaller than unloaded SYLOID (2.1 cc), indicating near-complete filling of the carrier. This newly developed SYLOID-stearic acid carrier will now be used to enhance formulation development as a platform to enhance protein oral drug delivery.</p>\",\"PeriodicalId\":12024,\"journal\":{\"name\":\"European Journal of Pharmaceutics and Biopharmaceutics\",\"volume\":\" \",\"pages\":\"114619\"},\"PeriodicalIF\":4.4000,\"publicationDate\":\"2025-02-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Pharmaceutics and Biopharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1016/j.ejpb.2024.114619\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/12/21 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Pharmaceutics and Biopharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.ejpb.2024.114619","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/12/21 0:00:00","PubModel":"Epub","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Stearic acid-capped mesoporous silica microparticles as novel needle-like-structured drug delivery carriers.
Mesoporous silica are widely utilised as drug carriers due to their large pore volume and surface area, which facilitate effective loading. Additionally, they can be used to enhance drugs stability and protect against enzymatic degradation due to their silica framework. However, without the addition of a capping material, the loaded cargo may be prematurely released before reaching the target site. This work reports the functionalisation of a commercially available silica microparticle (SYLOID XDP 3050) with stearic acid at various stearic acid loading concentrations (20-120 % w/w). Scanning electron microscopy (SEM) analysis revealed that the pores were capped with stearic acid, with the filling ratio increasing proportionally to the loading concentration. Notably, needle-like structures appeared when the stearic acid amount exceeded 80 % w/w, surpassing the calculated theoretical maximum pore filling ratio (64.32 %). The molecular interactions were highlighted using Fourier-transform infrared spectroscopy (FTIR), as the intensity of the CH3 increased with increased stearic acid loading concentrations. The needle-structures phenomenon was corroborated by 3D confocal imaging. It utilised the autofluorescence properties of stearic acid to demonstrate its presence within the carrier, with fluorescence intensity increasing alongside the stearic acid concentration. Differential scanning calorimetry (DSC) indicated the crystalline nature of these needle structures, which was further confirmed by X-ray diffraction (XRD) analysis, validating the crystallisation of the stearic acid needles. Moreover, nitrogen porosimetry was employed to assess the pore volume and surface area, where the formulation containing 120 % stearic acid exhibited the lowest pore volume (0.59 cc). This value was smaller than unloaded SYLOID (2.1 cc), indicating near-complete filling of the carrier. This newly developed SYLOID-stearic acid carrier will now be used to enhance formulation development as a platform to enhance protein oral drug delivery.
期刊介绍:
The European Journal of Pharmaceutics and Biopharmaceutics provides a medium for the publication of novel, innovative and hypothesis-driven research from the areas of Pharmaceutics and Biopharmaceutics.
Topics covered include for example:
Design and development of drug delivery systems for pharmaceuticals and biopharmaceuticals (small molecules, proteins, nucleic acids)
Aspects of manufacturing process design
Biomedical aspects of drug product design
Strategies and formulations for controlled drug transport across biological barriers
Physicochemical aspects of drug product development
Novel excipients for drug product design
Drug delivery and controlled release systems for systemic and local applications
Nanomaterials for therapeutic and diagnostic purposes
Advanced therapy medicinal products
Medical devices supporting a distinct pharmacological effect.