Pub Date : 2026-01-19DOI: 10.1016/j.ijpharm.2026.126594
Dan Hawthorne , Cheng-Chun Peng , Emma Ward , Susan Sandeman , Ananth SV Pannala , Dharmendra Jani , Inna Maltseva , Andrew W Lloyd
Topical delivery of osmoprotectants to ocular surface has been shown to be a promising solution to ocular discomfort thought to be associated with corneal hyperosmolarity. Currently, most osmoprotectants are administrated by aqueous eyedrops, which are associated with poor bioavailability and short residence time in the tear film, requiring repeated dosing to maintain the osmoprotectant concentration above the effective level. In response to this challenge, this work describes poly(vinyl glycine betaine) (PV-GB), a degradable ester quat polymer which gradually releases the osmoprotectant, glycine betaine (GB), over a period of days to weeks, with release rate strongly dependent on pH of its surroundings. PV-GB was embedded into commercial contact lenses (CLs) alongside a polyanion, hyaluronic acid (HA), to provide extended release of GB during a period reflecting the typical usage of a daily disposable CL wear of 8 – 16 h. A GB release lifetime of ≪48 hrs was achieved from a system comprising PV-GB/HA embedded within an anionic CL using a simple soaking method. Further experiments indicated the polymer was stable to autoclave sterilisation, had a shelf-life of 6 + months (under optimised solution conditions), and was likely to be mucoadhesive, which would be expected to enhance bioavailability of GB at the ocular surface.
{"title":"A contact lens-embedded betaine ester polymer for pH-responsive release of an osmoprotectant to the corneal surface","authors":"Dan Hawthorne , Cheng-Chun Peng , Emma Ward , Susan Sandeman , Ananth SV Pannala , Dharmendra Jani , Inna Maltseva , Andrew W Lloyd","doi":"10.1016/j.ijpharm.2026.126594","DOIUrl":"10.1016/j.ijpharm.2026.126594","url":null,"abstract":"<div><div>Topical delivery of osmoprotectants to ocular surface has been shown to be a promising solution to ocular discomfort thought to be associated with corneal hyperosmolarity. Currently, most osmoprotectants are administrated by aqueous eyedrops, which are associated with poor bioavailability and short residence time in the tear film, requiring repeated dosing to maintain the osmoprotectant concentration above the effective level. In response to this challenge, this work describes poly(vinyl glycine betaine) (PV-GB), a degradable ester quat polymer which gradually releases the osmoprotectant, glycine betaine (GB), over a period of days to weeks, with release rate strongly dependent on pH of its surroundings. PV-GB was embedded into commercial contact lenses (CLs) alongside a polyanion, hyaluronic acid (HA), to provide extended release of GB during a period reflecting the typical usage of a daily disposable CL wear of 8 – 16 h. A GB release lifetime of ≪48 hrs was achieved from a system comprising PV-GB/HA embedded within an anionic CL using a simple soaking method. Further experiments indicated the polymer was stable to autoclave sterilisation, had a shelf-life of 6 + months (under optimised solution conditions), and was likely to be mucoadhesive, which would be expected to enhance bioavailability of GB at the ocular surface.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126594"},"PeriodicalIF":5.2,"publicationDate":"2026-01-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146018532","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-18DOI: 10.1016/j.ijpharm.2026.126595
Yuzhe Wang , Lu Sheng , Lin Bu , Huijuan Li , Jianxin Wu , Qing Huang
Phospholipid vesicle-based permeation assay (PVPA) is widely applied as in vitro skin alternative model by mimicking stratum corneum to evaluate the transdermal application of drugs and chemicals. However, it is composed of lipid components only, which suffer from limitations of achieving accurate permeability prediction. To remedy this shortcoming, inactive immortalized human keratinocytes (HaCaT) were integrated as component to construct epidermal-mimicking model: EpiPVPA. The EpiPVPA could tolerate the pH 3–10 as well as up to 30% ethanol and was stable for 2 weeks at 4 ℃. And the permeation evaluation by Franz diffusion test of 14 drugs demonstrated that EpiPVPA model is comparable to porcine skin with strong correlation. After quantitative structure–property relationship (QSPR) analysis of physicochemical descriptors of 14 drugs, HLB, TPSA, and log P were selected as main factors applied to build multiple linear regression (MLR) equation, and the corresponding linear correlation R2 was elevated to 0.9010. EpiPVPA model is feasible to be applied to permeation evaluation of drugs and cosmetics.
{"title":"A novel epidermal mimicking phospholipid vesicle-based permeation assay: EpiPVPA for in vitro permeation evaluation","authors":"Yuzhe Wang , Lu Sheng , Lin Bu , Huijuan Li , Jianxin Wu , Qing Huang","doi":"10.1016/j.ijpharm.2026.126595","DOIUrl":"10.1016/j.ijpharm.2026.126595","url":null,"abstract":"<div><div>Phospholipid vesicle-based permeation assay (PVPA) is widely applied as <em>in vitro</em> skin alternative model by mimicking stratum corneum to evaluate the transdermal application of drugs and chemicals. However, it is composed of lipid components only, which suffer from limitations of achieving accurate permeability prediction. To remedy this shortcoming, inactive immortalized human keratinocytes (HaCaT) were integrated as component to construct epidermal-mimicking model: EpiPVPA. The EpiPVPA could tolerate the pH 3–10 as well as up to 30% ethanol and was stable for 2 weeks at 4 ℃. And the permeation evaluation by Franz diffusion test of 14 drugs demonstrated that EpiPVPA model is comparable to porcine skin with strong correlation. After quantitative structure–property relationship (QSPR) analysis of physicochemical descriptors of 14 drugs, HLB, TPSA, and log P were selected as main factors applied to build multiple linear regression (MLR) equation, and the corresponding linear correlation R<sup>2</sup> was elevated to 0.9010. EpiPVPA model is feasible to be applied to permeation evaluation of drugs and cosmetics.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126595"},"PeriodicalIF":5.2,"publicationDate":"2026-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146010282","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-18DOI: 10.1016/j.ijpharm.2026.126598
Junhua Xu , Haochen Wang , Kaizhi Li , Shulei Pan , Gang Guo , Kaiyun Liu , Ning Wang , Lin Xiang
Oral ulcers are a common and painful condition. Current treatments, including topical corticosteroids like dexamethasone, are hindered by poor drug penetration and systemic side effects. To address these challenges, we developed a dissolving microneedle patch incorporating protease-responsive gelatin nanoparticles encapsulating dexamethasone (DEX@GNPs) for localized delivery to the oral mucosa. This system is engineered to penetrate the mucosal barrier and release dexamethasone in response to the inflammatory microenvironment, thereby enhancing drug deposition at the ulcer site. In a rat buccal ulcer model, the DEX@GNP-loaded microneedles effectively delivered dexamethasone to the target tissue layers, significantly reduced ulcer size and promoted tissue regeneration. Moreover, the responsive release of dexamethasone in the presence of elevated protease levels was associated with a marked reduction in inflammation, as evidenced by decreased levels of key pro-inflammatory cytokines. These findings indicate that DEX@GNP-loaded microneedles provide a promising approach for the localized treatment of oral ulcers and may help to improve therapeutic outcomes by enabling efficient localized corticosteroid delivery.
{"title":"Localized treatment of oral ulcers via responsive microneedle patch by enhancing mucosal penetration","authors":"Junhua Xu , Haochen Wang , Kaizhi Li , Shulei Pan , Gang Guo , Kaiyun Liu , Ning Wang , Lin Xiang","doi":"10.1016/j.ijpharm.2026.126598","DOIUrl":"10.1016/j.ijpharm.2026.126598","url":null,"abstract":"<div><div>Oral ulcers are a common and painful condition. Current treatments, including topical corticosteroids like dexamethasone, are hindered by poor drug penetration and systemic side effects. To address these challenges, we developed a dissolving microneedle patch incorporating protease-responsive gelatin nanoparticles encapsulating dexamethasone (DEX@GNPs) for localized delivery to the oral mucosa. This system is engineered to penetrate the mucosal barrier and release dexamethasone in response to the inflammatory microenvironment, thereby enhancing drug deposition at the ulcer site. In a rat buccal ulcer model, the DEX@GNP-loaded microneedles effectively delivered dexamethasone to the target tissue layers, significantly reduced ulcer size and promoted tissue regeneration. Moreover, the responsive release of dexamethasone in the presence of elevated protease levels was associated with a marked reduction in inflammation, as evidenced by decreased levels of key pro-inflammatory cytokines. These findings indicate that DEX@GNP-loaded microneedles provide a promising approach for the localized treatment of oral ulcers and may help to improve therapeutic outcomes by enabling efficient localized corticosteroid delivery.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126598"},"PeriodicalIF":5.2,"publicationDate":"2026-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146010265","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-17DOI: 10.1016/j.ijpharm.2026.126597
Fabia Julliana Jorge de Souza , Francisco Alexandrino-Junior , Wógenes Nunes de Oliveira , Euzébio Guimarães Barbosa , Renato Medeiros de Paula , Éverton do Nascimento Alencar , Júlio Abreu Miranda , Maria Cecília Queiroga dos Santos , Mabel Calina de França Paz , Fábio Rocha Formiga , Eryvaldo Sócrates Tabosa do Egito
Ocular diseases, particularly infections such as fungal keratitis, present significant therapeutic challenges due to limited treatment options and low patient compliance. This study aimed to develop and characterize polyvinyl alcohol (PVA)-based hydrogel ophthalmic lenses (HOLs) incorporating amphotericin B (AmB) for potential use in treating fungal ocular infections. A central composite design (CCD) was employed to optimize the formulation, which was then evaluated for thickness, swelling degree, drug loading, release kinetics, and physicochemical properties via Fourier-transform infrared spectroscopy (FTIR), Powder X-ray diffraction (PXRD), and molecular dynamics simulations (MDS). Additional assessments included mass loss under physiological conditions (37 °C) and in vitro antifungal activity against clinical strains of Candida albicans, Candida parapsilosis, and Candida tropicalis. The CCD enabled precise mathematical modeling of swelling behavior, resulting in HOLs with controlled thickness (0.162 ± 0.011 mm to 0.265 ± 0.018 mm) and suitable hydration profiles. The results from FTIR and PXRD analyses confirmed effective crosslinking and indicated the presence of AmB in an amorphous or molecular dispersed state. After 30 days in artificial tear fluid (pH ∼ 7.4), the lenses exhibited low mass loss (4.4 ± 2.7%), supporting their structural stability. Release studies demonstrated a sustained and controlled AmB release profile, with cumulative release ranging from approximately 25% to 58% in the first 24 h among the tested formulations, consistent with the MDS findings that showed strong interactions between AmB, PVA, and sodium trimetaphosphate (STMP). The HOLs demonstrated antifungal efficacy, particularly against Candida parapsilosis. Overall, the developed PVA-based HOLs offer a promising platform for sustained ocular delivery of AmB in treatment of fungal infections.
{"title":"Eyes on the future: PVA-hydrogel lenses as a platform for amphotericin B ocular delivery","authors":"Fabia Julliana Jorge de Souza , Francisco Alexandrino-Junior , Wógenes Nunes de Oliveira , Euzébio Guimarães Barbosa , Renato Medeiros de Paula , Éverton do Nascimento Alencar , Júlio Abreu Miranda , Maria Cecília Queiroga dos Santos , Mabel Calina de França Paz , Fábio Rocha Formiga , Eryvaldo Sócrates Tabosa do Egito","doi":"10.1016/j.ijpharm.2026.126597","DOIUrl":"10.1016/j.ijpharm.2026.126597","url":null,"abstract":"<div><div>Ocular diseases, particularly infections such as fungal keratitis, present significant therapeutic challenges due to limited treatment options and low patient compliance. This study aimed to develop and characterize polyvinyl alcohol (PVA)-based hydrogel ophthalmic lenses (HOLs) incorporating amphotericin B (AmB) for potential use in treating fungal ocular infections. A central composite design (CCD) was employed to optimize the formulation, which was then evaluated for thickness, swelling degree, drug loading, release kinetics, and physicochemical properties via Fourier-transform infrared spectroscopy (FTIR), Powder X-ray diffraction (PXRD), and molecular dynamics simulations (MDS). Additional assessments included mass loss under physiological conditions (37 °C) and <em>in vitro</em> antifungal activity against clinical strains of <em>Candida albicans</em>, <em>Candida parapsilosis</em>, and <em>Candida tropicalis.</em> The CCD enabled precise mathematical modeling of swelling behavior, resulting in HOLs with controlled thickness (0.162 ± 0.011 mm to 0.265 ± 0.018 mm) and suitable hydration profiles. The results from FTIR and PXRD analyses confirmed effective crosslinking and indicated the presence of AmB in an amorphous or molecular dispersed state. After 30 days in artificial tear fluid (pH ∼ 7.4), the lenses exhibited low mass loss (4.4 ± 2.7%), supporting their structural stability. Release studies demonstrated a sustained and controlled AmB release profile, with cumulative release ranging from approximately 25% to 58% in the first 24 h among the tested formulations, consistent with the MDS findings that showed strong interactions between AmB, PVA, and sodium trimetaphosphate (STMP). The HOLs demonstrated antifungal efficacy, particularly against <em>Candida parapsilosis.</em> Overall, the developed PVA-based HOLs offer a promising platform for sustained ocular delivery of AmB in treatment of fungal infections.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126597"},"PeriodicalIF":5.2,"publicationDate":"2026-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146003708","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Creating high-quality datasets for training machine learning models in specialized domains like pharmaceutical research is often constrained by the manual effort required to extract and compute critical parameters from heterogeneous literature. A novel deep prompt-engineering framework was developed to transform GPT-4 into a robust tool for automated and accelerated generation of structured datasets. Using a multi-set prompt strategy, GPT-4 analysed 70 full-text articles from literature on pharmaceutical inkjet printing to extract and compute 23 domain-relevant variables. These variables were organized into three main parameter groups: (i) printing parameters, (ii) rheological properties, and (iii) drug dose parameters, which were analysed using dedicated prompts. The outputs were benchmarked against a human-curated dataset compiled over four months by four domain experts, previously used to train machine learning models for predicting inkjet printability. Iterative prompt engineering yielded an overall accuracy of 0.942 across 4,217 individual variable-level data points, with computed variables reaching 0.983 accuracy despite multi-step calculations and unit conversions. Inter-day reproducibility was stable, and sensitivity, specificity, and predictive values all exceeded 0.900. Remarkably, the workflow reduced processing time from hours of human effort to <3.5 min per article. This novel prompt-engineering approach enabled GPT-4 to generate reliable, high-quality, literature-derived datasets, dramatically reducing manual effort while maintaining expert-level accuracy. Ultimately, this novel strategy facilitates the scalability of machine learning in pharmaceutical, and other data-intensive domains.
{"title":"Accelerating dataset generation for machine learning using large language models: a pharmaceutical additive manufacturing case","authors":"Paola Carou-Senra , Lucía Rodríguez-Pombo , Carmen Alvarez-Lorenzo , Alvaro Goyanes","doi":"10.1016/j.ijpharm.2026.126587","DOIUrl":"10.1016/j.ijpharm.2026.126587","url":null,"abstract":"<div><div>Creating high-quality datasets for training machine learning models in specialized domains like pharmaceutical research is often constrained by the manual effort required to extract and compute critical parameters from heterogeneous literature. A novel deep prompt-engineering framework was developed to transform GPT-4 into a robust tool for automated and accelerated generation of structured datasets. Using a multi-set prompt strategy, GPT-4 analysed 70 full-text articles from literature on pharmaceutical inkjet printing to extract and compute 23 domain-relevant variables. These variables were organized into three main parameter groups: (i) printing parameters, (ii) rheological properties, and (iii) drug dose parameters, which were analysed using dedicated prompts. The outputs were benchmarked against a human-curated dataset compiled over four months by four domain experts, previously used to train machine learning models for predicting inkjet printability. Iterative prompt engineering yielded an overall accuracy of 0.942 across 4,217 individual variable-level data points, with computed variables reaching 0.983 accuracy despite multi-step calculations and unit conversions. Inter-day reproducibility was stable, and sensitivity, specificity, and predictive values all exceeded 0.900. Remarkably, the workflow reduced processing time from hours of human effort to <3.5 min per article. This novel prompt-engineering approach enabled GPT-4 to generate reliable, high-quality, literature-derived datasets, dramatically reducing manual effort while maintaining expert-level accuracy. Ultimately, this novel strategy facilitates the scalability of machine learning in pharmaceutical, and other data-intensive domains.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126587"},"PeriodicalIF":5.2,"publicationDate":"2026-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146003666","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-17DOI: 10.1016/j.ijpharm.2026.126590
Hao Zhang , Shenzhi Li , Jiaxi You , Liang Yin , Di Wang , Weiwei Zheng , Qiang Yuan , Yong Jin , Xingwei Sun
Globally, hepatocellular carcinoma (HCC) is among the most prevalent malignancies and is the third most common cause of cancer-related mortality. Thermal ablation therapies for hepatocellular carcinoma, such as microwave ablation (MWA) and radiofrequency ablation (RFA) guided by imaging devices, have been widely used in clinical practice and have achieved good therapeutic efficacy but still face the difficult problems of high dependence on the experience of the operator’s puncture and damage caused by the tissue puncture. In this study, magnetothermal microspheres (MMs) loaded with Fe3O4 nanoparticles, featuring a uniform particle size (45–55 μm) and a good eddy current heating effect, were prepared from polyvinyl alcohol (PVA) via Shirasu Porous Glass (SPG) membrane emulsification. Under the action of a high-frequency alternating magnetic field (AMF), the PVA@Fe3O4 MMs could be rapidly warmed in vitro and effectively inhibited the activity of tumor cells. We successfully constructed a rabbit VX2 orthotopic liver tumor model. Under DSA guidance, the microspheres were enriched precisely in the tumor tissue, and in vivo animal experiments confirmed that the therapeutic effect of the MMs was similar to that of puncture ablation under the effect of an AMF, and further sections of important organ tissues showed good in vivo safety. Compared with traditional percutaneous ablation, microsphere-mediated magnetic thermal ablation (MTA) significantly reduces puncture trauma and is applicable to other blood-rich solid tumors, demonstrating favorable clinical prospects.
{"title":"Preparation of high-performance PVA@Fe3O4 magnetothermal microspheres for precise ablation of orthotopic hepatocellular carcinoma in a rabbit model","authors":"Hao Zhang , Shenzhi Li , Jiaxi You , Liang Yin , Di Wang , Weiwei Zheng , Qiang Yuan , Yong Jin , Xingwei Sun","doi":"10.1016/j.ijpharm.2026.126590","DOIUrl":"10.1016/j.ijpharm.2026.126590","url":null,"abstract":"<div><div>Globally, hepatocellular carcinoma (HCC) is among the most prevalent malignancies and is the third most common cause of cancer-related mortality. Thermal ablation therapies for hepatocellular carcinoma, such as microwave ablation (MWA) and radiofrequency ablation (RFA) guided by imaging devices, have been widely used in clinical practice and have achieved good therapeutic efficacy but still face the difficult problems of high dependence on the experience of the operator’s puncture and damage caused by the tissue puncture. In this study, magnetothermal microspheres (MMs) loaded with Fe<sub>3</sub>O<sub>4</sub> nanoparticles, featuring a uniform particle size (45–55 μm) and a good eddy current heating effect, were prepared from polyvinyl alcohol (PVA) via Shirasu Porous Glass (SPG) membrane emulsification. Under the action of a high-frequency alternating magnetic field (AMF), the PVA@Fe<sub>3</sub>O<sub>4</sub> MMs could be rapidly warmed in vitro and effectively inhibited the activity of tumor cells. We successfully constructed a rabbit VX2 orthotopic liver tumor model. Under DSA guidance, the microspheres were enriched precisely in the tumor tissue, and in vivo animal experiments confirmed that the therapeutic effect of the MMs was similar to that of puncture ablation under the effect of an AMF, and further sections of important organ tissues showed good in vivo safety. Compared with traditional percutaneous ablation, microsphere-mediated magnetic thermal ablation (MTA) significantly reduces puncture trauma and is applicable to other blood-rich solid tumors, demonstrating favorable clinical prospects.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126590"},"PeriodicalIF":5.2,"publicationDate":"2026-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146003620","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-15DOI: 10.1016/j.ijpharm.2026.126596
Mingrui Ma , Marwa Nassar , Jason Teckoe , J. Axel Zeitler
Titanium dioxide (TiO2) is often used as a white base pigment in film coatings, but recent EU restrictions on its use in food have prompted pharmaceutical manufacturers to seek alternatives. Terahertz pulsed imaging (TPI) was used to examine the hydration of TiO2-free immediate release formulations, either without an opacifier or using calcium carbonate (CaCO3). The coatings, made from polyvinyl alcohol (PVA) or hydroxypropyl methylcellulose (HPMC), were approximately 100 µm thick. TPI results indicated that the type of film coating influenced hydration and scattering effects. However, there was no evidence that TiO2-free coatings compromised tablet disintegration. Although the HPMC coating with CaCO3 gelled upon hydration, the tablets fully hydrated within the required time. These findings offer insights into the mechanistic impacts of alternative coatings in the industry.
{"title":"Terahertz imaging of titanium dioxide-free film coating hydration and tablet core interactions","authors":"Mingrui Ma , Marwa Nassar , Jason Teckoe , J. Axel Zeitler","doi":"10.1016/j.ijpharm.2026.126596","DOIUrl":"10.1016/j.ijpharm.2026.126596","url":null,"abstract":"<div><div>Titanium dioxide (TiO<sub>2</sub>) is often used as a white base pigment in film coatings, but recent EU restrictions on its use in food have prompted pharmaceutical manufacturers to seek alternatives. Terahertz pulsed imaging (TPI) was used to examine the hydration of TiO<sub>2</sub>-free immediate release formulations, either without an opacifier or using calcium carbonate (CaCO<sub>3</sub>). The coatings, made from polyvinyl alcohol (PVA) or hydroxypropyl methylcellulose (HPMC), were approximately 100<!--> <!-->µm thick. TPI results indicated that the type of film coating influenced hydration and scattering effects. However, there was no evidence that TiO<sub>2</sub>-free coatings compromised tablet disintegration. Although the HPMC coating with CaCO<sub>3</sub> gelled upon hydration, the tablets fully hydrated within the required time. These findings offer insights into the mechanistic impacts of alternative coatings in the industry.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126596"},"PeriodicalIF":5.2,"publicationDate":"2026-01-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145994186","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2026-01-14DOI: 10.1016/j.ijpharm.2026.126593
A. De Man , B. Van Snick , T. Verbeek , M. Otava , A. Kumar , C. Vervaet , V. Vanhoorne , T. De Beer
The current study investigated the differences in volumetric twin-screw feeding behaviour of 15 commonly known oral solid dosage powder materials between two loss-in-weight feeders, differing in scale. Principal Component Analysis (PCA) was applied to study the importance of material properties on various volumetric feeding output parameters. In addition, the developed PCA model was used to explore material properties that could explain observed differences in screw filling as a function of the screw speed per feeder. To study changes in the importance of material properties of various powder materials between two loss-in-weight feeding systems, multiple Partial Least Squares (PLS) regression models were developed. These PLS models focused on predicting screw filling, feeding capacity decay and short-term feeding variability. Overall, the difference in overhead pressure between both studied feeders appeared to affect the importance of material properties, mostly for the maximum screw filling. The developed models highlighted the importance of material properties on twin-screw feeding behaviour per loss-in-weight feeder and will support future research on developing a surrogate material identification and selection methodology.
{"title":"Exploring twin-screw feeding behaviour across different loss-in-weight feeders","authors":"A. De Man , B. Van Snick , T. Verbeek , M. Otava , A. Kumar , C. Vervaet , V. Vanhoorne , T. De Beer","doi":"10.1016/j.ijpharm.2026.126593","DOIUrl":"10.1016/j.ijpharm.2026.126593","url":null,"abstract":"<div><div>The current study investigated the differences in volumetric twin-screw feeding behaviour of 15 commonly known oral solid dosage powder materials between two loss-in-weight feeders, differing in scale. Principal Component Analysis (PCA) was applied to study the importance of material properties on various volumetric feeding output parameters. In addition, the developed PCA model was used to explore material properties that could explain observed differences in screw filling as a function of the screw speed per feeder. To study changes in the importance of material properties of various powder materials between two loss-in-weight feeding systems, multiple Partial Least Squares (PLS) regression models were developed. These PLS models focused on predicting screw filling, feeding capacity decay and short-term feeding variability. Overall, the difference in overhead pressure between both studied feeders appeared to affect the importance of material properties, mostly for the maximum screw filling. The developed models highlighted the importance of material properties on twin-screw feeding behaviour per loss-in-weight feeder and will support future research on developing a surrogate material identification and selection methodology.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"691 ","pages":"Article 126593"},"PeriodicalIF":5.2,"publicationDate":"2026-01-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145989169","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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