Journal of Pharmaceutical Innovation最新文献

{"title":"Deep Eutectic System-Based Liquisolid Nanoparticles as Drug Delivery System of Curcumin for In-Vitro Colon Cancer Cells","authors":"Abdeh Nakaweh,&nbsp;Faisal Al-Akayleh,&nbsp;Mayyas Al-Remawi,&nbsp;Qasem Abdallah,&nbsp;Ahmed S.A. Ali Agha","doi":"10.1007/s12247-024-09826-w","DOIUrl":"10.1007/s12247-024-09826-w","url":null,"abstract":"<div><h3>Purpose</h3><p>This study aims to improve curcumin’s solubility and anti-cancer effectiveness by utilizing deep eutectic solvents (DES)-based liquisolid nanoparticles. This study aims to develop mesoporous silica nanoparticles (MSNs) containing curcumin and evaluate their therapeutic efficacy against the HCT 116 human colon cancer cell line.</p><h3>Methods</h3><p>The study focused on developing different DES formulations using Menthol and Capric Acid, evaluating the effectiveness of surfactants such as Labrasol and Tween 80 in enhancing curcumin dissolution, and synthesizing curcumin-loaded MSNs. The stability of nanoparticles in deep eutectic solvents (DES) and their pharmacological impact on colon cancer cells were thoroughly assessed.</p><h3>Results</h3><p>The solubility of curcumin was significantly enhanced through the use of deep eutectic solvent (DES) formulations, specifically when Tween 80 was employed as a surfactant. The in vitro tests showed that curcumin-loaded MSNs with Tween 80 demonstrated strong anti-cancer activity, as indicated by an IC50 value of around 100 µM.</p><h3>Conclusion</h3><p>The study effectively shows that DES-based MSNs can greatly improve curcumin’s solubility and anti-cancer effectiveness. Tween 80, as a surfactant, enhances its therapeutic potential, indicating promising prospects for future clinical applications in cancer treatment.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140579649","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In Vitro Profiling of Gliclazide-Loaded Aerosil 380 Solid Dispersion–Based Tablets with Co-Processed Excipients","authors":"Israt Zerin Alam,&nbsp;Jakia Sultana,&nbsp;Mohsin Kazi,&nbsp;Mohammad N. Uddin,&nbsp;Md Bytul Mokaddesur Rahman","doi":"10.1007/s12247-024-09817-x","DOIUrl":"10.1007/s12247-024-09817-x","url":null,"abstract":"&lt;div&gt;&lt;h3&gt;Purpose&lt;/h3&gt;&lt;p&gt;Gliclazide (GLC)-loaded Aerosil 380 solid dispersion (GA-SD)-based tablets with co-processed excipient composites were formulated to critically evaluate the physicochemical performance of the resulting tablets with enhanced drug release.&lt;/p&gt;&lt;h3&gt;Methods&lt;/h3&gt;&lt;p&gt;GA-SD was prepared using the solvent evaporation method with a 1:1 weight ratio based on a previously published report, and its drug release patterns were evaluated. Processed excipient composites, such as lactose-starch-povidone (LSP) and lactose-starch-povidone-sodium starch glycolate (LSPS), were prepared via a coprocessing strategy and evaluated for their ability to perform specific functions. At predetermined combination levels, aqueous dispersions of primary excipients were physically agglomerated at a controlled temperature below the gelatinization temperature (55 °C) before drying at 60 °C for 48 h. GA-SD and co-processed excipients (LSP and LSPS) were utilized to produce tablet batches GAC1 to GAC8 (Gliclazide-Aerosil 380–co-processed excipients, GAC) by direct compression. Through rigorous testing of tablet batches, the physicochemical properties of the resulting formulations were analyzed and compared to those of leading marketed formulations (MFs). FTIR studies were also conducted to detect drug-excipient interactions in the tablet formulations. The release mechanism of the GLC was determined by studying the dissolution process with various kinetic models. The GAC tablets were subjected to 40 °C/75% RH for 3 months to assess stability.&lt;/p&gt;&lt;h3&gt;Results&lt;/h3&gt;&lt;p&gt;All tablet formulations of GA-SD containing co-processed excipients met the weight, friability, disintegration time, mechanical strength, and homogeneity requirements. There was significantly more GLC released from the GAC formulations (&lt;i&gt;p&lt;/i&gt; &lt; 0.05) at each time point when the formulations were exposed to water than when the formulations were exposed to MFs. In vitro, testing revealed that the GAC5 to GAC8 formulations were the most efficient due to the presence of the superdisintegrant in the LSPS composite, which may be a contributing factor to the improvement in the dissolution rate by GA-SD. FTIR analysis revealed no notable chemical interactions between GLC and the excipients in the solid state. The Korsmeyer-Peppas model was the best-fit kinetic model, indicating that diffusion is the predominant mechanism of GLC dissolution. According to the commercial standards, the GAC tablets maintained an acceptable hardness, disintegration time, and drug content during the stability studies. Additionally, no significant changes in release profiles were observed in the selected batches (&lt;i&gt;p&lt;/i&gt; &lt; 0.05).&lt;/p&gt;&lt;h3&gt;Conclusion&lt;/h3&gt;&lt;p&gt;Compared with currently marketed formulations (MFs), GA-SD tablet formulations with co-processed excipients significantly improved the physicochemical properties, including the drug release rate. These findings could lead to the development of more effective and efficient ta","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140579655","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Chitosan Beeswax Matrix for Gastro-Retentive Delivery of Curcumin: A Promising Adjuvant Therapy for Helicobacter Infection","authors":"Nisrein Jaber,&nbsp;Mayyas Al-Remawi,&nbsp;Rami A. Abdel-Rahem","doi":"10.1007/s12247-024-09824-y","DOIUrl":"10.1007/s12247-024-09824-y","url":null,"abstract":"<div><h3>Purpose</h3><p>The main purpose of this study is to introduce a new adjuvant treatment for <i>H. pylori</i> that aims to enhance therapy outcomes. The research question is how to create a controlled-release gastro-retentive floating system using a combination of chitosan (CS) and beeswax (BW) and to evaluate the release behavior of curcumin as an active ingredient.</p><h3>Methods</h3><p>In this study, a new formula combining CS and BW was developed through a hot melting process to create a controlled-release gastro-retentive floating system. Response surface methodology (RSM) was employed to determine the optimal conditions and concentrations of CS and BW to produce the desired floating system. Parameters such as mixing time, processing melting temperature, and concentration of BW were evaluated.</p><h3>Results</h3><p>The study found that the optimal parameters for the CS/BW formulation were determined as follows: a mixing time of 3 min, a processing melting temperature of 92.2 °C, and a BW concentration of 13.3% (w/w). Curcumin was incorporated into the optimal tablet, and its release behavior was evaluated. The results showed a full floating behavior of the tablet and a zero-order release behavior in acidic conditions.</p><h3>Conclusions</h3><p>The study successfully introduced a new adjuvant treatment for <i>H. pylori</i> that utilizes a controlled-release gastro-retentive floating system. The combination of CS and BW, along with the incorporation of curcumin, showed promising results in terms of floating behavior and release kinetics. This new treatment approach has the potential to enhance therapy outcomes for <i>H. pylori</i> infections.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140315200","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Biosynthesis and Characterization of Silver Nanoparticle by Using Artocarpus altilis Fruit Extract for Its Biological Activity","authors":"Thasni PM,&nbsp;Abdul Vajid K,&nbsp;Najila Shirin U,&nbsp;Nivya K,&nbsp;Fathimath Shibila AP,&nbsp;Ilyas UK","doi":"10.1007/s12247-024-09819-9","DOIUrl":"10.1007/s12247-024-09819-9","url":null,"abstract":"<div><h3>Purpose</h3><p>The study of nanoparticles for antibacterial, antifungal, and anticancer action is an important sector in nanoscience. The use of plant extracts in nanoparticle synthesis is among the most simple, cost-effective, and ecologically acceptable strategies. The goal is to use <i>Artocarpus altilis</i> fruit extract to generate plant-mediated silver nanoparticles for its biological activity.</p><h3>Methods</h3><p>Phytochemical profiling of methanolic extract of <i>Artocarpus altilis</i> fruit was carried out. UV visible spectroscopy and scanning electron microscopy (SEM) are used to characterize the sample. The disc diffusion method was used to interpret antimicrobial activity. The MTT assay was used to determine the cytotoxicity.</p><h3>Results</h3><p>The presence of flavonoids, terpenoids, phenolic compounds, and others was discovered by phytochemical profiling. UV-visible spectroscopy was used to establish the existence of AgNPs, and a maximum absorbance range was obtained. The optimized nanoparticles were shown to have a spherical shape by the SEM pictures. Using the disc diffusion method, the defined AgNPs demonstrated antibacterial efficacy against <i>Escherichia coli</i>, <i>Pseudomonas aeruginosa</i>, <i>Bacillus subtilis</i>, and <i>Staphylococcus aureus</i> at various doses, as well as antifungal efficacy against <i>Aspergillus fumigates</i>. When compared to doxorubicin, the lung cancer cell lines (A549 cell line) demonstrated potential anticancer activity of silver nanoparticles.</p><h3>Conclusion</h3><p>We discovered that silver nanoparticles made from <i>Artocarpus altilis</i> fruit extract have a similar effect to ciprofloxacin. The cytotoxic activity anticipated against the lung cancer cell line (A549 cell line) shows that the percentage of cell viability is identical to that of doxorubicin which indicates the potential for the treatment of lung tumors.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140315201","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A Novel CFD Model of SMX Static Mixer Used in Advanced Continuous Manufacturing of Active Pharmaceutical Ingredients (API)","authors":"Athanasios Kritikos,&nbsp;Ravendra Singh,&nbsp;George Tsilomelekis,&nbsp;Fernando J. Muzzio","doi":"10.1007/s12247-024-09813-1","DOIUrl":"10.1007/s12247-024-09813-1","url":null,"abstract":"<div><h3>Purpose</h3><p>The growing demand for effective pharmaceutical treatments, notably amidst health challenges like COVID, highlights the urgency for improved drug production techniques. This study examines the simulation of the Sulzer SMX static mixer in laminar conditions for the continuous pharmaceutical manufacturing of significant pharmaceuticals, notably imatinib.</p><h3>Methods</h3><p>Computational fluid dynamics (CFD) were employed to assess the SMX static mixer’s hydrodynamics and mixing performance. Emphasis was on mixing efficiency and residence time distributions (RTD) in a mixer with SMX elements. We refined the model’s reliability and explored the correlation between friction factor and Reynolds number. The Definitive Screening Design (DSD) was used to determine major factors impacting mixer dynamics.</p><h3>Results</h3><p>We established a novel correlation between friction factor and Reynolds number. The study reveal that lower flowrates significantly impact mixing efficiency, with different solvents inducing mixing delays. The RTD study identified the total inlet flowrate’s influence on distribution, with higher flowrates leading to more distinct RTD profiles and decreased axial mixing. The screening analysis highlighted flowrate’s dominance over other factors in determining mixing efficiency and residence time.</p><h3>Conclusions</h3><p>Through precise computational fluid dynamics (CFD) simulations, the study affirms the robustness of the developed model and underscores the novel correlation between the friction factor and Reynolds number. Insights into flow rate’s pivotal role in dictating mixer efficiency and residence time distribution are discerned, culminating in a comprehensive guide for refining static mixer operations for optimized drug manufacturing.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140200536","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Design and Development of Immediate Release Pellets Formulation Containing Co Amorphous Mixture of Aceclofenac: In-Vitro and In-Vivo Study","authors":"Nahid Anjum Hafizuddin Chishti,&nbsp;Inayat Bashir Pathan,&nbsp;Mohamed Hassan G. Dehghan,&nbsp;Shripad M. Bairagi","doi":"10.1007/s12247-024-09823-z","DOIUrl":"10.1007/s12247-024-09823-z","url":null,"abstract":"<div><h3>Purpose</h3><p>Aceclofenac is a nonsteroidal anti-inflammatory drug (NSAID) belonging to BCS Class II, has a constraint over its therapeutic benefits owing to its poor aqueous solubility.</p><h3>Methods</h3><p>In this study, co-amorphous mixtures of Aceclofenac (ACE) with Aspartame (ASPA) of various molar ratios at specific milling times were produced through ball milling (BM) technique. The characterization was done using FTIR, DSC and PXRD. The pellets formulation was prepared by extrusion spheronization method using 3² full factorial design. The optimized formulation was evaluated for in-vitro and in-vivo performance.</p><h3>Results</h3><p>Amongst the co amorphous mixtures and pure ACE studied for solubility, ACE: ASPA (1:1) showed the significant increase in solubility and was further formulated as pellets. Solid-state characterization of mixture revealed amorphization of ACE after 120 min of ball milling. In-vitro dissolution study data of F4 pellets formulation revealed (99.00 ± 3.59%) significant increase (P &lt; 0.005) compared to pure drug (50.12 ± 2.52%) and other formulations. The in-vivo studies reveal a significant increase in percent inhibition of inflammation (61.7%) of the prepared formulation (p &lt; 0.05) as compared to the marketed formulation (53.19%), and pure drug (46.8%).</p><h3>Conclusion</h3><p>Therefore, the prepared pellets of co-amorphous mixture of aceclofenac and aspartame, boost the solubility and stability of aceclofenac which has a potential to be a promising approach in the management of pain.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140045234","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fluconazole Microsponges Loaded Bioadhesive Vaginal Film to Treat Vulvovaginal Candidiasiss","authors":"Priti L. Mandlik,&nbsp;Palakshi R. Lad,&nbsp;Ashlesha P. Pandit","doi":"10.1007/s12247-024-09822-0","DOIUrl":"10.1007/s12247-024-09822-0","url":null,"abstract":"<div><h3>Purpose</h3><p>The purpose of this study was to develop fluconazole microsponges loaded bioadhesive film, rolled into a torpedo-shaped capsule, to achieve ease of application and reduce application frequency for the treatment of vulvovaginal candidiasis. This was accomplished by using biodegradable polymer blend specifically designed to cater the busy lifestyle of working women.</p><h3>Methods</h3><p>Microsponges were prepared using the quasi-emulsion solvent diffusion method. Herein, fluconazole: ethyl cellulose (1:2.5, 1:3, 1:3.5) and polyvinyl alcohol (used as the external phase) were dissolved in dichloromethane (12.5, 15, 17.5 ml). Three-level, two-factor full-factorial design optimized the above process. Next, the developed microsponges were thoroughly evaluated for entrapment efficiency, drug release and antimicrobial study. Lastly, film was developed which was made up of blend of bioadhesive polymers, namely pectin and xanthan gum. Subsequently, film was rolled into a torpedo-shaped capsule shell.</p><h3>Results</h3><p>The spherical-shaped porous microsponges exhibited a notable entrapment efficiency (94.17%), size 14.68 μm and rapid drug release of 91.1 ± 1.54% within 10 h. Further, bioadhesive film revealed thickness 92 μm, folding endurance 440, moisture content 5.66 ± 0.51% w/w, and good tensile strength to withstand vaginal pressure and remarkable zone of inhibition against <i>Candida albicans</i> (19.1 mm).</p><h3>Conclusion</h3><p>Fluconazole microsponges loaded bioadhesive film, rolled into a torpedo-shaped capsule, exhibited an excellent aesthetic appearance. Moreover, strong bioadhesivity ensured a high efficacy in combating disease.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140045482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"An Understanding of the Relationship Between Mixing Performance and Power Consumption in a High-Shear Wet Granulation Pre-mixing","authors":"Zeng Liu,&nbsp;Chunling Liu,&nbsp;Renyu Fan,&nbsp;Yuting Wang,&nbsp;Linxiu Luo,&nbsp;Yanling Jiang,&nbsp;Jincao Tang,&nbsp;Zheng Lu,&nbsp;Libo Chen,&nbsp;Shuangkou Chen,&nbsp;Tianbing Guan,&nbsp;Chuanyun Dai","doi":"10.1007/s12247-024-09816-y","DOIUrl":"10.1007/s12247-024-09816-y","url":null,"abstract":"<div><h3>Introduction</h3><p>High-shear wet granulation (HSWG) is most commonly used in the pharmaceutical industry, with the advantages of being fully enclosed, having a good mixing effect, and being highly efficient. However, only a few studies are geared toward an in-depth understanding of the pre-mixing process in the high-shear wet granulator (HSWGr).</p><h3>Objectives</h3><p>In this paper, the effect of impeller speed and fill level on the mixing performance of particles is investigated using the discrete element method (DEM), which provides theoretical references for the energy-saving operation in HSWGr.</p><h3>Methods</h3><p>Relative standard deviation (RSD) was used as a mixing index to quantify mixing quality, particle temperature over a vertical distance to quantify particle motion bias, and total power consumption per unit mass to monitor the loss effect.</p><h3>Results</h3><p>The simulation results show that the impeller speed only affects the mixing process and does not change the mixing uniformity; the fill level has a significant effect on the particle mixing, and a higher fill level will inhibit the particle mixing; based on the uniform mixing, the fill level has little effect on the total power consumption per unit mass.</p><h3>Conclusion</h3><p>The results of the study show that increasing the fill level and impeller speed contributes to the energy-saving operation of HSWGr.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140008438","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Integrated Continuous Process Design for Crystallisation, Spherical Agglomeration, and Filtration of Lovastatin","authors":"Cameron J. Brown,&nbsp;John McGinty,&nbsp;Muhammad T. Islam,&nbsp;Nazer Rajoub,&nbsp;Omid Arjmandi-Tash,&nbsp;Sara Ottoboni,&nbsp;Muhid Shahid,&nbsp;Stephanie J. Urwin,&nbsp;Ye Seol Lee,&nbsp;Magdalene W. S. Chong,&nbsp;Foteini Papathanasiou,&nbsp;Aruna S. Prakash,&nbsp;Elke Prasad,&nbsp;Bronwyn Spence,&nbsp;Jan Sefcik,&nbsp;John Robertson,&nbsp;Rachel Smith,&nbsp;James D. Litster,&nbsp;Chris J. Price,&nbsp;Alison Nordon,&nbsp;Claire S. Adjiman,&nbsp;Alastair J. Florence","doi":"10.1007/s12247-024-09815-z","DOIUrl":"10.1007/s12247-024-09815-z","url":null,"abstract":"<div><h3>Purpose</h3><p>This work seeks to improve the particle processability of needle-like lovastatin crystals and develop a small-footprint continuous MicroFactory for its production.</p><h3>Methods</h3><p>General conditions for optimal spherical agglomeration of lovastatin crystals and subsequent product isolation are developed, first as batch processes, and then transferred to continuous MicroFactory operation.</p><h3>Results</h3><p>Methyl isobutyl ketone is a suitable bridging liquid for the spherical agglomeration of lovastatin. Practical challenges including coupling unit operations and solvent systems; mismatched flow rates and inconsistent suspension solid loading were resolved. The successful continuous production of lovastatin spherical agglomerates (D₅₀ = 336 µm) was achieved. Spherical agglomeration increased the density of the bulk lovastatin powder and improved product flowability from poor to good, whilst maintaining lovastatin tablet performance.</p><h3>Conclusion</h3><p>A continuous, integrated MicroFactory for the crystallisation, spherical agglomeration, and filtration of lovastatin is presented with improved product particle processability. Up to 16,800 doses of lovastatin (60 mg) can be produced per day using a footprint of 23 m².</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://link.springer.com/content/pdf/10.1007/s12247-024-09815-z.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140008571","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Assessment of Imaging Flow Cytometry for the Simultaneous Discrimination of Protein Particles and Silicone Oil Droplets in Biologicals","authors":"Ibrahim Fawaz,&nbsp;Simone Helene Schaz,&nbsp;Patrick Garidel,&nbsp;Udo Bakowsky,&nbsp;Michaela Blech","doi":"10.1007/s12247-024-09810-4","DOIUrl":"10.1007/s12247-024-09810-4","url":null,"abstract":"<div><h3>Purpose</h3><p>Silicone oil droplets in biopharmaceutical products can originate from sources such as siliconized surfaces of primary packaging materials, potentially triggering the formation of protein–silicone oil particles. To better understand this phenomenon, there is a need for particle detection devices that cannot only distinguish between protein particles and silicone oil droplets but also determine particle sizes ranging from nanometers to micrometers.</p><h3>Method</h3><p>In this study, we conducted a systematic assessment of imaging flow cytometry (IFC) using the FlowSight® instrument. Our first step was to investigate specific instrument settings using protein particle samples spiked with silicone oil for particle classification. Based on these findings, we established suitable, harmonized working templates. Next, we evaluated the instrument’s accuracy and precision for particle sizes within the range of 0.5 to 100 µm and their respective concentrations. Finally, we investigated any constraints in particle concentration within this size range.</p><h3>Results</h3><p>This study demonstrates that IFC can effectively distinguish protein particles from silicone oil droplets when the latter is labeled with a specific fluorescent dye. Our findings suggest that fluorescently labeled particles ≥ 0.5 µm can be reliably detected. Through our research, we determined the particle concentration limits for each particle size in the range of 0.5 to 10 µm, with a precision deviation of less than 15%. However, our study also revealed that IFC exhibited insufficient accuracy for the tested particle concentrations within this size range. Additionally, we showed that the measurements were significantly influenced by the instrument settings.</p><h3>Conclusion</h3><p>Although we addressed numerous new aspects to enhance the experimental procedure of IFC measurements, we conclude that IFC is not an ideal technique for quantifying sub-visible particles. Instead, it should be employed to provide supportive characterization data in conjunction with commonly used sub-visible particle detection methods. If distinguishing between protein particles and silicone oil droplets is essential, IFC is an option, as long as the fluorescent dye is carefully selected.</p><h3>Graphical Abstract</h3>\u0000<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 2","pages":""},"PeriodicalIF":2.7,"publicationDate":"2024-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140008440","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}