International Journal of Pharmaceutics: X最新文献_第4页

Development and optimization of the Glabridin-loaded dissolving microneedle for enhanced treatment of keloid 开发和优化格拉布林负载型溶解微针，加强对瘢痕疙瘩的治疗

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-07-01 DOI: 10.1016/j.ijpx.2024.100267

Juan Guo , Zhongtang Chen , Rong Huang , Dandan Tang , Yuhuan Wang , Pan Song , Liangyu Mei , Shuguang Hou , Wei Peng , Lisha He , Qiang Ren

{"title":"Development and optimization of the Glabridin-loaded dissolving microneedle for enhanced treatment of keloid","authors":"Juan Guo , Zhongtang Chen , Rong Huang , Dandan Tang , Yuhuan Wang , Pan Song , Liangyu Mei , Shuguang Hou , Wei Peng , Lisha He , Qiang Ren","doi":"10.1016/j.ijpx.2024.100267","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100267","url":null,"abstract":"<div><p>Glabridin (Gla) has been reported to have significant effects in scar treatment, and however, the water insolubility of Gla leads to its poor transdermal absorption ability, which affects its bioactivities. Therefore, we attempted to prepare the Gla dissolving microneedles (Gla-MN) to improve the absorbtion of Gla. After investigation of the 3 factors including the needle tip matrix concentration, the prescription concentration of backing material, and the dissolution method of Gla, we finally determined the process parameters of 10% hyaluronic acid (HA) as the needle tip and 5% polyvinyl alcohol (PVA) as the backing, according to which the Gla-MN was prepared with the good characteristics of high hardness, complete appearance and good in vitro dissolution ability. We then loaded Gla onto the microneedles and measured that the average drug loading of Gla-MN was 2.26 ± 0.11 μg/mg and the cumulative transdermal release of Gla-MN was up to 76.9% after 24 h. In addition, Gla-MN had good skin penetration properties, with Gla-MN penetrating at least 4 to 5 layers of parafilm. And the skin basically could return to normal after 4 h of piercing. Importantly, our results showed that Gla-MN had higher transdermal delivery and therapeutic effects against keloid than that of Gla at the same dosage.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":5.2,"publicationDate":"2024-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000392/pdfft?md5=8e17fc604d73151f78a88bc4a571a902&pid=1-s2.0-S2590156724000392-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141543122","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Process intensification of pharmaceutical powder blending at commercial throughputs by utilizing semi-continuous mini-blending 利用半连续性微型混合技术，在商业产量条件下强化药粉混合工艺

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-06-26 DOI: 10.1016/j.ijpx.2024.100264

Maarten Jaspers , Florian Tegel , Timo P. Roelofs , Fabian Starsich , Yunfei Li Song , Bernhard Meir , Richard Elkes , Bastiaan H.J. Dickhoff

{"title":"Process intensification of pharmaceutical powder blending at commercial throughputs by utilizing semi-continuous mini-blending","authors":"Maarten Jaspers , Florian Tegel , Timo P. Roelofs , Fabian Starsich , Yunfei Li Song , Bernhard Meir , Richard Elkes , Bastiaan H.J. Dickhoff","doi":"10.1016/j.ijpx.2024.100264","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100264","url":null,"abstract":"<div><p>Process intensification involves the miniaturization of equipment while retaining process throughput and performance. The pharmaceutical industry can benefit from this approach especially during drug product development, where the availability of active pharmaceutical ingredients (API) is often limited. It reduces the need for process scale up, as equipment used during product development and commercial production is identical. However, applications of process intensification for processing pharmaceutical powders are limited so far. Here we show that semi-continuous mini-blending can be utilized for process intensification of blending of API and excipients. Uniform blending at commercially relevant throughputs was achieved through mini-blends with a volume of less than ten liters. Our results demonstrate that blending speed, cycle time and blender fill level can be optimized without compromising blending performance. Acceptable blend uniformity is obtained over a broad range of operating parameters, by choosing the right excipients. The optimized throughput of the mini-blending process is in line with the desired throughput of a commercial Continuous Direct Compression (CDC) process.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":5.2,"publicationDate":"2024-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000367/pdfft?md5=89fff000d4ba805a50dd10ee04fa86a4&pid=1-s2.0-S2590156724000367-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484105","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Advanced applications of smart electrospun nanofibers in cancer therapy: With insight into material capabilities and electrospinning parameters 智能电纺纳米纤维在癌症治疗中的先进应用：深入了解材料性能和电纺参数

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-06-26 DOI: 10.1016/j.ijpx.2024.100265

Vahid Tayebi-Khorrami , Pouria Rahmanian-Devin , Mohammad Reza Fadaei , Jebraeel Movaffagh , Vahid Reza Askari

{"title":"Advanced applications of smart electrospun nanofibers in cancer therapy: With insight into material capabilities and electrospinning parameters","authors":"Vahid Tayebi-Khorrami , Pouria Rahmanian-Devin , Mohammad Reza Fadaei , Jebraeel Movaffagh , Vahid Reza Askari","doi":"10.1016/j.ijpx.2024.100265","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100265","url":null,"abstract":"<div><p>Cancer remains a major global health challenge, and despite available treatments, its prognosis remains poor. Recently, researchers have turned their attention to intelligent nanofibers for cancer drug delivery. These nanofibers exhibit remarkable capabilities in targeted and controlled drug release. Their inherent characteristics, such as a high surface area-to-volume ratio, make them attractive candidates for drug delivery applications. Smart nanofibers can release drugs in response to specific stimuli, including pH, temperature, magnetic fields, and light. This unique feature not only reduces side effects but also enhances the overall efficiency of drug delivery systems. Electrospinning, a widely used method, allows the precision fabrication of smart nanofibers. Its advantages include high efficiency, user-friendliness, and the ability to control various manufacturing parameters. In this review, we explore the latest developments in producing smart electrospun nanofibers for cancer treatment. Additionally, we discuss the materials used in manufacturing these nanofibers and the critical parameters involved in the electrospinning process.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":5.2,"publicationDate":"2024-06-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000379/pdfft?md5=a73c7428c60387bee2ba28056c722898&pid=1-s2.0-S2590156724000379-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484103","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Stability of Dexamethasone during Hot-Melt Extrusion of Filaments based on Eudragit® RS, Ethyl Cellulose and Polyethylene Oxide 地塞米松在基于 Eudragit® RS、乙基纤维素和聚氧化乙烯的纤维热熔挤压过程中的稳定性

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-06-21 DOI: 10.1016/j.ijpx.2024.100263

Vanessa Domsta , Tessa Boralewski , Martin Ulbricht , Philipp Schick , Julius Krause , Anne Seidlitz

{"title":"Stability of Dexamethasone during Hot-Melt Extrusion of Filaments based on Eudragit® RS, Ethyl Cellulose and Polyethylene Oxide","authors":"Vanessa Domsta , Tessa Boralewski , Martin Ulbricht , Philipp Schick , Julius Krause , Anne Seidlitz","doi":"10.1016/j.ijpx.2024.100263","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100263","url":null,"abstract":"<div><p>Hot-melt extrusion (HME) potentially coupled with 3D printing is a promising technique for the manufacturing of dosage forms such as drug-eluting implants which might even be individually adapted to patient-specific anatomy. However, these manufacturing methods involve the risk of thermal degradation of incorporated drugs during processing. In this work, the stability of the anti-inflammatory drug dexamethasone (DEX) was studied during HME using the polymers Eudragit® RS, ethyl cellulose and polyethylene oxide. The extrusion process was performed at different temperatures. Furthermore, the influence of accelerated screw speed, the addition of the plasticizers triethyl citrate and polyethylene glycol 6000 or the addition of the antioxidants butylated hydroxytoluene and tocopherol in two concentrations were studied. The DEX recovery was analyzed by a high performance liquid chromatography method suitable for the detection of thermal degradation products. The strongest impact on the drug stability was found for the processing temperature, which was found to reduce the DEX recovery to <20% for certain processing conditions. In addition, differences between tested polymers were observed, whereas the use of additives did not result in remarkable changes in drug stability. In conclusion, suitable extrusion parameters were identified for the processing of DEX with high drug recovery rates for the tested polymers. Moreover, the importance of a suitable analysis method for drug stability during HME that is influenced by several parameters was highlighted.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":5.2,"publicationDate":"2024-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000355/pdfft?md5=86eb9e5d792d12eb03f1ea0a51f72309&pid=1-s2.0-S2590156724000355-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141484104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Transfer of a rational formulation and process development approach for 2D inks for pharmaceutical 2D and 3D printing 转让用于制药 2D 和 3D 印刷的 2D 油墨的合理配方和工艺开发方法

IF 4.7 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-06-01 DOI: 10.1016/j.ijpx.2024.100256

Maximilian Schulz , Malte Bogdahn , Simon Geissler , Julian Quodbach

{"title":"Transfer of a rational formulation and process development approach for 2D inks for pharmaceutical 2D and 3D printing","authors":"Maximilian Schulz , Malte Bogdahn , Simon Geissler , Julian Quodbach","doi":"10.1016/j.ijpx.2024.100256","DOIUrl":"10.1016/j.ijpx.2024.100256","url":null,"abstract":"<div><p>The field of pharmaceutical 3D printing is growing over the past year, with Spitam® as the first 3D printed dosage form on the market. Showing the suitability of a binder jetting process for dosage forms. Although the development of inks for pharmaceutical field is more trail and error based, focusing on the <em>Z</em>-number as key parameter to judge the printability of an ink. To generate a more knowledgeable based ink development an approach from electronics printing was transferred to the field of pharmaceutical binder jetting. Therefore, a dimensionless space was used to investigate the limits of printability for the used Spectra S Class SL-128 piezo print head using solvent based inks. The jettability of inks could now be judged based on the capillary and weber number. Addition of different polymers into the ink narrowed the printable space and showed, that the ink development purely based on <em>Z</em>-numbers is not suitable to predict printability. Two possible ink candidates were developed based on the droplet momentum which showed huge differences in process stability, indicating that the used polymer type and concentration has a high influence on printability and process stability. Based on the study a more knowledgeable based ink design for the field of pharmaceutical binder jetting is proposed, to shift the ink design to a more knowledgeable based and process-oriented approach.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":4.7,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000288/pdfft?md5=8189bb3651f8aa022855fda939db55c1&pid=1-s2.0-S2590156724000288-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141036333","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Trends in amorphous solid dispersion drug products approved by the U.S. Food and Drug Administration between 2012 and 2023 2012 年至 2023 年美国食品和药物管理局批准的无定形固体分散体药物产品趋势

IF 4.7 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-06-01 DOI: 10.1016/j.ijpx.2024.100259

Dana E. Moseson , Trong Bien Tran , Bharathi Karunakaran , Rohan Ambardekar , Tze Ning Hiew

{"title":"Trends in amorphous solid dispersion drug products approved by the U.S. Food and Drug Administration between 2012 and 2023","authors":"Dana E. Moseson , Trong Bien Tran , Bharathi Karunakaran , Rohan Ambardekar , Tze Ning Hiew","doi":"10.1016/j.ijpx.2024.100259","DOIUrl":"10.1016/j.ijpx.2024.100259","url":null,"abstract":"<div><p>Forty-eight (48) drug products (DPs) containing amorphous solid dispersions (ASDs) have been approved by the U.S. Food and Drug Administration in the 12-year period between 2012 and 2023. These DPs comprise 36 unique amorphous drugs. Ten (10) therapeutic categories are represented, with most DPs containing antiviral and antineoplastic agents. The most common ASD polymers are copovidone (49%) and hypromellose acetate succinate (30%), while spray drying (54%) and hot melt extrusion (35%) are the most utilized manufacturing processes to prepare the ASD drug product intermediate (DPI). Tablet dosage forms are the most common, with several capsule products available. Line extensions of several DPs based on flexible oral solids and powders for oral suspension have been approved which provide patient-centric dosing to pediatric and other patient populations. The trends in the use of common excipients and film coating types are discussed. Eighteen (18) DPs are fixed-dose combinations, and some contain a mixture of amorphous and crystalline drugs. The DPs have dose/unit of amorphous drug ranging from <5 mg up to 300 mg, with the majority being ≤100 mg/unit. This review details several aspects of DPI and DP formulation and manufacturing of ASDs, as well as trends related to therapeutic category, dose, and patient-centricity.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":4.7,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000318/pdfft?md5=6970bbea42716c149de74327651504e5&pid=1-s2.0-S2590156724000318-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141279019","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Research on the loading and release kinetics of the vincristine sulfate liposomes and its anti-breast cancer activity 硫酸长春新碱脂质体的负载和释放动力学及其抗乳腺癌活性研究

IF 4.7 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-06-01 DOI: 10.1016/j.ijpx.2024.100258

Zixu Liu , Yang Liu , Zixuan Wu , Boyuan Liu , Linxuan Zhao , Tian Yin , Yu Zhang , Haibing He , Jingxin Gou , Xing Tang , Song Gao

{"title":"Research on the loading and release kinetics of the vincristine sulfate liposomes and its anti-breast cancer activity","authors":"Zixu Liu , Yang Liu , Zixuan Wu , Boyuan Liu , Linxuan Zhao , Tian Yin , Yu Zhang , Haibing He , Jingxin Gou , Xing Tang , Song Gao","doi":"10.1016/j.ijpx.2024.100258","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100258","url":null,"abstract":"<div><p>Vincristine (VCR), as a cytotoxic drug, is used clinically to treat acute lymphatic leukemia and breast cancer, and commonly used clinically as vincristine sulfate (VCRS). However, its clinical use is limited by unpredictable pharmacologic characteristics, a narrow therapeutic index, and neurotoxicity. The pH gradient method was used for active drug loading of VCRS, and the process route mainly includes the preparation of blank liposomes and drug-loaded liposomes. VCRS liposomes had suitable particle size, high encapsulation efficiency and good stability. The loading and release kinetics of VCRS liposomes were explored. By calculating the changes of encapsulation efficiency with time at different temperatures, it was confirmed that the drug-loading process of liposomes exhibited a first-order kinetic feature, and the activation energy required for the reaction was determined as 20.6 kcal/mol. The release behavior at different pH was also investigated, and it was demonstrated that the release behavior conformed to the first-order model, suggesting that the release mechanism of VCRS was simple transmembrane diffusion. VCRS liposomes also enhanced <em>in vitro</em> and <em>in vivo</em> antitumor activity. Thus, VCRS liposomes showed great potential for VCRS delivery, and the loading and release kinetics were well researched to provide a reference for investigating active drug loading liposomes.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":4.7,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000306/pdfft?md5=47b1a3d1b7a20ebacd9cca1514244fce&pid=1-s2.0-S2590156724000306-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141240443","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

QbD-guided phospholipid-tagged nanonized boswellic acid naturosomal delivery for effective rheumatoid arthritis treatment QbD 引导下的磷脂标记纳米化乳香酸纳豆体递送技术用于类风湿性关节炎的有效治疗

IF 4.7 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-05-19 DOI: 10.1016/j.ijpx.2024.100257

Poonam Usapkar , Suprit Saoji , Pradnya Jagtap , Muniappan Ayyanar , Mohan Kalaskar , Nilambari Gurav , Sameer Nadaf , Satyendra Prasad , Damiki Laloo , Mohd Shahnawaz Khan , Rupesh Chikhale , Shailendra Gurav

{"title":"QbD-guided phospholipid-tagged nanonized boswellic acid naturosomal delivery for effective rheumatoid arthritis treatment","authors":"Poonam Usapkar , Suprit Saoji , Pradnya Jagtap , Muniappan Ayyanar , Mohan Kalaskar , Nilambari Gurav , Sameer Nadaf , Satyendra Prasad , Damiki Laloo , Mohd Shahnawaz Khan , Rupesh Chikhale , Shailendra Gurav","doi":"10.1016/j.ijpx.2024.100257","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100257","url":null,"abstract":"<div><p>Studies have reported the potential role of Boswellic acids (BAs), bioactive pentacyclic triterpenes from <em>Boswellia serrata</em> (BS), in treating rheumatoid arthritis (RA). However, poor water solubility and limited oral absorption are restricting factors for its better therapeutic efficacy. Based on these assumptions, the current study aimed to develop naturosomal delivery of BAs to boost their extremely low bioavailability, colloidal stability, and water solubility. Nanonized naturosomes were developed and subsequently analyzed to show their physicochemical and functional features employing the quality-by-design approach. The solubility analysis of Boswellic acid naturosomes revealed a 16 times improvement in aqueous solubility compared to BS extract (BSE). The zeta potential and dynamic light scattering findings of BSE naturosomes (BSENs) have demonstrated their colloidal stability with regulated nano-size particles. Additionally, compared to BSE (⁓31%), <em>in-vitro</em> dissolution experiments showed that >99% of pentacyclic triterpenes were released from BSENs. Studies on <em>ex-vivo</em> permeation showed that BSENs' permeation (>79%) significantly improved over BSE's (⁓20%). <em>In-vivo</em> efficacy studies using CFA-prompted arthritis in rodents showed a critical expansion in body wt and an undeniable reduction in paw thickness, paw volume, and TNF-α treated with BSEN compared to the arthritis control and BSE-treated group. These findings suggest that BSENs can help treat RA drugs by demonstrating their efficacy in further clinical research to validate the significant improvements.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":4.7,"publicationDate":"2024-05-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S259015672400029X/pdfft?md5=c608a4a20a497fda980471a23e56bd44&pid=1-s2.0-S259015672400029X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141078184","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

RP-HPLC-CAD method for the rapid analysis of lipids used in lipid nanoparticles derived from dual centrifugation 采用 RP-HPLC-CAD 方法快速分析双离心法制备的纳米脂质颗粒中使用的脂质

IF 4.7 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-05-04 DOI: 10.1016/j.ijpx.2024.100255

Valentin Bender, Leon Fuchs, Regine Süss

{"title":"RP-HPLC-CAD method for the rapid analysis of lipids used in lipid nanoparticles derived from dual centrifugation","authors":"Valentin Bender, Leon Fuchs, Regine Süss","doi":"10.1016/j.ijpx.2024.100255","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100255","url":null,"abstract":"<div><p>The use of lipids as suitable excipients for drug carrier systems has been established for years. Liposomes or lipid nanoparticles (LNPs) in general have been shown capable of delivering both hydrophilic and hydrophobic drugs. The Covid-19 pandemic and the resulting vaccines have significantly increased interest in the potential for these lipid-based systems, which can carry different types of therapeutic RNAs. LNPs used for the transfection of RNA are usually a multi-component mixture of phospholipids and other lipids. Essential components are positively charged or ionizable lipids such as DOTAP or SM-102, but also uncharged helper lipids such as cholesterol, DOPE, DSPC, DMG-PEG<sub>2000</sub> or DSPE-PEG<sub>2000</sub>. Due to the differences in charge, simultaneous detection is a challenge. Here, we present a reversed-phase high-performance liquid chromatography charged-aerosol-detector method (RP-HPLC-CAD method) using a C-18 column for the simultaneous determination of charged and uncharged lipids. Our method has been validated according to the ICH-Q2 (R2) guideline for accuracy, precision, specificity and working range, including the limit of detection (LOD) and quantification (LOQ), as well as the calibration range. We were able to show satisfactory results in both precision and accuracy. The working range also shows great potential with a calibration range from 9.375 to 1000 μg/ml, LODs <1.85 μg/ml and LOQs <6.16 μg/ml. This method represents a fast and reproducible procedure for quantifying the lipids mentioned. In combination with the novel approach for the production of LNPs using dual centrifugation (DC), it offers the possibility of extremely rapid production of RNA-loaded LNPs, and the immediate analysis for their lipid components.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":null,"pages":null},"PeriodicalIF":4.7,"publicationDate":"2024-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000276/pdfft?md5=f7f09777fb062085e5bd0e1adbdcb8d5&pid=1-s2.0-S2590156724000276-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140894524","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Evaluation of gender differences in the pharmacokinetics of oral zileuton nanocrystalline formulation using a rat model 利用大鼠模型评估齐来顿纳米晶体口服制剂药代动力学的性别差异

IF 4.7 2区医学

International Journal of Pharmaceutics: X Pub Date : 2024-05-04 DOI: 10.1016/j.ijpx.2024.100254

Chandra Mohan Reddy Muthumula , Sangeeta Khare , Rajan Jog , Bhagya Wickramaratne , Angela Lee , Sushanta Chakder , Diane J. Burgess , Kuppan Gokulan

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