International Journal of Pharmaceutics最新文献

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Opensource semi-solid 3D printer designed for oral drug production in hospital pharmacies 开源半固态3D打印机,专为医院药房的口服药物生产而设计
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-24 DOI: 10.1016/j.ijpharm.2025.125998
François Rioblanc , Baptiste Heumel , Daniel Alloh Nammou , Julie Roupret-Serzec , Patrick Saulnier , Sylvie Crauste-Manciet , Thomas Storme
{"title":"Opensource semi-solid 3D printer designed for oral drug production in hospital pharmacies","authors":"François Rioblanc ,&nbsp;Baptiste Heumel ,&nbsp;Daniel Alloh Nammou ,&nbsp;Julie Roupret-Serzec ,&nbsp;Patrick Saulnier ,&nbsp;Sylvie Crauste-Manciet ,&nbsp;Thomas Storme","doi":"10.1016/j.ijpharm.2025.125998","DOIUrl":"10.1016/j.ijpharm.2025.125998","url":null,"abstract":"<div><div>Three-dimensional (3D) printing is a manufacturing technique with a growing interest in drug production, especially via semi-solid extrusion (SSE) where a material lying between a solid and a liquid is deposited to create the desired form. However, accessibility to SSE 3D printer is limited. This study aimed to develop and validate a SSE 3D printer equipped with an in-process weighing system. As a proof-of-concept, vaseline and low acyl gellan gum containing levetiracetam (LVT) were used to validate the developed SSE 3D printer. The developed printer heated the content of 20 mL syringes to the desired temperature within 20 min. The weighing system was able to weigh the printlets continuously during 3D printing with a deviation of 0.3 to 0.5 % compared with an external analytical balance. The 3D printer produced vaseline printlets with a proportionality between mass and volume (R<sup>2</sup> 0.9954) and with repeatability over 3 days (RSD 1,5%). It was able to produce 30 LVT printlets complying with the European Pharmacopeia for content uniformity (EP 2.9.40) with an average content of 143.9 mg (RSD 1.2 %) and an acceptance value of 5.7. This customizable and affordable SSE 3D printer with its own local network is promising for the democratization of personalized medicine in hospital pharmacies.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125998"},"PeriodicalIF":5.3,"publicationDate":"2025-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144714110","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}
引用次数: 0
Complex investigation of the effect mechanism of polyvinylpyrrolidone in the additive-assisted crystallization of famotidine 聚乙烯吡咯烷酮在法莫替丁助剂结晶过程中作用机理的复杂研究
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-24 DOI: 10.1016/j.ijpharm.2025.125994
György Nimród Stoffán , Tibor Höltzl , Zsolt Lőrincz , Éva Pusztai , Kornélia Tacsi , Attila Farkas , György János Marosi , Zsombor Kristóf Nagy , Hajnalka Pataki
{"title":"Complex investigation of the effect mechanism of polyvinylpyrrolidone in the additive-assisted crystallization of famotidine","authors":"György Nimród Stoffán ,&nbsp;Tibor Höltzl ,&nbsp;Zsolt Lőrincz ,&nbsp;Éva Pusztai ,&nbsp;Kornélia Tacsi ,&nbsp;Attila Farkas ,&nbsp;György János Marosi ,&nbsp;Zsombor Kristóf Nagy ,&nbsp;Hajnalka Pataki","doi":"10.1016/j.ijpharm.2025.125994","DOIUrl":"10.1016/j.ijpharm.2025.125994","url":null,"abstract":"<div><div>Utilizing the positive impact of additives, including pharmaceutical excipients, to achieve favorable crystal morphology and polymorphism is a widely researched area. Despite the obvious benefits of additive-assisted crystallization, the quantification of process parameter influences on the effect mechanism of additives is usually discussed only from a nucleation inhibition point of view or focusing on technological feasibility. Accordingly, the relevant literature can be divided into technological and mechanism studies, but it lacks a complex combined approach. However, to develop robust crystallization procedures, the systematic analysis of process conditions is essential. Thus, understanding the molecular-scale effect mechanism is also crucial to designing these complex processes. Therefore, in this work, the effect of a pharmaceutical binder, poly(vinyl pyrrolidone) (PVP), and several process parameters were investigated on the nucleation of famotidine (FMT), an antihistamine, both experimentally and theoretically. To systematically investigate the effect of PVP concentration, temperature, and supersaturation, we applied the Design of Experiment (DoE) methodology combined with a camera-aided analytical set-up. Based on the experimental data, the nucleation rate of FMT was studied according to the Classical Nucleation Theory (CNT). Finally, molecular simulations were conducted, and a possible effect mechanism was suggested for the PVP-effected nucleation of FMT. This way, the complex DoE-based process parameter investigation and molecular scale interpretation of these effects is a novel approach of the subject. The experimental results revealed that the nucleation inhibiting effect of PVP is dependent on the set temperature, while increasing FMT concentration generally counterforces it. Based on the CNT calculations, PVP decreased the nucleation rate of FMT by orders of magnitude. Additionally, molecular modelling suggests the effect mechanism of PVP is manifested through H-bonding and steric hindrance.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125994"},"PeriodicalIF":5.3,"publicationDate":"2025-07-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144714109","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}
引用次数: 0
Development and application of an AI-empowered acoustic monitoring system for misuse detection in dry powder inhalers 用于干粉吸入器误用检测的人工智能声学监测系统的开发和应用
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-23 DOI: 10.1016/j.ijpharm.2025.125997
Ziyi Fan , Yuqing Ye , Jiale Chen , Ying Ma , Jesse Zhu
{"title":"Development and application of an AI-empowered acoustic monitoring system for misuse detection in dry powder inhalers","authors":"Ziyi Fan ,&nbsp;Yuqing Ye ,&nbsp;Jiale Chen ,&nbsp;Ying Ma ,&nbsp;Jesse Zhu","doi":"10.1016/j.ijpharm.2025.125997","DOIUrl":"10.1016/j.ijpharm.2025.125997","url":null,"abstract":"<div><div>Misuse and poor inhalation techniques remain persistent issues in pulmonary drug delivery via dry powder inhalation. While acoustic-based monitoring has been a feasible strategy, existing approaches often depend on smartphones for signal collection, or wired connections for data transmission, limiting their scalability and practicality in real-world settings. More importantly, few studies have specifically focused on the detection of incorrect DPI usage via digital monitoring systems, and current methods still face limitations in accuracy. Therefore, in this study, an AI-empowered acoustic monitoring system was developed, combining edge sensing and cloud analytics to support continuous signal acquisition and misuse detection. Comprehensive featuring engineering and machine learning analysis have been performed to investigate their influence on inhalation activity recognition. The results suggested that feature fusion could significantly enhance classification performance, with the Support Vector Classifier (SVC) showing 99.5 % overall accuracy during cross-validation and 100% accuracy on the test set, along with rapid training and high stability. This proposed digital system achieves a near-perfect categorization on the inhalation-related events, and effectively detects unexpected exhalation into inhalers, showing strong potential in real-life applications for improved respiratory disease management.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125997"},"PeriodicalIF":5.3,"publicationDate":"2025-07-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144714181","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}
引用次数: 0
Dynamics of insertion and extraction of hollow pyramidal microneedles: experiments and numerical modelling 空心锥体微针的插拔动力学:实验与数值模拟
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-22 DOI: 10.1016/j.ijpharm.2025.125989
Rahul Nadda , Diganta Bhusan Das , Tahir Emre Yalcin , Abraham M. Abraham , Eneko Larrañeta , Ryan F. Donnelly
{"title":"Dynamics of insertion and extraction of hollow pyramidal microneedles: experiments and numerical modelling","authors":"Rahul Nadda ,&nbsp;Diganta Bhusan Das ,&nbsp;Tahir Emre Yalcin ,&nbsp;Abraham M. Abraham ,&nbsp;Eneko Larrañeta ,&nbsp;Ryan F. Donnelly","doi":"10.1016/j.ijpharm.2025.125989","DOIUrl":"10.1016/j.ijpharm.2025.125989","url":null,"abstract":"<div><div>The present study aimed to investigate the dynamics of HMNs’ insertion and extraction utilising HMN fabrication, laboratory experiments and numerical simulations. In particular, the study aims to develop an experimentally validated mathematical model to investigate the mechanics of the insertion and extraction of hollow pyramidal MNs, considering the nonlinear material behaviour of HMNs and skin. This study reveals good consistency between the experimental and computational results, providing confidence on the validity of the developed mathematical model. The model was then used to conduct detailed numerical simulations of the insertion and extraction of hollow pyramidal MN within a multi-layered skin model under different conditions, allowing us to assess the impacts of several key parameters (e.g., the base radius, length, and tip radius of HMNs) on the insertion and extractions dynamics of the HMNs. Overall, the findings of this paper indicate that HMN length &lt;600 µm, base diameter &lt;300 µm, tip diameter &lt;30 µm, needle spacing &gt;800 µm, and number of HMNs &lt;9 can significantly lower the forces required for insertion and extraction for the chosen pyramidal MN, while maintaining their mechanical and structural integrity.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125989"},"PeriodicalIF":5.3,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144703950","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}
引用次数: 0
Developing, fabrication and functionalization of soy bioactive peptides-nano particles therapeutic nano composites: A review 大豆生物活性肽-纳米颗粒治疗性纳米复合材料的开发、制备及功能化研究进展。
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-22 DOI: 10.1016/j.ijpharm.2025.125983
Khalid Amin , Jiaxin Li , Bo Lyu , Sainan Wang , Hongling Fu , Bin Liu , Hansong Yu
{"title":"Developing, fabrication and functionalization of soy bioactive peptides-nano particles therapeutic nano composites: A review","authors":"Khalid Amin ,&nbsp;Jiaxin Li ,&nbsp;Bo Lyu ,&nbsp;Sainan Wang ,&nbsp;Hongling Fu ,&nbsp;Bin Liu ,&nbsp;Hansong Yu","doi":"10.1016/j.ijpharm.2025.125983","DOIUrl":"10.1016/j.ijpharm.2025.125983","url":null,"abstract":"<div><div>Nanoparticles (NPs) therapeutics has emerged as advanced systems for personalized therapeutics. However, they encounter several obstacles in attaining exact specificity and sensitivity for disease therapies. Therefore, the development of NPs with novel approaches is critically important to improve their therapeutic efficacy. One intellectual approach is assembling and compositing them with active biomaterials like smart disease targeting peptides. Bioactive peptides derived from soybeans, are reported to involve in several physiological functions like reducing chronic diseases such as cancer, cardiovascular disease (CVD) obesity, insulin-resistance/type II diabetes, immune disorders and inflammatory diseases. Therefore, the conjugation of soy bioactive peptides with nanoparticles is a promising strategy towards engineered therapeutic nano systems. However, these conjugates of soy peptides-nanoparticles composites (SPNCs) are highly under considered. Engineered nanoparticles with peptides, captured attention as innovative therapeutic platforms. Consequently, SPNCs engineered nanostructure, have the high potential for future therapeutics as their composite/hybrid features of therapeutic NPs and soy bioactive peptides, can not only enhance their therapeutic behaviors but also can resolve their challenges they face as an individual. In this review for the first time, multimodal SPNCs with acclaimed therapeutic abilities are discussed which set a foundational understanding for the future nanotherapeutics. The foundational details of soy peptides, NPs and their chemistries and corresponding interactions with disease modes are discussed. Finally, precise guidelines for accuracy techniques to engineer SPNCs with efficient therapeutic abilities are explored. This study established the groundwork for advancement of composite soy bioactive peptides with NPs to achieve therapeutic SPNCs with high target specific abilities.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125983"},"PeriodicalIF":5.3,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144707441","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}
引用次数: 0
Corrigendum to “Transethosomal system for enhanced transdermal delivery and therapeutic effect of caryophyllene oxide” [Int. J. Pharm. 670 (2024) 125111] “经囊体系统增强氧化石竹烯的经皮传递和治疗效果”的勘误表[Int.]。[j]中华医学杂志,2016,32(5):1251 - 1251。
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-22 DOI: 10.1016/j.ijpharm.2025.125904
Hiba Natsheh , Mohammad Qneibi , Naim Kittana , Nidal Jaradat , Mohyeddin Assali , Bahaa Shaqour , Murad Abualhasan , Abdallatif Mayyala , Yaqeen Dawoud , Tala Melhem , Sawsan Abd Alhadi , Osama Hammoudi , Abdullah Samaro , Ahmed Mousa , Sosana Bdir , Mohammad Bdair , Samia Aldwaik
{"title":"Corrigendum to “Transethosomal system for enhanced transdermal delivery and therapeutic effect of caryophyllene oxide” [Int. J. Pharm. 670 (2024) 125111]","authors":"Hiba Natsheh ,&nbsp;Mohammad Qneibi ,&nbsp;Naim Kittana ,&nbsp;Nidal Jaradat ,&nbsp;Mohyeddin Assali ,&nbsp;Bahaa Shaqour ,&nbsp;Murad Abualhasan ,&nbsp;Abdallatif Mayyala ,&nbsp;Yaqeen Dawoud ,&nbsp;Tala Melhem ,&nbsp;Sawsan Abd Alhadi ,&nbsp;Osama Hammoudi ,&nbsp;Abdullah Samaro ,&nbsp;Ahmed Mousa ,&nbsp;Sosana Bdir ,&nbsp;Mohammad Bdair ,&nbsp;Samia Aldwaik","doi":"10.1016/j.ijpharm.2025.125904","DOIUrl":"10.1016/j.ijpharm.2025.125904","url":null,"abstract":"","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125904"},"PeriodicalIF":5.3,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144686576","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}
引用次数: 0
In-line Raman-based quantification of the anhydrous content in a fully integrated continuous powder-to-granule line 在完全集成的连续粉末到颗粒线中,基于拉曼的在线无水含量定量
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-22 DOI: 10.1016/j.ijpharm.2025.125995
Petra Záhonyi, Dániel Fekete, Erzsébet Moharos, Zsombor Kristóf Nagy, Edina Szabó
{"title":"In-line Raman-based quantification of the anhydrous content in a fully integrated continuous powder-to-granule line","authors":"Petra Záhonyi,&nbsp;Dániel Fekete,&nbsp;Erzsébet Moharos,&nbsp;Zsombor Kristóf Nagy,&nbsp;Edina Szabó","doi":"10.1016/j.ijpharm.2025.125995","DOIUrl":"10.1016/j.ijpharm.2025.125995","url":null,"abstract":"<div><div>This research is based on a fully integrated continuous twin-screw wet granulation line from powder feeding to dried granules. One of its crucial steps is continuous drying, which can influence the crystal form and thus, the quality of the granules. Therefore, the main objective of this research was to develop a Raman spectroscopic method for monitoring the crystal form transition in-line and real-time during the continuous process while applying different drying temperatures. Dextrose was used as a model material due to its high industrial relevance as an active pharmaceutical ingredient and excipient. The real-time monitoring of the granules’ crystal form demonstrated that drying at higher temperatures (100 °C and 120 °C) resulted in partial dehydration of the initial <em>α</em>-<span>d</span>-glucose monohydrate. Raman spectroscopy combined with multivariate data analysis proved suitable for real-time quantification of anhydrous content with a root mean square error of 3.3 % w/w. The results were validated by various conventional, off-line analytical techniques, which further confirmed the reliability of the model and the detected anhydrous content. This work shows the high predictive performance of Raman spectroscopy for in-line and real-time anhydrous content monitoring in a fully integrated continuous powder-to-granule line, enhancing process understanding and ensuring high and consistent product quality.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125995"},"PeriodicalIF":5.3,"publicationDate":"2025-07-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144695125","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}
引用次数: 0
Ascorbyl palmitate/hyaluronan-modified poloxamer 407 nanoparticles for the topical delivery of fisetin to counteract UVB-induced skin photoaging: A novel anti-aging formulation 抗坏血酸棕榈酸酯/透明质酸修饰的poloxamer 407纳米颗粒用于局部递送非瑟汀以对抗uvb诱导的皮肤光老化:一种新的抗衰老配方
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-21 DOI: 10.1016/j.ijpharm.2025.125988
Asmaa H. Elwan , Soha M. El-Masry , Doaa A. Habib , Mariam Zewail
{"title":"Ascorbyl palmitate/hyaluronan-modified poloxamer 407 nanoparticles for the topical delivery of fisetin to counteract UVB-induced skin photoaging: A novel anti-aging formulation","authors":"Asmaa H. Elwan ,&nbsp;Soha M. El-Masry ,&nbsp;Doaa A. Habib ,&nbsp;Mariam Zewail","doi":"10.1016/j.ijpharm.2025.125988","DOIUrl":"10.1016/j.ijpharm.2025.125988","url":null,"abstract":"<div><div>Fisetin (FIS) has recently been the focal point of multiple studies. Yet, its skin delivery has not been fully investigated due to its low aqueous solubility and high lipophilicity. Herein, FIS-loaded Poloxamer 407 (P407) nanoparticles were modified with Ascorbyl Palmitate (AS) and Hyaluronan (HYA), providing a multimodal approach to preventing UVB-induced skin photoaging. Optimal FIS-AS-HYA-P407 nanoparticles demonstrated a particle size of 214.10 ± 0.32 nm with a zeta potential of −16 ± 0.83 mV, a high entrapment efficiency of 95.61 ± 0.52 %, and a sustained release reaching 68.05 ± 3.32 % over 24 h. FT-IR and DSC confirmed the formation of the nanoparticles and the compatibility of the components. FIS-AS-HYA-P407 nanoparticles penetrated the skin with a flux of 9.23 ± 0.59 µg/cm<sup>2</sup>/h in 8 h. Confocal microscopy proved the skin penetration of the nanoparticles up to 80 µm with high FIS distribution. The nanoparticles were biocompatible due to the lack of irritation and exhibited potent <em>in vitro</em> antioxidant effects, as confirmed by the DPPH assay. The <em>in vivo</em> study on Wistar rats demonstrated the photoprotective ability of FIS-AS-HYA-P407 nanoparticles via reducing TNFα, NF-κB, and MMP9 and elevating SOD and CAT levels, showing remarkable anti-inflammatory, anti-aging, and antioxidant potential. JNK protein expression was reduced in skin samples pretreated with FIS-AS-HYA-P407 nanoparticles compared to FIS suspension, signifying a high photoprotective outcome. The novelty of this work is attributed to the formulation of FIS for the first time with HYA and AS in P407 nanoparticles to counteract UVB skin damage and photoaging.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125988"},"PeriodicalIF":5.3,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144695127","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}
引用次数: 0
Design of paclitaxel-loaded PLGA nanoparticles assisted by compatibility modeling 相容性建模辅助下紫杉醇负载PLGA纳米颗粒的设计。
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-21 DOI: 10.1016/j.ijpharm.2025.125985
Alžběta Zemánková , Anton Iemtsev , Martin Dinh , Alma Lucia Villela Zumaya , Vladimíra Svobodová Pavlíčková , Silvie Rimpelová , Barbora Vokatá , Fatima Hassouna , Michal Fulem
{"title":"Design of paclitaxel-loaded PLGA nanoparticles assisted by compatibility modeling","authors":"Alžběta Zemánková ,&nbsp;Anton Iemtsev ,&nbsp;Martin Dinh ,&nbsp;Alma Lucia Villela Zumaya ,&nbsp;Vladimíra Svobodová Pavlíčková ,&nbsp;Silvie Rimpelová ,&nbsp;Barbora Vokatá ,&nbsp;Fatima Hassouna ,&nbsp;Michal Fulem","doi":"10.1016/j.ijpharm.2025.125985","DOIUrl":"10.1016/j.ijpharm.2025.125985","url":null,"abstract":"<div><div>Many anticancer active pharmaceutical ingredients (APIs), such as paclitaxel (PTX), exhibit poor water solubility, which limits their bioavailability and necessitates the use of excipients. While biodegradable polymeric excipients combined with nanotechnology offer promising solutions, the high cost of polymers and APIs, along with the vast number of potential API–polymer combinations, poses significant challenges in developing effective drug delivery systems (DDS). This study explores the potential of API–polymer phase behavior modeling as part of the design of nanoparticle (NP)-based DDS for PTX using poly(lactide-<em>co</em>-glycolide) (PLGA) and poly(lactide-<em>co</em>-glycolide)-b-poly(ethylene glycol) (PLGA-PEG) with varying molecular weights. The phase behavior of PTX–PLGA/PLGA-PEG systems, which reflects the compatibility of PTX with polymeric excipients, was predicted using the Conductor-like Screening Model for Real Solvents (COSMO-RS). To investigate the correlation between the predictions and experimental observations, PTX–PLGA and PEGylated PLGA NPs were prepared via an emulsion-solvent evaporation method with varying initial PTX amounts. The predicted trends in PTX solubility in polymeric excipients were then compared with key NP characteristics, such as drug loading, solid-state properties, and cytotoxicity in HeLa, SKOV-3, and MRC-5 cells. COSMO-RS predictions indicated limited PTX solubility in PLGA, which aligns with experimental observations, where the maximum amorphous PTX loading did not exceed 2 wt%, regardless of the polymer molecular weight. COSMO-RS modeling predicted higher compatibility of PTX with PEG, suggesting that incorporating PEG would enhance PTX loading in PEGylated NPs. This trend was corroborated by experimental findings, which showed increased drug loading capacity and slower PTX release from PEGylated NPs during cytotoxicity studies. These results highlight the potential of API–polymer modeling as a tool for tailoring polymeric carriers and optimizing API consumption in NP-based DDS development.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125985"},"PeriodicalIF":5.3,"publicationDate":"2025-07-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144698493","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}
引用次数: 0
Pioglitazone/Curcumin co-loaded TPGS-functionalized nanocarriers: an auspicious repurposed therapeutic advance targeting lung and breast carcinoma 吡格列酮/姜黄素共载tpgs功能化纳米载体:一种针对肺癌和乳腺癌的治疗进展
IF 5.3 2区 医学
International Journal of Pharmaceutics Pub Date : 2025-07-20 DOI: 10.1016/j.ijpharm.2025.125991
Shaymaa Elsayed Khater , Riham A. El-Shiekh , Essam Abdel-Sattar , Jihad Mahmoud Alsofany
{"title":"Pioglitazone/Curcumin co-loaded TPGS-functionalized nanocarriers: an auspicious repurposed therapeutic advance targeting lung and breast carcinoma","authors":"Shaymaa Elsayed Khater ,&nbsp;Riham A. El-Shiekh ,&nbsp;Essam Abdel-Sattar ,&nbsp;Jihad Mahmoud Alsofany","doi":"10.1016/j.ijpharm.2025.125991","DOIUrl":"10.1016/j.ijpharm.2025.125991","url":null,"abstract":"<div><div>This work aims to fabricate D-alpha-tocopheryl polyethylene glycol succinate 1000 (TPGS)-coated bilosomes co-loaded with pioglitazone hydrochloride (PG) and curcumin (CR) to attain a synergistic anticancer activity against the lung and breast cancers cells. PG is a glucose-lowering drug that can disrupt the cancer cell metabolism, while CR is a natural anticancer compound. The bilosomes were first developed and optimized, then coated with TPGS, and finally characterized for their vesicle size (VS), zeta potential (ZP), encapsulation efficiencies (EE), morphological characters, in vitro release patterns, and cytotoxicity and cellular uptake studies on lung (A549) and breast (MCF7) cancer cell lines. The optimized uncoated bilosomes formula demonstrated a VS of 305.5 ± 2.5 nm, ZP of −46.4 ± 1.5 mV, and EE of 85.3 % ± 2.1 and 82.1 % ± 2.3 for CR and PG, respectively, compared to its TPGS-coated-formulation that had a VS of 353.2 ± 3.1 nm, ZP of −55.3 ± 2.5 mV, and EE of 82.4 % ± 2.1 and 80.5 % ± 1.3 for CR and PG, respectively. The optimized TPGS-coated bilosomes encapsulated amorphous drugs without any interactions between them and other formulation excipients. Moreover, it demonstrated a controlled release pattern for both CR and PG and showed 65.5 % ± 2.6 and 60.65 % ± 2.7 release in phosphate-buffer saline (pH 5.5) within 24 h, respectively. Furthermore, the TPGS coating of bilosomes enhanced their cellular uptake over time and amplified their cytotoxicity as it achieved combination indices of 0.89 and 0.73 on lung and breast cancer cell lines, respectively, compared to the free drugs solution. Accordingly, this study points out a propitious repurposed therapeutic approach of PG/CR combination against lung (A549) and breast (MCF7) cancer cells.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":"682 ","pages":"Article 125991"},"PeriodicalIF":5.3,"publicationDate":"2025-07-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144678813","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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