European Journal of Pharmaceutics and Biopharmaceutics最新文献

{"title":"Patches containing quercetin microcapsules to ameliorate dermal herpes simplex virus injuries in mice","authors":"Jéssica Bassetto Carra ,&nbsp;Maria Laura Goussain Darido ,&nbsp;Camila Felix Vecchi ,&nbsp;Mariana Carla de Oliveira ,&nbsp;Ricardo Luís Nascimento de Matos ,&nbsp;Pietra Mitiko Tateyama Pattini ,&nbsp;Bianca Larissa Masquetti ,&nbsp;Beatriz da Silva Tavares ,&nbsp;Marcos Luciano Bruschi ,&nbsp;Ana Paula Frederico Rodrigues Loureiro Bracarense ,&nbsp;Renê Oliveira do Couto ,&nbsp;Rubia Casagrande ,&nbsp;Sandra Regina Georgetti ,&nbsp;Waldiceu A. Verri Jr ,&nbsp;Ligia Carla Faccin Faccin-Galhardi ,&nbsp;Marcela Maria Baracat","doi":"10.1016/j.ejpb.2025.114631","DOIUrl":"10.1016/j.ejpb.2025.114631","url":null,"abstract":"<div><div>This study aimed to develop patches containing quercetin-loaded microcapsules and to evaluate their <em>in vitro</em> and <em>in vivo</em> safety and efficacy in preclinical surveys. A set of <em>in vitro</em> experiments evidenced the virucidal activity of quercetin against the HSV-1-KOS (sensitive to acyclovir) and HSV-1-AR (resistant to acyclovir) strains, with improved outcomes upon the first. The patches presented a homogeneous aspect, were easily handled, had a suitable bioadhesion, and possessed mechanical properties of soft and weak material, besides a pH compatible with human skin. The <em>in vitro</em> release profile of quercetin showed an initial burst release, followed by a controlled release rate, which was best described by Gompertz kinetics (R² of 0.93). Using quercetin-loaded patches for treating HSV-1-KOS-induced injuries was feasible since they were well tolerated in the <em>in vivo</em> skin irritation test and significantly decreased the injury scores until the fourth out of eight days of treatment in mice compared to acyclovir cream (50 mg/g). Altogether, the <em>in vitro</em> and <em>in vivo</em> antiviral assays indicate that this flavonol acts in the earlier stage of the infection, likely impairing the HSV-1 adsorption to the cell. The anti-inflammatory capacity of the quercetin-loaded patches was noteworthy as evidenced by histological analysis. These findings bring prospects for safer and more effective management of mucocutaneous HSV-1 injuries.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114631"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142982938","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}

{"title":"Development and characterization of pH-sensitive zerumbone-encapsulated liposomes for lung fibrosis via inhalation route","authors":"Nourhan Elsayed ,&nbsp;Chee Wun How ,&nbsp;Jhi Biau Foo","doi":"10.1016/j.ejpb.2024.114599","DOIUrl":"10.1016/j.ejpb.2024.114599","url":null,"abstract":"<div><div>Zerumbone (ZER), a compound derived from the rhizome of Zingiber Zerumbet (L.) Smith, has demonstrated anti-inflammatory properties but suffers from poor water solubility, limiting its clinical application. While ZER’s effects on lung inflammation are known, its role in lung fibrosis remains unexplored. Herein, ZER was encapsulated in pH-sensitive liposomes formulated with oleic acid, dipalmitoylphosphatidylcholine, and cholesterol to enhance ZER solubility and delivery to the acidic environment of lung fibrosis. The liposomes were optimized using Box-Behnken design, resulting in an average diameter of 87.8 ± 3.5 nm, a polydispersity index of 0.16 ± 0.2, and a zeta potential of −24 ± 0.32 mV. ZER release from the carrier followed zero-order kinetics and showed higher release in acidic settings. Cascade impactor and HPLC analyses confirmed that ZER liposome powder produced by freeze-drying reached stage 7, indicating effective delivery to deep lung regions. The uptake of ZER liposomes was concentration and pH-dependent, being higher in acidic conditions and greater in MRC-5 cells compared to A549 cells. Notably, ZER liposomes reduced cell migration and downregulated fibrotic markers such as fibronectin, MMP-2, and α-SMA in MRC-5 and A549 cells. This study suggests that ZER liposomes hold promise for treating lung fibrosis and merit further investigation.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114599"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142767337","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}

{"title":"Vaporized Hydrogen Peroxide Uptake by Tubing used for Aseptic Fill-Finish Manufacturing of Biopharmaceutical Drug Products","authors":"Dilara Ali ,&nbsp;Sarah S. Peláez ,&nbsp;Thomas Lemazurier ,&nbsp;Ariane Schroeter ,&nbsp;Michael Adler ,&nbsp;JaeHwi Bong ,&nbsp;Oliver Germershaus ,&nbsp;Hanns-Christian Mahler ,&nbsp;Andrea Allmendinger","doi":"10.1016/j.ejpb.2024.114618","DOIUrl":"10.1016/j.ejpb.2024.114618","url":null,"abstract":"<div><div>Aseptic filling of biopharmaceutical products requires a grade A cleanroom environment, preferably ensured by isolators in grade C surroundings. Isolators are decontaminated before the start of filling processes using vaporized hydrogen peroxide (VHP) and filling starts at pre-defined residual VHP levels (e.g., below 0.5 ppm) depending on product sensitivity towards VHP oxidation. Manufacturing equipment and consumables, including filling assemblies, are exposed to VHP during or after the decontamination cycle or after line interruptions. We studied the VHP uptake by tubing in a lab-scale model isolator to evaluate the impact of tubing properties including contact material, tubing dimensions, suppliers, and VHP exposure (concentration and exposure time). Quantifying the release of H₂O₂ from the tubing into solution using an Amplex Red Hydrogen Peroxide Assay, showed that H₂O₂ concentrations decreased linearly with an increase in wall thickness and increased with higher surface to volume ratio. We further conclude that thermoplastic elastomer and thermoplastic vulcanizate tubing did not show any measurable VHP uptake for the tested conditions, whereas significant VHP uptake occurred in different platinum cured silicone tubing depending on tubing material and supplier. We further verified the results in a GMP manufacturing isolator setting. Based on our findings, we recommend to evaluate VHP uptake of filling tubing used for fill-finish manufacturing in isolators, to reduce the risk of oxidation for active pharmaceutical ingredients or excipients.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114618"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142885478","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}

{"title":"Does needle clogging change the spatial distribution of injected drug in tissue? New insights by X-ray computed tomography","authors":"Fabiano Bonaventura ,&nbsp;Stefan Scheler ,&nbsp;Vladimir Novak ,&nbsp;Margie P. Olbinado ,&nbsp;Matthias Wagner ,&nbsp;Christian Grünzweig ,&nbsp;Alexander Zuern","doi":"10.1016/j.ejpb.2024.114615","DOIUrl":"10.1016/j.ejpb.2024.114615","url":null,"abstract":"<div><div>Prefilled syringes (PFS) are primary packaging materials that offer convenience and safety for subcutaneous injection of parenteral drug solutions. However, an increasingly common problem with the trend towards higher drug concentrations is the clogging of the needle during storage due to evaporative water loss and consequent solidification of the drug. In contrast to all previous studies on this topic, this work focuses on pharmacokinetically relevant aspects and investigates the effects of needle clogging on the spatial distribution of the injected drug in the tissue. X-ray computed tomography (XCT) (both tube-based and synchrotron-based) was used to visualize and analyze the spreading pattern and the fate of the injected liquid in porcine skin. By using controlled injection and force measurement the tissue distribution was correlated with the plunger force profile and the fluid dynamics of the jet. Studies of monoclonal antibody solution demonstrate that clogs, which are formed by evaporation of water and solidification of drug solution in the needle tip, usually dissolve in the flow of the liquid during injection. In the initial injection phase, the liquid jet starts to escape the needle only through a narrow channel in the clog. The resulting high dynamic pressure can alter the distribution of the liquid in the tissue, causing a long tail of liquid that penetrates deep into the fibrous network of the subcutaneous layer. However, the volume of this tail was calculated to be low relative to the overall volume of the injected drug solution (less than 2.4%) and is therefore unlikely to have a significant effect on the absorption kinetics of the injected drug. In addition, it was shown that if a clog were to enter the tissue, it would quickly dissolve.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114615"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142853393","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}

{"title":"In vitro and in vivo characterization of Invega Sustenna® (paliperidone palmitate long-acting injectable suspension)","authors":"Ji Li ,&nbsp;Antonela Rodriguez ,&nbsp;Kaikai Wang ,&nbsp;Karl Olsen ,&nbsp;Yan Wang ,&nbsp;Anna Schwendeman","doi":"10.1016/j.ejpb.2024.114613","DOIUrl":"10.1016/j.ejpb.2024.114613","url":null,"abstract":"<div><div>The aim of this study was to comprehensively characterize paliperidone palmitate (PP) long-acting suspension (Invega Sustenna®) through reverse engineering. We developed a series of analytical methods to assess critical quality attributes of four batches of Invega Sustenna®. The size distributions of the four batches of suspensions were measured using laser diffraction, and variations in the D50 and D90 parameters were observed. The morphology of suspension was determined through scanning electron microscope (SEM), which exhibited irregular granular shape across all batches. The size distributions determined by SEM images were similar to the laser diffraction results. Thermal characteristics were detected using differential scanning calorimetry (DSC) and crystalline properties were assessed by powder X-ray diffraction (PXRD), displaying consistency among the four batches in these two aspects. <em>In vitro</em> dissolution methods (sample separation and dialysis bag methods) were developed to evaluate the release behaviors of Invega Sustenna® and four lots showed a similar dissolution pattern. Furthermore, following a single-dose intramuscular administration to rats, two batches of Invega Sustenna® with the largest size differences demonstrated comparable plasma concentration–time profiles and pharmacokinetics parameters, indicative of one month long-acting release. In summary, we established a systematic quality characteristics assessment for Invega Sustenna®, including particle size distribution, particle morphology, thermal characteristics, crystalline properties, <em>in vitro</em> dissolution kinetics and <em>in vivo</em> pharmacokinetics. Our work will assist pharmaceutical companies and regulatory agencies in the development and regulatory assessment of novel or generic products of long-acting injectable suspension.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114613"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142794386","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}

{"title":"Enhanced wound healing properties by sodium alginate-carboxymethyl cellulose hydrogel enriched with decellularized amniotic membrane","authors":"Rounik Karmakar ,&nbsp;Mansi Dixit ,&nbsp;Kalyani Eswar ,&nbsp;Basu Bhattacharjee ,&nbsp;Basa Apoorva ,&nbsp;Mounika Gubige ,&nbsp;Amuthaveni Sengottaiyan ,&nbsp;Falguni Pati ,&nbsp;Aravind Kumar Rengan","doi":"10.1016/j.ejpb.2024.114621","DOIUrl":"10.1016/j.ejpb.2024.114621","url":null,"abstract":"<div><div>Skin, as the primary interface with the external environment, is susceptible to damage, posing a formidable challenge for complete restoration in adult skin injuries. Wound healing remains a clinical challenge, necessitating advanced biomaterials to support cell proliferation, modulate inflammation, and combat infections. Among several options, hydrogel can be a capable contender for biological dressings. Here, we developed and evaluated a novel hydrogel composed of sodium alginate (SA) and carboxymethyl cellulose (CMC), enriched with decellularized extracellular matrix of amniotic membrane (dAM), using calcium chloride (CaCl₂) as a crosslinker. An incorporation of dAM imparted biomimetic qualities, as evidenced by SEM, showing a fibrous extracellular matrix-like structure. Rheological studies demonstrated the optimal viscosity of SA-CMC-dAM for cell proliferation and adhesion, overcoming limitations of SA and CMC alone. The hydrogel exhibited the highest moisture absorption (12.27±0.59 %) and enhanced hydrophilicity, as confirmed by the contact angle assay, ensuring suitability for wound applications. Biological assessments revealed superior fibroblast migration in scratch assays and significant anti-biofilm activity (∼70 % reduction in <em>E. coli</em> biofilms) alongside antimicrobial efficacy, supported by FDA/PI assays. The zebrafish embryo studies validated its biocompatibility (20 μg/ml) and demonstrated potent anti-inflammatory effects, with a marked reduction in neutrophil recruitment (∼25 %) in tail transection models compared to controls. These findings suggest that the SA-CMC-dAM hydrogel synergises structural, antibacterial, and anti-inflammatory properties, making it a promising candidate for wound healing applications. The biomimetic and multifunctional design provides a strong basis for further translational studies in mammalian systems.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114621"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142893265","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}

{"title":"Dermatological Nanotechnology: Gelatin films with O/W emulsions for skin lesion repair","authors":"Ayelen M. Sosa ,&nbsp;Belen E. Berín ,&nbsp;Celeste Cottet ,&nbsp;María J. Prieto ,&nbsp;Carolina S. Martinez","doi":"10.1016/j.ejpb.2024.114602","DOIUrl":"10.1016/j.ejpb.2024.114602","url":null,"abstract":"<div><div>The development of films, scaffolds, hydrogels, and other innovations based on biopolymers for the treatment of skin injuries is on the rise. Therefore, it is important to focus on their functionality, influence on human use, and environmental impact. This work investigates the antimicrobial capacity of gelatin films that incorporate O/W emulsions encapsulating bactericidal and healing active ingredients (EA). Their biocompatibility was evaluated <em>in vitro</em> in human skin keratinocyte and murine fibroblast cell cultures, as well as <em>in vivo</em> using the zebrafish model. Finally, its potential to heal wounds was assessed through a keratinocyte cell migration assay. The EA films exhibited antimicrobial activity against <em>Pseudomonas aeruginosa</em> and <em>Staphylococcus aureus</em>. The films were biocompatible with monolayer cultures, without affecting cell viability, metabolic activity, or membrane integrity. The films did not exhibit general toxicological effects in zebrafish nor specific organ toxicity in the heart, liver, or brain. Further, the EA films promoted keratinocyte migration in the wound healing assay. In conclusion, the films could be used as a potential treatment for various types of skin injuries, being safe for both potential human application and the environment after use and disposal.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114602"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142794383","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}

{"title":"Thumb-sized 3D-Printed cymbal microneedle array (CyMA) for enhanced transdermal drug delivery","authors":"Ziyan Chen ,&nbsp;Kai Ye ,&nbsp;Huayi Wu ,&nbsp;Lanyuan Peng ,&nbsp;Zeyu Chen","doi":"10.1016/j.ejpb.2025.114629","DOIUrl":"10.1016/j.ejpb.2025.114629","url":null,"abstract":"<div><div>Transdermal drug delivery presents a compelling alternative to both needle injection and oral ingestion of medication, as it enhances patient adherence and convenience through its non-invasive and painless administration method. The use of microneedles penetrates the barrier of the stratum corneum, facilitating the sustained delivery of drugs across the skin. However, their efficacy has been limited by the slow diffusion of molecules and often requires external triggers. Herein, a lightweight and minimized 3D-printed microneedle array is introduced, employing a cymbal-type ultrasound transducer, as the external engine for deeper and faster transdermal drug delivery. A theoretical finite element model was developed and the optimization design was conducted for structural parameters. The optimized assembled prototype was fabricated using high-precision 3D printing and weighs only 20 g. <em>In vivo</em> experiments using a diabetic mouse model demonstrate that local insulin delivery with CyMA achieves systemic effects comparable to intraperitoneal administration. Such compact and effective microneedle delivery technology offers considerable promise therapeutic applications on the skin and intraoral use.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114629"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143002754","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}

{"title":"Multistage microfluidic assisted Co-Delivery platform for dual-agent facile sequential encapsulation","authors":"Shixin Li ,&nbsp;Bing Yang ,&nbsp;Liang Ye ,&nbsp;Shuqi Hu ,&nbsp;Benhong Li ,&nbsp;Yanjun Yang ,&nbsp;Yichuan Hu ,&nbsp;Xiaobin Jia ,&nbsp;Liang Feng ,&nbsp;Zhiwei Xiong","doi":"10.1016/j.ejpb.2024.114616","DOIUrl":"10.1016/j.ejpb.2024.114616","url":null,"abstract":"<div><div>The integration of multiple therapeutic agents within a single nano-drug carrier holds promise for advancing anti-tumor therapies, despite challenges posed by their diverse physicochemical properties. This study introduces a novel multi-stage microfluidic co-encapsulation platform designed to address these challenges. By carefully orchestrating the nano-precipitation process sequence, this platform achieves sequential encapsulation of two drugs with markedly different physicochemical characteristics. Using the multi-stage microfluidic TrH chip, hybrid nanoparticles (HNPs) loaded with paclitaxel (PTX)-simvastatin (SV), PTX-lenvatinib (LV), and SV-LV were synthesized. Unlike conventional Bulk methods and existing commercial microfluidic Tesla and Baffle chips, the HNPs produced here exhibit a core–shell structure and uniform particle size distribution, crucial for enhancing drug delivery efficacy. Notably, this method achieves nearly 100 % encapsulation efficiency for both drugs across a dual-drug feed ratio range from 1:4 to 4:1. Drug loading efficiencies were quantified for PTX-SV/HNPs (14.97 ± 1.19 %), PTX-LV/HNPs (16.58 ± 0.69 %), and SV-LV/HNPs (19.21 ± 2.38 %). PTX-SV/HNPs demonstrated sequential release characteristics of SV and PTX, as confirmed by <em>in vitro</em> drug release experiments. Significantly, PTX-SV/HNPs exhibited superior cytotoxicity against HepG2 cells compared to individual PTX and SV treatments, underscoring their potential in cancer therapy. In conclusion, the developed multi-stage microfluidic platform represents a robust strategy for co-encapsulating drugs with substantial physicochemical disparities, thereby offering a promising avenue for advancing multi-drug delivery in nanomedicine applications.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114616"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142853398","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}

{"title":"Enhancing therapeutic efficacy: In vivo mechanisms and biochemical effects of lycopene encapsulated in nanomicelles for acute inflammation and lipid metabolism","authors":"Stephanie Neves-Silva ,&nbsp;Isabelle Xavier-de-Britto ,&nbsp;Natália Cristina Gomes-da-Silva ,&nbsp;Álefe Roger Silva França ,&nbsp;Franciana Pedrochi ,&nbsp;Maria Nayane Queiroz ,&nbsp;Julia Moura-Silva ,&nbsp;David Majerowicz ,&nbsp;Eduardo Ricci-Junior ,&nbsp;Tatiana Paula Teixeira Ferreira ,&nbsp;Patrícia Martins Rodrigues e Silva Martins ,&nbsp;Yu Cai ,&nbsp;Pierre Basilio Almeida Fechine ,&nbsp;Luciana Magalhães Rebelo Alencar ,&nbsp;Celso Sant’anna ,&nbsp;Ralph Santos-Oliveira","doi":"10.1016/j.ejpb.2024.114585","DOIUrl":"10.1016/j.ejpb.2024.114585","url":null,"abstract":"<div><div>This study focuses on developing, characterizing, and evaluating lycopene nanomicelles formulations for their therapeutic potential in treating acute inflammation and obesity. Lycopene, a hydrophobic carotenoid with potent antioxidant, anti-inflammatory, and anticancer properties, faces challenges in bioavailability due to its poor solubility. To address this, the study utilized nanocarrier systems like liposomes, nanoparticles, and nanoemulsions to enhance the solubility, stability, and bioavailability of lycopene. The lycopene nanomicelles demonstrated significant anti-inflammatory and anticancer activities through multiple mechanisms. It inhibited the NF-κB pathway, reducing the expression of pro-inflammatory mediators, and modulated apoptotic pathways, leading to increased apoptosis and reduced cell proliferation in cancer cells. Furthermore, lycopene enhanced phase II detoxifying enzymes activity, interfered with gap junction communication, and potentially improved DNA repair mechanisms, contributing to its anticancer efficacy. In vivo studies revealed that lycopene nanomicelles effectively reduced leukocyte and neutrophil counts in an acute inflammation model, especially at higher doses, highlighting its potential as a nanodrug for inflammation management. However, the study found no significant alteration in triglyceride levels, indicating a need for further investigation into the effects of lycopene and its nanostructured forms on lipid metabolism. Biochemical analyses showed variations in liver enzyme levels, suggesting protective effects on the liver but also indicating potential pancreatic activity or stress and low glucose levels. These findings underscore the necessity for comprehensive safety evaluations. Overall, this research underscores the promising therapeutic applications of lycopene nanomicelles in inflammation and cancer while emphasizing the importance of addressing safety and metabolic effects for effective clinical translation.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"207 ","pages":"Article 114585"},"PeriodicalIF":4.4,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142767452","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}