European Journal of Pharmaceutics and Biopharmaceutics最新文献

{"title":"Nanomedicine for pediatric healthcare: A review of the current state and future prospectives.","authors":"Jiayi Chen, Zhifeng Zhao, Doaa Alantary, Jingjun Huang","doi":"10.1016/j.ejpb.2024.114597","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114597","url":null,"abstract":"<p><p>Nanomedicine has emerged as a valuable treatment and diagnosis option, due to its ability not only to address formulation challenges associated with new therapeutic moieties, but also to improve the existing drugs efficacy. Nanomedicine provides appealing advantages such as increased drug payload, enhanced stability, tailored drug release profile, improved bioavailability and targeted drug delivery, etc. Tremendous research and regulatory efforts have been made in the past decades to advance nanomedicine from the benchtop to clinic. Numerous nanotechnology-based formulation approaches have been seen succeeding in commercialization. Despite the progress in nanomedicine use in adults, the advancement in pediatric population has been much slower. Clearly the treatment of disease in children cannot be simplified by dose adjustment based on body weight or surface, due to the significant differences in physiology thus the drug absorption, distribution, metabolism, excretion and transport (ADMET), between children and adults. This inherent variable among others poses much more challenges when developing pediatric-specific nanomedicine or translating adult nanodrug to pediatric indication. This review therefore intends to highlight the physiological differences between children and adult, and the common pediatric diseases which are good candidates for nanomedicine. The formulation approaches utilized in the marketed nanomedicine with pediatric indications, including liposomes, nanocrystals, polymeric nanoparticles and lipid nanoemulsions are elaborated. Finally, the challenges and gaps in pediatric nanomedicine development and commercialization, and the future prospectives are discussed.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114597"},"PeriodicalIF":4.4,"publicationDate":"2024-12-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142794402","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, Antonela Rodriguez, Kaikai Wang, Karl Olsen, Yan Wang, Anna Schwendeman","doi":"10.1016/j.ejpb.2024.114613","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114613","url":null,"abstract":"<p><p>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. In vitro 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, in vitro dissolution kinetics and in vivo 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.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114613"},"PeriodicalIF":4.4,"publicationDate":"2024-12-06","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":"Dermatological Nanotechnology: Gelatin films with O/W emulsions for skin lesion repair.","authors":"Ayelen M Sosa, Belen E Berín, Celeste Cottet, María J Prieto, Carolina S Martinez","doi":"10.1016/j.ejpb.2024.114602","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114602","url":null,"abstract":"<p><p>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 in vitro in human skin keratinocyte and murine fibroblast cell cultures, as well as in vivo 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 Pseudomonas aeruginosa and Staphylococcus aureus. 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.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114602"},"PeriodicalIF":4.4,"publicationDate":"2024-12-06","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":"Fishroesomes show intrinsic anti-inflammatory bioactivity and ability as celecoxib carriers in vivo.","authors":"Marta Guedes, Joana Vieira de Castro, Ana Cláudia Lima, Virgínia M F Gonçalves, Maria Elizabeth Tiritan, Rui L Reis, Helena Ferreira, Nuno M Neves","doi":"10.1016/j.ejpb.2024.114587","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114587","url":null,"abstract":"<p><p>According to the World Health Organization (WHO), chronic inflammatory-related diseases represent the greatest threat to human health. Indeed, failure in the resolution of inflammation leads to serious pathological conditions, such as cardiovascular diseases, arthritis, cancer, diabetes, autoimmune diseases, and neurodegenerative disorders that are often associated with extremely high human suffering and societal and economic burdens. Despite the number and efficacy of available therapeutic agents have been increased, the serious side effects associated with some of them often create a very high risk/benefit ratio for patients. Therefore, herein, a drug delivery system was engineered to overcome important drawbacks of conventional therapies and to have a synergistic action with the incorporated drug. Indeed, it will have an added beneficial role in controlling inflammation. For that, sardine (Sardina pilchardus) roe was used as the lipidic source to produce bioactive liposomes, namely fishroesomes. These spherical vesicles with ≈326 nm in size and a significant negative surface charge (≈-31 mV) were able to encapsulate and control the release of the anti-inflammatory drug celecoxib. Moreover, fishroesomes were cytocompatible for different cell types (chondrocytes and macrophages), at concentrations in which they present anti-inflammatory properties. Importantly, fishroesomes were more effective in reducing pro-inflammatory mediators than the free drug. We also demonstrated that a single intra-articular injection of the fishroesomes encapsulating or not celecoxib in an experimental rat model of inflammatory arthritis was safe and more effective in controlling the pain and reducing the synovial inflammation compared to the free drug. Notably, as the celecoxib concentration in the sardine roe-derived liposomes was less than half of the amount of free drug, this study demonstrates the value of fishroesomes in counteracting inflammation. Therefore, the developed formulations may be considered a promising therapeutic option for inflammatory conditions.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114587"},"PeriodicalIF":4.4,"publicationDate":"2024-12-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142791338","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":"Application of microarray patches for the transdermal administration of psychedelics drugs in micro-doses.","authors":"Octavio E Fandino, Aaron R J Hutton, Chunyang Zhang, Marco T A Abbate, Yara A Naser, Yaocun Li, Alejandro J Paredes, Ryan F Donnelly","doi":"10.1016/j.ejpb.2024.114603","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114603","url":null,"abstract":"<p><p>Throughout history, psychedelic compounds have been used for religious, spiritual and recreational purposes. A plethora of studies have reported the use of psychedelic compounds in the treatment of various conditions, such as alcoholism, addictions, depressive state to borderline schizophrenia, personality disorder, among other mental disorders. Psychedelic microdosing, a common technique in recent years, involves the consumption of small doses of psychedelic drugs for therapeutic purposes. This study investigated the potential of hydrogel-forming microarray patches (HF-MAPs) to deliver N,N-dimethyltryptamine (DMT), 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT), and mescaline (MES) in small doses through the skin. To this purpose, HF-MAPs were prepared using poly(vinyl alcohol) (PVA) and poly(vinyl pyrrolidone) (PVP), using citric acid as the crosslinker. Two different reservoirs, containing PVP and PVA as the main components and poly(ethylene)glycol 400 (PEG400) and glycerol as plasticising agents, were used to deliver all the drugs from the HF-MAPs. Franz cells studies in excised neonatal porcine skin demonstrated that the permeation of DMT, 5-MeO-DMT and MES was better from the PEG400 reservoir, showing a permeation of 60.71 %, 59.61 % and 41.85 % respectively. Pharmacokinetic studies in rats showed that HF-MAP technology as a strategy for microdosing psychedelic compounds was also demonstrated with DMT. AUC_t0-final for the HF-MAP cohort (7186 ± 1296 ng/mL*h) was significantly greater than the IM cohort (1803 ± 53.25 ng/mL*h) (p = 0.0020), with a relative bioavailability of ∼ 72 %. Considering their pharmacokinetic profile, the frequency of DMT dosing could be reduced with HF-MAP when compared to the IM route.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114603"},"PeriodicalIF":4.4,"publicationDate":"2024-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142791334","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, Isabelle Xavier-de-Britto, Natália Cristina Gomes-da-Silva, Álefe Roger Silva França, Franciana Pedrochi, Maria Nayane Queiroz, Julia Moura-Silva, David Majerowicz, Eduardo Ricci-Junior, Tatiana Paula Teixeira Ferreira, Patrícia Martins Rodrigues E Silva Martins, Yu Cai, Pierre Basilio Almeida Fechine, Luciana Magalhães Rebelo Alencar, Celso Sant'anna, Ralph Santos-Oliveira","doi":"10.1016/j.ejpb.2024.114585","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114585","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114585"},"PeriodicalIF":4.4,"publicationDate":"2024-11-30","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}

{"title":"Development and characterization of pH-sensitive zerumbone-encapsulated liposomes for lung fibrosis via inhalation Route.","authors":"Nourhan Elsayed, Chee Wun How, Jhi Biau Foo","doi":"10.1016/j.ejpb.2024.114599","DOIUrl":"https://doi.org/10.1016/j.ejpb.2024.114599","url":null,"abstract":"<p><p>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.</p>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":" ","pages":"114599"},"PeriodicalIF":4.4,"publicationDate":"2024-11-29","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":"The effects of ligand distribution and density on the targeting properties of dual-targeting folate/biotin Pluronic F127/Poly (lactic acid) polymersomes","authors":"Qing Xiao Wang,&nbsp;Zi Ling Li,&nbsp;Yan Chun Gong,&nbsp;Xiang Yuan Xiong","doi":"10.1016/j.ejpb.2024.114598","DOIUrl":"10.1016/j.ejpb.2024.114598","url":null,"abstract":"<div><div>Targeted drug delivery systems modified with two or more ligands were expected to have better anti-tumor ability than those with just one ligand due to the complexity and heterogeneity of tumors. Thus, dual-targeting Pluronic/poly (lactic acid) polymersomes containing biotin (BT) and folic acid (FA) ligands (BT/FA-F127-PLA) were designed to study their targeting properties over human ovarian cancer cells (OVCAR-3). Two kinds of dual-ligand targeting polymersomes, BT/FA-F127-PLA and (BT + FA)-F127-PLA, were prepared to study the effect of the dual-ligand distribution on the cell targeting of polymersomes. BT/FA-F127-PLA had two ligands distributed in the same polymersomes whereas (BT + FA)-F127-PLA had two ligands distributed in different polymersomes. The in vitro cytotoxicity and cellular uptake, and in vivo pharmacokinetic behaviors of BT/FA-F127-PLA were superior to those of (BT + FA)-F127-PLA. It suggested that biotin and folate ligands distributed on the same polymersomes could have the targeting effect of synergistic promotion. Further experiments on cell uptake mechanisms of polymersomes showed that the uptake of targeted polymersomes was associated with energy-dependent endocytosis, involving clathrin, caveolin protein, macropinocytosis and ligand receptor-mediated endocytosis. In addition, the effect of different density ratios of dual ligands for BT/FA-F127-PLA was further studied. The results showed that the cellular targeting effect of BT/FA-F127-PLA was the strongest when the molar ratio of biotin to folic acid was 7.5 %: 7.5 %. In conclusion, BT/FA-F127-PLA dual-targeting polymersomes could be good candidates as targeted drug delivery carriers.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"206 ","pages":"Article 114598"},"PeriodicalIF":4.4,"publicationDate":"2024-11-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142756974","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":"Self-assembled nanovaccine based on apoferritin: Development and vaccine regimen evaluation","authors":"Camila Machado França de Almeida ,&nbsp;Wendy Martin Rios ,&nbsp;Maíra Peres Ferreira Duarte ,&nbsp;Izaíra Tincani Brandão ,&nbsp;Natalia Floriano Paiva ,&nbsp;Fabiana Testa Moura de Carvalho Vicentini","doi":"10.1016/j.ejpb.2024.114589","DOIUrl":"10.1016/j.ejpb.2024.114589","url":null,"abstract":"<div><div>Apoferritin-based systems have been explored last decade for their potential as vaccine delivery for viral diseases. The nanosized properties of an apoferritin-based system could increase immunogenicity, contribute to antigen stability, and reduce the vaccines’ adverse effects. The mutated extracellular portion of the epidermal growth factor receptor (EGFRvIII peptide, PEPvIII) can be applied as a specific tumoral antigen due to rare expression in normal cells. In this context, the present study proposed the development and the immunogenicity evaluation of an apoferritin-based system (AFt) to deliver a peptide vaccine for an antitumoral purpose. We developed a formulation with different PEPvIII:AFt ratios and during the association efficiency analysis, identified the dependence between the AFt concentration and the PEPvIII association percentage in the formulation. Besides, differences in the immune responses against EGFRvIII were observed depending on the PEPvIII concentration due to the different association efficiencies. Finally, the humoral immune response results showed a high antibody production against AFt, which might affect the immunological tolerance. Collectively, this study establishes the PEPvIII:AFt formulation process and highlights the determinant factors for guaranteeing vaccine safety and efficacy.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"206 ","pages":"Article 114589"},"PeriodicalIF":4.4,"publicationDate":"2024-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142746455","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":"Design, fabrication, and evaluation of antimicrobial sponge microneedles for the transdermal delivery of insulin","authors":"Xinyi Zhang ,&nbsp;Yuelian Zhang ,&nbsp;Huishan Zheng ,&nbsp;Xue Yang ,&nbsp;Shiqi Zou ,&nbsp;Jianmin Chen","doi":"10.1016/j.ejpb.2024.114586","DOIUrl":"10.1016/j.ejpb.2024.114586","url":null,"abstract":"<div><div>Transdermal drug delivery systems hold promise, but their effectiveness is often constrained by the skin’s barrier. Microneedles (MNs) improve drug permeability by creating micro-channels in the skin, yet they continue to face challenges such as infection risks and safety concerns. To overcome these challenges, a novel antimicrobial sponge MNs (ASMNs@PVP-INS) modified with polyvinylpyrrolidone (PVP) for insulin (INS) delivery was designed. Mechanical testing demonstrated that these MNs possess excellent mechanical strength, capable of withstanding at least 0.11 N per needle without rupture. In vitro drug penetration tests revealed that the MNs consistently released over 75 % of INS within a 6 h. In an animal model, ASMNs@PVP-INS reduced initial blood glucose levels from 22.4 to 5.72 mmol/L, effectively maintaining glucose control for more than 6 h without inducing hypoglycemia. Additionally, agar diffusion assays indicated that INS loading did not compromise the antimicrobial properties of antimicrobial sponge MNs (ASMNs). Skin irritation tests showed that ASMNs@PVP-INS exhibited mild irritation (PII &lt; 0.6), with skin damage fully recovering within 8 h. Safety assessments indicated no significant toxicity to mice, with biochemical markers remaining within normal ranges, thereby confirming their good biocompatibility. In conclusion, ASMNs@PVP-INS hold promise as a novel drug delivery vehicle.</div></div>","PeriodicalId":12024,"journal":{"name":"European Journal of Pharmaceutics and Biopharmaceutics","volume":"206 ","pages":"Article 114586"},"PeriodicalIF":4.4,"publicationDate":"2024-11-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142746456","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}