International Journal of Pharmaceutics: X最新文献

Terconazole loaded edge-activated hybrid elastosome for revamped corneal permeation in ocular mycosis: In-vitro characterization, statistical optimization, microbiological assessment, and in-vivo evaluation.

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-04-08 DOI: 10.1016/j.ijpx.2025.100333

Sadek Ahmed , Michael M. Farag , Heba Attia , Bander Balkhi , Islam M. Adel , Asmaa Ashraf Nemr

{"title":"Terconazole loaded edge-activated hybrid elastosome for revamped corneal permeation in ocular mycosis: In-vitro characterization, statistical optimization, microbiological assessment, and in-vivo evaluation.","authors":"Sadek Ahmed , Michael M. Farag , Heba Attia , Bander Balkhi , Islam M. Adel , Asmaa Ashraf Nemr","doi":"10.1016/j.ijpx.2025.100333","DOIUrl":"10.1016/j.ijpx.2025.100333","url":null,"abstract":"<div><div>Herein, we investigated the preparation and characterization of Terconazole loaded edge-activated hybrid elastosome (TCN-EHE) adopting thin film hydration technique for the treatment of ocular mycosis. Terconazole (TCN) is a broad spectrum antimycotic agent suffering from sparse aqueous solubility impeding its use in ophthalmic preparations. The scrutinized formulation variables namely X<sub>1</sub>: Surfactant: Edge activator ratio (SAA: EA), X<sub>2</sub>: Pluronic® L121 contribution (% of total SAA) and X<sub>3</sub>: EA concentration (%<em>w</em>/<em>v</em>) were optimized adopting D-optimal design. Ten runs were prepared and characterized regarding their entrapment efficiency, particle size, polydispersity index and zeta potential. An optimized formula was generated, with high desirability, exhibited satisfactory entrapment efficiency, nanoscaled particle size aligning with TEM, plausible zeta potential and bi-phasic release pattern which were not altered after short-term storage. The optimized TCN-EHE displayed 1.94-fold enhanced ex-vivo corneal permeation flux. Safety was ratified through measured corneal hydration level, pH and histopathological evaluation. In-vivo corneal uptake visualized by confocal laser microscopy demonstrated 2.7-fold deeper penetration. Moreover, Superior antifungal activity has been demonstrated displaying 37 % bigger zone of inhibition, 8-fold lower minimum inhibitory and minimum fungal concentration alongside significantly higher biofilm inhibition activity at all tested concentrations for the optimized TCN-EHE compared to TCN suspension. Conclusively, we could prospect that TCN-EHE might be a revamped therapeutic alternative for the delivery of poorly soluble antimycotic agents for the combat of ocular mycosis.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100333"},"PeriodicalIF":5.2,"publicationDate":"2025-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143817570","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

Does tablet shape and height influence survival of fluidized bed-granulated living microorganisms during compaction?

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-04-05 DOI: 10.1016/j.ijpx.2025.100332

Karl Vorländer , Lukas Bahlmann , Arno Kwade , Jan Henrik Finke , Ingo Kampen

{"title":"Does tablet shape and height influence survival of fluidized bed-granulated living microorganisms during compaction?","authors":"Karl Vorländer , Lukas Bahlmann , Arno Kwade , Jan Henrik Finke , Ingo Kampen","doi":"10.1016/j.ijpx.2025.100332","DOIUrl":"10.1016/j.ijpx.2025.100332","url":null,"abstract":"<div><div>The provision of effective probiotic formulations requires gentle processing to maintain the viability of the probiotic microorganisms, which is essential for their health-promoting effects. The drying of microorganisms by fluidized bed spray granulation and subsequent processing of the granules into tablets has proven to be a promising process route in previous studies of the same authors. In these, the influence of various factors was considered using cylindrical tablets with a diameter of 11.28 mm and a mass of 450 mg. These flat tablets are unpleasant to ingest and other tablet geometries should be considered for administration of probiotics but to date, no studies exist on the influence of geometric factors of the tableting tool and of the tablets on the survival of microorganisms. To address this aspect, the survival of <em>Saccharomyces cerevisiae</em> during the production of flat, round tablets with different tablet masses and thus heights as well as differently shaped convex tablets is determined and related to the physical-mechanical tablet properties to derive process-structure-property relationships. It turned out that higher tablet heights were advantageous regarding microbial survival and mechanical strength which is attributed to a lower elastic recovery. However, the use of differently shaped tools had a smaller influence on microbiological and mechanical tablet properties since the global tablet porosity was hardly affected.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100332"},"PeriodicalIF":5.2,"publicationDate":"2025-04-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143799764","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

An iterative process and mixture design approach for dry granulated ternary blends of filler-binders

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-04-01 DOI: 10.1016/j.ijpx.2025.100331

Niclas Märkle , Gernot Warnke , Miriam Pein-Hackelbusch

{"title":"An iterative process and mixture design approach for dry granulated ternary blends of filler-binders","authors":"Niclas Märkle , Gernot Warnke , Miriam Pein-Hackelbusch","doi":"10.1016/j.ijpx.2025.100331","DOIUrl":"10.1016/j.ijpx.2025.100331","url":null,"abstract":"<div><div>Roller compaction/dry granulation (RC/DG) is a key process in pharmaceutical manufacturing for improving powder flowability, density, and segregation resistance. Advanced statistical modeling was used to optimize RC/DG process parameters and subsequently binder compositions by employing process and mixture design experiments. The authors used microcrystalline cellulose (MCC), silicified MCC (SMCC), and dicalcium phosphate (DCP) as filler-binder examples in RC/DG experiments. Granule and tablet properties, including flowability, bulk and tapped densities, as well as resistance to crushing, were analyzed using compendial methods. The process design experiments confirmed that RC/DG reduces manufacturability compared to direct compression. Optimal processing conditions, balancing sufficient tablet strengths and granule formation, were identified to be between 20 (SCF * ϑ) [kN/cm] and ∼ 60 (SCF * ϑ) [kN/cm]. Thereby (ϑ) is defined as the screw-to-roll speed ratio and (SFC) as the specific compaction force. Mixture design experiments revealed optimal mixtures balancing SMCC, MCC, and DCP to achieve desired properties like low angle of repose, high bulk density, and strong tablets. These findings provide guidance for selecting formulations and process parameters in RC/DG applications. The derived ‘SCF * ϑ’- factor was found to effectively describe the granulation intensity. A superimposed mixture design model based on precise target values of the parameters bulk density, flow properties, and breaking force allowed identification of the best formulation.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100331"},"PeriodicalIF":5.2,"publicationDate":"2025-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143776954","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

Polycarboxybetaine in advanced drug delivery systems: From structure-function relationship to therapeutic applications

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-03-29 DOI: 10.1016/j.ijpx.2025.100329

Zhuang Liu , Yanan Zhai , Shunye Wang, Jiahui Bai, Dan Wang, Ziyang Wang, Xiang Gao, Jing Gao

{"title":"Polycarboxybetaine in advanced drug delivery systems: From structure-function relationship to therapeutic applications","authors":"Zhuang Liu , Yanan Zhai , Shunye Wang, Jiahui Bai, Dan Wang, Ziyang Wang, Xiang Gao, Jing Gao","doi":"10.1016/j.ijpx.2025.100329","DOIUrl":"10.1016/j.ijpx.2025.100329","url":null,"abstract":"<div><div>Zwitterionic polycarboxybetaines (PCBs), combining quaternary ammonium cations and carboxylate anions in their repeating units, have emerged as promising materials for drug delivery applications. Their exceptional hydration, biocompatibility, and antifouling properties make them attractive alternatives to polyethylene glycol (PEG), particularly given growing concerns about immunogenicity of PEG. PCBs can be functionalized through various methods, including modification of side-chain moieties, adjustment of spacer length between charged groups, and incorporation of responsive elements. When applied to delivery drug, PCBs have been successfully developed into multiple formats including micelles, hydrogels, liposomes, and nanoparticles. Notably, in protein drug delivery, PCBs demonstrate significant advantages such as enhancing protein stability, extending circulation time, improving penetration through biological barriers, and reducing immunogenicity. Despite these promising features, several challenges remain, including complex synthesis requirements, limited mechanical properties, and pending FDA approval as pharmaceutical excipients. This review provides a comprehensive analysis of PCBs from the structure-function relationship, synthesis methods, and applications in drug delivery systems, while examining current limitations and future prospects.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100329"},"PeriodicalIF":5.2,"publicationDate":"2025-03-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143747097","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

Enrofloxacin‑silver composite nano-emulsion as a scalable synergetic antibacterial platform for accelerating infected wound healing

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-03-25 DOI: 10.1016/j.ijpx.2025.100330

Jiahao Gong , Moxin Liu , Runan Zuo , Xinhao Song , Junqi Wang , Qindan Zuo , Yan Jiang , Yunfeng Long , Yuzhen Silang , Zeng Luo , Xiuge Gao , Dawei Guo

{"title":"Enrofloxacin‑silver composite nano-emulsion as a scalable synergetic antibacterial platform for accelerating infected wound healing","authors":"Jiahao Gong , Moxin Liu , Runan Zuo , Xinhao Song , Junqi Wang , Qindan Zuo , Yan Jiang , Yunfeng Long , Yuzhen Silang , Zeng Luo , Xiuge Gao , Dawei Guo","doi":"10.1016/j.ijpx.2025.100330","DOIUrl":"10.1016/j.ijpx.2025.100330","url":null,"abstract":"<div><div>The colonization of bacterial pathogens is a major concern in wound infection and becoming a notable medical issue. Enrofloxacin (ENR) can be applied to treat skin infections, while poor water solubility and bioavailability limit its clinical application. Nanostructured lipid carriers (NLCs) enhance the solubility and bioavailability of drugs by encapsulating them, making them effective for the topical treatment of skin wound infections. Additionally, to enhance treatment efficacy and further improve wound healing, silver nanoparticles (AgNPs) were attached to the aforementioned matrix, which also improved its colloidal stability and reduced toxicity. Herein, a scalable poly (vinyl alcohol) modified NLCs-based antibacterial platform was fabricated by high-pressure homogenization method, to co-load ENR and AgNPs for treating the bacterial-infected wounds. The growth of common wound bacterial pathogens (<em>Escherichia coli</em>, <em>Staphylococcus aureus</em> and <em>Pseudomonas aeruginosa</em>) was synergistically inhibited by released ENR and Ag<sup>+</sup> from the poly (vinyl alcohol) modified enrofloxacin‑silver composite nano-emulsion (ENR@PVA-NLCs/AgNPs). In the <em>in vivo</em> wound model, the <em>Staphylococcus aureus</em>-infected wound in rat almost completely disappeared after treatment with ENR@PVA-NLCs/AgNPs, and no suppuration symptom was observed. Importantly, this nanoplatform had negligible side effects <em>in vivo</em>. Taken together, the above results strongly demonstrate the promising potential of ENR@PVA-NLCs/AgNPs as a synergistic therapeutic agent for clinical wound infections.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100330"},"PeriodicalIF":5.2,"publicationDate":"2025-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143714285","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 healing potential of simple natural hydrogel loaded with sildenafil in combating infectious wounds

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-03-24 DOI: 10.1016/j.ijpx.2025.100328

Yifan Lai , Wa Zhang , Yizhang Chen , Jialu Weng , Yuhan Zeng , Shunfu Wang , Xiaoying Niu , Meilin Yi , Haobing Li , Xuchen Deng , Xiuhua Zhang , Danyun Jia , Wenzhang Jin , Fajing Yang

{"title":"Advanced healing potential of simple natural hydrogel loaded with sildenafil in combating infectious wounds","authors":"Yifan Lai , Wa Zhang , Yizhang Chen , Jialu Weng , Yuhan Zeng , Shunfu Wang , Xiaoying Niu , Meilin Yi , Haobing Li , Xuchen Deng , Xiuhua Zhang , Danyun Jia , Wenzhang Jin , Fajing Yang","doi":"10.1016/j.ijpx.2025.100328","DOIUrl":"10.1016/j.ijpx.2025.100328","url":null,"abstract":"<div><div>Infected wounds are common clinical injuries that often complicated by inflammation and oxidative stress due to bacterial invasion. These wounds typically suffer from impaired vascularization, which delays healing and increases the risk of complications such as sepsis and chronic wounds. Therefore, developing an effective treatment for infected wounds is highly necessary. Egg white can promote cell regeneration and repair, while chitosan is effective in resisting bacterial invasion. Sildenafil is believed to have the potential to promote angiogenesis. Based on these properties, we have prepared a new type of hydrogel using egg white and chitosan as the framework, loaded with sildenafil (CEHS). The hydrogel combines the benefits of its components, exhibiting good biocompatibility and promoting the proliferation and migration of NIH 3T3 (3T3) cells and human umbilical vein endothelial cells (HUVEC), as well as the angiogenesis in HUVEC. It also exhibits significant antioxidant, anti-inflammatory, and antibacterial properties against <em>Escherichia coli (E. coli)</em> and <em>Staphylococcus aureus (S. aureus)</em>. Additionally, in a mouse model of infected wounds, the CEHS effectively promoted wound healing through its excellent antioxidant and anti-inflammatory properties, antibacterial activity, and pro-angiogenic effects. In summary, this simple-to-prepare, multifunctional natural hydrogel shows great promise for the treatment of infected wounds.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100328"},"PeriodicalIF":5.2,"publicationDate":"2025-03-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143726016","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

Comparing the transfection efficiency of cationic monomer ratios in vinylimidazole and aminoethyl methacrylate copolymers

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-03-04 DOI: 10.1016/j.ijpx.2025.100327

Sahel Soghrati , Jaleh Varshosaz , Mahboubeh Rostami , Mina Mirian , Fariborz Sharifianjazi , Ketevan Ta-vamaishvili

{"title":"Comparing the transfection efficiency of cationic monomer ratios in vinylimidazole and aminoethyl methacrylate copolymers","authors":"Sahel Soghrati , Jaleh Varshosaz , Mahboubeh Rostami , Mina Mirian , Fariborz Sharifianjazi , Ketevan Ta-vamaishvili","doi":"10.1016/j.ijpx.2025.100327","DOIUrl":"10.1016/j.ijpx.2025.100327","url":null,"abstract":"<div><div>Employing polycations as non-viral gene delivery vectors has been extensively studied owing to their safety, efficiency and possibility of modifying them in an intended way compared with viral vectors. However, the main challenge is finding a biocompatible and transfection-efficient polymer. In this study, 2-aminoethyl methacrylate (A) and 1-vinyl imidazole (V) were copolymerized at three different molar ratios by a free radical polymerization method and novel biocompatible polycations with narrow molecular weight distribution were obtained. The resulting copolymers were used for condensation of plasmid DNA (pDNA) at different N/P ratios followed by physicochemical characterizations of resulting polyplexes. At N/P ratio of 2, the nanoplexes were smaller than 120 nm. The optimum formulations were stable in presence of polyanions and capable of protecting the condensed pDNA against nucleases. The polyplexes having V to A molar ratio of 1:1 were the most efficient carrier in transfecting HeLa cells and were introduced as a promising non-viral vector.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100327"},"PeriodicalIF":5.2,"publicationDate":"2025-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143563468","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

Reticuloendothelial system blockade does not enhance siRNA-LNP circulation or tumor accumulation in mice 网状内皮系统阻断不会增强 siRNA-LNP 在小鼠体内的循环或肿瘤蓄积

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-02-27 DOI: 10.1016/j.ijpx.2025.100324

Pol Escudé Martinez de Castilla , Mariona Estapé Senti , Sigrun Erkens , Wytske M. van Weerden , Sander A.A. Kooijmans , Marcel H. Fens , Pieter Vader , Raymond M. Schiffelers

{"title":"Reticuloendothelial system blockade does not enhance siRNA-LNP circulation or tumor accumulation in mice","authors":"Pol Escudé Martinez de Castilla , Mariona Estapé Senti , Sigrun Erkens , Wytske M. van Weerden , Sander A.A. Kooijmans , Marcel H. Fens , Pieter Vader , Raymond M. Schiffelers","doi":"10.1016/j.ijpx.2025.100324","DOIUrl":"10.1016/j.ijpx.2025.100324","url":null,"abstract":"<div><div>One of the biggest challenges for siRNA-based therapeutics is intracellular delivery into the target cell, which can be facilitated by encapsulating siRNA in lipid nanoparticles (LNPs). In this study, we formulated D-Lin-MC3-DMA-LNPs encapsulating siRNA against the androgen receptor (AR), a key driver in prostate cancer. We effectively knocked down AR expression at both the mRNA as well as protein levels <em>in vitro</em> in AR-expressing prostate cancer cell lines. However, when moving to <em>in vivo</em> studies, siRNA-LNP efficacy is hindered by rapid clearance by the reticuloendothelial system (RES) in the liver and spleen. We evaluated whether transient RES blockade through systemic pre-administration of dextran sulfate or liposomes could extend the circulation time and enhance tumor accumulation of siRNA-LNPs in tumor-bearing mice. In two different mouse prostate cancer (PCa) xenograft models, we observed that, upon systemic administration, LNPs still predominantly accumulated in the liver and spleen, with only limited tumor uptake. Our findings demonstrate that pre-treatment with dextran sulfate or liposomes did not enhance siRNA-LNP blood circulation time or tumor accumulation <em>in vivo</em>, indicating the need for alternative strategies to enhance siRNA-LNP delivery to tumors.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100324"},"PeriodicalIF":5.2,"publicationDate":"2025-02-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143528776","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

Fucoidan/Polyvinylpyrrolidone/Hesperitin nanoparticle complex for corneal injury treatment: Synthesis, characterization, and therapeutic efficacy

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-02-26 DOI: 10.1016/j.ijpx.2025.100325

Yalu Liu , Zhengpei Zhang , Lina Guan , Jie Li , Xing Ge , Xiaochen Wu , Haiyang Liu

{"title":"Fucoidan/Polyvinylpyrrolidone/Hesperitin nanoparticle complex for corneal injury treatment: Synthesis, characterization, and therapeutic efficacy","authors":"Yalu Liu , Zhengpei Zhang , Lina Guan , Jie Li , Xing Ge , Xiaochen Wu , Haiyang Liu","doi":"10.1016/j.ijpx.2025.100325","DOIUrl":"10.1016/j.ijpx.2025.100325","url":null,"abstract":"<div><div>Corneal injury is a common ailment that, if not addressed promptly and efficiently, has the potential to result in significant visual impairment. This study investigates the therapeutic potential of a novel FU/PVP/Hes nanoparticle complex composed of fucoidan (FU), polyvinylpyrrolidone (PVP), and hesperitin (Hes) for corneal injury treatment. The FU/PVP/Hes nanoparticles were synthesized using a solvent evaporation method and characterized for their morphology, size distribution, biocompatibility, antioxidant activity, and anti-inflammatory capacity. The nanoparticles demonstrated excellent biocompatibility with low hemolysis rates and minimal cytotoxicity. They also exhibited potent antioxidant and anti-inflammatory properties, which were attributed to the enhanced solubility and bioavailability of Hes through nanoparticle formation. <em>In vivo</em> investigations employing a mouse model of corneal injury induced by alkali burns showed that the FU/PVP/Hes nanoparticles significantly promoted corneal epithelial healing, reduced corneal opacity, and suppressed the elevation of inflammatory cytokines. Histopathological analysis confirmed the nanoparticles' ability to facilitate corneal tissue repair. The study concludes that the FU/PVP/Hes nanoparticle complex is a promising therapeutic agent for corneal injury treatment due to its biocompatibility and multifaceted therapeutic effects.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100325"},"PeriodicalIF":5.2,"publicationDate":"2025-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143552607","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

RGD peptide-functionalized micelles loaded with crocetin ameliorate doxorubicin-induced cardiotoxicity

IF 5.2 2区医学

International Journal of Pharmaceutics: X Pub Date : 2025-02-26 DOI: 10.1016/j.ijpx.2025.100326

Ting Wang , Zhimin Li , Jiawei Lei , Yuchen Zhang , Yingpeng Tong , Xingang Guan , Shuangshuang Wang

{"title":"RGD peptide-functionalized micelles loaded with crocetin ameliorate doxorubicin-induced cardiotoxicity","authors":"Ting Wang , Zhimin Li , Jiawei Lei , Yuchen Zhang , Yingpeng Tong , Xingang Guan , Shuangshuang Wang","doi":"10.1016/j.ijpx.2025.100326","DOIUrl":"10.1016/j.ijpx.2025.100326","url":null,"abstract":"<div><div>Doxorubicin (Dox)-induced cardiotoxicity presents a significant challenge to fully harnessing its chemotherapeutic potential. Crocetin (Cro), a dicarboxylic acid found in the crocus flower and gardenia fruit, has shown remarkable antioxidant and anti-inflammatory activities. However, its poor aqueous solubility and limited cellular uptake severely constrain its further application in treating diseases. In this study, we developed Arg-Gly-Asp (RGD) peptide-decorated nanomicelles delivering Cro to alleviate Dox-induced cardiac injury. The RGD@M(Cro) nanomicelles exhibited excellent aqueous solubility and a drug-loading efficiency of 93.3 %. RGD-decorated micelles could enhance the cellular uptake of Cro in cardiomyocytes and inhibit approximately 60 % of HL-1 cell apoptosis through efficient reactive oxygen species (ROS) scavenging. In a cardiomyopathy mouse model, RGD@M(Cro) substantially reduced cardiac damage and improved cardiac indicators. This study highlights the great potential of RGD-decorated micelles in treating cardiac injury and other diseases.</div></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"9 ","pages":"Article 100326"},"PeriodicalIF":5.2,"publicationDate":"2025-02-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143520145","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