International Journal of Pharmaceutics最新文献_第8页

Aggregation of therapeutic monoclonal antibodies due to thermal and air/liquid interfacial agitation stress: Occurrence, stability assessment strategies, aggregation mechanism, influencing factors, and ways to enhance stability 热应力和空气/液体界面搅拌应力导致治疗用单克隆抗体聚集：发生率、稳定性评估策略、聚集机制、影响因素以及提高稳定性的方法。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-24 DOI: 10.1016/j.ijpharm.2024.124735

{"title":"Aggregation of therapeutic monoclonal antibodies due to thermal and air/liquid interfacial agitation stress: Occurrence, stability assessment strategies, aggregation mechanism, influencing factors, and ways to enhance stability","authors":"","doi":"10.1016/j.ijpharm.2024.124735","DOIUrl":"10.1016/j.ijpharm.2024.124735","url":null,"abstract":"<div><div>Therapeutic proteins, such as monoclonal antibodies (mAbs) are known to undergo stability related issues during various stages of product life cycle resulting in the formation of aggregates and fragments. Aggregates of mAb might result in reduced therapeutic activity and could cause various adverse immunogenic responses. Sample containing mAb undergo aggregation due to various types of stress factors, and there is always a continuous interest among researchers and manufacturers to determine the effect of different factors on the stability of mAb. Thermal stress and air/liquid interfacial agitation stress are among two of the common stress factors to which samples containing mAb are exposed to during various stages. Initial part of this review articles aims to provide a generalized understanding of aggregation of mAb such as size ranges of aggregates, aggregate types, stress factors, analytical techniques, permissible aggregate limits, and stability assessment methods. This article further aims to explain different aspects associated with aggregation of mAb in liquid samples due to thermal and air/liquid interfacial agitation stress. Under each stress category, the occurrence of stress during product life cycle, type of aggregates formed, mechanism of aggregation, strategies used by various researchers to expose mAb containing samples to stress, different factors affecting aggregation, fate of aggregates in human body fluids, and strategies used to enhance mAb stability has been explained in detail. The authors hope that this article provides a detailed understanding about stability of mAb due to thermal and air/liquid interfacial stress with relevance to product life cycle from manufacturing to administration into patients.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346651","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

Advancements in photoacoustic imaging for cancer diagnosis and treatment 用于癌症诊断和治疗的光声成像技术取得进展。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-24 DOI: 10.1016/j.ijpharm.2024.124736

{"title":"Advancements in photoacoustic imaging for cancer diagnosis and treatment","authors":"","doi":"10.1016/j.ijpharm.2024.124736","DOIUrl":"10.1016/j.ijpharm.2024.124736","url":null,"abstract":"<div><div>Photoacoustic imaging provides in vivo morphological and functional information about tumors within surrounding tissue. By integrating ultrasound guidance, this technique enables precise localization and characterization of tumors. Moreover, the introduction of targeted contrast agents has further expanded the capabilities of photoacoustic imaging in the realm of in vivo molecular imaging. These contrast agents facilitate enhanced molecular and cellular characterization of cancer, enabling detailed insights into the disease. This review aims to provide a concise summary of the extensive research conducted in the field of Photoacoustic imaging for cancer management. It encompasses the development of the technology, its applications in clinical settings, and the advancements made in molecular imaging. By consolidating and synthesizing the existing knowledge, this review contributes to a better understanding of the potential of photoacoustic imaging in cancer care. In conclusion, photoacoustic imaging has emerged as a non-ionizing and noninvasive modality with the ability to visualize tissue’s optical absorption properties while maintaining ultrasound’s spatial resolution. Its integration with targeted contrast agents has enhanced molecular and cellular characterization of cancer. This review serves as a succinct overview of the extensive research conducted in the field, shedding light on the potential of photoacoustic imaging in the management of cancer.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346646","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

Microtubular and high porosity design of electrospun PEGylated poly (lactic-co-glycolic acid) fibrous implant for ocular multi-route administration and medication 用于眼部多途径给药和用药的电纺聚乙二醇化聚（乳酸-共聚-乙醇酸）纤维植入物的微管和高孔隙率设计。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-24 DOI: 10.1016/j.ijpharm.2024.124751

{"title":"Microtubular and high porosity design of electrospun PEGylated poly (lactic-co-glycolic acid) fibrous implant for ocular multi-route administration and medication","authors":"","doi":"10.1016/j.ijpharm.2024.124751","DOIUrl":"10.1016/j.ijpharm.2024.124751","url":null,"abstract":"<div><div>Electrospun fibers have been gaining popularity in ocular drug delivery and cellular therapies. However, most of electrospun fibers are planar-shape membrane with large dimension relative to intraocular space, making difficult to use as therapeutic implants. Herein, fibrous microtubes with a hollow center were fabricated by electrospinning using linear diblock mPEG<sub>2000</sub>-PLGA. Uniform microfibers with 0.809 μm diameter was tailored using Box-Behnken Design model for electrospinning process optimization. The microtubes were 1 mm long with a 0.386 mm diameter. Their suitability for intraocular administration was demonstrated by both injection <em>via</em> a 22-gauge needle and implant <em>via</em> integration of intraocular lens into the vitreous or anterior chamber of eyes, respectively. Electrospun mPEG<sub>2000</sub>-PLGA had higher porosity, smaller specific surface area, and smaller water contact angle, than that of PLGA. Macroscopically, mPEG<sub>2000</sub>-PLGA microfibers can maintain overall geometry upon exposure to aqueous buffer for 12 h while having high water uptake and exhibited good elasticity. Hydrolysis with 90 % polymeric degradation in 10.5 weeks underlied sustained slow release of anti-inflammatory drug dexamethasone. PEGylation of PLGA imparted preferential cell adhesion with markedly higher growth of human retinal epithelial cells than lens epithelial ones. This study highlights the potential utility of implantable electrospun PLGA-based microtubes for multiple intraocular delivery routes.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346648","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

Mesenchymal stem cell-delivered paclitaxel nanoparticles exhibit enhanced efficacy against a syngeneic orthotopic mouse model of pancreatic cancer 间充质干细胞递送的紫杉醇纳米粒子显示出更强的抗胰腺癌同种异体小鼠模型的疗效。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-24 DOI: 10.1016/j.ijpharm.2024.124753

{"title":"Mesenchymal stem cell-delivered paclitaxel nanoparticles exhibit enhanced efficacy against a syngeneic orthotopic mouse model of pancreatic cancer","authors":"","doi":"10.1016/j.ijpharm.2024.124753","DOIUrl":"10.1016/j.ijpharm.2024.124753","url":null,"abstract":"<div><div>Pancreatic cancer is considered the deadliest among various solid tumors, with a five-year survival rate of 13 %. One of the major challenges in the management of advanced pancreatic cancer is the inefficient delivery of chemotherapeutics to the tumor site. Even though nanocarriers have been developed to improve tumoral delivery of chemotherapeutics, less than 1 % of the drugs reach tumors, rendering inadequate concentration for effective inhibition of tumors. As a potential alternative, mesenchymal stem cells (MSCs) can effectively deliver their cargo to tumor sites because of their resistance to chemotherapeutics and inherent tumor tropism. In this study, we used MSCs for the delivery of dibenzocyclooctyne (DBCO)-functionalized paclitaxel (PTX)-loaded poly(lactide-co-glycolide)-b-poly (ethylene glycol) (PLGA) nanoparticles. MSCs were modified to generate artificial azide groups on their surface, allowing nanoparticle loading via endocytosis and surface conjugation via click chemistry. This dual drug loading strategy significantly improves the PTX-loading capacity of azide-expressed MSCs (MSC-Az, 55.4 pg/cell) compared to unmodified MSCs (28.1 pg/cell). The in vitro studies revealed that PTX-loaded MSC-Az, nano-MSCs, exhibited cytotoxic effects against pancreatic cancer without altering their inherent phenotype, differentiation abilities, and tumor tropism. In an orthotopic pancreatic tumor model, nano-MSCs demonstrated significant inhibition of tumor growth (p < 0.05) and improved survival (p < 0.0001) compared to PTX solution, PTX nanocarriers, and Abraxane. Thus, nano-MSCs could be an effective delivery system for targeted pancreatic cancer chemotherapy and other solid tumors.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346654","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

Detailed accounts of segregation mechanisms and the evolution of pharmaceutical blend segregation analysis: A review 详细介绍药物混合物的偏析机制和偏析分析的演变：综述。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-23 DOI: 10.1016/j.ijpharm.2024.124739

{"title":"Detailed accounts of segregation mechanisms and the evolution of pharmaceutical blend segregation analysis: A review","authors":"","doi":"10.1016/j.ijpharm.2024.124739","DOIUrl":"10.1016/j.ijpharm.2024.124739","url":null,"abstract":"<div><div>Segregation refers to the separation of components in a powder mixture, resulting in potential issues related to concentration inhomogeneity. Any well-mixed blend that undergoes secondary processing is inherently susceptible to segregation which, if unmitigated, will lead to active compound concentration variance and poorer product quality. The consequences range from adverse financial impact to manufacturers with product failures to the detrimental health effects to product users. Hence, the topic of segregation is of paramount importance to the industry, requiring it to be dissected and scrutinized intensively by scientists worldwide. This review provides a well-crafted theoretical framework designed to understand the common segregation mechanisms that manufacturing facilities face, followed by the efforts to gauge the degree of segregation. To minimize segregation in blends, various approaches – mathematical modeling, empirical experiments, and empirical methods with modeling consideration – have been utilized in segregation research and are covered in this review. The past segregation studies from many fields are discussed, with particular emphasis on pharmaceuticals. The review also discusses the evolution and advances in mixing technology and storage systems implemented by the pharmaceutical industry to prevent segregation. In the conclusion, the authors articulated their perspectives on potential mitigation measures, including suggestions for improvements and future studies.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346633","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

Nanotechnology based drug delivery systems for malaria 基于纳米技术的疟疾药物输送系统。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-23 DOI: 10.1016/j.ijpharm.2024.124746

{"title":"Nanotechnology based drug delivery systems for malaria","authors":"","doi":"10.1016/j.ijpharm.2024.124746","DOIUrl":"10.1016/j.ijpharm.2024.124746","url":null,"abstract":"<div><div>Malaria, caused by <em>Plasmodium</em> parasites transmitted through Anopheles mosquitoes, remains a global health burden, particularly in tropical regions. The most lethal species, <em>Plasmodium falciparum</em> and <em>Plasmodium vivax</em>, pose significant threats to human health. Despite various treatment strategies, malaria continues to claim lives, with Africa being disproportionately affected. This review explores the advancements in drug delivery systems for malaria treatment, focusing on polymeric and lipid-based nanoparticles. Traditional antimalarial drugs, while effective, face challenges such as toxicity and poor bio-distribution. To overcome these issues, nanocarrier systems have been developed, aiming to enhance drug efficacy, control release, and minimize side effects. Polymeric nanocapsules, dendrimers, micelles, liposomes, lipid nanoparticles, niosomes, and exosomes loaded with antimalarial drugs are examined, providing a comprehensive overview of recent developments in nanotechnology for malaria treatment. The current state of antimalarial treatment, including combination therapies and prophylactic drugs, is discussed, with a focus on the World Health Organization’s recommendations. The importance of nanocarriers in malaria management is underscored, highlighting their role in targeted drug delivery, controlled release, and improved pharmacological properties. This review bridges the gap in the literature, consolidating the latest advancements in nanocarrier systems for malaria treatment and offering insights into potential future developments in the field.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346655","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

A nanotechnology driven effectual localized lung cancer targeting approaches using tyrosine kinases inhibitors: Recent progress, preclinical assessment, challenges, and future perspectives 使用酪氨酸激酶抑制剂的纳米技术驱动的有效局部肺癌靶向方法：最新进展、临床前评估、挑战和未来展望。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-23 DOI: 10.1016/j.ijpharm.2024.124745

{"title":"A nanotechnology driven effectual localized lung cancer targeting approaches using tyrosine kinases inhibitors: Recent progress, preclinical assessment, challenges, and future perspectives","authors":"","doi":"10.1016/j.ijpharm.2024.124745","DOIUrl":"10.1016/j.ijpharm.2024.124745","url":null,"abstract":"<div><div>The higher incidence and mortality rate among all populations worldwide explains the unmet solutions in the treatment of lung cancer. The evolution of targeted therapies using tyrosine kinase inhibitors (TKI) has encouraged anticancer therapies. However, on-target and off-target effects and the development of drug resistance limited the anticancer potential of such targeted biologics. The advances in nanotechnology-driven-TKI embedded carriers that offered a new path toward lung cancer treatment. It is the inhalation route of administration known for its specific, precise, and efficient drug delivery to the lungs. The development of numerous TKI-nanocarriers through inhalation is proof of TKI growth. The future scopes involve using potential lung cancer biomarkers to achieve localized active cancer-targeting strategies. The adequate knowledge of <em>in vitro</em> absorption models usually helps establish better <em>in vitro − in vivo</em> correlation/extrapolation (IVIVC/E) to successfully evaluate inhalable drugs and drug products. The advanced <em>in vitro</em> and <em>ex vivo</em> lung tissue/ organ models offered better tumor heterogeneity, etiology, and microenvironment heterogeneity. The involvement of lung cancer organoids (LCOs), human organ chip models, and genetically modified mouse models (GEMMs) has resolved the challenges associated with conventional <em>in vitro</em> and <em>in vivo</em> models. To access potential inhalation-based drugtherapies, biological barriers, drug delivery, device-based challenges, and regulatory challenges must be encountered associated with their development. A proper understanding of material toxicity, size-based particle deposition at active disease sites, mucociliary clearance, phagocytosis, and the presence of enzymes and surfactants are required to achieve successful inhalational drug delivery (IDD). This article summarizes the future of lung cancer therapy using targeted drug-mediated inhalation using TKI.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346623","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

Copper-based metal–organic framework co-loaded doxorubicin and curcumin for anti-cancer with synergistic apoptosis and ferroptosis therapy 铜基金属有机框架共同负载多柔比星和姜黄素，可协同凋亡和铁凋亡疗法抗癌。

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-22 DOI: 10.1016/j.ijpharm.2024.124744

{"title":"Copper-based metal–organic framework co-loaded doxorubicin and curcumin for anti-cancer with synergistic apoptosis and ferroptosis therapy","authors":"","doi":"10.1016/j.ijpharm.2024.124744","DOIUrl":"10.1016/j.ijpharm.2024.124744","url":null,"abstract":"<div><div>The combination of chemotherapy and ferroptosis therapy can greatly improve the efficiency of tumor treatment. However, ferroptosis-based therapy is limited by the unsatisfactory Fenton activity and insufficient H<sub>2</sub>O<sub>2</sub> supply in tumor cells. In this work, a nano-drug delivery system Cur@DOX@MOF-199 NPs was constructed to combine ferroptosis and apoptosis by loading curcumin (Cur) and doxorubicin (DOX) based on the copper-based organic framework MOF-199. Cur@DOX@MOF-199 NPs decompose quickly by glutathione (GSH), releasing Cu<sup>2+</sup>, DOX and Cur. Cu<sup>2+</sup> can deplete GSH while also being reduced to Cu<sup>+</sup>; DOX can induce apoptosis and simultaneously boost H<sub>2</sub>O<sub>2</sub> production. Moreover, Cur enhanced the expression of intracellular heme oxygenase-1 (HO-1), for decomposing heme and releasing Fe<sup>2+</sup>, which further combined with Cu<sup>+</sup> to catalyze H<sub>2</sub>O<sub>2</sub> for hydroxyl radical (<sup><img></sup>OH) generation, leading to the accumulation of lipid peroxide and ferroptosis. As a result, Cur@DOX@MOF-199 NPs exhibited significantly enhanced antitumor efficacy in MCF-7 tumor-bearing mouse model, suggesting this nano formulation is an excellent synergetic pathway for apoptosis and ferroptosis.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142346629","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

Oregano essential oil-infused mucin microneedle patch for the treatment of hypertrophic scar 牛至精油注入粘蛋白微针贴片用于治疗增生性瘢痕

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-22 DOI: 10.1016/j.ijpharm.2024.124748

{"title":"Oregano essential oil-infused mucin microneedle patch for the treatment of hypertrophic scar","authors":"","doi":"10.1016/j.ijpharm.2024.124748","DOIUrl":"10.1016/j.ijpharm.2024.124748","url":null,"abstract":"<div><div>Hypertrophic scar (HS) manifests as abnormal dermal myofibroblast proliferation and excessive collagen deposition, leading to raised scars and significant physical, psychological, and financial burdens for patients. HS is difficult to cure in the clinic and current therapies lead to recurrence, pain, and side effects. In this study, a natural amphiphilic polymer mucin is used to prepare a dissolving microneedle (muMN) that is loaded with oregano essential oil (OEO) for HS therapy. muMN exhibits sufficient skin/scar tissue penetration, quick skin recovery time after removal, good loading of natural essential oil, fast dissolution and detachment from the base layer, and good biocompatibility to applied skin. In the rabbit HS model, OEO@muMN shows a significant reduction in scar thickness, epidermal thickness index, and scar elevation index. OEO@muMN also attenuates the mean collagen area fraction and decreases the number of capillaries in scar tissues. Biochemical Assay reveals that OEO@muMN significantly inhibits the expression of transforming growth factor-β1 (TGF-β1) and hydroxyproline (HYP). In summary, this study demonstrates the feasibility and good efficacy of using the anti-proliferative and anti-oxidative OEO for HS treatment. OEO@muMN is an efficient formulation that holds the potential for clinical anti-HS application. muMN is an efficient platform to load and apply essential oils transdermally.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142323749","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

Polymer nanotherapeutics with the controlled release of acetylsalicylic acid and its derivatives inhibiting cyclooxygenase isoforms and reducing the production of pro-inflammatory mediators 可控释放乙酰水杨酸及其衍生物的聚合物纳米疗法，抑制环氧化酶同工酶并减少促炎介质的产生

IF 5.3 2区医学

International Journal of Pharmaceutics Pub Date : 2024-09-22 DOI: 10.1016/j.ijpharm.2024.124742

{"title":"Polymer nanotherapeutics with the controlled release of acetylsalicylic acid and its derivatives inhibiting cyclooxygenase isoforms and reducing the production of pro-inflammatory mediators","authors":"","doi":"10.1016/j.ijpharm.2024.124742","DOIUrl":"10.1016/j.ijpharm.2024.124742","url":null,"abstract":"<div><div>The effective treatment of inflammatory diseases, particularly their chronic forms, is a key task of modern medicine. Herein, we report the synthesis and evaluation of biocompatible polymer conjugates based on <em>N</em>-2-(hydroxypropyl)methacrylamide copolymers enabling the controlled release of acetylsalicylic acid (ASA)-based anti-inflammatory drugs under specific stimuli. All polymer nanotherapeutics were proposed as water-soluble drug delivery systems with a hydrodynamic size below 10 nm ensuring suitability for the parenteral application and preventing opsonization by the reticuloendothelial system. The nanotherapeutics bearing an ester-bound ASA exhibited long-term release of the ASA/salicylic acid mixture, while the nanotherapeutics carrying salicylic acid hydrazide (SAH) ensured the selective release of SAH in the acidic inflammatory environment thanks to the pH-sensitive hydrazone bond between the polymer carrier and SAH. The ASA- and SAH-containing nanotherapeutics inhibited both cyclooxygenase isoforms and/or the production of pro-inflammatory mediators. Thanks to their favorable design, they can preferentially accumulate in the inflamed tissue, resulting in reduced side effects and lower dosage, and thus more effective and safer treatment.</div></div>","PeriodicalId":14187,"journal":{"name":"International Journal of Pharmaceutics","volume":null,"pages":null},"PeriodicalIF":5.3,"publicationDate":"2024-09-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142323750","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