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High Flavonoid Content in Apium graveolens Nanocrystals Improves Colitis in Dextran Sodium Sulfate-induced Colitis Mice. 高黄酮含量的荆芥纳米晶体改善右旋糖酐硫酸钠诱导结肠炎小鼠的结肠炎。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-05-12 DOI: 10.2174/0122117385358037250415034215
Verda Farida, Chandra Saputra, Ardian Dewangga, Widi Kurniawan, Muhammad Novrizal Abdi Sahid, Cornelia M Keck

Aim: To develop medicinal plant nanoparticles as colitis alternative/supplementary therapy.

Background: Limited reports exist on the effectiveness of medicinal plant nanocrystals in treating or preventing colitis.

Objectives: We investigated the effect of canonizing Apium graveolens (AG) on improving dextran sodium sulfate (DSS)- induced (4%) colitis.

Methods: Nanonization was performed via the bead milling process. The nanocrystal product was characterized (i.e., particle size, zeta potential (ZP), polydispersity index (PDI) values) and freezedried. Total flavonoids and phenolic compounds in nanocrystal products were compared with ethanolic extract of AG (AGEE). Anti-colitis activity of AG-nanocrystal water suspensions (AGNS) was compared to AG bulk powder suspensions (AGBS). Colitis severity was determined via physiological, macroscopic, and microscopic colon assessment. In addition, the fecal Enterobacteriaceae population and urine glucose levels were determined.

Results: The AG nanoparticle products are 200-400 nm, with PDI values 0.5-0.6, and ZP values -12 to -20 mV. The total flavonoid and phenolic compounds of AGNS were 115.12±4.32 ppm and 37.11±0.34 ppm, respectively. This value is higher compared to the content in AGEE. AGNS (350 mg/kg) improves physiological (i.e., fecal blood), macroscopic (i.e., length, diameter), and microscopic (i.e., structure and immune cell infiltration) colon conditions in a comparable level to the positive control of 5-aminosalicylic acid (100 mg/kg). AGNS have a compelling ability to restore colon microscopic and Enterobacteriaceae population compared to AGBS (700 mg/kg). AGNS (350 mg/kg) also recovered colon permeability as marked by the lower urine glucose concentration (9.90±0.15 mg/dL) compared to colitis mice (12.43±0.09 mg/dL).

Conclusion: The nanonization of AG contributes to improved anti-colitis activities compared to AGBS. Nanonization of medicinal plants will reduce organic solvent extraction, which supports the sustainable development goals.

目的:开发药用植物纳米颗粒作为结肠炎的替代/补充疗法。背景:关于药用植物纳米晶体治疗或预防结肠炎的有效性的报道有限。目的:观察加药荆芥(AG)对右旋糖酐硫酸钠(DSS)所致(4%)结肠炎的改善作用。方法:采用磨粒法进行纳米化。对纳米晶产物进行了表征(即粒径、ζ电位(ZP)、多分散性指数(PDI)值)并进行了冷冻。比较了AG乙醇提取物纳米晶产品中总黄酮和酚类化合物的含量。比较了AG纳米晶水悬浮液(AGNS)与AG散装粉末悬浮液(AGBS)的抗结肠炎活性。结肠炎的严重程度通过生理、宏观和微观结肠评估来确定。此外,还测定了粪便肠杆菌科菌群和尿糖水平。结果:制备的AG纳米颗粒粒径为200 ~ 400 nm, PDI值为0.5 ~ 0.6,ZP值为-12 ~ -20 mV。AGNS总黄酮和酚类化合物含量分别为115.12±4.32 ppm和37.11±0.34 ppm。该值高于AGEE中的含量。AGNS (350 mg/kg)将生理(即粪血)、宏观(即长度、直径)和微观(即结构和免疫细胞浸润)结肠状况改善到与5-氨基水杨酸阳性对照(100 mg/kg)相当的水平。与AGBS (700 mg/kg)相比,AGNS具有令人信服的恢复结肠显微和肠杆菌科种群的能力。与结肠炎小鼠(12.43±0.09 mg/dL)相比,AGNS (350 mg/kg)也能恢复结肠通透性(9.90±0.15 mg/dL)。结论:与AGBS相比,AG纳米化有助于提高抗结肠炎活性。药用植物的纳米化将减少有机溶剂提取,有利于实现可持续发展目标。
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引用次数: 0
Nanosponge Fortified Ciclopirox-Olamine for Antifungal Efficacy with Improved Topical Delivery. 纳米海绵强化环匹罗-奥拉明抗真菌效果与改善局部给药。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-05-05 DOI: 10.2174/0122117385363568250417003059
Megha Gupta, Kuldeep Vinchurkar, Dinesh Mishra, Pankaj Dixit, Sheetal Mane, Sudarshan Singh, Pooja V Nagime
<p><strong>Background: </strong>Topical drug delivery systems are most promising in the management of fungal skin infections; however, they often face challenges to achieve therapeutic efficacy due to low solubility, particle size, molecular weight, and skin barriers. In this regard, nanosponge [NS] offers a novel solution with its three-dimensional porous networks, enhancing drug solubility, bioavailability, and providing prolonged release.</p><p><strong>Objective: </strong>The aim of this study was to develop NS fortified with Ciclopirox olamine [CPO] with enhanced drug solubility, prolonged targeted delivery, and improved therapeutic efficacy for the management of fungal skin infections.</p><p><strong>Method: </strong>CPO-loaded ethyl cellulose and polyvinyl alcohol NS were synthesized using the emulsion solvent technique and subsequently evaluated for particle size, surface morphology through scanning electron microscopy [SEM], polydispersity index [PDI], zeta potential [ZP], entrapment efficiency [EE %], drug loading [DL %], drug-excipient interactions via differential scanning calorimetry, and in vitro dissolution studies. Furthermore, the antifungal test was conducted to assess the inhibitory effect on fungal growth.</p><p><strong>Results: </strong>The optimized formulation using ethyl cellulose and polyvinyl alcohol at 1.75 mg and 2 mg, respectively, emerged as the most effective, with a particle size of 526.1 nm and PDI of 0.332, indicating a uniform distribution. Moreover, the formulation demonstrated a high drug loading efficiency and sustained drug release over a 7 h period, achieving a drug release of 77.83 %. The pH of the gel formulations ranged from 5.35 to 7.40, the viscosity ranged from 3759 to 4710 cps, and the spreadability was adequate for topical application. Additionally, the optimized NS exhibited superior antifungal activity against Candida albicans and Aspergillus Niger, compared to drug alone and commercial fungicidal creams. Moreover, the in vitro studies confirmed the gel's effectiveness and its ability to sustain drug release, following Higuchi kinetics.</p><p><strong>Conclusion: </strong>The formulated CPO-loaded NS gels exhibit enhanced solubility, stability, and sustained drug release, significantly improving topical drug delivery with exceptional therapeutic efficacy. This novel approach underscores the potential of NSs for efficient and targeted medication delivery in both the pharmaceutical and cosmetic industries. Furthermore, their effective preparation method, excellent physicochemical properties, and antifungal activity make NSs a promising strategy for the oral delivery of poorly soluble drugs. The fungal skin infections are generally not serious but can be uncomfortable and persistent. With proper hygiene and appropriate treatment, most infections can be effectively managed. Therefore, understanding the types of fungi involved and recognizing symptoms early with an effective delivery system can lead to qu
背景:局部给药系统在真菌皮肤感染的治疗中最有前途;然而,由于低溶解度、粒径、分子量和皮肤屏障等原因,它们在达到治疗效果时经常面临挑战。在这方面,纳米海绵[NS]提供了一种新的解决方案,其三维多孔网络,提高药物的溶解度,生物利用度,并提供延长释放。目的:本研究的目的是开发添加环匹罗胺[CPO]的NS,增强药物溶解度,延长靶向给药时间,提高治疗真菌皮肤感染的疗效。方法:采用乳化溶剂法合成cpo负载的乙基纤维素和聚乙烯醇NS,并对其粒径、扫描电镜(SEM)表面形貌、多分散指数(PDI)、ζ电位(ZP)、包封效率(EE %)、载药量(DL %)、差示扫描量热法与赋形剂相互作用以及体外溶出度进行评价。此外,还进行了抗真菌试验,以评估其对真菌生长的抑制作用。结果:以乙基纤维素和聚乙烯醇分别为1.75 mg和2 mg的优化配方效果最佳,粒径为526.1 nm, PDI为0.332,分布均匀。此外,该制剂具有较高的载药效率和7 h的缓释时间,释药率为77.83%。凝胶制剂的pH值为5.35 ~ 7.40,粘度为3759 ~ 4710 cps,涂抹性适合外用。此外,优化后的NS对白色念珠菌和黑曲霉的抗真菌活性优于单独用药和市售杀菌剂。此外,体外研究证实了凝胶的有效性和维持药物释放的能力,遵循Higuchi动力学。结论:制备的cpo负载NS凝胶具有较好的溶解度、稳定性和药物缓释能力,显著改善了局部给药,具有良好的治疗效果。这种新颖的方法强调了NSs在制药和化妆品行业有效和有针对性的药物输送方面的潜力。此外,其有效的制备方法、优异的物理化学性质和抗真菌活性使NSs成为一种很有前途的口服难溶性药物的策略。真菌性皮肤感染通常不严重,但可能会感到不舒服和持续。通过适当的卫生和适当的治疗,大多数感染可以得到有效控制。因此,了解所涉及的真菌类型,并通过有效的输送系统及早识别症状,可以更快地恢复和复发。cpololoaded NS的开发代表了局部抗真菌治疗的一个有希望的进展。通过改善药物传递和疗效,这种创新配方可以显著提高真菌感染患者的治疗效果。此外,临床研究将是必要的,以验证这些发现,并探索潜在的应用在更广泛的皮肤病学背景。
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引用次数: 0
Nano Milling Application of Mutamba (West Indian Elm) Leaves Extract to Enhance its In vitro Bioactivity. 西印度榆树叶提取物纳米研磨提高其体外生物活性
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-04-29 DOI: 10.2174/0122117385338502250417020845
Yuda Prasetya Nugraha, Juniar Kalpika Resmi, Muhammad Luthfi Shidik, Rachmat Mauludin, Muhamad Insanu, Sophi Damayanti, Benny Permana, Siti Farah Rahmawati, Neng Fisheri Kurniati, Nizar Happyana, Ade Danova, Heni Rachmawati

Background: Guazuma ulmifolia or mutamba has been traditionally used for many years as a slimming agent. Various studies reported the antihyperlipidemic activity of mutamba leaves extract due to its flavonoid content.

Objective: This research was conducted to improve the bioactivity of mutamba leaves extract by applying ball-milling technology.

Methods: Unground dried mutamba leaves were extracted in ethanol 40%. The resulting extract (ME) was nano-milled and characterized for its physicochemical parameters. The ball milling process was optimized by performing in various durations, ball and powder ratios, and rotation speed.

Results: The optimized process of ball milling produced nano-extract (NanoME) with a particle size of 492,57±55,96 nm, confirmed with particle size and SEM. Compared with ME, the crystallinity and thermal behavior of NanoME did not change by particle size reduction. The reduction of particle size also did not improve the HMG-CoA reductase inhibitor activity. ME and NanoME showed comparable activity compared to Pravastatin. However, the bioactivities of NanoME, including DPPH antioxidant activities, improved 8-fold compared to ME.

Conclusion: The improvement of these activities was attributed to the increase in their flavonoid content. This study emphasizes the role of particle size reduction or nano-extract preparation in increasing the biological activity of plant extracts.

背景:番石榴作为一种减肥剂已经使用了很多年。各种研究报道了由于黄酮类化合物的含量而产生的抗高脂血症活性。目的:采用球磨工艺提高木犀叶提取物的生物活性。方法:用40%乙醇提取未研磨的干木叶。对所得提取物(ME)进行了纳米研磨,并对其理化参数进行了表征。在不同的时间、球粉比和转速下对球磨工艺进行了优化。结果:优化后的球磨工艺制备的纳米提取物(NanoME)粒径分别为492、57±55、96 nm,经粒度和扫描电镜验证。与ME相比,纳米ome的结晶度和热行为不受粒径减小的影响。颗粒大小的减小也没有提高HMG-CoA还原酶抑制剂的活性。与普伐他汀相比,ME和NanoME的活性相当。然而,NanoME的生物活性,包括抗DPPH活性,比ME提高了8倍。结论:这些活性的提高与黄酮类化合物含量的增加有关。本研究强调了减小颗粒尺寸或纳米提取物制备在提高植物提取物生物活性方面的作用。
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引用次数: 0
Advanced Preparation Techniques for Polymeric Nanoparticles and their Application in Drug Delivery. 高分子纳米颗粒的先进制备技术及其在药物传递中的应用。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-04-15 DOI: 10.2174/0122117385366838250314110525
Harish Bhardwaj, Soniya Sarthi, Rajendra Kumar Jangde

Nanotechnology has advanced significantly in recent decades, with the production and design of nanomaterials becoming a focal point of research. Nanomedicine, a key component of this field, involves the development of nanoscale materials for applications in imaging and drug delivery. Current research predominantly focuses on the synthesis of precisely characterized nanomaterials, particularly in terms of their size and morphology, as these parameters play a critical role in determining the behavior of nanomaterials in vivo. This paper reviews various methods for the preparation of polymeric nanoparticles, including solvent evaporation, nanoprecipitation, emulsification/ solvent diffusion, salting out, dialysis, supercritical fluid technology (SCF), and monomer polymerization techniques. Additionally, it discusses approaches such as emulsion, mini-emulsion, microemulsion, interfacial polymerization, controlled/living radical polymerization, and ionic gelation/ coacervation. Each preparation method is described in terms of its characteristics, advantages, limitations, and potential applications. The paper also explores pharmaceutical considerations and challenges associated with novel drug delivery systems. Recent literature examples are presented to highlight the impact of preparation techniques on the physicochemical properties of nanoparticles.

近几十年来,纳米技术取得了显著的进步,纳米材料的生产和设计成为研究的焦点。纳米医学是该领域的一个关键组成部分,涉及开发用于成像和药物输送的纳米级材料。目前的研究主要集中在精确表征纳米材料的合成上,特别是在它们的尺寸和形态方面,因为这些参数在决定纳米材料在体内的行为方面起着关键作用。本文综述了制备纳米聚合物的各种方法,包括溶剂蒸发、纳米沉淀、乳化/溶剂扩散、盐析、透析、超临界流体技术(SCF)和单体聚合技术。此外,还讨论了乳液、微乳液、微乳液、界面聚合、可控/活性自由基聚合和离子凝胶/凝聚等方法。介绍了每种制备方法的特点、优点、局限性和潜在应用。本文还探讨了与新型药物输送系统相关的药学考虑和挑战。最近的文献举例,以强调制备技术对纳米粒子的物理化学性质的影响。
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引用次数: 0
Advancements in Nanoparticle-Based Targeted Drug Delivery Systems for Breast Cancer. 基于纳米颗粒的乳腺癌靶向药物递送系统的研究进展。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-03-11 DOI: 10.2174/0122117385339882241206095441
Roshni Kunte, Prafulla Sabale, Suchita Waghmare, Manasi Nikam Jiwankar, Vidya Sabale

Cancer is a leading cause of death and life-threatening disease globally. It is connected to persistent tissue damage and unregulated cellular proliferation. In females, breast cancer plays a crucial role in death rates. Chemotherapy, alongside surgery, radiation, and hormone therapy, is a first-line treatment, but its non-specific action harms both cancerous and healthy cells, causing severe side effects. The treatment options for breast cancer are based on the disease stage, which spans from stages 0 to IV. To mitigate this issue, novel strategies focusing on specific targets have been introduced in recent times. Advanced nanocarriers are focused on tumor-specific drug delivery using active targeting based on ligand-receptor identification, this approach has the potential to demonstrate enhanced efficacy compared to passive targeting strategies in the context of therapy for human breast cancer. Surface alteration can assist overcome this issue. This overview focuses on modified nano-sized carriers, including liposomes, micelles, polymeric nanocarriers, carbon dots, and gold nanoparticles. It has been studied to improve therapeutics efficacy, bioavailability, and pharmacokinetics features via mechanisms. The primary aim is no longer confined to merely enveloping cancer medications in novel formulations for diverse delivery pathways; instead, the emphasis lies on precise cancer targeting. This review focuses on the stages of breast cancer, obstacles, types of breast cancer therapies, techniques, and various nanocarriers using ligand-mediated drug delivery systems and their mechanisms.

在全球范围内,癌症是导致死亡和危及生命的主要疾病。它与持续的组织损伤和不受调节的细胞增殖有关。在女性中,乳腺癌在死亡率中起着至关重要的作用。化疗与手术、放疗和激素治疗一样,都是一线治疗方法,但其非特异性作用对癌细胞和健康细胞都有伤害,会产生严重的副作用。乳腺癌的治疗选择基于疾病阶段,从0期到4期。为了缓解这一问题,近年来引入了针对特定目标的新策略。先进的纳米载体专注于基于配体受体识别的肿瘤特异性药物递送,与被动靶向策略相比,这种方法在治疗人类乳腺癌方面具有增强疗效的潜力。地表改造可以帮助克服这个问题。本文综述了改性纳米级载体,包括脂质体、胶束、聚合物纳米载体、碳点和金纳米颗粒。它已被研究通过机制来提高治疗效果、生物利用度和药代动力学特征。主要目标不再仅仅局限于将癌症药物包裹在不同递送途径的新配方中;相反,重点在于精确的癌症靶向。本文综述了乳腺癌的分期、障碍、乳腺癌治疗的类型、技术以及使用配体介导的药物传递系统的各种纳米载体及其机制。
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引用次数: 0
Nano Drug Delivery Carriers (Nanocarriers): A Promising Targeted Strategy in Tuberculosis and Pain Treatment. 纳米药物递送载体(纳米载体):在结核病和疼痛治疗中有前景的靶向策略。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-03-07 DOI: 10.2174/0122117385367493250224103839
Rahul Pal, Prachi Pandey, Himmat Singh Chawra, Zuber Khan

Background: Tuberculosis (TB) and chronic pain are global health concerns that affect millions of people, often requiring long-term, effective treatment strategies. The conventional therapies used to manage these conditions come with significant limitations. In TB, long treatment durations, poor compliance, drug resistance, and toxicity of first-line drugs are key challenges. Similarly, pain management faces issues, such as inadequate targeting, systemic side effects, and tolerance to analgesics, limiting traditional therapy efficacy.

Objective: The objective of this review is to explore the potential of nanocarriers as a targeted drug delivery strategy for improving treatment outcomes in TB and pain management. It aims to explore how these advanced systems improve drug bioavailability (BA), control release, reduce side effects, and enhance therapeutic outcomes.

Methods: This systematic review used databases like PubMed, Elsevier, Scopus, Google Scholar, Google Patents, and ResearchGate, etc., to collect original review articles from the past 15 years (September 1, 2007 to September 1, 2024).

Results: The review also revealed that these advanced systems offer promising solutions for overcoming the limitations of conventional therapies, such as poor patient compliance and drug toxicity. Nanocarriers represent a transformative approach in both TB and pain management, with the potential to revolutionize treatment paradigms and improve patient outcomes.

Conclusion: In conclusion, nanocarriers represent a highly promising approach for advancing treatment strategies in both TB and pain management. The review underscores that nanocarrier systems, such as nanoemulsion, nanosuspension, nanocrystal, liposomes, niosomes, dendrimer, and polymeric nanoparticles, offer substantial improvements in drug delivery by enhancing BA, ensuring targeted release, and reducing systemic side effects.

背景:结核病和慢性疼痛是影响数百万人的全球健康问题,往往需要长期有效的治疗策略。用于治疗这些疾病的传统疗法有很大的局限性。在结核病方面,治疗时间长、依从性差、耐药性和一线药物的毒性是主要挑战。同样,疼痛管理也面临着一些问题,如靶向性不足、全身副作用和对镇痛药的耐受性,限制了传统疗法的疗效。目的:本综述的目的是探索纳米载体作为一种靶向药物递送策略的潜力,以改善结核病和疼痛管理的治疗结果。它旨在探索这些先进的系统如何提高药物生物利用度(BA),控制释放,减少副作用,并提高治疗效果。方法:本系统综述使用PubMed、Elsevier、Scopus、谷歌Scholar、谷歌Patents、ResearchGate等数据库,收集近15年来(2007年9月1日至2024年9月1日)的原创综述文章。结果:综述还显示,这些先进的系统为克服常规治疗的局限性提供了有希望的解决方案,例如患者依从性差和药物毒性。纳米载体代表了结核病和疼痛管理的一种变革性方法,具有彻底改变治疗范例和改善患者预后的潜力。结论:总之,纳米载体代表了一种非常有前途的方法来推进结核病和疼痛管理的治疗策略。该综述强调,纳米载体系统,如纳米乳、纳米悬浮液、纳米晶体、脂质体、乳质体、树状大分子和聚合物纳米颗粒,通过增强BA、确保靶向释放和减少全身副作用,在药物传递方面提供了实质性的改进。
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引用次数: 0
Revealing the Antidiabetic Potential of Herbal Nanoparticles. 揭示草药纳米颗粒的抗糖尿病潜力。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-02-20 DOI: 10.2174/0122117385357690250214072827
Kunal Datta, Soubhik Bhattacharyya, Christina Narzary, Reshmi Mukherjee, Angana Naskar, Shazma Imam, Subarno Chakraborty, Dhrubajyoti Sarkar

Diabetes is a chronic metabolic disorder that is characterized by high postprandial blood sugar levels and increased fasting, which disrupts physiological balance and causes organ damage. Owing to the global health risk of type 2 diabetes, natural remedies have shown promise as viable alternatives because of their outstanding antidiabetic properties. Nevertheless, the therapeutic use of these compounds is rather restricted due to their inadequate solubility, instability in the gastrointestinal tract, low absorption, and other related factors. Currently, the development of nanoscale systems is a notable approach to enhancing the delivery of phytochemicals. This study aims to investigate the advancements in drug delivery techniques using nanoparticles, with a particular focus on enhancing the effectiveness of herbal remedies in the treatment of diabetes. This study aims to enrich our understanding of nanotechnology's potential in enlightening drug delivery systems by employing database repositories like PubMed, Scopus, Google Scholar, and Web of Science. Based on their categorization and structure, nano-systems are classified into liposomes, nanostructured lipid carriers, phytosomes, niosomes, solid lipid nanoparticles, self-nano emulsifying drug delivery systems, and inorganic nano-carriers. This study intricately describes the formulation process, selection criteria, and mechanism of herb-loaded nanoparticles using an example of the pharmacokinetic and pharmacodynamic properties of antidiabetic herbal drugs. Researchers have proven that nanoformulations of herb-loaded antidiabetic drugs improve compliance and therapeutic efficacy by resolving pharmacokinetic and biopharmaceutical issues. We could expect the creation of nanoformulations to be a viable method for optimizing the therapeutic effectiveness of plant-produced antidiabetic compounds.

糖尿病是一种慢性代谢性疾病,其特点是餐后血糖水平高,空腹时间增加,破坏生理平衡,造成器官损伤。由于2型糖尿病的全球健康风险,自然疗法因其突出的抗糖尿病特性而显示出作为可行替代方案的希望。然而,由于这些化合物的溶解度不足,在胃肠道中不稳定,吸收低以及其他相关因素,这些化合物的治疗用途相当有限。目前,纳米级系统的发展是提高植物化学物质传递的重要途径。本研究旨在研究纳米颗粒给药技术的进展,特别关注提高草药治疗糖尿病的有效性。本研究旨在通过使用PubMed、Scopus、b谷歌Scholar和Web of Science等数据库,丰富我们对纳米技术在启发药物输送系统方面的潜力的理解。根据其分类和结构,纳米系统分为脂质体、纳米结构脂质载体、磷脂质体、乳质体、固体脂质纳米颗粒、自纳米乳化给药系统和无机纳米载体。本研究以抗糖尿病草药的药代动力学和药效学特性为例,详细描述了草药负载纳米颗粒的制备过程、选择标准和机制。研究人员已经证明,草药抗糖尿病药物的纳米配方通过解决药代动力学和生物制药问题提高了依从性和治疗效果。我们可以期待纳米制剂的创造成为一种可行的方法来优化植物产生的抗糖尿病化合物的治疗效果。
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引用次数: 0
Ameliorating Paraquat-Induced Nephrotoxicity in Rats: Protective Effects of Nanocurcumin on Renal Histology and Molecular Pathways. 改善百草枯引起的大鼠肾毒性:纳米姜黄素对肾脏组织学和分子通路的保护作用。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-02-10 DOI: 10.2174/0122117385361582250112083125
Davood Ahmadi Moghaddam, Mehdi Rahimi, Nejat Kheiripour, Zohre Sadeghian, Sara Soleymani Asl, Zahra Azizi, Akram Ranjbar

Background: Paraquat (PQ) is a common herbicide, and its mortality results from injury to several organs, including the kidneys. Nanocurcumin and curcumin have anti-inflammatory and anti-oxidative activities, but their involvement in PQ-induced kidney damage is unclear. Therefore, the goal of our study was to compare nanocurcumin and curcumin in male rats whose kidneys were damaged by PQ.

Method: 42 eight-week male albino Wistar rats were put into six groups at random as control, control + curcumin, control + nanocurcumin, PQ, PQ + curcumin, PQ + nanocurcumin for 7 days. The kidney tissues and serum were collected at the end of this period. Total antioxidant capacity (TAC), lipid peroxidation (LPO), total thiol Molecule (TTM), urea, creatinine, and blood urea nitrogen (BUN) levels were assessed. The histopathological evaluation of kidney damage was performed at the end of our study. Moreover, the gene expression was assessed by biochemical and Reverse transcription polymerase chain reaction (RT-PCR) analysis.

Result: Curcumin and nanocurcumin administration alleviated PQ-induced renal injury, as evidenced by reduced serum creatinine and BUN levels. The levels of antioxidant markers, like TAC and TTM, increased and decreased the levels of oxidative stress indexes like LPO. Furthermore, our result shows up-regulating the expression of nuclear factor-like 2 (Nrf2), NAD (P) H: quinine oxidoreductase 1 (NQO1), Heme oxygenase 1 (HO-1), and down-regulating the expression of Kelchlike ECH-associated protein 1 (Keap-1) in renal tissue.

Conclusion: Niosomal curcumin was more advantageous than ordinary curcumin in lowering oxidative stress and renal tissue damage induced by paraquat intoxication.

背景:百草枯(PQ)是一种常见的除草剂,其致死性是由于对包括肾脏在内的多个器官的伤害。纳米姜黄素和姜黄素具有抗炎和抗氧化活性,但它们在pq诱导的肾损伤中的作用尚不清楚。因此,我们的研究目的是比较纳米姜黄素和姜黄素在PQ肾损伤的雄性大鼠中的作用。方法:将42只8周龄雄性白化Wistar大鼠随机分为6组,分别为对照组、对照组+姜黄素、对照组+纳米姜黄素、PQ、PQ +姜黄素、PQ +纳米姜黄素,连续7 d。试验结束后采集大鼠肾脏组织及血清。测定总抗氧化能力(TAC)、脂质过氧化(LPO)、总硫醇分子(TTM)、尿素、肌酐和血尿素氮(BUN)水平。在研究结束时进行肾脏损伤的组织病理学评估。此外,通过生化和逆转录聚合酶链反应(RT-PCR)分析来评估基因表达。结果:姜黄素和纳米姜黄素可降低血清肌酐和BUN水平,减轻pq所致的肾损伤。抗氧化标志物(如TAC和TTM)水平升高或降低氧化应激指标(如LPO)水平。此外,我们的研究结果显示,核因子样2 (Nrf2)、NAD (P) H:奎宁氧化还原酶1 (NQO1)、血红素加氧酶1 (HO-1)的表达上调,Kelchlike ECH-associated protein 1 (Keap-1)的表达下调。结论:Niosomal姜黄素比普通姜黄素更有利于降低百草枯中毒引起的氧化应激和肾组织损伤。
{"title":"Ameliorating Paraquat-Induced Nephrotoxicity in Rats: Protective Effects of Nanocurcumin on Renal Histology and Molecular Pathways.","authors":"Davood Ahmadi Moghaddam, Mehdi Rahimi, Nejat Kheiripour, Zohre Sadeghian, Sara Soleymani Asl, Zahra Azizi, Akram Ranjbar","doi":"10.2174/0122117385361582250112083125","DOIUrl":"https://doi.org/10.2174/0122117385361582250112083125","url":null,"abstract":"<p><strong>Background: </strong>Paraquat (PQ) is a common herbicide, and its mortality results from injury to several organs, including the kidneys. Nanocurcumin and curcumin have anti-inflammatory and anti-oxidative activities, but their involvement in PQ-induced kidney damage is unclear. Therefore, the goal of our study was to compare nanocurcumin and curcumin in male rats whose kidneys were damaged by PQ.</p><p><strong>Method: </strong>42 eight-week male albino Wistar rats were put into six groups at random as control, control + curcumin, control + nanocurcumin, PQ, PQ + curcumin, PQ + nanocurcumin for 7 days. The kidney tissues and serum were collected at the end of this period. Total antioxidant capacity (TAC), lipid peroxidation (LPO), total thiol Molecule (TTM), urea, creatinine, and blood urea nitrogen (BUN) levels were assessed. The histopathological evaluation of kidney damage was performed at the end of our study. Moreover, the gene expression was assessed by biochemical and Reverse transcription polymerase chain reaction (RT-PCR) analysis.</p><p><strong>Result: </strong>Curcumin and nanocurcumin administration alleviated PQ-induced renal injury, as evidenced by reduced serum creatinine and BUN levels. The levels of antioxidant markers, like TAC and TTM, increased and decreased the levels of oxidative stress indexes like LPO. Furthermore, our result shows up-regulating the expression of nuclear factor-like 2 (Nrf2), NAD (P) H: quinine oxidoreductase 1 (NQO1), Heme oxygenase 1 (HO-1), and down-regulating the expression of Kelchlike ECH-associated protein 1 (Keap-1) in renal tissue.</p><p><strong>Conclusion: </strong>Niosomal curcumin was more advantageous than ordinary curcumin in lowering oxidative stress and renal tissue damage induced by paraquat intoxication.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-02-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143414773","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Cancer Therapy with Polymeric Nanocarriers and the Transition to Targeted Cancer Therapy: Advances and Future Directions. 高分子纳米载体的癌症治疗和向靶向癌症治疗的过渡:进展和未来方向。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-02-04 DOI: 10.2174/0122117385350610250112112855
Panagiotis Theodosis-Nobelos, Elina N Kitiri, Melina Christou, Maria Pantelidou, Maria Rikkou-Kalourkoti

The development of targeted cancer therapies has become crucial in addressing the limitations of conventional chemotherapy, particularly its lack of specificity and severe side effects. Polymeric nanocarriers have emerged as a transformative solution, providing enhanced drug solubility, selective targeting, and controlled release of therapeutics. This review discusses recent advances in polymeric nanocarriers, emphasizing their capacity to incorporate multiple drugs and optimize delivery through both active and passive targeting strategies, and especially the transition to targeted cancer therapy through the various applied methods in the field. Mechanisms such as the enhanced permeability and retention (EPR) effect for passive targeting, and the use of ligands, peptides, and proteins for active targeting, are explored in depth. Furthermore, the potential of these nanocarriers to improve therapeutic outcomes through targeting specific cellular and subcellular sites, including the nucleus, mitochondria, and endoplasmic reticulum, is examined. These innovations pave the way for the development of safer and more effective cancer treatments with the potential to enhance clinical outcomes.

靶向癌症治疗的发展已成为解决传统化疗局限性的关键,特别是其缺乏特异性和严重的副作用。聚合物纳米载体已经成为一种变革性的解决方案,提供增强的药物溶解度,选择性靶向和治疗药物的控制释放。本文综述了聚合物纳米载体的最新进展,强调了它们通过主动和被动靶向策略结合多种药物和优化递送的能力,特别是通过各种应用方法向靶向癌症治疗的过渡。机制,如增强渗透性和保留(EPR)效应的被动靶向,和使用配体,肽和蛋白质的主动靶向,深入探讨。此外,研究了这些纳米载体通过靶向特定的细胞和亚细胞部位(包括细胞核、线粒体和内质网)来改善治疗效果的潜力。这些创新为开发更安全、更有效的癌症治疗方法铺平了道路,并有可能提高临床结果。
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引用次数: 0
Diosgenin-Loaded Silver Nanoparticles Mitigate B[a]P-Induced Lung Fibrosis Through Modulation of Oxidative Stress and Inflammatory Pathways. 负载薯蓣皂苷元的银纳米颗粒通过调节氧化应激和炎症途径减轻B - p诱导的肺纤维化。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-31 DOI: 10.2174/0122117385337401250116040312
Ahmed Salah, Maiven M Edward, Mohammed A Hussein, Tamer Roshdy, Mohamed S Basiouny

Background: Lung fibrosis, characterized by the thickening and scarring of lung tissue, is a serious condition often triggered by environmental toxins like Benzo[a]pyrene (B[a]P). Diosgenin, a natural steroidal sapogenin found in plants such as fenugreek and wild yam, has shown potential to protect against lung damage due to its anti-inflammatory and antioxidant properties. However, its clinical application is limited by poor solubility and bioavailability.

Objective: The current investigation aims at developing diosgenin-loaded silver nanoparticles (DioAgNPs) to enhance their delivery and efficacy. This study investigates the preparation, characterization, and protective effects of Dio-AgNPs against B[a]P-induced lung fibrosis in mice.

Methods: Acute toxicity studies in mice were conducted to determine the lethal dose (LD50) of DioAgNPs. Sub-lethal doses (1/50 and 1/20 LD50) were selected for subsequent experiments. Mice were exposed to B[a]P to induce lung fibrosis. Dio-AgNPs were administered to assess their protective effects. Biochemical assays measured levels of total cholesterol (TC), triglycerides (TG), malondialdehyde (MDA), nuclear factor kappa B (NF-κB), interleukin-6 (IL-6), matrix metalloproteinase-2 (MMP2), and matrix metalloproteinase-12 (MMP12). Additionally, high-density lipoprotein cholesterol (HDL-C), glutathione (GSH), catalase (CAT), and glutathione peroxidase (GPx) levels were evaluated. Quantitative PCR (qPCR) was used to analyze the expression levels of lung signal transducer and activator of transcription 3 (STAT3), transforming growth factor- β1(TGF-β1), and Sirtuin 1 genes. Insilico molecular docking studies were performed to evaluate the binding affinity of diosgenin with SIRT1, STAT3, and TGF-β1 proteins, with binding energies (ΔG) calculated to predict interaction strength.

Results: The synthesized Dio-AgNPs exhibited a mean diameter of 51.60±1.54 nm, a zeta potential of -19.5 mV, and encapsulation efficiency of 84.98%, confirming their stability through spectral analysis. In B[a]P-exposed mice, there was a significant elevation in TC, TG, MDA, NF-κB, IL-6, MMP2, and MMP12 levels, alongside a reduction in HDL-C, GSH, CAT, and glutathione peroxidase (GPx) levels. Additionally, lung STAT3 and TGF-β1 gene expression was upregulated, while SIRT1 gene expression was downregulated. Administration of Dio-AgNPs to B[a]P-treated mice resulted in a significant reduction in TC, TG, and HDL-C levels, improvement in lung MDA, NF-κB, IL-6, MMP2, and MMP12 levels, downregulation of lung STAT3 and TGF-β1, and upregulation of SIRT1 gene expression. In-silico molecular docking studies demonstrated strong binding affinities of diosgenin with SIRT1, STAT3, and TGF-β1 proteins, with binding energies (ΔG) of -9.7, -9.6, - 10.1, and -9.7 kcal/mol, respectively.

Conclusion: This study innovatively enhances the delivery and efficac

背景:肺纤维化以肺组织增厚和瘢痕形成为特征,是一种严重的疾病,常由苯并[a]芘(B[a]P)等环境毒素引发。薯蓣皂苷元是一种天然甾体皂苷元,存在于葫芦巴和野生山药等植物中,由于其抗炎和抗氧化特性,已显示出保护肺部免受损伤的潜力。但其溶解度和生物利用度较差,限制了其临床应用。目的:研究薯蓣皂苷元载银纳米颗粒(DioAgNPs),以提高其给药效果。本研究探讨Dio-AgNPs的制备、表征及其对B[a] p诱导小鼠肺纤维化的保护作用。方法:采用小鼠急性毒性实验,测定其致死剂量(LD50)。后续实验选用亚致死剂量(1/50和1/20 LD50)。用B[a]P诱导小鼠肺纤维化。给予Dio-AgNPs以评估其保护作用。生化测定总胆固醇(TC)、甘油三酯(TG)、丙二醛(MDA)、核因子κB (NF-κB)、白细胞介素-6 (IL-6)、基质金属蛋白酶-2 (MMP2)、基质金属蛋白酶-12 (MMP12)水平。此外,还评估了高密度脂蛋白胆固醇(HDL-C)、谷胱甘肽(GSH)、过氧化氢酶(CAT)和谷胱甘肽过氧化物酶(GPx)水平。采用定量PCR (qPCR)分析肺信号转导及转录激活因子3 (STAT3)、转化生长因子-β1 (TGF-β1)、Sirtuin 1基因的表达水平。通过Insilico分子对接研究,评估薯蓣皂苷元与SIRT1、STAT3和TGF-β1蛋白的结合亲和力,计算结合能(ΔG)预测相互作用强度。结果:合成的Dio-AgNPs平均直径为51.60±1.54 nm, zeta电位为-19.5 mV,包封效率为84.98%,通过光谱分析证实了其稳定性。在B[a] p暴露的小鼠中,TC、TG、MDA、NF-κB、IL-6、MMP2和MMP12水平显著升高,同时HDL-C、GSH、CAT和谷胱甘肽过氧化物酶(GPx)水平降低。肺STAT3、TGF-β1基因表达上调,SIRT1基因表达下调。对B[a] p处理的小鼠给予Dio-AgNPs可显著降低TC、TG和HDL-C水平,改善肺MDA、NF-κB、IL-6、MMP2和MMP12水平,下调肺STAT3和TGF-β1水平,上调SIRT1基因表达。硅分子对接研究表明薯蓣皂苷元与SIRT1、STAT3和TGF-β1蛋白具有较强的结合亲和力,结合能(ΔG)分别为-9.7、-9.6、- 10.1和-9.7 kcal/mol。结论:本研究通过开发负载薯蓣皂苷元的银纳米粒子(Dio-AgNPs),创新地提高了薯蓣皂苷元的递送和功效,解决了其溶解度和生物利用度的挑战。Dio-AgNPs对B[a] p诱导的小鼠肺纤维化具有显著的保护作用,在调节STAT3、TGF-β1和SIRT1等关键基因的同时减少氧化应激和炎症。分子对接研究证实了很强的结合亲和力,强调了Dio-AgNPs的治疗潜力。这项研究标志着纳米医学和呼吸治疗的重大进展,为治疗肺纤维化和相关疾病提供了一种有前途的方法。
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引用次数: 0
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Pharmaceutical nanotechnology
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