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Innovations in Glycosaminoglycan Delivery: Transforming Joint Health Therapies. 糖胺聚糖输送的创新:改变关节健康疗法。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-31 DOI: 10.2174/0122117385329819241212040246
Mahkesha Nisha, Mohammad Adnan, Kalyani Sakure, Ajazuddin, Parag Jain

This thorough analysis looks critically at how glycosaminoglycan (GAG) supports joint health. It emphasizes the importance of GAG in particular, clarifies the underlying processes linked to joint pain, and assesses the shortcomings of traditional therapy modalities. Additionally, the research delves into several traditional approaches, such as injectable GAG therapy and oral supplements, carefully evaluating the benefits and drawbacks of each. The study then explores novel GAG drug delivery technologies, acknowledging the urgent need for better treatment approaches. The article highlights the potential of hydrogel-based systems, liposomal/micellar carriers, and nanoparticles in addressing current challenges in GAG delivery. These challenges include achieving sustained release, improving bioavailability, facilitating targeted delivery, and reducing safety concerns related to biocompatibility. Examining these elements closely and critically, the review seeks to provide a thorough grasp of the developments, difficulties, and possible breakthroughs in GAG delivery systems. In the end, this thorough investigation will greatly aid in the improvement of joint pain therapies. The results imply that by shielding articular joints from erosive effects, early use of GAG therapy-particularly hyaluronic acid-can reduce joint deterioration associated with arthritis. Even though GAG-based therapies have shown promise in lowering inflammation and increasing joint flexibility, further study is required to improve their effectiveness in treating joint pain, particularly in diseases like osteoarthritis.

这个彻底的分析着眼于糖胺聚糖(GAG)如何支持关节健康。它特别强调了GAG的重要性,阐明了与关节疼痛相关的潜在过程,并评估了传统治疗方式的缺点。此外,该研究还深入研究了几种传统方法,如注射GAG疗法和口服补充剂,仔细评估了每种方法的优缺点。该研究随后探索了新的GAG药物输送技术,承认迫切需要更好的治疗方法。文章强调了基于水凝胶的系统、脂质体/胶束载体和纳米颗粒在解决当前GAG递送挑战方面的潜力。这些挑战包括实现持续释放、提高生物利用度、促进靶向给药以及减少与生物相容性相关的安全问题。审查这些因素密切和批判性,审查旨在提供一个全面掌握的发展,困难和可能的突破在GAG输送系统。最后,这项深入的研究将大大有助于改善关节疼痛的治疗方法。结果表明,通过保护关节免受侵蚀作用,早期使用GAG治疗,特别是透明质酸,可以减少关节炎相关的关节恶化。尽管基于gag的疗法在降低炎症和增加关节灵活性方面显示出了希望,但还需要进一步的研究来提高其治疗关节疼痛的有效性,特别是在骨关节炎等疾病中。
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引用次数: 0
Crocin and Nano-Crocin Mitigate Paraquat Hepatotoxicity by Modulating Expression of Genes Involved in Oxidative Stress and Inflammation. 藏红花素和纳米藏红花素通过调节参与氧化应激和炎症的基因表达减轻百草枯肝毒性。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-30 DOI: 10.2174/0122117385323941241211084423
Zahra Khaksari, Freshteh Mehri, Mohadeseh Haji Abdolvahab, Mohammad Amin Manavi, Mohammad Hosein Fathian Nasab, Ashkan Karbasi, Maryam Baeeri, Akram Ranjbar
<p><strong>Introduction: </strong>Crocin, a natural compound found in saffron, has shown promising potential as an anti-inflammatory and antioxidant agent. Paraquat is a widely used herbicide known to cause severe oxidative stress and inflammation in the liver, leading to significant tissue damage. This study explores the potential of crocin and its nanoformulation for mitigating paraquat-induced liver damage associated with inflammation and oxidative stress.</p><p><strong>Materials and methods: </strong>The experimental design included 30 male Wistar rats divided into a control group, a paraquat group (5 mg/kg/day for 1 week, i.p.), and four treatment groups: crocin (20 mg/kg/day for 1 week, i.p.), nano-crocin (20 mg/kg/day for 1 week, i.p.), crocin+paraquat, and nano-crocin+paraquat. The levels of TNF-α, IL-1β, and NF-κB mRNA, reactive oxygen species (ROS), lipid peroxidation (LPO) generation, thiol level, and superoxide dismutase (SOD) activity were assessed.</p><p><strong>Results: </strong>According to the results, the TNF-α, IL-1β, and NF-κB mRNA levels, as well as LPO and ROS generation increased following paraquat administration. Furthermore, both treatment groups showed significantly lower levels compared to the paraquat group (p<0.0001), with the nano-crocin group showing the most significant reduction (p<0.0001). On the other hand, reduced thiol level and SOD activity in the paraquat group were significantly attenuated by crocin and nano-crocin administration (p<0.0001). Notably, nano-crocin exhibited superior protective effects, with a greater reduction in inflammatory markers and oxidative stress indicators compared to crocin (p<0.01).</p><p><strong>Discussion: </strong>This study provides strong evidence that nano-crocin offers superior hepatoprotective effects over crocin in mitigating paraquat-induced liver injury by reducing oxidative stress and inflammation. The results suggest that nano-crocin could be a promising candidate for the development of novel antioxidant therapies targeting liver diseases characterized by oxidative stress. The study further elucidates the underlying mechanisms of action, highlighting the role of nano-crocin in modulating inflammatory pathways and enhancing antioxidant defenses, which may be attributed to its improved bioavailability and targeted delivery. Future studies should focus on the long-term safety and efficacy of nano-crocin, as well as exploring its potential applications in other models of liver injury and systemic oxidative stress-related diseases.</p><p><strong>Conclusion: </strong>In conclusion, nano-crocin treatment exerted more protective effects than crocin on the liver against inflammation and oxidative stress induced by paraquat. These findings suggest that nano-crocin could serve as a promising therapeutic candidate for the management of liver diseases characterized by oxidative stress and inflammation. Future studies should focus on exploring the long-term safety and efficacy of na
藏红花素是一种在藏红花中发现的天然化合物,具有抗炎和抗氧化剂的潜力。百草枯是一种广泛使用的除草剂,已知会引起严重的氧化应激和肝脏炎症,导致严重的组织损伤。本研究探讨了藏红花素及其纳米制剂减轻百草枯引起的与炎症和氧化应激相关的肝损伤的潜力。材料与方法:实验设计雄性Wistar大鼠30只,分为对照组、百草枯组(5 mg/kg/d, 1周,灌胃)、藏红花素(20 mg/kg/d, 1周,灌胃)、纳米藏红花素(20 mg/kg/d, 1周,灌胃)、藏红花素+百草枯、纳米藏红花素+百草枯4个治疗组。测定大鼠血清TNF-α、IL-1β和NF-κB mRNA水平、活性氧(ROS)、脂质过氧化(LPO)生成、硫醇水平和超氧化物歧化酶(SOD)活性。结果:结果显示,百草枯给药后大鼠TNF-α、IL-1β、NF-κB mRNA水平升高,LPO和ROS生成增加。此外,与百草枯组相比,两个治疗组的水平都显著降低(讨论:本研究提供了强有力的证据,表明纳米藏红花素在减轻百草枯引起的肝损伤方面具有优于藏红花素的肝保护作用,通过减少氧化应激和炎症。这些结果表明,纳米藏红花素可能是开发以氧化应激为特征的肝脏疾病的新型抗氧化疗法的有希望的候选药物。该研究进一步阐明了其潜在的作用机制,强调了纳米藏红花素在调节炎症途径和增强抗氧化防御方面的作用,这可能归因于其改善的生物利用度和靶向递送。未来的研究应关注纳米藏红花素的长期安全性和有效性,并探索其在其他肝损伤模型和系统性氧化应激相关疾病中的潜在应用。结论:纳米藏红花素对百草枯诱导的肝脏炎症和氧化应激的保护作用优于藏红花素。这些发现表明,纳米藏红花素可以作为一种有希望的治疗候选药物,用于治疗以氧化应激和炎症为特征的肝脏疾病。未来的研究应重点探索纳米藏红花素的长期安全性和有效性,以及其在其他肝损伤模型和相关氧化应激障碍中的潜在应用。
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引用次数: 0
Metallic Nanostructures: An Updated Review on Synthesis, Stability, Safety, and Applications with Tremendous Multifunctional Opportunities. 金属纳米结构:合成、稳定性、安全性和具有巨大多功能机会的应用的最新综述。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-27 DOI: 10.2174/0122117385358312250108180301
Pooja V Nagime, Nishat M Shaikh, Sudarshan Singh, Vaishali S Chandak, Vijay R Chidrawar, Eloise Parry Nweye

Metallic nanostructures play a vital role in technological advancement, providing exceptional performance and improved adaptability in comparison to their bulk equivalents. Conventional synthesis techniques frequently depend on dangerous reducing agents to transform metal ions into Nanoparticles (NPs), which presents considerable environmental and health issues. In contrast, the approach of green synthesis, which emphasizes the use of non-toxic reagents, has garnered significant interest as a sustainable method for the fabrication of Metallic Nanoparticles (MNPs). This sustainable approach utilizes biological sources, like actinomycetes, algae, fungi, polymers, crops, waste biomass, and yeast, recognized for their excellent biocompatibility, availability, affordability, and efficiency. Biological extracts act as reducing and stabilizing agents, with the metabolites and enzymes present in these extracts aiding in the conversion of metal ions into nanoparticles. This review offers an in-depth examination of different MNPs, such as copper, gold, platinum, silver, and zinc, emphasizing their distinct characteristics and a variety of synthesis methods. The review further explores the diverse applications of MNPs in biomimetics, agriculture, and various industrial sectors, including energy, catalysis, and wastewater treatment, along with optical enhancement. This review explores stability and toxicity profiles, filling a significant gap in the existing knowledge base and providing valuable insights into the broad applicability of MNPs.

金属纳米结构在技术进步中起着至关重要的作用,与它们的体等效物相比,它提供了卓越的性能和改进的适应性。传统的合成技术往往依赖于危险的还原剂将金属离子转化为纳米粒子,这带来了相当大的环境和健康问题。相比之下,强调使用无毒试剂的绿色合成方法作为一种可持续制造金属纳米颗粒(MNPs)的方法,已经引起了人们的极大兴趣。这种可持续的方法利用生物资源,如放线菌、藻类、真菌、聚合物、作物、废弃生物质和酵母,以其出色的生物相容性、可用性、可负担性和效率而闻名。生物提取物作为还原剂和稳定剂,这些提取物中的代谢物和酶有助于金属离子转化为纳米颗粒。本文对铜、金、铂、银和锌等不同的MNPs进行了深入的研究,强调了它们的独特特性和各种合成方法。本文进一步探讨了MNPs在仿生学、农业和各种工业领域的各种应用,包括能源、催化、废水处理以及光学增强。本综述探讨了MNPs的稳定性和毒性概况,填补了现有知识库中的重大空白,并为MNPs的广泛适用性提供了有价值的见解。
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引用次数: 0
Revolutionizing Drug Delivery: A Design Professional's Approach to Drug-loaded Transferosomal Vesicles for Transdermal Use. 革命性的药物传递:经皮使用的载药转移体囊泡的设计专业方法。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-27 DOI: 10.2174/0122117385346215250109142123
Gopinath Subramaniyan, Rubina Shaik, Bachu Venkata Ramana, Meriton Stanley A, Devasena Srinivasan

Aim: This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.

Background: Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution.

Objective: The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration.

Method: Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties.

Results: The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h.

Conclusion: The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation.

目的:研制氯诺昔康(LXM)硫代秋水仙苷(TCS)转移体透皮贴剂,并对其进行评价。背景:口服LXM和TCS可导致胃刺激,需要替代给药方式来缓解疼痛和炎症。将LXM和TCS结合到透皮贴片内的转移体中提供了一个潜在的解决方案。目的:本研究的目的是开发和评估含有LXM和TCS的转移体透皮贴剂,并将芦荟叶粘液(AVLM)和石灰油(LO)作为渗透性增强剂。目的是增强这些药物的皮肤渗透,同时减轻与口服药物相关的胃刺激。方法:采用薄膜水合法制备转移体,根据磷脂酰胆碱、反应时间、反应跨度80、超声时间3个自变量确定9个配方。作为因变量评估包封效率和第6 h药物释放。然后通过中心复合设计将优化后的组合配制成透皮贴剂,评估AVLM和LO对氯诺昔康排出及其他理化性质的影响。结果:斑块的平均重量和厚度分别为7.52±0.75 ~ 8.07±0.11g和1.69±0.01 ~ 1.82±0.02mm,差异最小。LXM/TCS含量均匀性范围为92.84±3.55 ~ 94.07±4.61%,TCS含量均匀性范围为90.17±1.98 ~ 93.18±2.98%。较高比例的磷脂酰胆碱和span 80,以及较短的超声时间,导致氯诺昔康的包埋改善。体外放液研究表明,最佳放液条件为较高的磷脂酰胆碱比例、中等比例的跨度80、较长的超声时间。转移体贴片在24、48和72 h时的LXM和TCS放电率均为零级,结论:TDP-8配方中加入了3g芦荟叶粘液(AVLM)和柠檬油(LO)作为渗透性增强剂,具有良好的放电特性。这表明其作为LXM和TCS的有效透皮给药系统的潜力,提供了一个有希望的替代疼痛和炎症缓解,同时最大限度地减少胃刺激。该研究成功地开发和评估了LXM和TCS的转移体透皮贴剂,提供了一种最小化胃刺激的替代给药方法。
{"title":"Revolutionizing Drug Delivery: A Design Professional's Approach to Drug-loaded Transferosomal Vesicles for Transdermal Use.","authors":"Gopinath Subramaniyan, Rubina Shaik, Bachu Venkata Ramana, Meriton Stanley A, Devasena Srinivasan","doi":"10.2174/0122117385346215250109142123","DOIUrl":"https://doi.org/10.2174/0122117385346215250109142123","url":null,"abstract":"<p><strong>Aim: </strong>This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.</p><p><strong>Background: </strong>Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution.</p><p><strong>Objective: </strong>The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration.</p><p><strong>Method: </strong>Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties.</p><p><strong>Results: </strong>The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h.</p><p><strong>Conclusion: </strong>The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2025-01-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143053130","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
Unraveling the Mysteries of Brain Cancer from Diagnosis to Treatment. 揭开脑癌从诊断到治疗的奥秘。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-24 DOI: 10.2174/0122117385331332241226101149
Dyandevi Mathure, Sejal Bhandare, Dipanjan Karati, Mohammad Adnan, Dileep Kumar

Even with recent advancements in surgery and multimodal adjuvant therapy, brain cancer treatment is still difficult. The blood-brain barrier and the potentially deadly medications' nonspecificity have made pharmacological treatment for brain cancer particularly ineffective. The nanoparticle has surfaced as a viable brain delivery vector that can solve the issues with existing approaches. Furthermore, it is possible to integrate many functions into a single nanoplatform to enable tumor-specific diagnosis, therapy, and follow-up observation. Conventional technology does not allow for such multitasking. Recent developments in brain cancer treatment and detection using nanoparticles are discussed in this study. The benefits of delivery via nanoparticles are discussed, along with the kinds of nanoparticle systems being studied and their potential uses.

即使最近外科手术和多模式辅助治疗取得了进展,脑癌的治疗仍然很困难。血脑屏障和可能致命的药物的非特异性使得脑癌的药物治疗特别无效。纳米颗粒作为一种可行的大脑传递载体已经浮出水面,它可以解决现有方法存在的问题。此外,可以将许多功能集成到一个纳米平台中,从而实现肿瘤特异性诊断、治疗和随访观察。传统技术不允许这样的多任务处理。本研究讨论了纳米颗粒在脑癌治疗和检测方面的最新进展。讨论了通过纳米颗粒输送的好处,以及正在研究的纳米颗粒系统的种类和它们的潜在用途。
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引用次数: 0
Enhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles using a Central Composite Design. 利用中心复合设计开发和优化固体脂质纳米颗粒以提高BCS二类药物伊曲康唑的溶解度。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-21 DOI: 10.2174/0122117385341583250119054309
Irfan A Mohammed, Sriramakamal Jonnalagadda

Background: Itraconazole (ICZ) has been approved by the FDA to treat many fungal infections including, blastomycosis, histoplasmosis, and aspergillosis. ICZ can be also used as prophylaxis in the population who are at high risk for developing systemic fungal infections, such as HIV patients, and chemotherapy patients.

Aim: However, since ICZ is a BCS Class II drug that has low solubility and high permeability, leads to low oral bioavailability. In addition, the absorption of ICZ from commercial oral dosage forms is highly affected by food intake and pH.

Objective: The current study aimed to develop, optimize, and characterize ICZ-loaded solid lipid nanoparticles (ICZ-SLNs) using a Central Composite Design for improved solubility and extendedrelease profile.

Methods: ICZ-SLNs were optimized based on physicochemical characteristics. ICZ-SLNs were also evaluated for differential scanning calorimetry (DSC), in-vitro release, lyophilization, transmission electron microscopy (TEM), and physicochemical stability at refrigerated and room temperatures for three months.

Results: The optimized ICZ-SLNs formulation showed particle size, polydispersity index, zeta potential, drug content, and entrapment efficiency of 335.6±8.0 nm, 0.25±0.02, -23.8±0.5 mV, 98.3±2.5%, and 99.5±1.5%, respectively. ICZ-SLN dispersions showed extended-release profiles for ICZ compared to the control solution over 24 h. The absence of the endothermic melting drug peak of the lyophilized formulation indicated that the drug was converted to its amorphous form inside the solid matrix. In addition, TEM studies showed spherical shape nanoparticles. Moreover, the optimized ICZ-SLN formulation was stable at both tested storage conditions.

Conclusion: The current ICZ formulation could exhibit improved oral bioavailability with better therapeutic outcomes during the treatment of systemic fungal infections.

背景:伊曲康唑(ICZ)已被FDA批准用于治疗多种真菌感染,包括芽孢菌病、组织胞浆菌病和曲霉病。ICZ也可用于发生全身性真菌感染的高危人群,如HIV患者和化疗患者。目的:然而,由于ICZ是BCS II类药物,具有低溶解度和高通透性,导致口服生物利用度低。此外,商业口服剂型中ICZ的吸收受到食物摄入量和ph的高度影响。目的:本研究旨在利用中心复合设计来开发、优化和表征装载ICZ的固体脂质纳米颗粒(ICZ- slns),以改善其溶解度和缓释特性。方法:基于理化特性对icz - sln进行优化。对icz - sln进行了差示扫描量热法(DSC)、体外释放、冻干、透射电镜(TEM)和冷藏和室温下3个月的理化稳定性评估。结果:优化后的ICZ-SLNs粒径为335.6±8.0 nm,多分散性指数为0.25±0.02,zeta电位为-23.8±0.5 mV,药物含量为98.3±2.5%,包封效率为99.5±1.5%。与对照溶液相比,ICZ- sln分散体在24 h内表现出ICZ的缓释特征。冻干制剂中没有吸热融化峰,表明药物在固体基质内转化为无定形。此外,透射电镜研究显示球形纳米颗粒。此外,优化后的ICZ-SLN配方在两种测试条件下都是稳定的。结论:该制剂在治疗全身性真菌感染中具有较好的口服生物利用度和治疗效果。
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引用次数: 0
Polymeric Nano-discs: A Versatile Nanocarrier Platform for Delivering Topical Theranostics. 聚合纳米片:一种用于局部治疗的多功能纳米载体平台。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-17 DOI: 10.2174/0122117385353188241218153916
Devesh U Kapoor, Mansi Gaur, Hetal Hingalajia, Sudarshan Singh, Bhupendra G Prajapati

Polymeric nano-discs offer a promising and adaptable nanocarrier platform for topical applications involving the targeted administration of drugs. These biocompatible polymer-based, disc-shaped, nanoscale structures have drawn interest due to their exceptional capacity to encapsulate a diverse range of theranostics. Theranostics, the concept of combining treatments and diagnostics into a single system, is the core of attraction. Precision and fewer adverse effects are provided by the regulated and prolonged release of these drugs made possible by polymeric nano-discs. They also offer the perfect foundation for keeping track of the effectiveness of treatments. The selection of polymeric materials that provide biocompatibility and customized release mechanisms is critical to effectively implementing polymeric nano-discs. Recent pre-clinical and clinical research has demonstrated efficacy in targeted therapeutic interventions. Nevertheless, there are obstacles and restrictions in real-world implementation, and more study is necessary to fully realize their potential. Hence polymeric nano-discs offer controlled drug release and simultaneous diagnostic capabilities, making them a flexible and viable path forward for topical theranostics. Their advancement has opportunities for improved treatment results; however, more study is needed to properly resolve obstacles and realize their therapeutic potential.

聚合物纳米片提供了一个有前途的和适应性强的纳米载体平台,用于局部应用,包括靶向给药。这些生物相容性聚合物基的圆盘状纳米结构因其封装各种治疗药物的特殊能力而引起了人们的兴趣。将治疗和诊断结合为一个单一系统的治疗学概念是吸引人的核心。聚合物纳米片提供了精确和更少的不良反应,提供了这些药物的调节和延长释放。它们还为跟踪治疗效果提供了完美的基础。选择具有生物相容性和定制释放机制的聚合物材料是有效实现聚合物纳米片的关键。最近的临床前和临床研究已经证明了靶向治疗干预的有效性。然而,在实际应用中存在障碍和限制,需要更多的研究来充分发挥其潜力。因此,聚合物纳米片提供了控制药物释放和同时诊断能力,使其成为局部治疗的灵活可行的途径。它们的进步有机会改善治疗效果;然而,需要更多的研究来妥善解决障碍并发挥其治疗潜力。
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引用次数: 0
Preparation and In-Vitro Characterization of Solid Lipid Nanoparticles Containing Artemisinin and Curcumin. 含青蒿素和姜黄素的固体脂质纳米颗粒的制备和体外表征
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385296893240626061552
Bhagyashri Khatri, Vaishali Thakkar, Saloni Dalwadi, Avani Shah, Hardik Rana, Purvi Shah, Tejal Gandhi, Bhupendra Prajapati

Background: Malaria remains a formidable public health obstacle across Africa, Southeast Asia, and portions of South America, exacerbated by resistance to antimalarial medications, such as artemisinin-based combinations. The combination of curcumin and artemisinin shows promise due to its potential for dose reduction, reduced toxicity, synergistic effects, and suitability for drug delivery improvement.

Objectives: This research aims to enhance the solubility and dissolution rates of curcumin and artemisinin by employing Solid Lipid Nanoparticles (SLNs). Oral delivery of both drugs faces challenges due to their poor water solubility, inefficient absorption, and rapid metabolism and elimination.

Methods: The study focuses on formulating and optimizing Solid Lipid Nanoparticles (SLNs) encapsulating artemisinin (ART) and curcumin (CUR). SLNs were developed using the hot homogenization method, incorporating ultrasonication. Drug-excipient compatibility was evaluated using Differential Scanning Calorimetry (DSC). Lipid and surfactant screening was performed to select suitable components. A 3² full factorial design was utilized to investigate the influence of lipid and surfactant concentrations on key parameters, such as entrapment efficiency (%EE) and cumulative drug release (%CDR). Additionally, evaluations of %EE, drug loading, particle size, zeta potential, and in-vitro drug release were conducted.

Results: Successful development of artemisinin and curcumin SLNs was achieved using a full factorial design, demonstrating controlled drug release and high entrapment efficiency. The optimized nanoparticles exhibited a size of 114.7nm, uniformity (PDI: 0.261), and a zeta potential of -9.24 mV. Artemisinin and curcumin showed %EE values of 79.1% and 74.5%, respectively, with cumulative drug release of 85.1% and 80.9%, respectively. The full factorial design indicated that increased lipid concentration improved %EE, while higher surfactant concentration enhanced drug release and %EE. Stability studies of the optimized batch revealed no alterations in physical or chemical characteristics.

Conclusion: The study successfully developed Solid Lipid Nanoparticles (SLNs) for artemisinin and curcumin, achieving controlled drug release, high entrapment efficiency, and desired particle size and uniformity. This advancement holds promise for enhancing drug delivery of herbal formulations.

背景:疟疾仍然是非洲、东南亚和南美洲部分地区的一个严重公共卫生障碍,对青蒿素类复方制剂等抗疟药物的抗药性加剧了这一问题。姜黄素和青蒿素的复方制剂具有减少剂量、降低毒性、协同增效以及改善给药方式的潜力,因此前景广阔:本研究旨在利用固体脂质纳米颗粒(SLNs)提高姜黄素和青蒿素的溶解度和溶出率。由于这两种药物的水溶性差、吸收效率低、代谢和消除速度快,口服给药面临挑战:研究重点是配制和优化包裹青蒿素(ART)和姜黄素(CUR)的固体脂质纳米颗粒(SLNs)。固体脂质纳米颗粒是采用热均质法和超声波法研制而成的。使用差示扫描量热法(DSC)评估了药物与赋形剂的相容性。对脂质和表面活性剂进行了筛选,以选出合适的成分。采用 3² 全因子设计研究了脂质和表面活性剂浓度对夹持效率(%EE)和累积药物释放率(%CDR)等关键参数的影响。此外,还对夹带率、药物负载、粒度、ZETA电位和体外药物释放进行了评估:结果:采用全因子设计成功开发了青蒿素和姜黄素 SLNs,显示出药物释放受控和较高的夹持效率。优化后的纳米颗粒大小为 114.7nm,均匀度(PDI:0.261)和 zeta 电位为 -9.24 mV。青蒿素和姜黄素的 %EE 值分别为 79.1% 和 74.5%,累积药物释放率分别为 85.1% 和 80.9%。全因子设计表明,增加脂质浓度可提高释放率,而增加表面活性剂浓度则可提高药物释放率和释放率。对优化批次的稳定性研究表明,其物理和化学特性没有发生变化:该研究成功开发了青蒿素和姜黄素的固体脂质纳米颗粒(SLNs),实现了药物的可控释放、高包埋效率以及理想的粒度和均匀性。这一进步有望提高草药制剂的给药效果。
{"title":"Preparation and <i>In-Vitro</i> Characterization of Solid Lipid Nanoparticles Containing Artemisinin and Curcumin.","authors":"Bhagyashri Khatri, Vaishali Thakkar, Saloni Dalwadi, Avani Shah, Hardik Rana, Purvi Shah, Tejal Gandhi, Bhupendra Prajapati","doi":"10.2174/0122117385296893240626061552","DOIUrl":"10.2174/0122117385296893240626061552","url":null,"abstract":"<p><strong>Background: </strong>Malaria remains a formidable public health obstacle across Africa, Southeast Asia, and portions of South America, exacerbated by resistance to antimalarial medications, such as artemisinin-based combinations. The combination of curcumin and artemisinin shows promise due to its potential for dose reduction, reduced toxicity, synergistic effects, and suitability for drug delivery improvement.</p><p><strong>Objectives: </strong>This research aims to enhance the solubility and dissolution rates of curcumin and artemisinin by employing Solid Lipid Nanoparticles (SLNs). Oral delivery of both drugs faces challenges due to their poor water solubility, inefficient absorption, and rapid metabolism and elimination.</p><p><strong>Methods: </strong>The study focuses on formulating and optimizing Solid Lipid Nanoparticles (SLNs) encapsulating artemisinin (ART) and curcumin (CUR). SLNs were developed using the hot homogenization method, incorporating ultrasonication. Drug-excipient compatibility was evaluated using Differential Scanning Calorimetry (DSC). Lipid and surfactant screening was performed to select suitable components. A 3² full factorial design was utilized to investigate the influence of lipid and surfactant concentrations on key parameters, such as entrapment efficiency (%EE) and cumulative drug release (%CDR). Additionally, evaluations of %EE, drug loading, particle size, zeta potential, and <i>in-vitro</i> drug release were conducted.</p><p><strong>Results: </strong>Successful development of artemisinin and curcumin SLNs was achieved using a full factorial design, demonstrating controlled drug release and high entrapment efficiency. The optimized nanoparticles exhibited a size of 114.7nm, uniformity (PDI: 0.261), and a zeta potential of -9.24 mV. Artemisinin and curcumin showed %EE values of 79.1% and 74.5%, respectively, with cumulative drug release of 85.1% and 80.9%, respectively. The full factorial design indicated that increased lipid concentration improved %EE, while higher surfactant concentration enhanced drug release and %EE. Stability studies of the optimized batch revealed no alterations in physical or chemical characteristics.</p><p><strong>Conclusion: </strong>The study successfully developed Solid Lipid Nanoparticles (SLNs) for artemisinin and curcumin, achieving controlled drug release, high entrapment efficiency, and desired particle size and uniformity. This advancement holds promise for enhancing drug delivery of herbal formulations.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":"199-211"},"PeriodicalIF":0.0,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141748762","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
An Insight into Cubosomal Drug Delivery Approaches: An Explicative Review. 洞察立方体给药方法:说明性综述。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385306495240529052911
Swarupananda Mukherjee, Ayon Dutta, Dipanjana Ash, Dipanjan Karati

Cubosomes, a novel drug delivery system, have gained significant attention in recent years due to their unique self-assembled structures and enhanced drug encapsulation capabilities. They are administered by oral, ophthalmic, transdermal, and chemotherapeutic routes, to name a few. Due to their many potential benefits-which include high drug dispersal due to the cubic structure, a large surface area, a relatively simple manufacturing process, biodegradability, the capacity to encapsulate hydrophobic, hydrophilic, and amphiphilic compounds, targeted and controlled release of bioactive agents, and the biodegradability of lipids-cubosomes show enormous promise in drug nanoformulations for cancer therapeutics. The most common preparation method involves emulsifying a monoglyceride with a polymer, homogenizing, and then sonicating the mixture. Two distinct approaches to preparing are top-down and bottom-up. This evaluation will examine the materials, methods of preparation, cubosome-related drug encapsulating techniques, drug loading, release mechanism, and their uses. The following databases were used for literature searches: PubMed, Frontiers, Science Direct, Springer, Wiley, and MDPI. For the purpose of finding pertinent articles and contents (2015-2024), the keywords "cubosome; drug delivery systems, nano-carrier, theranostic, drug release mechanism" and others of a similar nature were utilized. This review will conduct a comprehensive analysis of the cubosome-related composition, production methods, drug encapsulating strategies, drug release mechanisms, and applications. Moreover, the difficulties encountered in fine-tuning different parameters to improve loading capabilities and prospects are also discussed. Innovation in pharmaceutical research and development can be stimulated by the knowledge gathered about cubosomal drug delivery methods. Through the clarification of the mechanisms involved in drug release from cubosomes and the investigation of innovative fabrication procedures, scientists can enhance the cubosomal formulation design for targeted therapeutic uses.

立方体是一种新型给药系统,近年来因其独特的自组装结构和更强的药物封装能力而备受关注。它们可通过口服、眼科、透皮和化疗等途径给药。由于它们具有许多潜在的优点--包括立方结构带来的高药物分散性、大表面积、相对简单的制造工艺、生物可降解性、封装疏水性、亲水性和两性化合物的能力、生物活性剂的定向和控制释放以及脂质的生物可降解性--在癌症治疗药物纳米制剂方面显示出巨大的前景。最常见的制备方法是将单甘酯与聚合物乳化、均质,然后对混合物进行超声处理。自上而下和自下而上是两种不同的制备方法。本评估将研究材料、制备方法、立方体相关的药物封装技术、药物负载、释放机制及其用途。文献检索使用了以下数据库:PubMed、Frontiers、Science Direct、Springer、Wiley 和 MDPI。为了查找相关文章和内容(2015-2024 年),使用了关键词 "cubosome; drug delivery systems, nano-carrier, theranostic, drug release mechanism "及其他类似性质的关键词。本综述将全面分析立方体的相关组成、生产方法、药物封装策略、药物释放机制和应用。此外,还将讨论在微调不同参数以提高装载能力方面遇到的困难和前景。有关立方体给药方法的知识可以促进药物研发的创新。通过阐明立方体释放药物的机制和研究创新的制造程序,科学家们可以提高立方体配方设计的针对性治疗用途。.
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引用次数: 0
Nanotechnology Platform for the Delivery of Docetaxel and Tyrosine Kinase Inhibitors for HER2-Positive Breast Cancer Therapy. 纳米技术平台递送多西紫杉醇和酪氨酸激酶抑制剂用于her2阳性乳腺癌治疗。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385373466250219070753
Bharathi Mandala, Yvonne Berko, Gantumur Battogtokh, Funmilola Fisusi, Haijun Gao, Emmanuel O Akala

Background: HER2-positive breast cancer is an aggressive subtype characterized by the overexpression of the HER2 receptor, a transmembrane glycoprotein critical for tumor progression. Current therapies often face challenges like drug resistance and systemic toxicity, necessitating the development of advanced drug delivery systems.

Objective: This study aimed to fabricate and determine the cytotoxicity of pH-sensitive PLA nanoparticles dual-loaded with docetaxel and each of the small molecule tyrosine kinase inhibitors (STKIs) (tucatinib, neratinib, lapatinib) in HER2-positive breast cancer cells.

Method: Nanoparticles were synthesized by a dispersion polymerization method using an acidlabile crosslinking agent, PEG and lactide macromonomers. They were characterized for structure (TEM), surface morphology (SEM), particle size, polydispersity index, zeta potential, and drug loading capacity. Cytotoxicity was assessed in vitro on SKBR3 and MCF7 breast cancer cell lines, with IC50 values compared across formulations.

Results: The nanoparticles were spherical with nanoscale sizes and negative zeta potential values. In vitro studies demonstrated enhanced antiproliferative effects of the drug-loaded nanoparticles, with synergistic activity observed between docetaxel and the STKIs. The drug concentrations were halved in combination formulations and resulted in better cytotoxicity compared to single-drug treatments, particularly against SKBR3 cells. The IC50 values were lower in SKBR3 cells than in MCF7 cells, highlighting the role of HER2 expression in the activity of TKIs.

Conclusion: The pH-sensitive PLA nanoparticles effectively co-delivered docetaxel and STKIs and demonstrated enhanced efficacy and reduced drug dosages in HER2-positive breast cancer models. This study provides a foundation for further exploration of nanoparticle-based combination therapies with potential applications in treating other aggressive cancer types.

背景:HER2阳性乳腺癌是一种侵袭性亚型,其特征是HER2受体过表达,HER2受体是一种跨膜糖蛋白,对肿瘤进展至关重要。目前的治疗方法经常面临耐药性和全身毒性等挑战,需要开发先进的给药系统。目的:制备双负载多西紫杉醇和各小分子酪氨酸激酶抑制剂(STKIs)(图卡替尼、纳拉替尼、拉帕替尼)的ph敏感聚乳酸纳米颗粒,并测定其对her2阳性乳腺癌细胞的细胞毒性。方法:以酸性交联剂、聚乙二醇和丙交酯为原料,采用分散聚合法制备纳米颗粒。对其结构(TEM)、表面形貌(SEM)、粒径、多分散性指数、zeta电位和载药量进行了表征。体外评估SKBR3和MCF7乳腺癌细胞系的细胞毒性,并比较不同配方的IC50值。结果:纳米颗粒呈纳米级球形,zeta电位为负。体外研究表明,载药纳米颗粒具有增强的抗增殖作用,并在多西紫杉醇和STKIs之间观察到协同作用。在联合制剂中,药物浓度减半,与单药治疗相比,产生更好的细胞毒性,特别是针对SKBR3细胞。IC50值在SKBR3细胞中低于MCF7细胞,突出了HER2表达在TKIs活性中的作用。结论:ph敏感的聚乳酸纳米颗粒在her2阳性乳腺癌模型中有效地共同递送多西紫杉醇和STKIs,并显示出增强的疗效和减少的药物剂量。该研究为进一步探索基于纳米颗粒的联合疗法在治疗其他侵袭性癌症类型中的潜在应用提供了基础。
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引用次数: 0
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Pharmaceutical nanotechnology
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