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A Comprehensive Review on Plant Bioactive Compounds-Based Novel Drug Delivery System for the Treatment of Rheumatoid Arthritis. 基于植物活性化合物的新型类风湿性关节炎药物传递系统研究综述。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-23 DOI: 10.2174/0122117385333643241016075918
Akshat Agrawal, Vijayalakshmi Ghosh, Ajaz Uddin, Parag Jain

Rheumatoid Arthritis (RA) is a chronic autoimmune disorder characterized by inflammation in the joints, leading to pain, swelling, stiffness, and eventual joint damage. This condition occurs when the body's immune system mistakenly attacks the synovium, the lining of the membranes surrounding the joints. Treatment focuses on reducing inflammation, alleviating pain, and preventing joint damage through a combination of medications, physical therapy, and lifestyle modifications. Recently, biological therapies have been introduced, including Tumour Necrosis Factor (TNF) blockers (such as etanercept, infliximab, and adalimumab), IL-6 inhibitors (tocilizumab), and interleukin- 1 inhibitors (anakinra). These treatments can lead to various side effects. The use of herbalbased treatments, such as secondary metabolites, has gained popularity due to their better tolerability, safety, and effectiveness compared to conventional therapies. However, there are also some limitations, like poor bioavailability and permeability and lower stability; to overcome these issues, Novel Drug Delivery Systems (NDDS) have been introduced as better treatment options in recent years. Polymer science advancements and nanotechnology applications have opened new avenues for RA treatment, emphasizing the development of smart drug delivery systems. These systems aim to improve therapeutic outcomes while minimizing adverse effects. Additionally, newly synthesized biocompatible drug delivery systems, combined with anti-inflammatory drugs composed of secondary metabolites, offer potential solutions for RA.

类风湿性关节炎(RA)是一种慢性自身免疫性疾病,其特征是关节炎症,导致疼痛、肿胀、僵硬和最终的关节损伤。当身体的免疫系统错误地攻击关节周围的膜层滑膜时,就会发生这种情况。治疗的重点是通过药物治疗、物理治疗和生活方式的改变来减少炎症、减轻疼痛和防止关节损伤。最近,生物疗法已被引入,包括肿瘤坏死因子(TNF)阻滞剂(如依那西普、英夫利昔单抗和阿达木单抗)、IL-6抑制剂(托珠单抗)和白细胞介素- 1抑制剂(阿那金那)。这些治疗方法可能会导致各种副作用。与传统疗法相比,以草药为基础的治疗方法,如次生代谢物,由于其更好的耐受性、安全性和有效性而越来越受欢迎。但也存在一些局限性,如生物利用度和渗透性差,稳定性较低;为了克服这些问题,近年来引入了新型药物输送系统(NDDS)作为更好的治疗选择。聚合物科学的进步和纳米技术的应用为类风湿关节炎的治疗开辟了新的途径,强调了智能给药系统的发展。这些系统旨在改善治疗结果,同时尽量减少不良反应。此外,新合成的生物相容性药物传递系统,结合由次生代谢物组成的抗炎药物,为RA的治疗提供了潜在的解决方案。
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引用次数: 0
Rationalization Progress of Novel Drug Delivery System for Intra-Periodontal Pockets Against Periodontitis. 治疗牙周炎的新型牙周袋内给药系统的研究进展。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-23 DOI: 10.2174/0122117385334802241122094148
Rishabh Maurya, Prashant Kumar, Gaurav Tiwari

Periodontitis (PD) is a pathological condition that results in chronic swelling in the tissue around a tooth, which results in advanced periodontal structural injury to the encircling soft and hard tissues with eventual exfoliation and movement of teeth. It affects around 60% of the world's population, indicating a relatively high prevalence. Therefore, the discovery of efficient therapeutic interventions for dental disorders is a primary goal of the health sciences, and periodontitis is a significant public health problem. Currently, perioceutics plays a revolutionary role in periodontal therapy with the introduction of both systemic and local route administration of therapeutic drugs as supportive therapy to SRP (Scaling and Root Planning). The key to effective periodontal treatment is the selection of the proper antibacterial agent and the local route of medication delivery. The items mentioned, including irrigation systems, gels, fibers, films, thin strips, microvesicles, zero-dimensional nanomaterial, and moderate-dose biocide agents, reflect the innovative site-specific drug delivery available in the sector, resulting in the fulfillment of antimicrobial substances to sites of periodontal disease with low to non-existent negative impacts on other bodily systems. The current report seeks to present the most recent technologies in local biomaterial-based delivery with different properties that play a significant role in gum disease so that the practitioners are able to select appropriate bioactive agents for LDDS that are custom-tailored for a given clinical condition, identify present obstacles, and determine the future research opportunities.

牙周炎(PD)是一种导致牙齿周围组织慢性肿胀的病理状态,其结果是对周围软硬组织的晚期牙周结构损伤,最终导致牙齿脱落和移动。它影响着世界上约60%的人口,表明患病率相对较高。因此,发现有效的牙齿疾病治疗干预措施是健康科学的主要目标,牙周炎是一个重要的公共卫生问题。目前,牙周药物在牙周治疗中发挥着革命性的作用,引入了全身和局部途径的治疗药物作为支持治疗的SRP (Scaling and Root Planning)。有效牙周治疗的关键是选择合适的抗菌药物和局部给药途径。所提到的项目,包括灌溉系统、凝胶、纤维、薄膜、薄条、微泡、零维纳米材料和中剂量杀菌剂,反映了该部门现有的创新的针对特定部位的药物输送,从而实现了将抗菌物质输送到牙周病部位,对其他身体系统的负面影响很小甚至不存在。本报告旨在介绍在牙龈疾病中发挥重要作用的具有不同特性的局部生物材料递送的最新技术,以便从业者能够为LDDS选择适合特定临床条件的生物活性药物,确定当前的障碍,并确定未来的研究机会。
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引用次数: 0
Current Updates on Nanotechnology-based Drug Delivery Platforms for Treating Alzheimer's with Herbal Drugs. 基于纳米技术的中草药治疗阿尔茨海默病药物传递平台的最新进展。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-23 DOI: 10.2174/0122117385335626241204165702
Shakeel Ahmed Ansari, Asim Muhammad Alshanberi, Rukhsana Satar, Jakleen Abujamai, Ghulam Md Ashraf

Alzheimer's disease (AD) is an irreversible brain disorder that led to memory loss and disrupts daily life. Earlier strategies to treat AD such as acetylcholinesterase inhibitor (AChEI) drugs are not showing effectiveness due to the inability to cross the blood-brain barrier. Moreover, traditional AChEI provides limited efficacy in terms of bioavailability and solubility for treating AD treatment. Many of the current drugs such as donepezil taken to treat the disease exhibited harmful side effects. Hence, researchers are keen to find the alternative effective therapeutic agents for treating AD. This review summarizes the recent advancement in nanotechnology-based drug delivery systems of herbal drugs such as Curcumin, Ginkgo biloba, Salvia officinalis, etc for the prevention and cure of AD. Herbal drugs proved useful in treating neuronal disorders such as AD but exhibited some limitations like low bioavailability via oral drug delivery. Such limitations were overcome by tagging these drugs by nanoparticles which enables them to cross the blood-brain barrier and offer the delivery of greater concentration of herbal drugs to the brain. Inorganic nanoparticle-based drugdelivery systems such as gold nanoparticles and magnetic nanoparticles, organic nanoparticulate systems like polymeric micelles and dendrimers, and solid polymeric nanoparticles were some of the effective methods that have earlier shown potential for enhancing the delivery of herbal drugs to the brain. Long-term repeated injection of drugs loaded on nanomaterials can lead to the accumulation of nanomaterials in the body without timely and effective degradation which can cause serious issues to the brain. Hence, nanotechnology-based strategies should involve the formulation of nontoxic nanoparticles in such a way that they can significantly transport the drugs across the BBB followed by effective degradation of nanoparticles.

阿尔茨海默病(AD)是一种不可逆转的脑部疾病,会导致记忆丧失并扰乱日常生活。早期治疗阿尔茨海默病的策略,如乙酰胆碱酯酶抑制剂(AChEI)药物,由于无法通过血脑屏障,没有显示出有效性。此外,传统的AChEI在治疗AD的生物利用度和溶解度方面的疗效有限。目前用于治疗这种疾病的许多药物,如多奈哌齐,都显示出有害的副作用。因此,研究人员迫切希望找到治疗AD的替代有效药物。本文综述了姜黄素、银杏、鼠尾草等中药纳米给药系统在防治阿尔茨海默病中的研究进展。草药被证明在治疗神经疾病如阿尔茨海默氏症方面是有用的,但表现出一些局限性,如口服给药的生物利用度低。通过给这些药物贴上纳米颗粒的标签,克服了这些限制,使它们能够穿过血脑屏障,并向大脑输送更高浓度的草药。无机纳米颗粒为基础的药物输送系统,如金纳米颗粒和磁性纳米颗粒,有机纳米颗粒系统,如聚合物胶束和树状大分子,以及固体聚合物纳米颗粒是一些有效的方法,早期已经显示出增强草药向大脑输送的潜力。长期反复注射装载在纳米材料上的药物会导致纳米材料在体内的积累,而不能及时有效地降解,从而对大脑造成严重的问题。因此,基于纳米技术的策略应该包括无毒纳米颗粒的配方,这样它们就可以在有效降解纳米颗粒之后显著地将药物运输过血脑屏障。
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引用次数: 0
Formulation, Development, and Optimization of Fast Dissolving Tablets Containing Tapentadol Hydrochloride. 盐酸他他多速溶片的研制与优化。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-23 DOI: 10.2174/0122117385350217241122151638
Chandrashekar Thalluri, Mallikarjun Vasam, Rajkumar Jampala, Shanmugarathinam Alagarsamy, Anubhav Dubey, Amit Lather, Tanuj Hooda
<p><strong>Background: </strong>Tapentadol hydrochloride is a potent analgesic commonly used to manage moderate to severe pain. Rapidly dissolving tablets of Tapentadol offer a significant advantage in enhancing patient compliance by providing quick pain relief. The development of fast-dissolving tablets (FDTs) requires careful consideration of formulation parameters to achieve optimal disintegration and dissolution profiles. In this study, the aim was to fabricate Tapentadol FDTs by selecting suitable super disintegrating agents such as croscarmellose sodium and crospovidone, which serve as two independent variables. The direct compression method was employed to formulate nine different Tapentadol hydrochloride formulations (TH1 to TH9).</p><p><strong>Materials and methods: </strong>The study utilized Design-Expert® software version 13.0 and the Response Surface Methodology (RSM) for the optimization of Tapentadol FDTs. The formulations were prepared using the direct compression method with varying concentrations of the super disintegrants, croscarmellose sodium, and crospovidone. The primary response variables considered in this optimization study included disintegration time (Y1), percentage drug release at 15 minutes (Q15, Y2), and percentage drug release at 30 minutes (Q30, Y3). All pre-compressional and postcompressional parameters were evaluated for each formulation, along with in vitro dissolution studies. Furthermore, DD Solver, a statistical tool, was employed to determine the kinetics of drug release and the release order mechanism based on regression coefficient value (r²), Akaike Information Criterion (AIC), and Model Selection Criteria (MSC).</p><p><strong>Results: </strong>The evaluation studies indicated that the TH5 formulation exhibited the most rapid disintegration time and the highest drug release percentage within the specified time frame. The super disintegrants used demonstrated a significant impact on the response variables, notably enhancing the solubility and dissolution rate of Tapentadol hydrochloride. Based on the exponent release (n) value, the study concluded that the TH5 formulation followed a first-order release kinetics and Fickian diffusion mechanism for drug release. Stability studies were performed following the International Council for Harmonization (ICH) guidelines to assess the shelf-life of the optimized formulation. The ANOVA data revealed that the p-value was greater than 0.05, indicating no significant differences during the storage period. Additionally, a similarity factor (f2) analysis was conducted to compare the optimized formulation with the marketed formulation (Tydol 100 mg).</p><p><strong>Discussion: </strong>The findings highlight the crucial role of super disintegrants in fast-dissolving tablet formulation, significantly impacting disintegration time and dissolution profile. The TH5 formulation excelled in rapid disintegration and drug release, optimized using RSM and Design-Expert software,
背景:盐酸他他多是一种强效镇痛药,常用于治疗中度至重度疼痛。快速溶解的他他多片提供显著的优势,提高患者的依从性,提供快速缓解疼痛。速溶片的开发需要仔细考虑处方参数,以达到最佳的崩解和溶出度。本研究的目的是通过选择合适的超崩解剂如交联棉糖钠和交联维酮作为两个自变量来制备他他多fdt。采用直接加压法制备了9种不同的盐酸他他多尔(TH1 ~ TH9)制剂。材料和方法:本研究采用Design-Expert®软件13.0版,采用响应面法(RSM)对他他多fdt进行优化。采用不同浓度的超崩解剂、交联棉糖钠和交联维酮直接压缩法制备配方。本优化研究考虑的主要响应变量包括崩解时间(Y1)、15分钟释药百分比(Q15, Y2)和30分钟释药百分比(Q30, Y3)。对每种制剂的所有压缩前和压缩后参数进行评估,并进行体外溶出研究。基于回归系数值(r²)、Akaike信息准则(AIC)和模型选择准则(MSC),采用DD Solver统计工具确定药物释放动力学和释放顺序机制。结果:评价研究表明,该制剂崩解时间最快,规定时限内释药率最高。所使用的强力崩解剂对反应变量有显著影响,显著提高了盐酸他他他多的溶解度和溶出率。根据指数释放(n)值,研究认为TH5制剂符合一级释放动力学和菲克扩散机制。稳定性研究是按照国际协调理事会(ICH)的指导方针进行的,以评估优化制剂的保质期。方差分析数据显示,p值大于0.05,说明在贮存期间差异不显著。并进行相似因子(f2)分析,将优化后的配方与市售的Tydol 100mg进行比较。讨论:研究结果强调了超级崩解剂在速溶片配方中的关键作用,显著影响崩解时间和溶出谱。采用RSM和Design-Expert软件对处方进行优化,结果表明TH5具有快速崩解和药物释放的特点,经统计分析证实其具有Fickian扩散释药机制。结论:采用直接压缩法和响应面法,研制并优化了他他多速溶片。该制剂崩解迅速,释药效果最佳,在ICH条件下具有稳定性。这突出了超级崩解剂在FDT配方中对快速行动和患者依从性的重要性。
{"title":"Formulation, Development, and Optimization of Fast Dissolving Tablets Containing Tapentadol Hydrochloride.","authors":"Chandrashekar Thalluri, Mallikarjun Vasam, Rajkumar Jampala, Shanmugarathinam Alagarsamy, Anubhav Dubey, Amit Lather, Tanuj Hooda","doi":"10.2174/0122117385350217241122151638","DOIUrl":"https://doi.org/10.2174/0122117385350217241122151638","url":null,"abstract":"&lt;p&gt;&lt;strong&gt;Background: &lt;/strong&gt;Tapentadol hydrochloride is a potent analgesic commonly used to manage moderate to severe pain. Rapidly dissolving tablets of Tapentadol offer a significant advantage in enhancing patient compliance by providing quick pain relief. The development of fast-dissolving tablets (FDTs) requires careful consideration of formulation parameters to achieve optimal disintegration and dissolution profiles. In this study, the aim was to fabricate Tapentadol FDTs by selecting suitable super disintegrating agents such as croscarmellose sodium and crospovidone, which serve as two independent variables. The direct compression method was employed to formulate nine different Tapentadol hydrochloride formulations (TH1 to TH9).&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Materials and methods: &lt;/strong&gt;The study utilized Design-Expert® software version 13.0 and the Response Surface Methodology (RSM) for the optimization of Tapentadol FDTs. The formulations were prepared using the direct compression method with varying concentrations of the super disintegrants, croscarmellose sodium, and crospovidone. The primary response variables considered in this optimization study included disintegration time (Y1), percentage drug release at 15 minutes (Q15, Y2), and percentage drug release at 30 minutes (Q30, Y3). All pre-compressional and postcompressional parameters were evaluated for each formulation, along with in vitro dissolution studies. Furthermore, DD Solver, a statistical tool, was employed to determine the kinetics of drug release and the release order mechanism based on regression coefficient value (r²), Akaike Information Criterion (AIC), and Model Selection Criteria (MSC).&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Results: &lt;/strong&gt;The evaluation studies indicated that the TH5 formulation exhibited the most rapid disintegration time and the highest drug release percentage within the specified time frame. The super disintegrants used demonstrated a significant impact on the response variables, notably enhancing the solubility and dissolution rate of Tapentadol hydrochloride. Based on the exponent release (n) value, the study concluded that the TH5 formulation followed a first-order release kinetics and Fickian diffusion mechanism for drug release. Stability studies were performed following the International Council for Harmonization (ICH) guidelines to assess the shelf-life of the optimized formulation. The ANOVA data revealed that the p-value was greater than 0.05, indicating no significant differences during the storage period. Additionally, a similarity factor (f2) analysis was conducted to compare the optimized formulation with the marketed formulation (Tydol 100 mg).&lt;/p&gt;&lt;p&gt;&lt;strong&gt;Discussion: &lt;/strong&gt;The findings highlight the crucial role of super disintegrants in fast-dissolving tablet formulation, significantly impacting disintegration time and dissolution profile. The TH5 formulation excelled in rapid disintegration and drug release, optimized using RSM and Design-Expert software, ","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142882708","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
Synthesis of Gold Nanoparticles Using Cucurbitacin E-Glycoside and Methyl Gallate Isolated from Citrullus colocynthis L. Fruit and Evaluation of their Antibacterial and Antibiofilm Activities. 瓜素e -糖苷和没食子酸甲酯合成纳米金及其抑菌和抗膜活性评价
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-19 DOI: 10.2174/0122117385314421241009075737
Achyut Adhikari, Asmita Sapkota, Syed Muhammad Zaki Shah, Kapil Aryal, Prajwal Acharya

Introduction: Metal nanoparticles have received much attention due to their unique physical dynamics, chemical reactivity, and promising biological applications. Green synthesis using natural compounds is an alternative to traditional chemical methods for the synthesis of nanoparticles.

Materials and methods: Herein, two secondary metabolites were isolated from different fractions of methanolic extract of Citrullus colocynthis (bitter apple) Schard. and identified as cucurbitacin Eglycoside (1) and methyl gallate (2). Both compounds were used in the green nanoformulation of gold nanoparticles. Mass spectrometry and NMR spectroscopy were used for structure elucidation of compound 1 and compound 2. UV-vis spectroscopy, FTIR, and AFM were performed to confirm the formation of AuNPs.

Result and discussions: The spectra of UV-Vis showed a characteristic peak at 519 nm and 548 nm for compounds 1 and 2, respectively. AuNPs ranged mostly between 1 and 50 nm measured using AFM. The FTIR analysis confirmed the presence of phytochemicals on the surface of AuNPs. The synthesized AuNPs showed good antibacterial activity against Escherichia coli, Bacillus subtilis, and Pseudomonas aeruginosa.

Conclusion: The synthesized AuNPs demonstrated good antibiofilm activity against Streptococcus mutans. Thus, the green synthesized AuNPs can combat the pathogenicity of several human pathogens.

金属纳米颗粒因其独特的物理动力学、化学反应性和广阔的生物应用前景而受到广泛关注。利用天然化合物进行绿色合成是一种替代传统化学方法合成纳米颗粒的方法。材料与方法:从苦苹果(Citrullus colocynthis)醇提物的不同部位分离得到两种次生代谢物。鉴定为葫芦素糖苷(1)和没食子酸甲酯(2)。这两种化合物都用于绿色纳米金的制备。用质谱法和核磁共振谱法对化合物1和2的结构进行了分析。紫外可见光谱、红外光谱和原子力显微镜证实了aunp的形成。结果和讨论:化合物1和2的紫外可见光谱分别在519 nm和548 nm处有特征峰。使用原子力显微镜测量的AuNPs范围主要在1 ~ 50 nm之间。FTIR分析证实了aunp表面存在植物化学物质。合成的AuNPs对大肠杆菌、枯草芽孢杆菌和铜绿假单胞菌具有良好的抑菌活性。结论:合成的AuNPs对变形链球菌具有良好的抗菌活性。因此,绿色合成的AuNPs可以对抗几种人类病原体的致病性。
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引用次数: 0
Biological Synthesis of Metallic Nanoparticles: Latest Insights and Applications. 金属纳米粒子的生物合成:最新见解和应用。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-12 DOI: 10.2174/0122117385353296241119072148
Khadija El Ouardy, Hassan Ahmoum, Youssef Mir

Nanotechnology is rapidly transforming various fields, including medicine, environmental conservation, agriculture, and pharmaceuticals. The production of metallic nanoparticles is a key area within this field, known for its innovative applications. However, traditional chemical and physical methods used for nanoparticle synthesis often involve toxic chemicals and are expensive, making them unsuitable for large-scale production. To address these issues, there has been a growing focus on developing sustainable, cost-effective, and eco-friendly methods. One promising approach is the biological synthesis of metallic nanoparticles. This technique combines principles from biology and nanotechnology, using natural sources such as plant extracts, bacteria, fungi, yeast, and algae to produce nanoparticles in an environmentally friendly way. This review examines the biological synthesis of various metal nanoparticles, including platinum, palladium, gold, and silver. It explores different green methods used for their production and discusses the mechanisms that enable these biological processes. Additionally, the review highlights the diverse applications of these nanoparticles, from environmental cleanup and heavy metal removal to cancer treatment and drug delivery. By focusing on green synthesis methods, this approach not only reduces environmental impact but also offers a scalable, sustainable alternative to traditional nanoparticle production techniques. As research in this area advances, these eco-friendly methods are expected to play a crucial role in the future of nanotechnology.

纳米技术正在迅速改变各个领域,包括医学、环境保护、农业和制药。金属纳米颗粒的生产是该领域的关键领域,以其创新应用而闻名。然而,用于纳米颗粒合成的传统化学和物理方法往往涉及有毒化学品,而且价格昂贵,不适合大规模生产。为了解决这些问题,人们越来越关注开发可持续的、具有成本效益的和环保的方法。生物合成金属纳米粒子是一种很有前途的方法。这项技术结合了生物学和纳米技术的原理,利用植物提取物、细菌、真菌、酵母和藻类等天然来源以一种环保的方式生产纳米颗粒。本文综述了各种金属纳米颗粒的生物合成,包括铂、钯、金和银。它探讨了用于生产的不同绿色方法,并讨论了使这些生物过程成为可能的机制。此外,该综述还强调了这些纳米颗粒的多种应用,从环境清理和重金属去除到癌症治疗和药物输送。通过专注于绿色合成方法,这种方法不仅减少了对环境的影响,而且还提供了一种可扩展的、可持续的替代传统纳米颗粒生产技术。随着这一领域研究的深入,这些生态友好的方法有望在未来的纳米技术中发挥关键作用。
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引用次数: 0
A Critical Review on Lipid Nanoparticle-based siRNA Formulations for Breast Cancer Management. 基于脂质纳米粒子的 siRNA 制剂在乳腺癌治疗中的应用综述
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-12 DOI: 10.2174/0122117385330006241120084721
Phool Chandra, Vaibhav Rastogi, Mayur Porwal, Himanshu Sharma, Anurag Verma, Neetu Sachan

Breast cancer poses a formidable challenge due to its inherent difficulty in treatment. Recognizing the imperative need for new therapeutic approaches, this study focuses on a groundbreaking technique that has the potential to reshape breast cancer treatment: siRNA formulations based on lipid nanoparticles (LNPs). This novel method holds promise for transforming the landscape of breast cancer therapy. The primary objective of this research is to conduct a comprehensive assessment of the current state of the art in the field, specifically exploring the potential applications of siRNA treatments encapsulated in LNPs for breast cancer. The research methodology involves a detailed literature review covering breast cancer, siRNA therapy, and lipid nanoparticles. The study investigates the fundamental principles of siRNA therapy, highlighting its capacity to selectively silence genes critical to breast cancer development. Additionally, the application of LNPs in delivering therapeutic siRNA payloads is explored, with an emphasis on the benefits of LNPs, including their biocompatibility and effective siRNA incorporation. Safety and effectiveness characteristics of LNP-based siRNA formulations are also assessed to pave the way for potential therapeutic applications. Findings from the study illuminate the promising characteristics of LNP-siRNA formulations in the treatment of breast cancer. The investigation provides insights into targeting strategies, such as the enhanced permeability and retention (EPR) effect and the utilization of ligand-conjugated nanoparticles. The study outlines potential avenues for therapeutic use, drawing attention to the safety and effectiveness of LNP-based siRNA formulations. In summary, this study aims to reveal intricate interactions between lipid nanoparticle-based siRNA formulations and breast cancer treatment, fostering a transformation in the field by highlighting current developments, future trends, and innovative strategies for next-gen LNP-based siRNA formulations.

乳腺癌由于其固有的治疗困难而构成了一个巨大的挑战。认识到迫切需要新的治疗方法,本研究侧重于一项具有重塑乳腺癌治疗潜力的突破性技术:基于脂质纳米颗粒(LNPs)的siRNA配方。这种新方法有望改变乳腺癌治疗的前景。本研究的主要目的是对该领域的现状进行全面评估,特别是探索LNPs封装的siRNA治疗乳腺癌的潜在应用。研究方法包括详细的文献综述,涵盖乳腺癌、siRNA治疗和脂质纳米颗粒。该研究调查了siRNA治疗的基本原理,强调了其选择性沉默对乳腺癌发展至关重要的基因的能力。此外,还探讨了LNPs在递送治疗性siRNA有效载荷中的应用,重点介绍了LNPs的益处,包括它们的生物相容性和有效的siRNA结合。还评估了基于lnp的siRNA制剂的安全性和有效性特征,为潜在的治疗应用铺平了道路。研究结果阐明了LNP-siRNA制剂在乳腺癌治疗中的前景。该研究为靶向策略提供了见解,例如增强渗透性和保留性(EPR)效应和配体共轭纳米颗粒的利用。该研究概述了治疗用途的潜在途径,引起人们对lnp基siRNA制剂的安全性和有效性的关注。总之,本研究旨在揭示基于脂质纳米颗粒的siRNA制剂与乳腺癌治疗之间复杂的相互作用,通过强调当前发展、未来趋势和下一代基于lnp的siRNA制剂的创新策略,促进该领域的转型。
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引用次数: 0
Formulation and Assessment of an Optimized Glimepiride Transdermal Therapeutic System Using 32 Full Factorial Design Approach. 采用32全因子设计方法优化格列美脲透皮治疗系统的配方和评价。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-10 DOI: 10.2174/0122117385348069241017070659
Audumbar Mali, Sunayana Mali

Background: Currently, a large number of populations are suffering from diabetes mellitus, which significantly increases the burden on public health. Glimepiride is an antidiabetic drug with a shorter half-life (approximately 5 hours), low bioavailability, and first-pass metabolism. Due to these limitations, it is required to maintain a uniform therapeutic level, and it has been chosen as a transdermal drug delivery approach.

Objectives: The main objective of this investigation was to evaluate glimepiride-loaded transdermal patches on the skin to treat diabetes mellitus. To overcome the issue of oral glimepiride and provide a localized effect, a transdermal drug delivery approach was developed.

Methods: The glimepiride transdermal drug delivery approach was developed by using the solvent evaporation method. To examine the impact of altering amounts of polyvinyl alcohol (X1) and polyvinyl pyrrolidone (X2) on tensile strength, % of glimepiride released in 12 hours (Q12), and % of glimepiride released in 24 hours (Q24), as reliant on variables, a 32 complete factorial design was employed. For dependent variables, regression estimation and estimation of variance were employed. In-vitro release statistics were fixed to different models for various glimepiride release kinetics. In-vitro glimepiride release was tested using the best formulation.

Results: The formulation F4 with 1300.00 milligrams of polyvinyl alcohol and 600.00 milligrams of polyvinyl pyrrolidone demonstrated a release of 96.17% for up to 24 hours and zero order release kinetics consisting of r2=0.987, which was the best batch. The optimized formulation F4 showed a controlled release of glimepiride and better permeation and deposition properties.

Conclusion: The findings of this research work demonstrated the potential of the 32 full factorial mathematical models created to anticipate formulations with additional desirable release and permeability qualities for the treatment of diabetes mellitus.

背景:目前,大量人群患有糖尿病,这大大增加了公共卫生负担。格列美脲是一种降糖药,半衰期短(约5小时),生物利用度低,首过代谢。由于这些限制,它需要保持一个统一的治疗水平,并已被选择作为透皮给药方法。目的:本研究的主要目的是评估格列美脲皮肤透皮贴片对糖尿病的治疗效果。为了克服口服格列美脲的问题并提供局部效果,研究人员开发了一种经皮给药方法。方法:采用溶剂蒸发法建立格列美脲经皮给药途径。为了研究改变聚乙烯醇(X1)和聚乙烯醇吡咯烷酮(X2)的量对抗拉强度、格列美脲在12小时内释放的百分比(Q12)和格列美脲在24小时内释放的百分比(Q24)的影响,采用了32全因子设计。因变量采用回归估计和方差估计。将体外释放统计数据固定在不同模型上,用于各种格列美脲释放动力学。采用最佳配方测试格列美脲体外释放度。结果:以1300.00 mg聚乙烯醇和600.00 mg聚乙烯醇吡罗烷酮为最佳配方,其24 h的释放度为96.17%,零级释放动力学r2=0.987。优化后的配方F4具有控释格列美脲和较好的渗透沉积性能。结论:本研究工作的发现证明了32个全因子数学模型的潜力,这些模型可以预测治疗糖尿病的处方具有额外的理想释放和通透性。
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引用次数: 0
Green Synthesis of Curcumin-Loaded Bacterial Nanocellulose for Topical Application: Preparation and In vivo Study. 外用负载姜黄素的细菌纳米纤维素的绿色合成:制备和体内研究。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-10 DOI: 10.2174/0122117385330452241015071605
Juniar Kalpika Resmi, Safira Prisya Dewi, Heni Rachmawati

Background: Bacterial nanocellulose (BNC) is typically produced through fermentation using Hestrin Schramm (HS) médium. However, its high cost limits its use in industry. Moreover, curcumin, as a model substance, is a potential bioactive compound but has low bioavailability. This also limits its use for clinical application. Thus, a delivery system using more affordable production of BNC was develop to improve the lack property of curcumin, focusing on topical route.

Objective: This study aims to determine the best substrate component according to yield value and evaluate the physical properties as well as the permeation capability of BNC as a delivery matrix system for curcumin.

Methods: The optimization of Gluconacetobacter xylinus culture media to produce BNC was conducted using 6 variation substrates consisting of Palmyra sap (PS) and tofu pulp with certain concentrations. Following a nine-day period, the yield of BNC was calculated. The selected BNCs were then impregnated with curcumin-DMSO and curcumin in the form of nanoemulsion (curcumin- NE). Subsequently, the BNCs containing these curcumin forms were characterized. In vitro testing of curcumin reléased from BNC was conducted using Franz difusión cells. In addition, the penetration ability of curcumin across the mice skin was observed using confocal microscopy. In vivo testing was also conducted to ascertain the safety of BNC-loaded curcumin on mice skin.

Results: PS-TP substrate (100:0, S-6) was the most appropriate substrate for BNC production, yielding 118.5±0.09 g/L. CR-DMSO and CR-NE were successfully impregnated into BNC. Confocal data showed that both formulations were able to penétrate the dermis layer. There was no significant difference was observed between the administration of BNC/CR-DMSO and BNC/CR-NE against the control.

Conclusion: BNC successfully produced using palmyra sap shows promising biomembrane for topical delivery of curcumin. No evidence inflammation or neovascularization in BNC/CR-DMSO- and BNC/CR-NE-treated mice confirms the safety use of this biomembrane.

背景:细菌纳米纤维素(BNC)通常是通过赫斯特林施拉姆(HS)胞质发酵生产的。然而,它的高成本限制了它在工业上的应用。此外,姜黄素作为一种模式物质,是一种潜在的生物活性化合物,但其生物利用度较低。这也限制了其临床应用。因此,本文以局部途径为重点,开发了一种使用成本更低的BNC产品来改善姜黄素缺乏特性的给药系统。目的:根据产率值确定最佳底物组分,并评价BNC作为姜黄素传递基质体系的物理性质和渗透能力。方法:采用棕榈树液(PS)和豆腐浆(一定浓度)组成的6种变异基质,对木醋杆菌生产BNC的培养基进行优化。经过9天的周期,计算BNC的收益率。然后用姜黄素- dmso和姜黄素以纳米乳(姜黄素- NE)的形式浸渍所选的bnc。随后,对含有这些姜黄素形式的bnc进行了表征。用Franz difusión细胞对BNC中姜黄素的释放进行了体外实验。此外,用共聚焦显微镜观察姜黄素对小鼠皮肤的渗透能力。体内实验也证实了bnc负载的姜黄素在小鼠皮肤上的安全性。结果:PS-TP底物(100:0,S-6)为产BNC的最佳底物,产率为118.5±0.09 g/L。CR-DMSO和CR-NE成功浸渍到BNC中。共聚焦数据表明,这两种配方都能够穿透真皮层。BNC/CR-DMSO和BNC/CR-NE对对照组的影响无显著性差异。结论:用棕榈树液成功制备的BNC具有良好的姜黄素外用生物膜应用前景。在BNC/CR-DMSO-和BNC/ cr - ne -处理的小鼠中,没有证据表明炎症或新生血管的形成证实了这种生物膜的安全性。
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引用次数: 0
Emerging Trends in Transdermal Drug Delivery: Nanoparticle Formulations and Technologies for Enhanced Skin Penetration and Drug Efficiency. 经皮给药的新趋势:纳米颗粒配方和技术,以增强皮肤渗透和药物效率。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-10 DOI: 10.2174/0122117385331393241111073911
Kiran Dudhat

Transdermal drug delivery systems (TDDS) have emerged as a popular non-invasive approach for treating skin-related disorders, offering quick and reliable drug delivery into the skin, thereby accelerating therapeutic efficacy. In India, there is a growing interest in TDDS due to its perceived safety and effectiveness. Researchers are actively developing new formulations and technologies to enhance drug delivery efficiency and reduce side effects. Recent trends indicate a focus on overcoming challenges such as low permeability and stability issues through innovative nanoparticle-based delivery systems. Nanotechnology has revolutionized transdermal drug delivery by offering precise control over nanoparticle properties, enabling enhanced skin permeation and targeted delivery. Various nanoparticle formulations, including polymeric nanoparticles, liposomes, nanotubes, solid lipid nanoparticles, and nanoemulsions, have shown promise in improving drug solubility, bioavailability, and sustained release. Additionally, microneedles have emerged as a successful transdermal delivery method, offering advantages over traditional creams and patches. Metallic nanocarriers and nanoemulsions are also being explored for their potential in targeted drug delivery and enhanced skin penetration. Despite these advancements, challenges such as toxicity and biocompatibility need to be addressed for widespread clinical translation. Overall, the growing interest in transdermal drug delivery systems in India reflects the potential for improved therapeutic outcomes and patient convenience through innovative nanoparticle- based formulations and technologies.

透皮给药系统(TDDS)已成为一种流行的非侵入性方法,用于治疗皮肤相关疾病,提供快速和可靠的给药到皮肤,从而加快治疗效果。在印度,由于TDDS的安全性和有效性,人们对其越来越感兴趣。研究人员正在积极开发新的配方和技术,以提高药物输送效率和减少副作用。最近的趋势表明,通过创新的基于纳米颗粒的输送系统来克服诸如低渗透率和稳定性问题等挑战是重点。纳米技术通过提供对纳米颗粒特性的精确控制,使透皮给药发生了革命性的变化,从而增强了皮肤渗透和靶向给药。各种纳米颗粒配方,包括聚合物纳米颗粒、脂质体、纳米管、固体脂质纳米颗粒和纳米乳液,在改善药物溶解度、生物利用度和缓释方面显示出希望。此外,微针已经成为一种成功的透皮给药方法,与传统的面霜和贴剂相比具有优势。金属纳米载体和纳米乳液在靶向药物递送和增强皮肤渗透方面的潜力也正在被探索。尽管取得了这些进展,但为了广泛的临床转化,还需要解决诸如毒性和生物相容性等挑战。总的来说,印度对透皮给药系统日益增长的兴趣反映了通过创新的基于纳米颗粒的配方和技术改善治疗结果和患者便利性的潜力。
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Pharmaceutical nanotechnology
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