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Solid Lipid Nanoparticles: A Review of their Biomedical Applications and Preparation. 固体脂质纳米颗粒:固体脂质纳米颗粒:生物医学应用与制备综述》。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385312175240502100018
Mayukh Jana, Ujjwal Kumar Biswas, Chandra Sekhar Patro, Biplab Debnath, Suraj Sharma, Sweet Naskar

Solid lipid nanoparticles (SLNs) are gaining significant attention in the pharmaceutical industry due to their biocompatibility and biodegradability, making them a popular functional nanocarrier. SLNs are a popular nanocarrier due to their ability to bypass the spleen and liver, offer high drug stability, and improve bioavailability, sterilization, immobilization, targeted drug release, and biocompatible ingredients. This article discusses various SLN preparation techniques, including high shear homogenization, hot homogenization, cold homogenization, microemulsion-based, solvent evaporation, solvent emulsification-evaporation, supercritical fluid-based, spray drying, double emulsion, and precipitation techniques, focusing on methodological aspects. This review discusses the physicochemical behavior of SLNs, including drug loading, release, particle size, stability, cytotoxicity, and cellular uptake, and their major biomedical applications.

固体脂质纳米颗粒(SLNs)因其生物相容性和生物可降解性而成为一种流行的功能性纳米载体,在制药行业受到极大关注。SLNs 能够绕过脾脏和肝脏,具有较高的药物稳定性,并能提高生物利用度、杀菌、固定、靶向药物释放和生物相容性成分,因此是一种广受欢迎的纳米载体。本文讨论了各种 SLN 制备技术,包括高剪切均质、热均质、冷均质、微乳化、溶剂蒸发、溶剂乳化-蒸发、超临界流体、喷雾干燥、双乳化和沉淀技术,重点关注方法学方面。本综述讨论了 SLNs 的理化行为,包括药物负载、释放、粒度、稳定性、细胞毒性和细胞吸收,以及它们的主要生物医学应用。
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引用次数: 0
Liquid Crystalline Lipid Nanoparticles: Emerging Trends and Applications in Skin Cancer. 液晶脂质纳米颗粒:皮肤癌的新趋势和应用。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2025-01-01 DOI: 10.2174/0122117385312450240816055942
Kamya Varshney, Rupa Mazumder, Anjna Rani, Pratibha Pandey, Malakapogu Ravindra Babu

Liquid crystalline lipid nanoparticles (LCNPs) represent a type of membrane-based nano-carriers formed through the self-assembly of lyotropic lipids. These lipids, such as unsaturated monoglycerides, phospholipids, and co-lipids, create liquid crystals or vesicles with an aqueous core enclosed by a natural or synthetic phospholipid bilayer upon exposure to an aqueous medium. Liquid crystalline lipid nanoparticles (LCNPs), akin to liposomes, have garnered significant attention as nanocarriers suitable for a diverse range of hydrophobic and hydrophilic molecules. Their notable structural advantage lies in a mono-channel network organization and the presence of multiple compartments, resulting in heightened encapsulation efficiency for various substances. Cubosomes, spongosomes, hexosomes, and multicompartment nanoparticles are examples of lipid nanocarriers with interior liquid crystalline structures that have recently gained a lot of interest as effective drug delivery systems. Additionally, LCNPs facilitate the sustained release of encapsulated compounds, including therapeutic macromolecules. This review delves into the structure of liquid crystalline lipid nanoparticles, explores preparation techniques, and outlines their applications in the context of skin cancer.

液晶脂质纳米粒子(LCNPs)是一种基于膜的纳米载体,通过溶解性脂质的自组装形成。这些脂质(如不饱和单甘酯、磷脂和辅脂)在暴露于水性介质后会形成液晶或囊泡,其水性核心由天然或合成磷脂双分子层包裹。液晶脂质纳米粒子(LCNPs)类似于脂质体,作为适用于各种疏水性和亲水性分子的纳米载体,已经引起了广泛关注。其显著的结构优势在于单通道网络组织和多个隔室的存在,从而提高了对各种物质的封装效率。立方体、海绵体、六方体和多隔室纳米粒子都是具有内部液晶结构的脂质纳米载体,它们作为有效的给药系统最近受到了广泛关注。此外,LCNPs 还能促进封装化合物(包括治疗性大分子)的持续释放。这篇综述深入探讨了液晶脂质纳米粒子的结构,探讨了制备技术,并概述了它们在皮肤癌方面的应用。
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引用次数: 0
A Comprehensive Review of Strategies of Topical Niosomes and Their Synergistic Effect for Enhanced Therapeutic Outcomes 外用Niosomes策略及其协同作用对提高治疗效果的综合综述。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-30 DOI: 10.2174/0122117385345369241212071947
N Bharathi Sai Thilagam, V P Karthik, R Gnanasambandan, C Sowmya

The review aims to assess the potential of niosomes-nonionic surfactant-based vesicular systems-as carriers for topical and transdermal drug delivery. Niosomes enable targeted and controlled drug release while minimizing systemic toxicity. The investigation centers on their structure, stability, and capacity to entrap both hydrophilic and lipophilic drugs, as well as their use in managing various dermatological and systemic disorders. Recent studies have examined the formulation of niosomes, particularly highlighting the roles of nonionic surfactants and cholesterol in enhancing the stability and entrapment efficiency of these vesicles. Research on permeability enhancers has been reviewed for their ability to work together to improve drug transport and bioavailability. It also provides a detailed discussion on the use of niosomes in treating various dermatological conditions, as well as their applications in systemic diseases, with a particular focus on co-delivery systems in cancer therapies. Niosomes exhibit efficacy in drug delivery by providing an increase in penetration through the stratum corneum, targeting hydrophilic and lipophilic drugs for dermatological and systemic applications. The Development of niosomal therapy has expanded into immunization, antiinflammatory treatments, and the control of pigmentation. Permeability enhancers further increase their efficacy, bioavailability, and tissue localization. Anticancer treatment using niosomes for codelivery of agents demonstrates synergistic effects with reduced side effects. Niosomes have tremendous potential in advancing topical and transdermal drug delivery, offering controlled, targeted release and improved patient outcomes. With optimized fabrication and comprehensive toxicity evaluation, niosomes can potentially revolutionize topical therapies, making them safer, more effective, and patient-friendly for a range of next-generation treatment options across dermatology and beyond.

这篇综述的目的是评估肿瘤小体——基于非离子表面活性剂的囊泡系统——作为局部和透皮药物递送载体的潜力。溶酶体能够靶向和控制药物释放,同时最大限度地减少全身毒性。研究的重点是它们的结构、稳定性和捕获亲水和亲脂药物的能力,以及它们在治疗各种皮肤病和全身疾病中的应用。最近的研究检查了纳米体的配方,特别强调了非离子表面活性剂和胆固醇在提高这些囊泡的稳定性和包封效率方面的作用。对渗透性增强剂的研究进行了综述,因为它们能够共同作用以改善药物的运输和生物利用度。它还详细讨论了乳质体在治疗各种皮肤病中的应用,以及它们在全身性疾病中的应用,特别关注癌症治疗中的共递送系统。Niosomes通过增加角质层的渗透,靶向皮肤病学和全身应用的亲水性和亲脂性药物,在药物递送方面表现出功效。niosomal therapy的发展已扩展到免疫、抗炎治疗和色素沉着的控制。渗透性增强剂进一步提高了它们的功效、生物利用度和组织定位。抗癌治疗使用niosome共递送药物显示协同作用,减少副作用。Niosomes在推进局部和透皮给药、提供可控、靶向释放和改善患者预后方面具有巨大的潜力。通过优化制造和全面的毒性评估,纳米体可能会彻底改变局部治疗方法,使其更安全,更有效,对患者更友好,适用于皮肤病学和其他领域的下一代治疗选择。
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引用次数: 0
Nanoparticle Carriers for Drug Delivery: An Updated Review. 纳米颗粒药物递送载体:最新综述。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-30 DOI: 10.2174/0122117385340986241208123048
Somayeh Hajipour, Alireza Ghiasvand

The drug was initially administrated relying on pills, eye drops, ointments, and intravenous solutions. In the last decades, several novel technologies have emerged to overcome significant challenges including poor solubility, drug aggregation, low bioavailability, limited biodistribution, poor absorption in the body, lack of selectivity, or to minimize the adverse effects of therapeutic drugs. Drug delivery systems (DDS) can be designed to the technologies that carry drugs into or throughout the body of humans or animals to enhance therapeutic efficacy. DDS can also be considered for in vivo delivery, particularly for their use in peptide and protein therapeutics. Continued research may show the trends and perspectives of how drugs are delivered. In addition, this article includes comprehensive information regarding the trends and perspectives in DDS technologies.

这种药物最初是依靠药片、眼药水、药膏和静脉溶液来给药的。在过去的几十年里,一些新技术已经出现,以克服重大挑战,包括溶解度差,药物聚集,低生物利用度,有限的生物分布,体内吸收差,缺乏选择性,或尽量减少治疗药物的不良反应。药物输送系统(DDS)可以被设计成携带药物进入或穿过人类或动物的身体以提高治疗效果的技术。DDS也可以被考虑用于体内递送,特别是用于肽和蛋白质治疗。持续的研究可能会显示出药物递送的趋势和前景。此外,本文还包括有关DDS技术的趋势和前景的全面信息。
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引用次数: 0
Development of Nanoemulsion-Based Gel of Betulin for the Treatment of Psoriasis-Like Skin Inflammation in a Small Animal Model. 小动物模型中治疗牛皮癣样皮肤炎症的纳米乳脂凝胶的研制。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-30 DOI: 10.2174/0122117385336297241210053845
Dev Prakash, Anjali Chaudhari

Introduction/ Background: This study aimed to introduce a gel (NEG) formulation containing betulin-loaded nanoemulsions for topical psoriasis treatment.

Materials and methods: The prepared nanoemulsions were optimized for smaller particle size and higher drug content using a response surface methodology that exhibited uniform distribution and high drug loading (21.17±3.55%).

Results: The gel demonstrated skin-compatible pH and good spreadability. The developed gel showed slower release compared to nanoemulsion. In vivo pharmacokinetics demonstrated elevated AUC (55835.1 μg/cm2.h) and extended Tmax (720 min) for the gel than NE, indicating extended skin retention. Improved skin hydration (35%) and lipid content (28%) were observed, along with significant reductions in PASI scores and cytokine levels.

Discussion: Provided with enhanced skin retention, improved hydration, and lipid content, along with significant therapeutic efficacy in psoriasis treatment, betulin-loaded nanoemulsion gel demonstrated prolonged drug release and notably reduced PASI scores and cytokine levels, highlighting its effectiveness against psoriasis.

Conclusion: This highlights the promising potential of NEG for topical psoriasis management.

简介/背景:本研究旨在介绍一种含有白桦素负载纳米乳液的凝胶(NEG)配方,用于局部治疗银屑病。材料与方法:采用响应面法优化制备的纳米乳具有粒径小、药物含量高、分布均匀、载药量高(21.17±3.55%)的特点。结果:该凝胶具有良好的皮肤相容性和涂抹性。与纳米乳相比,凝胶的释放速度较慢。体内药代动力学显示,与NE相比,凝胶的AUC升高(55835.1 μg/cm2.h), Tmax延长(720 min),表明皮肤滞留时间延长。观察到皮肤水合作用(35%)和脂质含量(28%)改善,PASI评分和细胞因子水平显著降低。讨论:白桦素纳米乳凝胶具有增强皮肤保持性,改善水合作用和脂质含量,在银屑病治疗中具有显著的治疗效果,可延长药物释放时间,显著降低PASI评分和细胞因子水平,突出其治疗银屑病的有效性。结论:这突出了NEG治疗局部银屑病的潜力。
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引用次数: 0
An Enhanced Scrutiny of Mechanistic and Translational Approaches to Extinguish Cancer Hypoxia. 加强对消除癌症缺氧的机制和转化方法的审查。
Q2 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2024-12-26 DOI: 10.2174/0122117385328105241216042016
Arun Radhakrishnan, Nikhitha K Shanmukhan, Linda Christabel S

Cancer continues to pose a formidable challenge in global health due to its incidence and increasing resistance to conventional therapies. A key factor driving this resistance is tumor hypoxia, characterized by reduced oxygen levels within cancer cells. This hypoxic environment triggers a variety of adaptive mechanisms, significantly compromising the efficacy of cancer treatments. Notably, hypoxia promotes metastasis and reshapes the tumor microenvironment (TME), thereby aggravating treatment resistance. Central to this process are hypoxia-inducible factors (HIFs), which mediate cellular adaptations such as metabolic shifts and enhanced survival pathways. These adaptations render therapies like chemotherapy, radiotherapy, and photodynamic therapy (PDT) less effective. Additionally, hypoxia-induced vascular irregularities further impede drug delivery, amplifying the therapeutic challenge. This review provides a comprehensive examination of the roles of hypoxia in cancer, its contributions to drug resistance, and its interplay with apoptosis and autophagy. By evaluating novel mechanistic and translational approaches to target hypoxia, this study highlights the potential to improve therapeutic outcomes and offers insights into overcoming treatment resistance in cancer.

由于癌症的发病率和对常规疗法的抵抗力不断增强,癌症继续对全球健康构成巨大挑战。驱动这种抵抗的一个关键因素是肿瘤缺氧,其特征是癌细胞内氧水平降低。这种低氧环境触发了多种适应机制,显著影响了癌症治疗的效果。值得注意的是,缺氧促进转移和重塑肿瘤微环境(TME),从而加重治疗抵抗。这个过程的核心是缺氧诱导因子(hif),它介导细胞适应,如代谢变化和增强的生存途径。这些适应性使得化疗、放疗和光动力疗法(PDT)等疗法效果降低。此外,缺氧引起的血管不规则进一步阻碍了药物输送,增加了治疗挑战。本文综述了缺氧在肿瘤中的作用、对耐药的贡献以及与细胞凋亡和自噬的相互作用。通过评估靶向缺氧的新机制和转化方法,本研究强调了改善治疗结果的潜力,并为克服癌症治疗耐药提供了见解。
{"title":"An Enhanced Scrutiny of Mechanistic and Translational Approaches to Extinguish Cancer Hypoxia.","authors":"Arun Radhakrishnan, Nikhitha K Shanmukhan, Linda Christabel S","doi":"10.2174/0122117385328105241216042016","DOIUrl":"https://doi.org/10.2174/0122117385328105241216042016","url":null,"abstract":"<p><p>Cancer continues to pose a formidable challenge in global health due to its incidence and increasing resistance to conventional therapies. A key factor driving this resistance is tumor hypoxia, characterized by reduced oxygen levels within cancer cells. This hypoxic environment triggers a variety of adaptive mechanisms, significantly compromising the efficacy of cancer treatments. Notably, hypoxia promotes metastasis and reshapes the tumor microenvironment (TME), thereby aggravating treatment resistance. Central to this process are hypoxia-inducible factors (HIFs), which mediate cellular adaptations such as metabolic shifts and enhanced survival pathways. These adaptations render therapies like chemotherapy, radiotherapy, and photodynamic therapy (PDT) less effective. Additionally, hypoxia-induced vascular irregularities further impede drug delivery, amplifying the therapeutic challenge. This review provides a comprehensive examination of the roles of hypoxia in cancer, its contributions to drug resistance, and its interplay with apoptosis and autophagy. By evaluating novel mechanistic and translational approaches to target hypoxia, this study highlights the potential to improve therapeutic outcomes and offers insights into overcoming treatment resistance in cancer.</p>","PeriodicalId":19774,"journal":{"name":"Pharmaceutical nanotechnology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142932287","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
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

Background: 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).

Materials and methods: 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).

Results: 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).

Discussion: 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。
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Pharmaceutical nanotechnology
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