Drug delivery system

药物递送系统
  • 文章类型: Journal Article
    胃肠道(GI)环境受几个因素的影响(性别、遗传学,性别,疾病状态,食物)导致口服药物吸收变异性或生物利用度低。在这种情况下,胃滞留药物递送系统(GRDDS)已经开发,以解决吸收问题,导致更有效的局部治疗或允许在比典型的口服持续释放剂型更长的时间段内持续释放药物。在所有的GRDDS中,漂浮系统似乎为实现长的胃内停留时间和持续释放曲线提供了有希望和实用的方法。在过去的几年里,正在使用一种新技术来制造这种系统:三维(3D)打印技术。该技术提供了制造个性化药物递送系统的通用且容易的方法。这项工作提出了一个系统的审查,提出了最新的制造浮动系统的主要3D打印设计。我们还总结了涉及浮力和系统持续释放的最重要参数,以促进将该技术扩大到工业水平。最后,一节讨论了材料对药物释放的影响,它们的生物相容性和安全性考虑已经包括在内。
    Gastrointestinal (GI) environment is influenced by several factors (gender, genetics, sex, disease state, food) leading to oral drug absorption variability or to low bioavailability. In this scenario, gastroretentive drug delivery systems (GRDDS) have been developed in order to solve absorption problems, to lead to a more effective local therapy or to allow sustained drug release during a longer time period than the typical oral sustained release dosage forms. Among all GRDDS, floating systems seem to provide a promising and practical approach for achieving a long intra-gastric residence time and sustained release profile. In the last years, a novel technique is being used to manufacture this kind of systems: three-dimensional (3D) printing technology. This technique provides a versatile and easy process to manufacture personalized drug delivery systems. This work presents a systematic review of the main 3D printing based designs proposed up to date to manufacture floating systems. We have also summarized the most important parameters involved in buoyancy and sustained release of the systems, in order to facilitate the scale up of this technology to industrial level. Finally, a section discussing about the influence of materials in drug release, their biocompatibility and safety considerations have been included.
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  • 文章类型: Journal Article
    Curcumol(Cur),一种愈创木型倍半萜半缩酮,是一种重要且具有代表性的生物活性成分,从郁金香根茎的精油中提取而来,在中药中也被称为“苔竹”。最近,Cur由于其良好的药理活性而受到了研究界的广泛关注,包括抗癌,保肝,抗炎,抗病毒,抗惊厥药,和其他活动,并对各种癌症发挥了治疗作用,肝脏疾病,炎症性疾病,和传染病。药代动力学研究表明,灌胃给药后,Cur在小肠和结肠中的高浓度迅速分布在大鼠的几乎所有器官中。一些关注Cur的构效关系(SAR)的研究表明,一些Cur衍生物,在C-8或C-14化学修饰,表现出比Cur本身更有效的抗癌活性和更低的毒性。这篇综述旨在全面总结Cur在过去十年中的药理和药代动力学特性的最新进展,重点是其抗癌和肝脏保护潜力。以及迄今为止Cur在药物传递系统和潜在应用方面的研究进展,为研究人员提供最新信息,强调了现阶段相关研究的局限性以及未来研究中应解决的问题。我们的结果表明,Cur及其衍生物可以作为治疗多种疾病的潜在新型药物。特别是癌症和肝脏疾病。
    Curcumol (Cur), a guaiane-type sesquiterpenoid hemiketal, is an important and representative bioactive component extracted from the essential oil of the rhizomes of Curcumae rhizoma which is also known as \"Ezhu\" in traditional Chinese medicine. Recently, Cur has received considerable attention from the research community due to its favorable pharmacological activities, including anti-cancer, hepatoprotective, anti-inflammatory, anti-viral, anti-convulsant, and other activities, and has also exerted therapeutic effect on various cancers, liver diseases, inflammatory diseases, and infectious diseases. Pharmacokinetic studies have shown that Cur is rapidly distributed in almost all organs of rats after intragastric administration with high concentrations in the small intestine and colon. Several studies focusing on structure-activity relationship (SAR) of Cur have shown that some Cur derivatives, chemically modified at C-8 or C-14, exhibited more potent anti-cancer activity and lower toxicity than Cur itself. This review aims to comprehensively summarize the latest advances in the pharmacological and pharmacokinetic properties of Cur in the last decade with a focus on its anti-cancer and hepatoprotective potentials, as well as the research progress in drug delivery system and potential applications of Cur to date, to provide researchers with the latest information, to highlighted the limitations of relevant research at the current stage and the aspects that should be addressed in future research. Our results indicate that Cur and its derivatives could serve as potential novel agents for the treatment of a variety of diseases, particularly cancer and liver diseases.
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  • 文章类型: Journal Article
    缺血性卒中(IS)的发病率随着全球人口老龄化而上升。迫切需要深入研究病理机制并开发新的神经保护策略。在本次审查中,我们讨论了在IS治疗中靶向小胶质细胞极化的各种纳米药物递送系统(NDDS)的最新进展和研究。此外,我们批判性地讨论不同的策略。NDDS已经证明了卓越的品质,可以有效地渗透血脑屏障,聚集在缺血性损伤部位,并在适当修改后靶向大脑内的特定细胞类型。因此,NDDS具有重塑小胶质细胞极化表型的巨大潜力,可能是IS的前瞻性治疗策略。IS的治疗仍然是一个挑战。然而,这篇综述为以小胶质细胞极化为中心的IS治疗提供了一个新的神经纳米医学观点,从而激发新的研究思路和方向。
    The incidence of ischemic stroke (IS) is rising in tandem with the global aging population. There is an urgent need to delve deeper into the pathological mechanisms and develop new neuroprotective strategies. In the present review, we discuss the latest advancements and research on various nanodrug delivery systems (NDDSs) for targeting microglial polarization in IS treatment. Furthermore, we critically discuss the different strategies. NDDSs have demonstrated exceptional qualities to effectively permeate the blood-brain barrier, aggregate at the site of ischemic injury, and target specific cell types within the brain when appropriately modified. Consequently, NDDSs have considerable potential for reshaping the polarization phenotype of microglia and could be a prospective therapeutic strategy for IS. The treatment of IS remains a challenge. However, this review provides a new perspective on neuro-nanomedicine for IS therapies centered on microglial polarization, thereby inspiring new research ideas and directions.
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  • 文章类型: Systematic Review
    中链三酰甘油(MCT)是一种具有6或7至12个碳链的三酰甘油。它由连接到一个甘油分子的三个脂肪酸分子组成。药物递送系统(DDS)定义为将药物分配到人体内的制剂。MCT的独特性质引起了在DDS中使用它们作为赋形剂的兴趣。尽管使用MCT有许多显著的影响,特别是在调节各种DDS中的药物递送速率方面,它们都是有限的和间歇性的。这保证了对以前在各种DDS中使用MCT的研究的详细总结。因此,这篇综述的重点是对过去6年中有关MCTs使用的研究进行系统回顾,并探讨了使用各种类型递送途径的MCTs对DDS的类型和影响.通过PubMed进行系统搜索,进行了ScienceDirect和Scopus。关键词如“中链甘油三酯”,“中链脂肪酸”,“中链甘油三酯及其馏分”,“中链脂肪酸及其馏分”,\"MCT\",“MCFA”,“在药物递送中”,使用“在药物递送系统中”及其组合。单词的同义词也用于扩展搜索。共确定了17篇符合纳入标准的文章。本综述的发现已经确定了DDS中使用的几种MCT及其部分,topic,透皮,肠胃外,和肺部给药途径。该评论还强调,在DDS中使用MCT可以更好地将药物运输到人体中。
    Medium-chain triacylglycerol (MCT) is a type of triacylglycerol that has six or seven to twelve carbon chains. It consists of three molecules of fatty acids attached to one molecule of glycerol. Drug delivery system (DDS) is defined as a formulation to distribute drugs into the human body. The unique properties of MCTs have garnered interest in using them as excipients in DDS. Even though there are many significant effects attributed to the use of MCTs, especially in modulating the rate of drug delivery in various DDS, they are all limited and intermittent. This warrants a detailed summary of the previous studies on the use of MCTs in various DDS. Therefore, this review focuses on presenting a systematic review of previous studies on the use of MCTs in the last six years and explores the types and effects of MCTs on DDS that employ various types of delivery routes. A systematic search through PubMed, Science Direct and Scopus was performed. Keywords like \"medium-chain triglycerides\", \"medium-chain fatty acids\", \"medium-chain triglycerides and their fractions\", \"medium-chain fatty acids and their fractions\", \"MCTs\", \"MCFA\", \"in drug delivery\", \"in drug delivery system\" and their combinations were used. The synonyms of the words were also used to extend the search. A total of 17 articles that met the inclusion criteria were identified. Findings from this review have identified the several MCTs and their fractions used in DDS that employed the oral/enteral, topical, transdermal, parenteral, and pulmonary routes of drug delivery. The review also highlights that the usage of MCTs in DDS results in a better transportation of drugs into the human body.
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  • 文章类型: Journal Article
    肺癌代表了一个显著的全球公共卫生问题。尽管现有的治疗方式,肺癌患者的平均5年生存率仅为20%。由于全身给药途径有许多不良反应,迫切需要开发一种专门针对肺癌患者的新型治疗策略.非侵入性雾化吸入,作为一种给药途径,在呼吸系统疾病的背景下拥有独特的优势。近年来,纳米材料在生物医学研究领域有着广泛的应用。本研究对分类进行了全面回顾,根据现有的肺癌临床治疗方式和肺癌中与可吸入微米/纳米颗粒药物递送系统(DDS)相关的挑战进行了总结。通过吸入实现肺癌临床前模型的局部治疗被认为是可行的。然而,需要进一步的研究来证实可吸入微米/纳米颗粒DDS在肺癌临床治疗中的有效性和长期安全性.
    Lung cancer represents a marked global public health concern. Despite existing treatment modalities, the average 5‑year survival rate for patients with patients with lung cancer is only ~20%. As there are numerous adverse effects of systemic administration routes, there is an urgent need to develop a novel therapeutic strategy tailored specifically for patients with lung cancer. Non‑invasive aerosol inhalation, as a route of drug administration, holds unique advantages in the context of respiratory diseases. Nanoscale materials have extensive applications in the field of biomedical research in recent years. The present study provides a comprehensive review of the classification, applications summarized according to existing clinical treatment modalities for lung cancer and challenges associated with inhalable micron/nanoparticle drug delivery systems (DDSs) in lung cancer. Achieving localized treatment of lung cancer preclinical models through inhalation is deemed feasible. However, further research is required to substantiate the efficacy and long‑term safety of inhalable micron/nanoparticle DDSs in the clinical management of lung cancer.
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  • 文章类型: Journal Article
    结直肠癌是第三大最常见的癌症,在癌症相关死亡病例中排名第二。综合疗法会产生许多不良影响,让病人放弃。近年来已经研究了纳米技术以规避局限性。由聚合物组成的组,脂质,和无机纳米粒子是最有目的的。因此,这项工作的目的是提供有关纳米系统如何改善结直肠癌化疗治疗的信息。因此,在“LILACS”等期刊中搜索,执行了“SciELO”和“PubMed/Medline”,在应用搜索引擎“纳米粒子”时发现了25,000篇文章,\"\"结直肠癌,“恶性肿瘤,“和”化疗。“在包含和排除因素之后,剩下24条,这些都被用作这次综合审查的基础。结果表明,不管矩阵的选择,纳米颗粒显示活性物质的生物利用度增加,半衰期增加了13倍,修改版本,以及肿瘤大小的显著减小,细胞活力比测试的免费药物低20%,在不同的结直肠癌细胞系中,例如HCT-116、HT-29和CaCo-2。然而,需要进行更多的体内和临床研究,不管它的矩阵是什么,旨在提高患者的安全性和制剂的稳定性,以及其药代动力学和药效学的详细指标的知识,寻求避免对受体生物体的进一步损害。
    Colorectal cancer is the third most common cancer and the second in cases of cancer-related death. Polytherapy generates many adverse effects, leading the patient to give up. Nanotechnology has been studied in recent years to circumvent limitations. Groups composed of polymeric, lipid, and inorganic nanoparticles are the most purpose. Thus, the objective of this work is to bring information on how nanosystems can improve the chemotherapeutic treatment for colorectal cancer. Therefore, a search in journals such as \"LILACS\", \"SciELO\" and \"PubMed/Medline\" was performed, resulting in 25,000 articles found when applied the search engines \"nanoparticle,\" \"colorectal cancer,\" \"malignant neoplasms,\" and \"chemotherapy.\" After inclusion and exclusion factors, 24 articles remained, which were used as the basis for this integrative review. The results reveal that, regardless of the choice of matrix, nanoparticles showed an increase in bioavailability of the active, increasing the half-life by up to 13 times, modified release, as well as a significant reduction in tumor size, with cell viability up to 20% lower than the free drug tested, in different colorectal cancer cell lines, such as HCT-116, HT-29, and CaCo-2. However, more in vivo and clinical studies need to be performed, regardless of the formulation of its matrix, aiming at a higher rate of safety for patients and stability of the formulations, as well as knowledge of detailed indices of its pharmacokinetics and pharmacodynamics, seeking to avoid further damage to the recipient organism.
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  • 文章类型: Journal Article
    前列腺癌(PCa)是最常见的实体器官恶性肿瘤,严重影响男性健康。前列腺癌治疗的副作用可对患者造成继发性损害。纳米治疗学,具有特殊的靶向能力和受控的治疗释放曲线,可作为PCa治疗的替代药物。目前,已经开发了许多纳米疗法来治疗PCa,并且在动物中显示出比传统疗法更好的治疗效果。尽管PCa纳米疗法非常有吸引力,在临床实践中很少报道成功的病例。为了帮助研究人员为PCa治疗设计有价值的纳米疗法,避免无用的努力,在这里,我们首先回顾了前列腺癌治疗的策略和挑战.随后,我们提出了用于PCa治疗的纳米疗法的全面综述,包括他们的瞄准方法,控制释放策略,治疗方法和机制。最后,我们提出了纳米治疗PCa的未来前景。
    Prostate cancer (PCa) is the most prevalent solid organ malignancy and seriously affects male health. The adverse effects of prostate cancer therapeutics can cause secondary damage to patients. Nanotherapeutics, which have special targeting abilities and controlled therapeutic release profiles, may serve as alternative agents for PCa treatment. At present, many nanotherapeutics have been developed to treat PCa and have shown better treatment effects in animals than traditional therapeutics. Although PCa nanotherapeutics are highly attractive, few successful cases have been reported in clinical practice. To help researchers design valuable nanotherapeutics for PCa treatment and avoid useless efforts, herein, we first reviewed the strategies and challenges involved in prostate cancer treatment. Subsequently, we presented a comprehensive review of nanotherapeutics for PCa treatment, including their targeting methods, controlled release strategies, therapeutic approaches and mechanisms. Finally, we proposed the future prospects of nanotherapeutics for PCa treatment.
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  • 文章类型: Journal Article
    骨质疏松,骨密度低,骨折风险增加,这是一个重大的医疗挑战。抗吸收和合成代谢药物现在用于治疗骨质疏松症,以减少骨质流失和增加骨量。由于目前的疗法具有缺点,因此需要创新的方法。纳米技术提供了改善骨骼健康和药物输送的有希望的选择。双膦酸盐与四环素和寡肽,在其他靶向骨骼的化合物中,更容易为骨组织提供特定的药物。此外,纳米载体对于治疗骨质疏松症的有机和无机纳米颗粒的给药至关重要。药物包封和控制释放可以使用有机纳米颗粒以多种方式进行。无机纳米粒子具有特殊的品质,有助于药物运输和骨修复。这篇综述探讨了基于纳米颗粒的策略在骨质疏松症治疗中的潜力。
    Osteoporosis, characterized by low bone density and increased risk of fractures, represents a major healthcare challenge. Anti-resorptive and anabolic medications are now used to treat osteoporosis in an effort to reduce bone loss and increase bone mass. Innovative methods are required since current therapies have drawbacks. Promising options for improving bone health and medicine delivery are provided by nanotechnology. Bisphosphonates with tetracyclines and oligopeptides, among other compounds that target the bone, make it easier to provide a particular medication to bone tissue. Additionally, nanocarriers are essential for the administration of both organic and inorganic nanoparticles in the treatment of osteoporosis. Drug encapsulation and controlled release may be done in a variety of ways using organic nanoparticles. Inorganic nanoparticles have special qualities that help in medication transport and bone repair. This review explores the potential of nanoparticle-based strategies in the treatment of osteoporosis.
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  • 纳米凝胶是纳米级的三维网络,可以通过使用聚合物的物理或化学过程来制造。这些纳米粒子的生物相容性,显著的稳定性,有效的载药量,和配体结合能力使它们非常适合用作药物递送工具。此外,它们表现出对内源性和外源性刺激作出反应的能力,其中可能包括温度等因素,照明,pH值,以及各种各样的其他因素。这有助于将药物一致地施用到预期部位。由于其生物相容性,海藻酸盐生物聚合物已被用于封装抗癌药物,亲水性能,和成本效益。基于藻酸盐纳米凝胶的系统在癌症治疗中的功效已通过多项研究得到证明,这些研究支持其在临床实施方面的进展。本文全面综述了海藻酸盐及其相关系统在药物递送系统中的应用。
    Nanogels are three-dimensional networks at the nanoscale level that can be fabricated through physical or chemical processes using polymers. These nanoparticles\' biocompatibility, notable stability, efficacious drug-loading capacity, and ligand-binding proficiency make them highly suitable for employment as drug-delivery vehicles. In addition, they exhibit the ability to react to both endogenous and exogenous stimuli, which may include factors such as temperature, illumination, pH levels, and a diverse range of other factors. This facilitates the consistent administration of the drug to the intended site. Alginate biopolymers have been utilized to encapsulate anticancer drugs due to their biocompatible nature, hydrophilic properties, and cost-effectiveness. The efficacy of alginate nano gel-based systems in cancer treatment has been demonstrated through multiple studies that endorse their progress toward clinical implementation. This paper comprehensively reviews alginate and its associated systems in drug delivery systems.
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  • 文章类型: Journal Article
    在药物研发领域,在过去的十年中,熔融沉积模型(FDM)3D打印(3DP)引起了人们越来越多的兴趣。热塑性聚合物的使用,结合原材料的熔化过程,提供了制造无定形固体分散体(ASD)的可能性。在制药行业,ASD的制剂是广泛使用的策略,以改善难溶性药物(由生物药物分类系统(BCS)分类为II类和IV类)的溶解度。在这次审查中,对开发出含有BCSII类或IV类活性物质的FDM打印形式的研究进行了分析。重点放在评估活性分子(结晶或无定形)的固态和研究其溶解曲线上。因此,这项工作的目的是强调FDM3DP通过形成ASD来诱导II类和IV类活性物质的非晶化现象的兴趣,结果提高了它们的溶解度。
    In the field of pharmaceutical research and development, Fused Deposition Modelling (FDM) 3D printing (3DP) has aroused growing interest within the last ten years. The use of thermoplastic polymers, combined with the melting process of the raw materials, offers the possibility of manufacturing amorphous solid dispersions (ASDs). In the pharmaceutical industry, the formulation of an ASD is a widely used strategy to improve the solubility of poorly soluble drugs (classified by the Biopharmaceutical Classification System (BCS) as class II and IV). In this review, an analysis of studies that have developed a FDM printed form containing a BCS class II or IV active substance was performed. The focus has been placed on the evaluation of the solid state of the active molecules (crystalline or amorphous) and on the study of their dissolution profile. Thus, the aim of this work is to highlight the interest of FDM 3DP to induce the amorphisation phenomenon of Class II and IV active substances by forming an ASD, and as result improving their solubility.
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