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Nanogel development and its importance in ophthalmic drug delivery system 纳米凝胶的发展及其在眼科给药系统中的重要性
Q3 Medicine Pub Date : 2022-09-15 DOI: 10.2174/2468187312666220915150636
S. Gaikwad, Sahil Jadhav, K. Salunkhe
The current review focuses on ophthalmic nanogels, their applications,their benefits over traditional gels, and the challenges and opportunities of nanogels. The major goalis to investigate ophthalmic nanogels from preparation through characterization and how nanogelsare the future of the ophthalmic drug delivery system compared to traditional gels, eye drops, andointments.Because of the ophthalmic bioavailability, delivery to the eye is crucial. The lacrimal fluid in the eye clears the eye surface, and the ocular sight is washed away as a result of this medicine.The limited ocular bioavailability was also due to the different obstacles present. Drug nano-gellingsystems are effective in improving ocular bioavailability and corneal permeation time. Nanoparticles abound in these nanogels. Various natural polymers, such as Chitosan and Alginate, and synthetic polymers, such as PLA and PLGA, can be used to make nanogels. The use of nanotechnologyimproves medicine bioavailability and penetration in the eye. However, nanotechnology has somelimits, such as large-scale manufacturing, restricting medicine dNanotechnology offers much clinical potential when it comes to treating eye issues.Although ophthalmic nanogels are suited for effective drug delivery, they must meet several requirements. First, the drug component must be encapsulated adequately in a stable polymer complex. In ocular drug delivery, nanogels are a preferable option since they can improve patient compliance and therapeutic impact. In addition, the nanogel has a faster corneal penetration time andhigher bioavailability
目前的综述主要集中在眼科纳米凝胶、其应用、与传统凝胶相比的优势以及纳米凝胶的挑战和机遇。主要目标是从制备到表征研究眼科纳米凝胶,以及与传统凝胶、滴眼液和注射剂相比,纳米凝胶如何成为眼科药物递送系统的未来。由于眼科的生物利用度,输送到眼睛是至关重要的。眼睛里的泪液会清除眼睛表面,这种药物会冲走眼睛的视力。眼部生物利用度有限也是由于存在不同的障碍。药物纳米凝胶系统在提高眼睛生物利用度和角膜渗透时间方面是有效的。这些纳米凝胶中有大量的纳米粒子。各种天然聚合物,如壳聚糖和海藻酸盐,以及合成聚合物,如PLA和PLGA,可用于制备纳米凝胶。纳米技术的使用提高了药物的生物利用度和在眼睛中的渗透性。然而,纳米技术也有一些局限性,比如大规模生产,限制了医学。纳米技术在治疗眼部问题方面具有很大的临床潜力。尽管眼科纳米凝胶适用于有效的药物递送,但它们必须满足几个要求。首先,药物成分必须充分封装在稳定的聚合物复合物中。在眼部给药中,纳米凝胶是一种优选的选择,因为它们可以提高患者的依从性和治疗效果。此外,纳米凝胶具有更快的角膜穿透时间和更高的生物利用度
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引用次数: 0
Possibility of liver cancer treatment by nanoformulation of phenolic phytochemicals. 酚类植物化学物质纳米配方治疗肝癌的可能性。
Q3 Medicine Pub Date : 2022-09-08 DOI: 10.2174/2468187312666220908094042
Prasun Patra, Debayan Banik
Cancer is a group of disease where the body cells continuously grow without proper cell division thereby, causing tumours and leading to metastasis. Among many types of cancer, liver cancer remains a common and leading cause of human death. Plants have always been a great source of medicine and pharmacotherapy. Phytochemicals are plant produced metabolites and phenolic phytochemicals are a subclass of it. Phenolic phytochemicals like curcumin, gallic acid and EGCG are secondary plant metabolites. They have been found to be effective and can improve the cell signalling pathways that govern cancer cell proliferations, inflammations, nearby invasions, and apoptosis. These phenolic phytochemicals greatly induce cell apoptosis and inhibit cancer cell growth. In this review article, we discuss how to improve the mentioned phytochemical's potency against hepatocellular carcinoma (HCC). One of the best approaches to improve the efficacy of these natural phytochemicals is to prepare nano formulations of these phytochemicals. Nano formulations impressively increase bioavailability, stability, absorption in the body and increased efficiency of these phytochemicals. The diverse character of many nanoparticles (NP) discussed in this article enables these systems to exhibit strong anticancer activity, emphasising combined therapy's benefits and necessity to combat cancer. In addition, nano formulations of these phenolic phytochemicals remarkably show a high apoptosis rate against HepG2 cells (HCC).
癌症是一组身体细胞在没有适当细胞分裂的情况下持续生长,从而导致肿瘤并导致转移的疾病。在许多类型的癌症中,癌症仍然是人类死亡的常见和主要原因。植物一直是医学和药物治疗的重要来源。植物化学物质是植物产生的代谢产物,酚类植物化学物质属于其中的一个亚类。姜黄素、没食子酸和EGCG等酚类植物化学品是次生植物代谢产物。它们被发现是有效的,可以改善控制癌症细胞增殖、炎症、附近侵袭和凋亡的细胞信号通路。这些酚类植物化学物质极大地诱导细胞凋亡并抑制癌症细胞生长。在这篇综述文章中,我们讨论了如何提高上述植物化学物质对肝细胞癌(HCC)的效力。提高这些天然植物化学物质功效的最佳方法之一是制备这些植物化学物质的纳米制剂。纳米制剂显著提高了生物利用度、稳定性、在体内的吸收,并提高了这些植物化学物质的效率。本文中讨论的许多纳米颗粒(NP)的多样性使这些系统表现出强大的抗癌活性,强调了联合治疗对抗癌症的益处和必要性。此外,这些酚类植物化学物质的纳米制剂显著显示出对HepG2细胞(HCC)的高凋亡率。
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引用次数: 0
Development and Evaluation of Topical Nanoemulgel Formulation of Tazarotene for Effective Treatment of Excision Wounds 他沙罗汀纳米凝胶外用治疗切除伤口的研究进展
Q3 Medicine Pub Date : 2022-08-20 DOI: 10.2174/2468187312666220820161123
Shanta Mahajan, Kirandeep Kaur, N. Saini, T. Chaudhary, Lovedeep Nim, Neena Bedi
The aim of the present investigation entails the development and evaluation of topical nanoemulgel formulation of tazarotene for effective treatment of excision woundsTazarotene (TZR) is a retinoid derivative marketed for the treatment of acne and psoriasis and the recent investigations indicate its excellent wound healing potential. Despite having magnificent wound healing potential, it suffers from pharmacokinetic limitations of low aqueous solubility and local bioavailability. Conventional marketed formulations of TZR have been reported to cause significant skin irritation and redness after its topical application. Keeping this in view, present investigation was designed to develop nanoemulsion based gel with intention to resolve the above mentioned pharmacokinetic and pharmacodynamic issues.The goal of the study was to develop a stable and effective tazarotene-loaded nanoemulgel for treating excision wounds which can also overcome the issues associated with the native drug.Various oils, surfactants and co-surfactants were selected on the basis of their solubilisation potential for tazarotene. Pseudoternary phase plots were constructed to obtain stable nanoemulsion region for various proportions of oil, surfactant: co-surfactant (Smix) and water and determine optimized concentration ranges for robust formulation of tazarotene. Various characterization parameters were studied to investigate the optimized formulation having desired attributes of nanoemulsion. Reducing power assay and phamacodymanic studies were conducted to determine the wound healing potential of developed nanoemulgel.TZR loaded nanoemulsion was successfully developed with nano-sized globules using tea tree oil with Tween 20 as surfactant and PEG 400 as co-surfactant. Prepared nanoemulsions were thermodynamically stable and were further gellified using Carbopol 940 as biodegradable gelling polymer. Prepared gels showed good spreadability, drug permeation and stability. In vivo investigations demonstrated that optimized formulation successfully masked the irritant nature of tazarotene. Moreover, the pharmacodynamic evaluation of developed nanoemulsion gel revealed its significant analgesic, anti-inflammatory properties in addition to its markable wound contraction as compared to control.The results demonstrated potential of developed nanoemulgel over marketed formulation to overcome the drawbacks like redness and erythema. It also showed significant healing efficacy over other
本研究的目的是开发和评估他扎罗汀的局部纳米乳液制剂,用于有效治疗切除伤口。塔扎罗汀(TZR)是一种用于治疗痤疮和银屑病的类视黄醇衍生物,最近的研究表明其具有良好的伤口愈合潜力。尽管它具有巨大的伤口愈合潜力,但它存在低水溶性和局部生物利用度的药代动力学限制。据报道,TZR的常规市售制剂在局部应用后会引起严重的皮肤刺激和发红。有鉴于此,本研究旨在开发基于纳米乳液的凝胶,以解决上述药代动力学和药效学问题。该研究的目的是开发一种稳定有效的负载他扎罗汀的纳米乳胶凝胶,用于治疗切除伤口,也可以克服与天然药物相关的问题。根据其对他扎罗汀的增溶潜力,选择了各种油、表面活性剂和助表面活性剂。构建了假三元相图,以获得不同比例的油、表面活性剂:共表面活性剂(Smix)和水的稳定纳米乳液区域,并确定他扎罗汀稳健配方的最佳浓度范围。研究了各种表征参数,以研究具有所需性质的纳米乳液的优化配方。进行了还原力分析和阶段性研究,以确定所开发的纳米乳胶凝胶的伤口愈合潜力。以茶树油为原料,以吐温20为表面活性剂,PEG400为共表面活性剂成功制备了TZR负载纳米乳液。所制备的纳米乳液是热力学稳定的,并且使用Carbopol 940作为可生物降解的胶凝聚合物进一步胶凝。制备的凝胶具有良好的铺展性、药物渗透性和稳定性。体内研究表明,优化配方成功掩盖了他扎罗汀的刺激性。此外,与对照组相比,所开发的纳米乳液凝胶的药效学评估显示,除了显著的伤口收缩外,还具有显著的镇痛和抗炎特性。结果表明,与市场上的配方相比,所开发的纳米乳液有潜力克服发红和红斑等缺点。与其他药物相比,它也显示出显著的治疗效果
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引用次数: 0
Dexamethasone Loaded Electrospun Nanocomposite Ocular Insert: In-vitro Drug Release and Mechanical Assessment 地塞米松负载电纺纳米复合材料眼内植入物的体外药物释放和力学评价
Q3 Medicine Pub Date : 2022-08-06 DOI: 10.2174/2468187312666220806133901
R. Agarwal, Dhwani Rana, Sagar Salave, Derajram Benival
Dexamethasone is currently available as suspension for the treatment of anterior ocular inflammatory diseases that are given through eye drops. Upon topical delivery by eye-drops, less than 5% of the drug gets absorbed when applied topically as eye drops. The major portion of administered drug either comes out from the eye or gets subjected to nasolacrimal drainage resulting in poor bioavailability.The present study is aimed at developing polymeric ocular insert containing dexamethasone as a drug by employing the use of electrospinning technique.Dexamethasone (0.1% w/v) loaded electrospun sheet was also made using 10% w/v EC: HPMC: PEO (60:20:20) in solvent system of ethanol: water (90:10) at optimized electrospinning parameters of 12kV with a flow rate of 0.8mL/hr and distance of 20 cm between tip and collector.The prepared nanocomposite insert was characterized for DSC and FTIR-ATR spectroscopy revealing no physical-chemical interaction between drug with polymers. The thickness of the electrospun sheet was found to be 270±0.02 μm and % drug content was found to be 0.43±0.01% w/w. The release profile showed that around 95% drug was released in 48 hrs. This release profile showed the prepared drug-loaded electrospun ocular insert was best suitable for once-a-day delivery. Assessment of mechanical properties like young’s modulus, tensile strength, and % elongation showed that the prepared insert can be handled easily without any breakage or damage.Upon delivery in conjunctival sac, this is best suitable for once-a-day delivery. The developed electrospun insert, consisting of a unique polymer composite of biodegradable polymers, avails the benefits of nanofibers imparting prolonged release and this novel formulation overcomes the limitations of conventional therapies. This reduces the dosing frequency and improves patient compliance.
地塞米松目前可作为眼前炎性疾病的悬浮液,通过滴眼液给予治疗。当局部滴眼液时,不到5%的药物被吸收。给药的大部分药物要么从眼睛流出,要么通过鼻泪引流,导致生物利用度差。本研究旨在利用静电纺丝技术开发含地塞米松的聚合物眼植入物。在乙醇:水(90:10)的溶剂体系中,以10% w/v EC: HPMC: PEO(60:20:20)为负载地塞米松(0.1% w/v)的静电纺丝片,最佳静电纺丝参数为12kV,流速为0.8mL/hr,针尖与捕集剂之间的距离为20cm。用DSC和FTIR-ATR对制备的纳米复合插入物进行了表征,发现药物与聚合物之间没有物理化学相互作用。电纺丝片的厚度为270±0.02 μm,药物含量为0.43±0.01% w/w。释放谱显示,约95%的药物在48小时内释放。该释放谱显示所制备的载药电纺丝眼植入物最适合每天一次给药。杨氏模量、抗拉强度和伸长率等机械性能的评估表明,制备的插入物可以很容易地处理,没有任何断裂或损坏。在结膜囊内分娩时,最适合每天一次分娩。所开发的电纺丝插入物由一种独特的可生物降解聚合物复合材料组成,利用纳米纤维延长释放的优点,这种新配方克服了传统疗法的局限性。这减少了给药频率,提高了患者的依从性。
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引用次数: 1
Iron oxide nano particles and its applications to cure HER2-positive mediated breast cancer 氧化铁纳米颗粒及其在治疗her2阳性介导乳腺癌中的应用
Q3 Medicine Pub Date : 2022-07-29 DOI: 10.2174/2468187312666220729160759
Dilpreet K Singh, B. Kurmi, GS Sarma, Sankha Bhattacharya, Sanjay A. Nagdev
Breast cancer is the second leading cause of death in women worldwide. The extremely rapid rate of metastasis and the propensity to develop resistance to all non-traditional treatments make them equally difficult to treat, which are the causes of increased morbidity and death in breast melanoma patients. Experts all around the world have been focusing on the first detection of a breast lump so that action can be taken at the earliest possible time. Furthermore, traditional treatment procedures such as chemotherapy, radiation, and local surgical treatment suffer from a slew of drawbacks, including toxicity, normal cell genetic modification, and cancer cell spread to healthy tissues. As a result, new therapy regimens with little toxicity to normal cells must be developed very away.Iron oxide nanoparticles are still widely utilized for heat targeting and imaging of breast development cells. Using an external magnetic field, they can be coupled with medicines, proteins, enzymes, antibodies, or nucleotides and delivered to target organs, tissues, or malignancies.Both in vitro and in vivo, iron oxide nanoparticles have been found to be effective as theranostics treating breast cancer. Furthermore, their interactions with pharmaceuticals or functional biomolecules improve drug delivery efficiency and reduce drug systemic toxicity.The multipurpose presentations of superparamagnetic iron oxide nanoparticles on the analysis, behavior, and perceiving development of breast disease remedy are emphasized in this assessment. Because of their remarkable superparamagnetic, biocompatible, and biodegradable qualities, they are widely used.
乳腺癌是全世界妇女死亡的第二大原因。转移的极快速度和对所有非传统治疗方法产生耐药性的倾向使其同样难以治疗,这是乳房黑色素瘤患者发病率和死亡率增加的原因。世界各地的专家都在关注首次发现乳房肿块,以便尽早采取措施。此外,传统的治疗方法,如化疗、放疗和局部手术治疗,都有一系列的缺点,包括毒性、正常细胞基因修饰和癌细胞扩散到健康组织。因此,对正常细胞毒性小的新治疗方案必须在很远的地方开发出来。氧化铁纳米颗粒仍广泛用于乳腺发育细胞的热靶向和成像。利用外部磁场,它们可以与药物、蛋白质、酶、抗体或核苷酸结合,并递送到目标器官、组织或恶性肿瘤。无论是在体内还是体外,氧化铁纳米颗粒都被发现是治疗乳腺癌的有效药物。此外,它们与药物或功能性生物分子的相互作用提高了药物传递效率,降低了药物的全身毒性。超顺磁性氧化铁纳米颗粒在乳腺疾病治疗的分析、行为和感知发展方面的多用途展示在本评估中被强调。由于其优异的超顺磁性、生物相容性和可生物降解性,被广泛应用。
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引用次数: 1
Meet the Editorial Board Member 会见编辑委员会成员
Q3 Medicine Pub Date : 2022-07-01 DOI: 10.2174/246818731202221019161211
A. Al Moustafa
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引用次数: 0
Nanogel development and its application in transdermal drug delivery system 纳米凝胶的研制及其在透皮给药系统中的应用
Q3 Medicine Pub Date : 2022-06-30 DOI: 10.2174/2468187312666220630152606
S. Gaikwad, Nisarga V. Akalade, K. Salunkhe
Nanogels are hydrophilic polymer networks that range in size from 20 to 200 nanometers. Polymer is used to make nanogels, which can come from natural or manufactured sources. Nanogels can deliver peptides, antigens, carbohydrates, oligonucleotides, proteins, and genes, among other things. These nanogels also provide inorganic materials such as silver nanoparticles and quantum dots. Both solid and liquid nanogels have the same properties. These nanogels penetrate the stratum corneum more effectively than conventional gels. Dermatology and cosmetology have both experimented with nanoscale technology.The medication can penetrate the stratum corneum through a variety of routes. One of the ways lipids can infiltrate the skin membrane is through the transcellular route. Cream, gel, ointment, lotion, thin-film, and foams are among the topical preparations used. Nanogels are categorised into two types: those that respond to stimuli and those that cross-link. For the manufacture of nanogels, numerous polymers of synthetic, natural, or semisynthetic origin are commonly employed. Nanoprecipitation, emulsion polymerization, and dispersion polymerization are all ways for making these nanogels. These nanogels are rarely released by diffusion mechanism by Fick’s law.The nano gel is a new advanced technology that allows us to improve drug molecule penetration in the stratum corneum. If poorly soluble and permeable medications are administered through this nanogel technology, their solubility and permeability will be improved.
纳米凝胶是一种亲水性聚合物网络,尺寸从20纳米到200纳米不等。聚合物用于制造纳米凝胶,纳米凝胶可以来自天然或人造来源。纳米凝胶可以传递多肽、抗原、碳水化合物、寡核苷酸、蛋白质和基因等。这些纳米凝胶也提供了无机材料,如银纳米粒子和量子点。固体和液体纳米凝胶具有相同的性质。这些纳米凝胶比传统凝胶更有效地穿透角质层。皮肤病学和美容学都在试验纳米技术。药物可通过多种途径进入角质层。脂质渗透皮肤膜的途径之一是通过跨细胞途径。乳霜、凝胶、软膏、乳液、薄膜和泡沫是使用的外用制剂。纳米凝胶分为两种:一种是对刺激有反应的,另一种是交联的。为了制造纳米凝胶,通常使用许多合成的、天然的或半合成的聚合物。制备纳米凝胶的方法有纳米沉淀法、乳液聚合法和分散聚合法。根据菲克定律,这些纳米凝胶很少通过扩散机制被释放。纳米凝胶是一种新的先进技术,它使我们能够提高药物分子在角质层中的渗透。如果通过这种纳米凝胶技术施用低溶性和渗透性药物,它们的溶解度和渗透性将得到改善。
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引用次数: 0
Pickering emulsions: a potential strategy to limiting cancer development 皮克林乳剂:限制癌症发展的潜在策略
Q3 Medicine Pub Date : 2022-05-26 DOI: 10.2174/2468187312666220526102023
Sushilkumar Singh, Aseem Setia, Shambhavi Singh, Yudhishthir Singh, D. Joshi, Sankha Bhattacharya
Pickering Emulsion therapy is a novel approach to treating various human diseases, including cancer. Traditional cancer treatment modalities, such as surgery, radiation, radiotherapy, and immunotherapy, have only achieved a minimal level of success. The use of Pickering emulsion in cancer therapeutics has given cancer patients new hope. Pickering Emulsions have grown in popularity over the last 15 years, owing to their highly desirable properties, which are similar to those of ordinary emulsions, namely their excellent stability. This review focused on the benefits, drawbacks, characterization parameters (droplet size and stability, for example), opportunities, and different development procedures of Pickering Emulsion for cancer diseases. This review also addressed recent developments in Pickering Emulsions' technological issues. It looked at the advantages and disadvantages of using such formulations for topical pharmaceutical and cosmetic applications instead of traditional surfactant-based methods. Pickering Emulsion's evolution as a multifunctional dosage form carrier reflects renewed optimism of the pharmaceutical and cosmetic industries.
皮克林乳剂疗法是一种治疗包括癌症在内的各种人类疾病的新方法。传统的癌症治疗方式,如手术、放疗、放射治疗和免疫疗法,只取得了最低程度的成功。皮克林乳剂在癌症治疗中的应用给癌症患者带来了新的希望。皮克林乳液在过去的15年里越来越受欢迎,因为它们具有与普通乳液相似的非常理想的性能,即优异的稳定性。这篇综述的重点是Pickering乳液治疗癌症疾病的益处、缺点、特征参数(例如液滴大小和稳定性)、机会和不同的开发程序。这篇综述还讨论了皮克林乳液技术问题的最新进展。它考察了将这种制剂用于局部药物和化妆品应用而不是传统的基于表面活性剂的方法的优点和缺点。皮克林乳液作为一种多功能剂型载体的发展反映了制药和化妆品行业的新乐观情绪。
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引用次数: 0
Nanomedicine in neuroscience: An application towards the treatment of various neurological diseases 神经科学中的纳米医学:在治疗各种神经系统疾病中的应用
Q3 Medicine Pub Date : 2022-05-16 DOI: 10.2174/2468187312666220516144008
Vajagathali M, Iyshwarya B.K, R. V
The effectiveness, cell viability, and selective delivery of medications and diagnostic substances to target organs, tissues, and organs are typical concerns in the care and prognosis of numerous illnesses. Neurological diseases pose complex challenges, as cerebral targeting represents a yet unresolved challenge in pharmacotherapy, owing to the blood-brain boundary, a densely compacted membrane of endothelial cells that prohibits undesired chemicals from reaching the brain. Engineered nanoparticles, components with aspects of 1–100 nm, deliver intriguing biomedicine techniques possibly allowed to fix these issues, including the ability to pass the blood-brain barrier. Nanoparticles have been substantially explored in the previous century, contributing to substantial progress in biomedical studies and medical procedures. Furthermore, the use of many synthesized nanoparticles on the molecular levels has given many potential gains in various domains of regenerative medicine, such as illness detection, cascaded cell treatment, tissue regeneration, medication, and gene editing.The recent milestone in nanotechnology is to attempt to cure various neurological diseases such as Alzheimer's, Parkinson's, multiple sclerosis, and psychiatric disorders. This review will encapsulate the novel developments of nanostructured components used in neurological diseases with an underline on the most recent discoveries and forecasts for the future of varied biological nanoparticles for tissue repair, drug inventions, and the synthesizing of the delivery mechanism.Based on the information obtained from the literature, it is concluded that nanotechnology has been considered the novel therapeutic strategy to protect and regenerate the neurons in various diseases.
药物和诊断物质对靶器官、组织和器官的有效性、细胞活力以及选择性递送是许多疾病护理和预后的典型问题。神经系统疾病带来了复杂的挑战,因为脑靶向是药物治疗中一个尚未解决的挑战,这是由于血脑边界,即一层密集的内皮细胞膜,阻止不需要的化学物质进入大脑。工程纳米颗粒是1-100纳米的组件,提供了有趣的生物医学技术,可能可以解决这些问题,包括通过血脑屏障的能力。纳米颗粒在上个世纪已经被大量探索,为生物医学研究和医疗程序的重大进展做出了贡献。此外,许多合成的纳米颗粒在分子水平上的使用在再生医学的各个领域带来了许多潜在的收获,如疾病检测、级联细胞治疗、组织再生、药物和基因编辑。纳米技术最近的里程碑是试图治愈各种神经疾病,如阿尔茨海默氏症、帕金森氏症、多发性硬化症和精神障碍。这篇综述将概述用于神经疾病的纳米结构成分的最新发展,重点介绍用于组织修复、药物发明和递送机制合成的各种生物纳米颗粒的最新发现和未来预测。根据从文献中获得的信息,可以得出结论,纳米技术被认为是在各种疾病中保护和再生神经元的新治疗策略。
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引用次数: 0
Formulation and Evaluation of Naproxen Sodium Loaded Invasomes for Topical Delivery 萘普生钠局部给药血管内舒的处方与评价
Q3 Medicine Pub Date : 2022-05-13 DOI: 10.2174/2468187312666220513113117
A. Shailaja, Uzma Afreen
Naproxen sodium is a Non-steroidal anti-inflammatory agent used in treatment of rheumatoid arthritis, ankylosing spondylitis to relieve pain and inflammation. It is mainly act by inhibiting COX1 and COX2 receptors. By inhibiting COX1 receptor it causes severe gastric bleeding and peptic ulcer and by inhibiting COX2 receptor it causes cardiovascular side effects.In order to avoid the adverse effects of naproxen there is need to develop novel drug delivery system. So that invasomes because of its vesicular structure they are capable of penetrating more into the systemic circulation and they will be acting locally as well as systemically.In this study attempts have been made to prepare and characterize Naproxen sodium loaded invasomes. Naproxen sodium loaded invasomes were prepared by thin film hydration technique by using soya lecithin as lipid, span60 as surfactant, limonene as terpene and methanol, ethanol and chloroform as organic solvents. Total twelve formulations (INV1-INV12) of invasomes were prepared, in which four formulations were prepared by varying drug to surfactant ratio and eight formulations were prepared by varying drug to lipid ratio.All the formulations were evaluated for drug content, entrapment efficiency, particle size, zeta potential and invitro drug release. Among the twelve formulations of invasomestheINV2 formulation (1:1) ratio containing 40mg drug and 40mg surfactant (span60) was found to be the best formulation with drug content of 96.62%, entrapment efficiency of 90.9%, zeta potential of -68.5mV, mean particle diameter of 572.4 nm and invitro drug release of 91.6% in a time period of 12 hrs and followed the zero order kinetics with non fickian diffusion mechanism.In this present study naproxen sodium loaded invasomes were successfully prepared and evaluated.
萘普生钠是一种非甾体抗炎药,用于治疗类风湿关节炎、强直性脊柱炎,减轻疼痛和炎症。它主要通过抑制COX1和COX2受体起作用。它通过抑制COX1受体引起严重的胃出血和消化性溃疡,通过抑制COX2受体引起心血管副作用。为了避免萘普生的不良反应,需要开发新的给药系统。因此侵入体由于它的囊泡结构它们能够深入到体循环中它们既能局部作用也能全身作用。本研究试图制备并表征萘普生钠负载侵入体。以大豆卵磷脂为脂质,span60为表面活性剂,柠檬烯为萜烯,甲醇、乙醇和氯仿为有机溶剂,采用薄膜水合技术制备了萘普生钠负载侵入体。共制备了12种侵入体制剂(inv1 ~ inv12),其中4种为变药脂比制剂,8种为变药脂比制剂。对各制剂进行药物含量、包封效率、粒径、zeta电位和体外药物释放度评价。12个制剂中,以含40mg药物与40mg表面活性剂(span60)比例为1:1的inv2制剂为最佳制剂,其药物含量为96.62%,包封效率为90.9%,zeta电位为-68.5mV,平均粒径为572.4 nm, 12 h的体外释药率为91.6%,符合零级动力学,具有非动力学扩散机制。本研究成功制备了萘普生钠负载侵入体并对其进行了评价。
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引用次数: 1
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Current Nanomedicine
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