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Chitosan-based Nanomedicine in the Management of Age-related MacularDegeneration: A Review 基于壳聚糖的纳米药物在老年性黄斑变性治疗中的应用:综述
Q3 Medicine Pub Date : 2024-03-01 DOI: 10.2174/0124681873261772230927074628
Swarupananda Mukherjee, D. Karati, Sudarshan Singh, Bhupendra G. Prajapati
Age-related macular degeneration (AMD) is a leading cause of permanent blindness globally. Due to the various obstacles, highly invasive intravitreal (IVT) injections are the prima-ry method used to deliver medications to the tissues of the posterior eye. An utmost patient-friendly topical ocular delivery approach has been extensively researched in recent years. Muco-adhesive compositions extend precorneal residence time while reducing precorneal clearance. They increase the likelihood of adhesion to corneal and conjunctival surfaces and, as a result, al-low for enhanced delivery to the posterior eye segment. Due to its remarkable mucoadhesive characteristics, chitosan (CS) has undergone the most extensive research of any mucoadhesive polymer. Drug delivery to the front and back of the eye is still difficult. The pharmaceutical in-dustry has shown greater interest in drug delivery systems (DDSs) based on nanotechnology (NT) in recent years, particularly those made from natural polymers like chitosan, alginate, etc. Be-cause of their incredible adaptability, higher biological effects, and favourable physicochemical properties, CS-oriented nanomaterials (NMs) are explored by researchers as prospective nanocar-riers. CS are the right substrates to develop pharmaceutical products, such as hydrogels, nanopar-ticles (NP), microparticles, and nanofibers, whether used alone or in composite form. CS-based nanocarriers deliver medicine, such as peptides, growth factors, vaccines, and genetic materials in regulated and targeted form. This review highlights current developments and challenges in chi-tosan-mediated nano therapies associated with AMD.
年龄相关性黄斑变性(AMD)是导致全球永久性失明的主要原因。由于存在各种障碍,高侵入性的玻璃体内注射(IVT)是向后眼组织输送药物的主要方法。近年来,一种最方便患者的局部眼部给药方法得到了广泛研究。粘液粘合剂成分可延长角膜前停留时间,同时降低角膜前清除率。它们增加了粘附在角膜和结膜表面的可能性,因此,可以更好地向后眼节给药。由于壳聚糖(CS)具有显著的粘附特性,因此在所有粘附聚合物中,壳聚糖的研究最为广泛。将药物输送到眼球的前部和后部仍然很困难。近年来,制药行业对基于纳米技术(NT)的给药系统(DDSs)表现出了更大的兴趣,尤其是由壳聚糖、海藻酸盐等天然聚合物制成的给药系统。由于 CS 具有令人难以置信的适应性、更高的生物效应和良好的物理化学特性,研究人员正在探索将 CS 纳米材料(NMs)作为未来的纳米载体。无论是单独使用还是以复合形式使用,希尔思都是开发水凝胶、纳米颗粒(NP)、微颗粒和纳米纤维等医药产品的合适基质。以 CS 为基础的纳米载体能以受控和定向的形式输送药物,如肽、生长因子、疫苗和遗传物质。本综述将重点介绍与 AMD 相关的气溶胶介导纳米疗法的当前发展和挑战。
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引用次数: 0
Advances in Nanoparticulate Therapeutics for Acute Lung Injury:Addressing Unmet Clinical Needs through Targeted Therapy andControlled Delivery of Drug 急性肺损伤纳米微粒疗法的进展:通过靶向治疗和可控给药满足未满足的临床需求
Q3 Medicine Pub Date : 2024-02-28 DOI: 10.2174/0124681873285123240206094443
Piyushkumar Sadhu, Mamta Kumari, Hemraj Singh Rajput, Vipul P. Patel, Falguni Rathod, Nirmal Shah, Avinash Kumar Seth
Acute lung injury (ALI) is a life-threatening condition characterized bysevere invasion of inflammatory cells, lung edema, and the development of intestinal fibrosis. Theactivation of proinflammatory cytokines like TNF-α, IL-6, and others results in the developmentof several risk factors for ALI. It has been observed that no viable therapies for lung injuries exist.Therefore, there is a significant need for healthcare requirements. However, few effective nonpharmacologicaland pharmacological treatments are available, which may have assisted doctorsin reducing the likelihood of illness development. Still, not much progress has been made in illnessmanagement.This review aimed to briefly discuss pharmacological and non-pharmacological approachesfor treating ALI.Nowadays, drug delivery and illness diagnosis are the most advanced areas of modernnanotechnology research, particularly concerning the lungs. So, we focused on various novel approaches,viz., organic nanoparticles, inorganic nanoparticles, metal nanoparticles, and bio nanoparticles,that combat ALI and improve lung functions. This review discussed many studies andthe advancement of different nanomaterials as novel drug carriers in the lungs that can influencethe immune system, suppressing proinflammatory cytokines and improving lung functions.Another aspect of studying nanotechnology is the release kinetics of nanoparticles andsafety when administered to a targeted tissue.The higher uptake of nanomaterials and, thus, the drugs is another advancement innanotechnology. Herein, we explored different approaches to improving and curing acute lung injury.
急性肺损伤(ALI)是一种危及生命的疾病,其特征是炎症细胞的严重入侵、肺水肿和肠纤维化的发展。TNF-α、IL-6 等促炎细胞因子的激活导致了多种 ALI 危险因素的出现。据观察,目前尚无治疗肺损伤的可行疗法。然而,目前有效的非药物和药物治疗方法很少,这可能有助于医生降低疾病发生的可能性。本综述旨在简要讨论治疗 ALI 的药物和非药物方法。如今,药物输送和疾病诊断是现代纳米技术研究的最前沿领域,尤其是在肺部方面。因此,我们重点研究了各种新型方法,即有机纳米粒子、无机纳米粒子、金属纳米粒子和生物纳米粒子,以对抗 ALI 并改善肺功能。研究纳米技术的另一个方面是纳米颗粒的释放动力学以及在靶组织中给药的安全性。在此,我们探讨了改善和治疗急性肺损伤的不同方法。
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引用次数: 0
Nanostructured Lipid Carriers: A Novel Platform in the Formulation ofTargeted Drug Delivery Systems 纳米结构脂质载体:配制靶向给药系统的新平台
Q3 Medicine Pub Date : 2024-02-22 DOI: 10.2174/0124681873283751240206071835
Naga Sri Devi Putchakayala, Keerthana Morusu, Sireesha Ramisetty, Nagaraju Ravoaru
Lipid-based formulations, such as Nanostructured lipid carriers (NLCs),have been thoroughly studied as drug delivery platforms. NLCs are binary systems composed ofboth solid and liquid lipids that aim to produce a lipidic core that is less ordered. Components ofNLCs particularly influence the physicochemical characteristics and efficacy of the final product.They contain a solid matrix at room temperature and are thought to be superior tomany other conventional lipids-based nanocarriers, such as solid lipid nanoparticles (SLNs), nanoemulsions,and liposomes because of their improved stability, drug loading capacity, good biocompatibility,enhanced permeability, bioavailability, extended half-life, fewer side effects, tissue-specific delivery and also a wide range of potential applications.NLCs have multiple applications in the manufacturing of pharmaceuticals and cosmeticsdue to their ease of preparation, the feasibility of scale-up, non-toxicity, improved targetingefficiency, and potential for site-specific delivery via various routes of administration.This review enlightens about the most recent developments of NLCs as a drugdelivery system, types of NLCs, current techniques to prepare NLCs, and characterization techniquesthat are essential for the development of safe, effective and stable formulation. It also highlightsthe potential of using NLCs for various administration routes and recent developments inpharmaceutical applications with successful outcomes.This review also provides great insight into formulation considerations using designexperts and modification strategies for improved targeting. On the whole, NLCs are broadly exploredand preferred lipid nanocarrier systems with several advantages.
以脂质为基础的制剂,如纳米结构脂质载体(NLCs),作为药物输送平台已得到深入研究。纳米结构脂质载体是由固态和液态脂质组成的二元体系,其目的是产生一个有序性较差的脂质核心。NLCs 在室温下含有固体基质,被认为优于其他许多传统的脂质纳米载体,如固体脂质纳米颗粒(SLNs)、纳米乳液和脂质体,因为它们具有更好的稳定性、载药能力、良好的生物相容性、更高的渗透性、生物利用度、更长的半衰期、更少的副作用、组织特异性给药以及广泛的潜在应用。本综述介绍了作为给药系统的 NLC 的最新发展、NLC 的类型、目前制备 NLC 的技术以及对开发安全、有效和稳定的制剂至关重要的表征技术。本综述还重点介绍了将 NLCs 用于各种给药途径的潜力,以及成功应用于制药领域的最新进展。总体而言,NLCs 是一种被广泛探索和首选的脂质纳米载体系统,具有多种优势。
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引用次数: 0
Biogenic Synthesis and Characterization of Ethyl Ferulate Gold Nanoparticle and its Efficacy against Triple-Negative Breast Cancer Cells 阿魏酸乙酯金纳米粒子的生物合成与表征及其对三阴性乳腺癌细胞的疗效
Q3 Medicine Pub Date : 2024-02-06 DOI: 10.2174/0124681873280022240130062923
Jyothsna Unnikrishnan, Mangala Hegde, Aviral Kumar, Sosmitha Girisa, Priyadarshi Satpati, A. Kunnumakkara
Triple-Negative Breast Cancer (TNBC) presents a significant challengedue to its aggressive nature and lack of responsive hormone receptors, predominantly affectingyounger premenopausal women. Ethyl ferulate (EF), a notable phytochemical, has demonstratedpromising anti-cancer properties. This study aimed to enhance the efficacy of EF by synthesizingand characterizing ethyl ferulate gold nanoparticles (EF-AuNps) to passively target TNBC cellsvia the enhanced permeability and retention (EPR) effect.We synthesized EF-AuNps using a direct reduction method and characterized the NPsby employing various techniques, including UV-visible spectroscopy, DLS, XRD, EDX, TEM,and FT-IR. The anti-proliferative activity against MDA-MB-231 cells was assessed using MTTand colony formation assays, alongside evaluating cell viability with PI-FACS and live/dead assays.Furthermore, a Western blot was performed to determine the mechanism of action of EFAuNpsin TNBC cells.We successfully synthesized triangular EF-AuNps (<100nm) and observed a substantial inhibitionof cell proliferation (IC50 18μg/ml). Compared to EF alone, EF-AuNps significantly enhancedcell death in TNBC cells, as confirmed by flow cytometry and viability assays. Besides,Western blot analysis verified that the expression of apoptotic-related signal proteins, such as survivin,caspase 3, and caspase 9, were modulated by EF-AuNps.EF-AuNps showed higher anti-cancer efficacy than EF in the MDA-MB-231 cellline. These findings suggest the therapeutic potential of EF-AuNps for TNBC treatment, advocatingfor further preclinical and clinical investigations into this promising anti-cancer formulation.
三阴性乳腺癌(TNBC)因其侵袭性和缺乏反应性激素受体而面临严峻挑战,主要影响绝经前的年轻女性。阿魏酸乙酯(EF)是一种著名的植物化学物质,具有良好的抗癌特性。本研究旨在通过合成和表征阿魏酸乙酯金纳米粒子(EF-AuNps),利用增强渗透性和滞留性(EPR)效应被动靶向 TNBC 细胞,从而提高 EF 的功效。我们成功合成了三角形 EF-AuNps(<100nm),并观察到其对细胞增殖有显著抑制作用(IC50 18μg/ml)。流式细胞术和细胞存活率测定证实,与单用 EF 相比,EF-AuNps 能显著增强 TNBC 细胞的细胞死亡。此外,Western 印迹分析证实,EF-AuNps 可调节存活素、caspase 3 和 caspase 9 等凋亡相关信号蛋白的表达。这些研究结果表明,EF-AuNps 具有治疗 TNBC 的潜力,因此需要对这种前景广阔的抗癌制剂进行进一步的临床前和临床研究。
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引用次数: 0
Biogenic Synthesis and Characterization of Ethyl Ferulate Gold Nanoparticle and its Efficacy against Triple-Negative Breast Cancer Cells 阿魏酸乙酯金纳米粒子的生物合成与表征及其对三阴性乳腺癌细胞的疗效
Q3 Medicine Pub Date : 2024-02-06 DOI: 10.2174/0124681873280022240130062923
Jyothsna Unnikrishnan, Mangala Hegde, Aviral Kumar, Sosmitha Girisa, Priyadarshi Satpati, A. Kunnumakkara
Triple-Negative Breast Cancer (TNBC) presents a significant challengedue to its aggressive nature and lack of responsive hormone receptors, predominantly affectingyounger premenopausal women. Ethyl ferulate (EF), a notable phytochemical, has demonstratedpromising anti-cancer properties. This study aimed to enhance the efficacy of EF by synthesizingand characterizing ethyl ferulate gold nanoparticles (EF-AuNps) to passively target TNBC cellsvia the enhanced permeability and retention (EPR) effect.We synthesized EF-AuNps using a direct reduction method and characterized the NPsby employing various techniques, including UV-visible spectroscopy, DLS, XRD, EDX, TEM,and FT-IR. The anti-proliferative activity against MDA-MB-231 cells was assessed using MTTand colony formation assays, alongside evaluating cell viability with PI-FACS and live/dead assays.Furthermore, a Western blot was performed to determine the mechanism of action of EFAuNpsin TNBC cells.We successfully synthesized triangular EF-AuNps (<100nm) and observed a substantial inhibitionof cell proliferation (IC50 18μg/ml). Compared to EF alone, EF-AuNps significantly enhancedcell death in TNBC cells, as confirmed by flow cytometry and viability assays. Besides,Western blot analysis verified that the expression of apoptotic-related signal proteins, such as survivin,caspase 3, and caspase 9, were modulated by EF-AuNps.EF-AuNps showed higher anti-cancer efficacy than EF in the MDA-MB-231 cellline. These findings suggest the therapeutic potential of EF-AuNps for TNBC treatment, advocatingfor further preclinical and clinical investigations into this promising anti-cancer formulation.
三阴性乳腺癌(TNBC)因其侵袭性和缺乏反应性激素受体而面临严峻挑战,主要影响绝经前的年轻女性。阿魏酸乙酯(EF)是一种著名的植物化学物质,具有良好的抗癌特性。本研究旨在通过合成和表征阿魏酸乙酯金纳米粒子(EF-AuNps),利用增强渗透性和滞留性(EPR)效应被动靶向 TNBC 细胞,从而提高 EF 的功效。我们成功合成了三角形 EF-AuNps(<100nm),并观察到其对细胞增殖有显著抑制作用(IC50 18μg/ml)。流式细胞术和细胞存活率测定证实,与单用 EF 相比,EF-AuNps 能显著增强 TNBC 细胞的细胞死亡。此外,Western 印迹分析证实,EF-AuNps 可调节存活素、caspase 3 和 caspase 9 等凋亡相关信号蛋白的表达。这些研究结果表明,EF-AuNps 具有治疗 TNBC 的潜力,因此需要对这种前景广阔的抗癌制剂进行进一步的临床前和临床研究。
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引用次数: 0
A Systematic Review on the Potential Applications of Theranostic Nanoparticles in Diabetes and its Associated Complication Diabetic Neuropathy 系统综述治疗纳米粒子在糖尿病及其相关并发症糖尿病神经病变中的潜在应用
Q3 Medicine Pub Date : 2024-01-19 DOI: 10.2174/0124681873265152231229042106
U. Patangia, Kalpita Bhatta, Himangi Vig, Dr Sneh Priya, Dr. Ankita Wal, Dr. Lalit Kumar Tyagi, Dr. Pranay Wal
Diabetes neuropathy is a frequent ailment that has a substantial impact on patients by increasing the risk of falls and causing discomfort. The lower extremities are where diabetic neuropathy patients first feel pain. This discomfort could seem like a pinprick, an electric shock, or something else.Here, we give a comprehensive overview of this quickly developing theranostic appli-cation that includes all relevant imaging, diagnostic, therapeutic, and monitoring elements for the management of diabetes and diabetes neuropathy.The data for the current study was gathered by searching PubMed and Google Scholar. Several research and review publications from various publishers, including Springer Nature, Bentham Science, PLOS one, MDPI, and ACS Publishing Centre, were evaluated to compile the data.Recent developments in theranostics have shown promise as alternate management ap-proaches for diabetes and ailments linked to diabetes. Numerous nanotechnology-built biosen-sors, including multiwalled carbon nanotubes, copper nanowires, zinc oxide tetrapods, and nano-particle-embedded contact lenses, offer benefits in monitoring diabetic neuropathy.The potency, usability, and dependability of insulin substitutes have been demon-strated by a variety of innovative methods for the management of diabetes, which includes nano-technology approaches using Gene-Based Nanoparticles (siRNA), Liposomes, Exo-somes/Extracellular Vesicles, Neuromodulation, and Inhalable Nanoparticles. Over the past few years, the development of various theranostic nanoparticles for Diabetic neuropathy has experi-enced an unprecedented expansion. Even though much work needs to be done to precisely evalu-ate the genuine benefits provided by these particles, such as issues with nanotoxicity, theranostic nanoparticles will have a significant impact on the field of nanomedicine.
糖尿病神经病变是一种常见疾病,会增加患者跌倒的风险并引起不适,对患者造成很大影响。下肢是糖尿病神经病变患者最先感到疼痛的部位。在这里,我们将全面介绍这种快速发展的治疗应用,其中包括用于糖尿病和糖尿病神经病变管理的所有相关成像、诊断、治疗和监测要素。本研究的数据是通过搜索 PubM 和 Google Scholar 收集的,并评估了来自不同出版商(包括 Springer Nature、Bentham Science、PLOS one、MDPI 和 ACS Publishing Centre)的一些研究和评论出版物,以汇编数据。许多采用纳米技术制造的生物传感器,包括多壁碳纳米管、纳米铜线、氧化锌四面体和纳米粒子嵌入式隐形眼镜,都能在监测糖尿病神经病变方面带来益处。胰岛素替代品的有效性、可用性和可靠性已通过各种创新的糖尿病治疗方法得到证实,其中包括使用基因纳米粒子(siRNA)、脂质体、外体/细胞外囊泡、神经调节和可吸入纳米粒子的纳米技术方法。在过去几年中,针对糖尿病神经病变的各种治疗纳米粒子的开发经历了前所未有的扩张。尽管还有许多工作要做,以精确评估这些微粒带来的真正益处,如纳米毒性问题,但治疗用纳米微粒将对纳米医学领域产生重大影响。
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引用次数: 0
Nanomedicine as a Better Therapeutic Approach: An Overview 纳米医学作为一种更好的治疗方法:概述
Q3 Medicine Pub Date : 2024-01-19 DOI: 10.2174/0124681873283310231228125729
Arnab Das, Srijita Chakrabarti
The fields of nanotechnology and nanomedicine have undergone a revolution. There has been a striking rise in authorized nanomedicines since 1980. Apart from functioning as therapeutic agents, they also act as carriers for delivering various active pharmaceuticals to target organs. The ultimate goal of nanomedicine has always been the generation of translational technologies that can improve current therapies. Nanocrystals, nanotubes, liposomes, exosomes, solid lipid nanoparticles, polymeric nanoparticles, and metallic and magnetic nanoparticles are examples of nanostructures that are now in the market as well as in ongoing research. The preparation of these nanomaterials requires consideration of a number of difficulties. Only a few of these nano-materials were successful in obtaining marketing permission after passing all required toxicological and ethical evaluations and making them affordable to users and, at the same time, profitable to investors. Cancer, Central nervous system (CNS) diseases, and Cardiovascular (CVS) diseases represented the primary targets of nanotechnology applied to medicine. Therefore, this review article is focused on providing a summary of several nano-based delivery systems, including their limitations and prospects in different therapeutic fields.
纳米技术和纳米医学领域经历了一场革命。自 1980 年以来,获得授权的纳米药物显著增加。除了作为治疗剂外,它们还作为载体将各种活性药物输送到目标器官。纳米医学的最终目标一直是产生能够改进当前疗法的转化技术。纳米晶体、纳米管、脂质体、外泌体、固体脂质纳米颗粒、聚合物纳米颗粒以及金属和磁性纳米颗粒都是目前市场上和正在研究中的纳米结构的例子。制备这些纳米材料需要考虑许多困难。其中只有少数纳米材料在通过所有必要的毒理学和伦理学评估后,成功地获得了市场许可,使用户能够负担得起,同时也使投资者有利可图。癌症、中枢神经系统(CNS)疾病和心血管系统(CVS)疾病是纳米技术应用于医学的主要目标。因此,这篇综述文章重点总结了几种基于纳米的给药系统,包括它们在不同治疗领域的局限性和前景。
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引用次数: 0
Design Formulation of Nanospanlastic Novel Carriers as a Promising Approach to Enhanced Bioavailability in Intranasal Drug Delivery for Sinusitis: Statistical Optimization and In vitro and In vivo Characterization 纳米弹性新型载体的设计配方是提高鼻窦炎鼻内给药生物利用度的有效方法:统计优化与体内外特性分析
Q3 Medicine Pub Date : 2024-01-19 DOI: 10.2174/0124681873262019231105201433
A. Chettupalli, Srivani Ajmera, M. Kuchukuntla, Venkatesan Palanivel, Sunand Katta
Most new biologically active chemicals require better water solubility and slower dissolution rates. Cefdinir (CFD) has a very low bioavailability in its crystalline form and is poorly soluble in water.Most new and current biologically active chemicals have poor water solubility and slow dissolution rates. Cefdinir has a very low bioavailability in its crystalline form and is poorly soluble in water.By preparing cefdinir's spanlastic nanovesicles (SNVs) using the ethanol injection method, the current study has attempted to enhance the drug's solubility and bioavailability using a statistical design approach.Independent variables, including the nonionic surfactant concentration, edge activator (EA), sonication time, SNVs entrapment effectiveness, particle size, zeta potential, PDI, and in vitro release, have been evaluated. The best CFD-SNVs have been positioned within in situ gel with mucoadhesive properties made of hydroxypropyl methylcellulose and deacetylated gellan gum. By contrasting intranasal injection of the produced gel with an IV solution, animal models have been used to investigate CFD's systemic and cerebral dynamics.Statistical analysis has suggested an ideal SNVs formulation with nonionic surfactant (65 mg), EA (15 mg), and sonication (3 min). The sol-gel temperature for forming the mucoad-hesive in situ gel containing SNVs has been found to be 34.03°C, and 18.36 minutes has been the extended mucociliary transit time. Following intranasal injection, compared to SNV dispersion, the gelling system has exhibited higher brain bioavailability (2251.9 ± 75 vs. 5281.6 ± 51%, re-spectively). The gel has also demonstrated effective drug targeting of the brain with higher direct transport percentage indices.Mucoadhesive in situ gel with CFD-loaded SNVs can be administered via the in-tranasal route. To enhance bioavailability in the brain and drug targeting from the nose to the brain, nasal in situ gel loaded with CFD-SNVs could be a new carrier to be employed in sinusitis.
大多数新的生物活性化学品需要更好的水溶性和更慢的溶解速度。头孢地尼(CFD)的晶体生物利用度非常低,在水中的溶解度也很低。通过使用乙醇注射法制备头孢地尼的spanlastic纳米微粒(SNVs),本研究尝试使用统计设计方法提高药物的溶解度和生物利用度。最好的 CFD-SNV 被置于由羟丙基甲基纤维素和去乙酰化结冷胶制成的具有粘附性的原位凝胶中。统计分析表明,非离子表面活性剂(65 毫克)、EA(15 毫克)和超声(3 分钟)是理想的 SNVs 配方。研究发现,形成含有 SNVs 的粘液粘附性原位凝胶的溶胶-凝胶温度为 34.03°C,延长的粘液纤毛转运时间为 18.36 分钟。鼻内注射后,与 SNV 分散体相比,凝胶系统显示出更高的脑生物利用度(2251.9 ± 75 vs. 5281.6 ± 51%,对比)。这种凝胶还表现出了有效的脑部药物靶向性,具有更高的直接转运百分比指数。为了提高药物在大脑中的生物利用度和从鼻腔到大脑的靶向性,鼻腔原位凝胶中装载的CFD-SNVs可作为一种新的载体用于鼻窦炎的治疗。
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引用次数: 0
Formulation, Optimization and Evaluation of Dabigartan Etexilate Encapsulated Solid Supersaturated Self-Nanoemulsifying Drug Delivery System 达比加坦-依替沙坦酯包封固体过饱和自纳米乳化给药系统的配方、优化与评估
Q3 Medicine Pub Date : 2024-01-19 DOI: 10.2174/0124681873276409231213115328
Nithya Shanthi, Heena Mittal, Manish Kumar, Arun Mahato, Brahmeshwar Mishra
The present study proposed Dabigatran Etexilate loaded solid supersaturat-ed self-nanoemulsifying drug delivery system (solid S-SNEDDS) for enhancement of payload, drug solubility, dissolution rate as well as minimization of drug precipitation.The study involved formulation optimization using the Box-Behnken design. The op-timal SNEDDS consisting of Caprylic acid (32.9% w/w), Cremophor EL (50.2% w/w) and Transcutol HP (18.8% w/w) as Oil, Surfactant and Co-surfactant, respectively were formulated and evaluated for particle size, PDI, Zeta potential and saturation solubility. The SNEDDS was further incorporated with PPIs for the preparation of supersaturated SNEDDS (S-SNEDDS) to in-crease the drug payload in the formulation. S-SNEDDS was converted to solid S-SNEDDS by ad-sorption onto the porous carrier i.e., Aerosil®200. The in-vitro drug release study was also con-ducted for solid S-SNEDDS.SNEDDS had size, PDI, and Zeta potential of 82nm, 0.347, -10.50mV, respectively. SNEDDS enhanced the saturation solubility of the drug by 93.65-fold. Among PPIs, HPMC K4M showed the most effective response for the formulation of S-SNEDDS. The S-SNEDDS had a more substantial drug payload, which further increased the solubility by 150 times of pure drugs and 16 times of SNEDDS. Solid S-SNEDDS exhibited free-flowing properties. Reconstituted sol-id S-SNEDDS had acceptable size, PDI, and Zeta potential of 131.3nm, 0.457, and -11.3 mV, re-spectively. In-vitro drug release study revealed higher drug dissolution and minimized drug pre-cipitation by SNEDDS compared to marketed products and pure drugs.Proposed nano-formulation was found to efficiently improve the aqueous solubility of the drug and avoid the drug precipitation, thereby avoiding drug loss and improving drug bioa-vailability.
本研究提出了达比加群酯固体超饱和自纳米乳化给药系统(固体 S-SNEDDS),以提高有效载荷、药物溶解度和溶解速率,并最大限度地减少药物沉淀。研究采用 Box-Behnken 设计对配方进行了优化。研究人员配制了由 Caprylic acid(32.9% w/w)、Cremophor EL(50.2% w/w)和 Transcutol HP(18.8% w/w)分别作为油、表面活性剂和辅助表面活性剂组成的最佳 SNEDDS,并对其粒度、PDI、Zeta 电位和饱和溶解度进行了评估。在制备过饱和 SNEDDS(S-SNEDDS)时,将 SNEDDS 与 PPIs 进一步结合,以增加制剂中的药物载量。通过吸附在多孔载体 Aerosil®200 上,S-SNEDDS 变成了固体 S-SNEDDS。SNEDDS的尺寸、PDI和Zeta电位分别为82nm、0.347和-10.50mV。SNEDDS使药物的饱和溶解度提高了93.65倍。在 PPIs 中,HPMC K4M 对配制 S-SNEDDS 的反应最为有效。S-SNEDDS 的载药量更大,使溶解度进一步提高,纯药的溶解度提高了 150 倍,SNEDDS 的溶解度提高了 16 倍。固体 S-SNEDDS 具有自由流动的特性。冲调后的固体 S-SNEDDS 具有可接受的尺寸、PDI 和 Zeta 电位,分别为 131.3 纳米、0.457 和 -11.3 mV。体外药物释放研究表明,与市售产品和纯药物相比,SNEDDS 的药物溶解度更高,药物预沉淀最小。
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引用次数: 0
The Potential of Quality Target Product Profile in the Optimization of Nanoemulsions 优质目标产品简介在优化纳米乳剂中的潜力
Q3 Medicine Pub Date : 2024-01-19 DOI: 10.2174/0124681873280769231217084737
Devesh U. Kapoor, Rajiv R Kukkar, Mansi Gaur, Bhupendra G. Prajapati, R. Malviya
The application of Quality Target Product Profile (QTPP) in optimizing nanoemulsion (NEM) shows immense potential in advancing pharmaceutical formulation design for effective drug delivery. By aligning QTPP with nanoemulsion attributes, this approach offers a pathway to tailored formulations that meet specific therapeutic objectives and responses. Incorporating QTPP facilitates informed choices in formulating design, covering pivotal factors like stability, drug re-lease kinetics, bioavailability, and precise targeting. Moreover, this review extensively explores the real-world application of QTPP-guided tactics in refining nanoemulsion optimization. It high-lights their pivotal role in anticipating and regulating in vivo responses, encompassing vital as-pects like pharmacokinetics and pharmacodynamics. By conducting thorough examinations of case studies and research outcomes, this article clarifies the effectiveness of aligning QTPP crite-ria with NEM characteristics. This approach fosters the creation of customized formulations pre-cisely suited to achieve distinct therapeutic objectives. This review amalgamates contemporary insights into harnessing QTPP for nanoemulsion optimization, illuminating its capacity to stream-line formulation design, amplify treatment effectiveness by desiring drug release, and catalyze transformative shifts in pharmaceutical research.
在优化纳米乳剂(NEM)过程中应用优质目标产品简介(QTPP),在推进有效给药的药物配方设计方面显示出巨大的潜力。通过将 QTPP 与纳米乳液属性相匹配,这种方法为满足特定治疗目标和反应的定制配方提供了途径。纳入 QTPP 有利于在配方设计中做出明智的选择,涵盖稳定性、药物再释放动力学、生物利用度和精确靶向等关键因素。此外,本综述还广泛探讨了 QTPP 指导策略在完善纳米乳剂优化方面的实际应用。它强调了 QTPP 在预测和调节体内反应方面的关键作用,包括药代动力学和药效学等重要方面。通过对案例研究和研究成果进行深入探讨,本文阐明了将 QTPP 标准与 NEM 特性相结合的有效性。这种方法有助于创造定制的配方,以实现不同的治疗目标。这篇综述综合了当代对利用 QTPP 优化纳米乳液的见解,阐明了 QTPP 简化配方设计、通过期望的药物释放提高治疗效果以及促进制药研究变革的能力。
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引用次数: 0
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Current Nanomedicine
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