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Preparation, Characterization, and Evaluation of Mesoporous Silica Nanoparticles in Enhancing Oral Bioavailability of Poorly Water-Soluble Drugs. 介孔二氧化硅纳米颗粒的制备、表征和在提高水溶性差药物口服生物利用度方面的评估
Pub Date : 2024-01-01 DOI: 10.2174/0115672018273792240101062603
Hong Zhang, Fanjiao Zuo, Boyao Wang, Xilong Qiu

Background: Breviscapine (BVP) is one of the extracts of several flavonoids of Erigeron breviscapus, which has been widely used in the treatment of cerebral infarction and its sequelae, cerebral thrombus, coronary heart disease, and angina pectoris. But BVP has poor solubility.

Objective: The objective of the study is to develop mesoporous silica nanoparticles (MSNs) that can be loaded with a drug with poor water solubility. The MSNs, which were designed for oral administration, enhanced both the dissolution rate and drug loading capacity.

Methods: The use of MSNs as an oral drug delivery system was investigated by SEM, TEM, BETBJH, XRD, FT-IR, and HPLC. Additionally, we examined the oral bioavailability of BVP loaded onto MSNs and examined the cellular cytotoxicity of MSNs.

Results: The results indicate that the oral bioavailability of BVP after loading onto MSNs was greater than that of a marketed product. Furthermore, we studied the mechanism by which MSNs enhance the oral absorption of BVP.

Conclusion: MSNs have the potential to enhance the oral bioavailability of poorly water-soluble drugs by accelerating the drug dissolution rate.

背景:布维司卡平(BVP)是布维司卡平(Erigeron breviscapus)几种黄酮类化合物的提取物之一,已被广泛用于治疗脑梗塞及其后遗症、脑血栓、冠心病和心绞痛。但 BVP 的溶解性较差:本研究的目的是开发可装载水溶性差的药物的介孔二氧化硅纳米粒子(MSNs)。方法:将介孔二氧化硅纳米颗粒用作口服药物,可以提高药物的溶解速率和载药量:方法:通过扫描电镜、电子显微镜、BETBJH、XRD、傅立叶变换红外光谱和高效液相色谱法研究了 MSNs 作为口服给药系统的用途。此外,我们还考察了载入 MSNs 的 BVP 的口服生物利用度,并考察了 MSNs 的细胞毒性:结果表明,负载到 MSN 上的 BVP 的口服生物利用度高于市售产品。此外,我们还研究了 MSNs 促进 BVP 口服吸收的机制:结论:MSN 有可能通过加快药物溶解速度来提高水溶性差的药物的口服生物利用度。
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引用次数: 0
Dextran-based Drug Delivery Approaches for Lung Diseases: A Review. 基于葡聚糖的肺部疾病给药方法:综述。
Pub Date : 2024-01-01 DOI: 10.2174/0115672018267737231116100812
Manisha Kumari, Sanyam Sharma, Navjot Kanwar, Subh Naman, Ashish Baldi

Respiratory disorders, such as tuberculosis, cystic fibrosis, chronic obstructive pulmonary disease, asthma, lung cancer, and pulmonary inflammation, are among the most prevalent ailments in today's world. Dextran, an exopolysaccharide formed by Leuconostoc mesenteroides (slimeproducing bacteria), and its derivatives are investigated for several therapeutic utilities. Dextranbased drug delivery system can become an innovative strategy in the treatment of several respiratory ailments as it offers numerous advantages, such as mucolytic action, airway hydration, antiinflammatory properties, and radioprotective effect as compared to other polysaccharides. Being biocompatible, flexible hydrophilic nature, biodegradable, tasteless, odourless, non-mutagenic, watersoluble and non-toxic edible polymer, dextran-based drug delivery systems have been explored for a wide range of therapeutic applications, especially in lungs and respiratory diseases. The present article comprehensively discusses various derivatives of dextran with their attributes to be considered for drug delivery and extensive therapeutic benefits, with a special emphasis on the armamentarium of dextran-based formulations for the treatment of respiratory disorders and associated pathological conditions. The information provided will act as a platform for formulation scientists as important considerations in designing therapeutic approaches for lung and respiratory diseases. With an emphasis on lung illnesses, this article will offer an in-depth understanding of dextran-based delivery systems in respiratory illnesses.

肺结核、囊性纤维化、慢性阻塞性肺病、哮喘、肺癌和肺部炎症等呼吸系统疾病是当今世界最普遍的疾病之一。右旋糖酐是一种由肠道黏液产生菌(Leuconostoc mesenteroides)形成的外多糖,其衍生物被研究用于多种治疗用途。与其他多糖相比,葡聚糖具有多种优势,如粘液溶解作用、气道水合作用、抗炎特性和放射保护作用,因此,以葡聚糖为基础的给药系统可以成为治疗多种呼吸系统疾病的创新策略。葡聚糖是一种具有生物相容性、柔性亲水性、可生物降解、无味、无臭、无致突变性、水溶性和无毒的可食用聚合物,以葡聚糖为基础的给药系统已被广泛应用于治疗领域,尤其是肺部和呼吸系统疾病。本文全面论述了葡聚糖的各种衍生物,以及它们在给药方面的特性和广泛的治疗效果,特别强调了以葡聚糖为基础的配方在治疗呼吸系统疾病和相关病症方面的作用。所提供的信息将为制剂科学家提供一个平台,作为设计肺部和呼吸系统疾病治疗方法的重要考虑因素。本文将以肺部疾病为重点,深入介绍基于葡聚糖的给药系统在呼吸系统疾病中的应用。
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引用次数: 0
Supersaturation Behavior: Investigation of Polymers Impact on Nucleation Kinetic Profile for Rationalizing the Polymeric Precipitation Inhibitors. 过饱和行为:研究聚合物对成核动力学曲线的影响,以使聚合物沉淀抑制剂合理化。
Pub Date : 2024-01-01 DOI: 10.2174/0115672018261505231018100329
Uditi Handa, Anuj Malik, Kumar Guarve, Nidhi Rani, Prerna Sharma

Background: Although nucleation kinetic data is quite important for the concept of supersaturation behavior, its part in rationalizing the crystallization inhibitor has not been well understood.

Objective: This study aimed to investigate the nucleation kinetic profile of Dextromethorphan HBr (as an ideal drug, BCS-II) by measuring liquid-liquid phase segregation, nucleation induction time, and Metastable Zone width.

Methods: Surfeit action was examined by a superfluity assay of the drug. The concentration was scrutinized by light scattering techniques (UV spectrum (novel method) and Fluorometer (CL 53)).

Results: The drug induction time was 20 min without polymer and 90 and 110 min with polymers, such as HPMC K15M and Xanthan Gum, respectively. Therefore, the order of the polymer's ability to inhibit nucleation was Xanthan Gum > HPMC K15M in the medium (7.4 pH). Similarly, the drug induction time was 30 min without polymer and 20, 110, and 90 min with polymers, such as Sodium CMC, HPMC K15M, and Xanthan Gum, respectively. Therefore, the order of the polymer's ability to inhibit nucleation was HPMC K15M > Xanthan Gum > Sodium CMC in SIFsp (6.8 pH), which synchronizes the polymer's potentiality to interdict the drug precipitation.

Conclusion: The HPMC K15M and xanthan Gum showed the best crystallization inhibitor effect for the maintenance of superfluity conditions till the drug absorption time. The xanthan gum is based on the "glider" concept, and this shows the novelty of this preliminary research. The screening methodology used for rationalizing the best polymers used in the superfluity formulations development successfully.

背景:尽管成核动力学数据对于过饱和行为的概念非常重要,但它在合理化结晶抑制剂方面的作用还没有得到很好的理解。目的:本研究旨在通过测量液-液相偏析、成核诱导时间和亚稳态区宽度,研究理想药物右美沙芬HBr的成核动力学特性。方法:采用药物过量试验法检测表面活性。结果:不含聚合物的诱导时间为20min,含HPMCK15M和黄原胶的诱导时间分别为90min和110min。因此,在介质(7.4 pH)中,聚合物抑制成核的能力的顺序是黄原胶>HPMC K15M。类似地,药物诱导时间在没有聚合物的情况下为30分钟,在有聚合物的情况(例如CMC钠、HPMC K15M和黄原胶)下分别为20、110和90分钟。因此,在SIFsp(6.8 pH)中,聚合物抑制成核的能力顺序为HPMC K15M>黄原胶>CMC钠,这同步了聚合物阻断药物沉淀的潜力。结论:HPMC K15M和黄原胶在维持药物过量条件直至药物吸收时间方面显示出最佳的结晶抑制剂效果。黄原胶是基于“滑翔机”的概念,这表明了这项初步研究的新颖性。用于合理化多余配方中使用的最佳聚合物的筛选方法成功开发。
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引用次数: 0
Nanoformulations Insights: A Novel Paradigm for Antifungal Therapies and Future Perspectives. 纳米制剂洞察:抗真菌治疗的新范式和未来展望。
Pub Date : 2024-01-01 DOI: 10.2174/0115672018270783231002115728
Ashima Ahuja, Meenakshi Bajpai

Currently, fungal infections are becoming more prevalent worldwide. Subsequently, many antifungal agents are available to cure diseases like pemphigus, athlete's foot, acne, psoriasis, hyperpigmentation, albinism, and skin cancer. Still, they fall short due to pitfalls in physiochemical properties. Conventional medications like lotion, creams, ointments, poultices, and gels are available for antifungal therapy but present many shortcomings. They are associated with drug retention and poor penetration problems, resulting in drug resistance, hypersensitivity, and diminished efficacy. On the contrary, nanoformulations have gained tremendous potential in overcoming the drawbacks of conventional delivery. Furthermore, the potential breakthroughs of nanoformulations are site-specific targeting. It has improved bioavailability, patient-tailored approach, reduced drug retention and hypersensitivity, and improved skin penetration. Nowadays, nanoformulations are gaining popularity for antifungal therapy against superficial skin infections. Nanoformulations-based liposomes, niosomes, nanosponges, solid lipid nanoparticles, and potential applications have been explored for antifungal therapy due to enhanced activity and reduced toxicity. Researchers are now more focused on developing patient-oriented target-based nano delivery to cover the lacunas of conventional treatment with higher immune stimulatory effects. Future direction involves the construction of novel nanotherapeutic devices, nanorobotics, and robust methods. In addition, for the preparations of nanoformulations for clinical studies, animal modeling solves the problems of antifungal therapy. This review describes insights into various superficial fungal skin infections and their potential applications, nanocarrier-based drug delivery, and mechanism of action. In addition, it focuses on regulatory considerations, pharmacokinetic and pharmacodynamic studies, clinical trials, patents, challenges, and future inputs for researchers to improve antifungal therapy.

目前,真菌感染在世界范围内越来越普遍。随后,许多抗真菌药物可用于治疗天疱疮、脚癣、痤疮、牛皮癣、色素沉着、白化病和皮肤癌症等疾病。尽管如此,由于理化性质的缺陷,它们还是达不到要求。常规药物如乳液、乳膏、软膏、膏药和凝胶可用于抗真菌治疗,但存在许多缺点。它们与药物滞留和渗透性差有关,导致耐药性、超敏反应和疗效下降。相反,纳米制剂在克服传统递送的缺点方面获得了巨大的潜力。此外,纳米制剂的潜在突破是位点特异性靶向。它提高了生物利用度,为患者量身定制了方法,减少了药物滞留和超敏反应,并改善了皮肤渗透性。如今,纳米制剂在对抗浅表皮肤感染的抗真菌治疗中越来越受欢迎。基于纳米制剂的脂质体、niosomes、纳米池、固体脂质纳米颗粒以及由于增强活性和降低毒性而在抗真菌治疗中的潜在应用已被探索。研究人员现在更专注于开发面向患者的靶向纳米递送,以覆盖具有更高免疫刺激效果的传统治疗的空白。未来的方向包括构建新型纳米治疗设备、纳米机器人和稳健的方法。此外,对于用于临床研究的纳米制剂的制备,动物模型解决了抗真菌治疗的问题。这篇综述描述了对各种浅表真菌皮肤感染及其潜在应用、基于纳米载体的药物递送和作用机制的见解。此外,它还关注监管考虑、药代动力学和药效学研究、临床试验、专利、挑战以及研究人员改进抗真菌治疗的未来投入。
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引用次数: 0
Convection-enhanced Diffusion: A Novel Tactics to Crack the BBB. 对流增强扩散:破解 BBB 的新策略。
Pub Date : 2024-01-01 DOI: 10.2174/0115672018266501231207095127
Meenakshi Dhanawat, Garima, Kashish Wilson, Sumeet Gupta, Rishabh Chalotra, Nidhi Gupta

Although the brain is very accessible to nutrition and oxygen, it can be difficult to deliver medications to malignant brain tumours. To get around some of these issues and enable the use of therapeutic pharmacological substances that wouldn't typically cross the blood-brain barrier (BBB), convection-enhanced delivery (CED) has been developed. It is a cutting-edge strategy that gets beyond the blood-brain barrier and enables targeted drug administration to treat different neurological conditions such as brain tumours, Parkinson's disease, and epilepsy. Utilizing pressure gradients to spread the medicine across the target area is the main idea behind this diffusion mechanism. Through one to several catheters positioned stereotactically directly within the tumour mass, around the tumour, or in the cavity created by the resection, drugs are given. This method can be used in a variety of drug classes, including traditional chemotherapeutics and cutting-edge investigational targeted medications by using positive-pressure techniques. The drug delivery volume must be optimized for an effective infusion while minimizing backflow, which causes side effects and lowers therapeutic efficacy. Therefore, this technique provides a promising approach for treating disorders of the central nervous system (CNS).

虽然大脑的营养和氧气非常容易获得,但要向恶性脑肿瘤输送药物却很困难。为了解决这些问题,并使用通常无法通过血脑屏障(BBB)的治疗药物,对流增强给药(CED)应运而生。这是一种超越血脑屏障、实现靶向给药的尖端策略,可用于治疗脑肿瘤、帕金森病和癫痫等不同的神经系统疾病。利用压力梯度将药物扩散到目标区域是这种扩散机制的主要理念。通过一根至数根导管,以立体定向方式将药物直接置于肿瘤内、肿瘤周围或切除后形成的空腔中。这种方法可用于多种药物类别,包括传统的化疗药物和利用正压技术研究的前沿靶向药物。必须优化给药量以实现有效输注,同时尽量减少回流,因为回流会导致副作用并降低疗效。因此,这种技术为治疗中枢神经系统(CNS)疾病提供了一种前景广阔的方法。
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引用次数: 0
Mannose: A Promising Player in Clinical and Biomedical Applications. 甘露糖:在临床和生物医学应用中大有可为。
Pub Date : 2024-01-01 DOI: 10.2174/0115672018275954231220101637
Sijing Chen, Kana Wang, Qiao Wang

Mannose, an isomer of glucose, exhibits a distinct molecular structure with the same formula but a different atom arrangement, contributing to its specific biological functions. Widely distributed in body fluids and tissues, particularly in the nervous system, skin, testes, and retinas, mannose plays a crucial role as a direct precursor for glycoprotein synthesis. Glycoproteins, essential for immune regulation and glycosylation processes, underscore the significance of mannose in these physiological activities. The clinical and biomedical applications of mannose are diverse, encompassing its anti-inflammatory properties, potential to inhibit bacterial infections, role in metabolism regulation, and suggested involvement in alleviating diabetes and obesity. Additionally, mannose shows promise in antitumor effects, immune modulation, and the construction of drug carriers, indicating a broad spectrum of therapeutic potential. The article aims to present a comprehensive review of mannose, focusing on its molecular structure, metabolic pathways, and clinical and biomedical applications, and also to emphasize its status as a promising therapeutic agent.

甘露糖是葡萄糖的一种异构体,具有独特的分子结构,其分子式相同,但原子排列不同,因此具有特殊的生物功能。甘露糖广泛分布于体液和组织中,尤其是在神经系统、皮肤、睾丸和视网膜中,作为糖蛋白合成的直接前体,甘露糖发挥着至关重要的作用。糖蛋白是免疫调节和糖基化过程中必不可少的物质,这突出了甘露糖在这些生理活动中的重要作用。甘露糖的临床和生物医学应用多种多样,包括其抗炎特性、抑制细菌感染的潜力、在新陈代谢调节中的作用,以及参与缓解糖尿病和肥胖症的建议。此外,甘露糖在抗肿瘤作用、免疫调节和构建药物载体方面也大有可为,显示出广泛的治疗潜力。本文旨在对甘露糖进行全面综述,重点介绍其分子结构、代谢途径以及临床和生物医学应用,并强调其作为一种有前景的治疗剂的地位。
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引用次数: 0
Recent trends in nanoparticulate delivery system for amygdalin as potential therapeutic herbal bioactive agent for cancer treatment. 苦杏仁苷纳米颗粒递送系统作为潜在的癌症治疗草药生物活性剂的研究进展。
Pub Date : 2023-11-27 DOI: 10.2174/0115672018280381231119150732
Mahendra Prajapati, Dr Rohitas Deshmukh, Dr Ranjit K Harwansh

Cancer is the deadliest and most serious health problem. The mortality rate of cancer patients has increased significantly worldwide in recent years. There are several treatments available, but these treatments have many limitations, such as non-specific targeting, toxicity, bioavailability, solubility and permeability problems, serious side effects, and a higher dose. Many people prefer phytomedicine because it has fewer side effects. However, amygdalin is a naturally occurring phytoconstituent. It has many harmful effects due to the cyanide group present in the chemical structure. Many scientists and researchers have given their thoughts associated with amygdalin and its toxicities. However, there is a need for a more advanced, effective, and newer delivery system for amygdalin to reduce its toxic effect. Nanotechnology has become a more refined and emerging medical approach, offering innovative ways to treat cancer. This review focuses on the use of amygdaline as herbal medicine encapsulating into several nanoparticulate delivery systems such as silver nanoparticles, graphene oxide nanoparticles, gold nanoparticles, nanofibers, nanocomposites, niosomes, and magnetic nanoparticles in the treatment of cancer. In addition, this article provides information on amygdalin structure and physical properties, pharmacokinetics, toxicity, and challenges with amygdalin.

癌症是最致命、最严重的健康问题。近年来,世界范围内癌症患者的死亡率显著上升。有几种可用的治疗方法,但这些治疗方法有许多局限性,如非特异性靶向、毒性、生物利用度、溶解度和渗透性问题、严重的副作用和较高的剂量。许多人更喜欢植物药,因为它的副作用更小。然而,苦杏仁苷是一种天然存在的植物成分。由于氰化物基团存在于化学结构中,它有许多有害的影响。许多科学家和研究人员对苦杏仁苷及其毒性提出了自己的看法。然而,需要一种更先进、更有效和更新的苦杏仁苷输送系统来减少其毒性作用。纳米技术已经成为一种更加精细和新兴的医疗方法,为治疗癌症提供了创新的方法。本文综述了将苦杏仁碱作为草药包封在几种纳米颗粒递送系统(如银纳米颗粒、氧化石墨烯纳米颗粒、金纳米颗粒、纳米纤维、纳米复合材料、纳米体和磁性纳米颗粒)中治疗癌症的应用。此外,本文还介绍了苦杏仁苷的结构和物理性质、药代动力学、毒性以及对苦杏仁苷的挑战。
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引用次数: 0
Targeted Polymeric Nanoparticles as a Strategy for the Treatment of Glioblastoma: A Review. 靶向聚合纳米颗粒作为治疗胶质母细胞瘤的策略:综述。
Pub Date : 2023-11-27 DOI: 10.2174/0115672018257713231107060630
Geanne Aparecida de Paula, Mariana Carlomagno de Paula, Jessyca Aparecida Paes Dutra, Suzana Gonçalves Carvalho, Leonardo Delello Di Filippo, Janaína Cecília Oliveira Villanova, Marlus Chorilli

Glioblastoma multiforme is the most common and aggressive malignant tumor that affects the central nervous system, with high mortality and low survival. Glioblastoma multiforme treatment includes resection tumor surgery, followed by radiotherapy and chemotherapy adjuvants. However, the drugs used in chemotherapy present some limitations, such as the difficulty of crossing the bloodbrain barrier and resisting the cellular mechanisms of drug efflux. The use of polymeric nanoparticles has proven to be an effective alternative to circumvent such limitations, as it allows the exploration of a range of polymeric structures that can be modified in order to control the biodistribution and cytotoxic effect of the drug delivery systems. Nanoparticles are nanometric in size and allow the incorporation of targeting ligands on their surface, favoring the transposition of the blood-brain barrier and the delivery of the drug to specific sites, increasing the selectivity and safety of chemotherapy. The present review has described the characteristics of chitosan, poly(vinyl alcohol), poly(lactic-coglycolic acid), poly(ethylene glycol), poly(β-amino ester), and poly(ε-caprolactone), which are some of the most commonly used polymers in the manufacture of nanoparticles for the treatment of glioblastoma multiforme. In addition, some of the main targeting ligands used in these nanosystems are presented, such as transferrin, chlorotoxin, albumin, epidermal growth factor, and epidermal growth factor receptor blockers, explored for the active targeting of antiglioblastoma agents.

多形性胶质母细胞瘤是影响中枢神经系统的最常见和侵袭性恶性肿瘤,死亡率高,生存率低。多形性胶质母细胞瘤的治疗包括肿瘤切除手术,然后辅以放疗和化疗。然而,用于化疗的药物存在一些局限性,如难以穿过血脑屏障和抵抗药物外排的细胞机制。聚合物纳米颗粒的使用已被证明是规避这些限制的有效替代方案,因为它允许探索一系列可以修改的聚合物结构,以控制药物输送系统的生物分布和细胞毒性作用。纳米颗粒的尺寸为纳米级,允许靶向配体在其表面结合,有利于血脑屏障的转移和药物的递送到特定部位,增加化疗的选择性和安全性。本文综述了壳聚糖、聚乙烯醇、聚乳酸-乙醇酸、聚乙二醇、聚β-氨基酯、聚ε-己内酯等制备多形性胶质母细胞瘤纳米粒子最常用的几种聚合物的特点。此外,介绍了这些纳米系统中使用的一些主要靶向配体,如转铁蛋白、氯毒素、白蛋白、表皮生长因子和表皮生长因子受体阻滞剂,探索了抗胶质母细胞瘤药物的活性靶向。
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引用次数: 0
WITHDRAWN: Long-time-released Transdermal Microneedle Delivery System. 撤回:长效透皮微针给药系统。
Pub Date : 2023-11-23 DOI: 10.2174/0115672018266536231107053636
Xiaofei Tang, Huaiying Qin, Xiaoyun Zhang, Haiyun Yang, Jianhua Yang, Ping Chen, Yinli Jin, Lu Yang

The article has been withdrawn at the request of the authors of the journal "Current Drug Delivery", Bentham Science apologizes to the readers of the journal for any inconvenience this may have caused. The Bentham Editorial Policy on Article Withdrawal can be found at https://benthamscience.com/editorial-policies-main.php. BENTHAM SCIENCE DISCLAIMER: It is a condition of publication that manuscripts submitted to this journal have not been published and will not be simultaneously submitted or published elsewhere. Furthermore, any data, illustration, structure or table that has been published elsewhere must be reported, and copyright permission for reproduction must be obtained. Plagiarism is strictly forbidden, and by submitting the article for publication the authors agree that the publishers have the legal right to take appropriate action against the authors, if plagiarism or fabricated information is discovered. By submitting a manuscript the authors agree that the copyright of their article is transferred to the publishers if and when the article is accepted for publication.

应《当前药物输送》杂志作者的要求,文章已被撤回,边沁科学为由此可能造成的不便向该杂志的读者道歉。边沁关于文章撤稿的编辑政策可在https://benthamscience.com/editorial-policies-main.php找到。BENTHAM SCIENCE免责声明:投稿至本刊的稿件未被发表,也不会在其他地方同时投稿或发表。此外,在其他地方发表的任何数据、插图、结构或表格必须报告,并必须获得版权许可才能复制。抄袭是严格禁止的,通过提交文章发表,作者同意出版商有法律权利对作者采取适当的行动,如果发现抄袭或捏造信息。通过提交手稿,作者同意如果文章被接受出版,其文章的版权将转移给出版商。
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引用次数: 0
Withdrawn: Cytotoxicity and Cellular uptake of 5-Fluorouracil loaded methylcellulose nanohydrogel for treatment of oral cancer. 撤回:用于治疗口腔癌的 5-氟尿嘧啶负载甲基纤维素纳米水凝胶的细胞毒性和细胞摄取。
Pub Date : 2016-10-13
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引用次数: 0
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