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Analytical Method Validation of Testosterone Undecanoate Soft Gelatin Capsule by RP-HPLC Method 反相高效液相色谱法验证十一酸睾酮软明胶胶囊的分析方法
Pub Date : 2018-04-25 DOI: 10.4172/2329-6631.1000184
Didarul Islam, M. MehediHasan, T. Mohiuddin, M. Hassan, Asheful Latif, Papia Haque
A rapid, sensitive, selective reversed phase HPLC method has been validated for the quantification of testosterone undecanoate from Andriol® soft gelatin capsule. During validation active pharmaceutical ingredient (API) has been separated by C18 (4.6 mm × 250 mm, 5 μm) column, 100% methanol as mobile phase, flow rate of 0.8 ml/min and detection wavelength at 240 nm. The method was validated according to USP and ICH guideline requirements which includes specificity, accuracy, precision, linearity and range and robustness. Linearity of standard spiked sample was observed for each working day and coefficient of determination (r2) has been found >0.99 each day in concentration ranging from 20-60 ppm. Recovery was found from 98.87-100.02% for 20, 40 and 60 ppm of testosterone undecanoate spiked sample. Precision and intermediate precision showed that % RSD of test sample solution were 0.26 and 0.19 respectively and absolute difference between them was 0.52, all of the values were within acceptable limit. The method was also found robust in changing column oven temperature (± 5°C) and flow rate change (± 0.1).
建立了一种快速、灵敏、选择性的反相高效液相色谱法定量测定Andriol®软明胶胶囊中十一酸睾酮的方法。采用C18柱(4.6 mm × 250 mm, 5 μm)分离原料药,流动相为100%甲醇,流速为0.8 ml/min,检测波长为240 nm。根据USP和ICH指南要求对该方法进行了验证,包括特异性、准确度、精密度、线性和范围以及鲁棒性。在每个工作日观察到标准加标样品的线性关系,并且发现在20-60 ppm的浓度范围内,决定系数(r2)每天>0.99。对20、40、60 ppm的十一酸睾酮加样回收率为98.87 ~ 100.02%。精密度和中间精密度显示,样品溶液的% RSD分别为0.26和0.19,两者的绝对差值为0.52,均在可接受范围内。该方法在改变柱箱温度(±5℃)和流量变化(±0.1℃)时也很稳定。
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引用次数: 0
QSAR and Structure Based Modeling of Marine Derived Anticancer Hymenialdisine Compounds 海洋抗癌膜二胺类化合物的QSAR及结构建模
Pub Date : 2018-01-01 DOI: 10.4172/2329-6631.1000185
Ankita Sharma, Deepak Teotia, S. Nandi
Drug discovery research based on marine organisms is a big challenge. However, lack of facilities and competent human resources stand as a barrier on the way of research. More in-depth study especially on deep-sea natural products needs to be carried out to solidify the research on the potential for marine organisms to contribute to the future of drug discovery. The total drug discovery processes including collection of marine organisms, extraction, isolation, structure elucidation, biological assay and experimental screening as well as clinical trials is a very long journey and big challenge. Therefore, researchers pay a big attempt to design and discovery of synthetic congeneric leads by derivatizing the natural potent compounds. Therefore, In-silico High throughput screening based on QSAR and molecular docking has been attempted in the present study for the design and discovery of promising anticancer compounds considering existed marine sponge-derived hymenialdisine analogs which are protein kinase inhibitors having nanomolar activities against CDKs, Mek1, GSK 3β and CK1. It may crystallize crucial features for the design and discovery of promising anticancer HMD compounds which could be proposed for further synthesis and testing. QSAR and molecular docking analysis of HMD analogs are being carried out by freely accessible open source software which are very economical and potential in drug discovery attempt.
基于海洋生物的药物发现研究是一个巨大的挑战。然而,缺乏设备和合格的人力资源是研究道路上的障碍。需要进行更深入的研究,特别是对深海天然产物的研究,以巩固海洋生物对未来药物发现的潜力的研究。整个药物发现过程包括海洋生物的采集、提取、分离、结构解析、生物分析和实验筛选以及临床试验,这是一个非常漫长的过程和巨大的挑战。因此,研究人员在设计和发现天然有效化合物衍生化的合成同源先导物方面付出了巨大的努力。因此,本研究尝试基于QSAR和分子对接的硅基高通量筛选,以设计和发现有前途的抗癌化合物,考虑到现有的海洋海绵来源的膜苯二胺类似物是对CDKs, Mek1, GSK 3β和CK1具有纳米摩尔活性的蛋白激酶抑制剂。它可以为设计和发现有前途的抗癌HMD化合物提供关键特征,这些化合物可以提出进一步的合成和测试。HMD类似物的QSAR和分子对接分析正在通过免费的开源软件进行,这在药物发现尝试中非常经济和有潜力。
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引用次数: 4
Nanostructured Lipid Carriers: A Review 纳米结构脂质载体研究进展
Pub Date : 2018-01-01 DOI: 10.4172/2329-6631.1000191
A. Sharma, Ashish Baldi
Lipid-containing drug delivery systems like NLC are well-established methods for preparing pharmaceuticals for all major kind of drug delivery systems of nanoscience. Lipid formulations require a variety of product-related requirements and problems associated with NLC, which is discussed thoroughly in this chapter. There are multiple DDS currently available which leads to enhance the solubility of the drugs in different medium as well as also increase the bioavailability of the drugs in different conditions and environments. NLC’s are a novel type of DDS which are stable in different environment and which have capabilities to form concentrated dispersions. In this chapter, we discussed different process variables, steps involved in the manufacturing of NLC and responses with their outcome. NLC’s can increase the drug distribution to the target organ, change the pharmacokinetic characteristics of drug carriers to enhance the therapeutic effect, and reduce adverse side effects.
像NLC这样的含脂药物传递系统是制备药物的成熟方法,适用于所有主要的纳米科学药物传递系统。脂质配方需要与NLC相关的各种产品相关要求和问题,本章将对此进行深入讨论。目前已有多种DDS,可提高药物在不同介质中的溶解度,提高药物在不同条件和环境下的生物利用度。nlc是一种新型的DDS,在不同的环境中具有稳定性和形成集中分散的能力。在本章中,我们讨论了不同的过程变量,在NLC制造过程中所涉及的步骤以及它们的结果的响应。nlc可以增加药物向靶器官的分布,改变药物载体的药代动力学特性,提高治疗效果,减少不良副作用。
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引用次数: 18
Preparation and Characterization of Paracetamol Loaded Eudragit S100 Nanoparticles by Salting Out Technique 盐析法制备负载对乙酰氨基酚的乌龙茶S100纳米颗粒及表征
Pub Date : 2018-01-01 DOI: 10.4172/2329-6631.1000183
Ayesha Siddiqua Gazi, A. Sailaja
The aim of this study was to prepare Paracetamol loaded Eudragit S100 nanoparticles by salting out (SO) technique. Eudragit S100 (ED) was used as a polymer. Paracetamol and polymer were dissolved in ethanol at various drug-polymer ratios (1:1, 1:2 and 1:3), among three formulations 1:3 was found to be the best formulation with drug content of 80.3% and entrapment efficiency was found to be 99.8%. Loading capacity was found to be more for 1:3 formulation. Na.cmc was used as stabilizer and ZnSO4.7H2O was used as a salting out agent and ethanol were used as solvent.
本研究的目的是采用盐析(SO)技术制备对乙酰氨基酚负载的乌龙茶S100纳米颗粒。采用Eudragit S100 (ED)作为聚合物。将扑热息痛和聚合物以不同的药聚合物比(1:1、1:2和1:3)溶于乙醇中,3种配方中以1:3为最佳配方,药物含量为80.3%,包封率为99.8%。发现1:3配方的承载能力更大。Na。以cmc为稳定剂,ZnSO4.7H2O为盐析剂,乙醇为溶剂。
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引用次数: 4
Formulation and Evaluation of Modified Liposome for Transdermal Drug 透皮药修饰脂质体的制备及评价
Pub Date : 2018-01-01 DOI: 10.4172/2329-6631.1000186
Ghule Mm, Bhoyar Gs
Objective: Pramipexole is widely used in the treatment of anti-Parkinson’s, however it is associated with several side effects so the objective was to develop liposomal drug delivery of Pramipexole and thus reduce its side effect and toxicity and improve bioavaibility, efficacy and therapeutic index. Further study to modify drug delivery and to determine effect of stearylamine and sodium cholate content on the liposomal characteristics was investigated.Methods: In the present study the modified liposomes were prepared by using Pramipexole, phosphotidylcholine, cholesterol, stearylamine and sodium cholate in different ratio. These liposomes were prepared using thin film hydration method and characterized for vesicle size, drug entrapment studies, in-vitro release, and zeta potential, ex-vivo study.Results: The preparation of pramipexole loaded liposome was initiated by studying the influencing of drug lipid ratio on drug entrapment in vesicles. The drug bearing capacity of liposome was found to be invariably dependent on drug lipid ratio employed in liposomal composition, then formulation addition of stearylamine and sodium cholate to determine penetration enhancer. Modified liposome of optimized liposomal batches was formulated. Further modified liposomes were evaluated for entrapment efficiency, in-vitro release, zeta potential, and vesicle size. Thus, positive charged liposome seen to be promising as carrier for pramipexole drug thought transdermal drug delivery system.Conclusion: Incorporation of stearylamine enhanced the percent entrapment of pramipexole owing to rigidizaton effect on the membrane packing. Modified Liposomes of pramipexole can be promising carriers for the effective treatment of Parkinson’s.
目的:普拉克索被广泛应用于抗帕金森病的治疗,但其存在多种副作用,目的是研究普拉克索的脂质体给药,从而降低其毒副作用,提高其生物利用度、疗效和治疗指标。进一步研究改变给药方式,确定硬脂胺和胆酸钠含量对脂质体特性的影响。方法:采用普拉克索、磷脂酰胆碱、胆固醇、硬脂胺和胆酸钠按不同比例制备改性脂质体。这些脂质体采用薄膜水合法制备,并进行了囊泡大小、药物包裹、体外释放、zeta电位、离体研究等表征。结果:通过研究药物脂质比对药物囊泡包埋的影响,初步制备了载普拉克索脂质体。脂质体的药物承载能力始终取决于脂质体组成中采用的药物脂质比,然后通过添加硬脂胺和胆酸钠来确定渗透增强剂。对优化后的脂质体批次进行了修饰。进一步的修饰脂质体被评估包裹效率,体外释放,zeta电位和囊泡大小。因此,带正电荷的脂质体有望作为普拉克索药物经皮给药系统的载体。结论:硬脂胺的加入使普拉克索的包封率增加,这是由于其对膜填料的硬化作用所致。改性普拉克索脂质体有望成为治疗帕金森病的有效载体。
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引用次数: 14
Formulation and Evaluation of Licozinat Matrix Tablet Licozinat基质片的处方及评价
Pub Date : 2018-01-01 DOI: 10.4172/2329-6631.1000190
D. Otgonsuren, Davaasuren Ts, B. Enkhtuul, D. Davaadagva, D. Jambaninj
Objective: Monoammonium glycyrrhizinate of Glycyrrhiza root has been used as an expectorant, detoxificator, anti-allergic, and antioxidant. Japanese researchers have been determined it has anti-viral activity in case of hepatitis A, B, C, D. We have isolated monoammonium glycyrrhizinate from Glycyrrhiza root, grown in Mongolia through a method presented in a previous study. The objective of the study was to develop prolonged release matrix tablet with hepatoprotective effect and to evaluate their pharmacotechnical qualities and the in vivo performance. Licozinat matrix tablets contained monoammonium glycyrrhizinate 140 mg; glycine 50 mg; LD-methionin 50 mg in each tablet. Methods: In the present study the matrix tablet were prepared using HPMC K4000, lactose, glucose, microcrystalline cellulose, PVP-K30, talc and magnesium stearate in different ratios. The matrix tablet were prepared by wet granulation method and evaluated for weight variation, hardness, friability, in-vitro release, and in vivo study. Results: Appropriate excipients were chosen for the matrix tablets: lactose as a diluent, 5% of PVP-K30 as a binder, HPMC as a matrix former, 3% of talc and 1% of magnesium stearate as a glidiant or lubricant. We have prepared the matrix tablets by wet granulation method and compressed the tablet mixture by a 2.5 kPa pressure. Formulation 5 (F5) was determined to be the most appropriate tablet design and it released the drug in a prolonged way during the in vitro testing. The hepatoprotective effect of matrix tablet in comparison to Glycyron tablet, were studied on CCl4 induced hepatotoxicity in rats. The effect of Licozinat matrix tablet were compared with the Glycyron tablet that were administered to CCl4 treated rats. On administration Licozinat matrix tablet decreased the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), total bilirubin and alkaline phosphatise (ALP). Conclusion: We have developed and evaluated prolonged/controlled release matrix tablets with hepatoprotective effect. The Licozinat matrix tablets satisfied the quality criteria. On administration Licozinat matrix tablet decreased the level of alanine aminotransferase (ALT), aspartate aminotransferase (AST) and total bilirubin and alkaline phosphatise (ALP).
目的:甘草的甘草酸一铵具有祛痰、解毒、抗过敏、抗氧化等作用。日本研究人员已经确定它对甲型肝炎、乙型肝炎、丙型肝炎和丁型肝炎具有抗病毒活性。我们已经从蒙古种植的甘草根中分离出甘草酸一铵,通过先前研究中提出的方法。本研究的目的是研制具有保肝作用的缓释基质片,并对其药物技术质量和体内性能进行评价。甘草酸一铵Licozinat基质片140mg;甘氨酸50毫克;ld -蛋氨酸50mg /片。方法:采用HPMC - K4000、乳糖、葡萄糖、微晶纤维素、PVP-K30、滑石粉、硬脂酸镁按不同比例制备基质片。采用湿造粒法制备基质片,并对其进行重量变化、硬度、脆性、体外释放度和体内研究。结果:基质片选用合适的辅料:乳糖作为稀释剂,5%的PVP-K30作为粘合剂,HPMC作为基质成形剂,3%的滑石粉和1%的硬脂酸镁作为滑脂剂或润滑剂。采用湿造粒法制备基质片剂,并以2.5 kPa的压力对片剂混合物进行压缩。体外试验确定配方5 (F5)为最合适的片剂设计,且释放时间较长。研究了基质片与甘草酸片对CCl4致大鼠肝毒性的保护作用。比较Licozinat基质片与甘草素片对CCl4治疗大鼠的作用。甘草齐那特基质片可降低丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)、总胆红素和碱性磷酸酶(ALP)水平。结论:研制并评价了具有保肝作用的缓释/控释基质片。Licozinat基质片符合质量标准。口服甘草嗪基片可降低血清丙氨酸转氨酶(ALT)、天冬氨酸转氨酶(AST)、总胆红素和碱性磷酸酶(ALP)水平。
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引用次数: 2
Acute Respiratory Distress Syndrome Associated with Intravenous Lipid Emulsion Therapy for Verapamil Toxicity, Successfully Treated with Veno-Venous ECMO 急性呼吸窘迫综合征与静脉脂质乳剂治疗维拉帕米毒性相关,静脉-静脉ECMO成功治疗
Pub Date : 2017-11-21 DOI: 10.4172/2329-6631.1000182
T. Friedman, Y. Feld, Z. Adler, G. Bolotin, Y. Bentur
Calcium channel blocker (CCB) overdose is a potentially fatal poisoning. The use of intravenous lipid emulsion (ILE) therapy for CCB poisoning has emerged in the past few years. In 2017, the American College of Medical Toxicology published interim guidance for the use of ILE resuscitation in these cases. We report an uncommon complication of ILE, acute respiratory distress syndrome, treated with veno-venous extracorporeal membrane oxygenation (ECMO). Case report: A 40-year-old hypertensive woman presented with shock (blood pressure 62/34 mmHg, pulse 86/ min) following ingestion of 4,800 mg verapamil slow release and 1,500 mcg clonidine during a suicide attempt. She was treated with calcium gluconate, sodium bicarbonate, IV high dose insulin, IV glucagon, cardiac amines and vasopressors without response (blood pressure 69/37 mmHg, pulse 78/min). ILE was initiated, and two hours later, she developed acute respiratory failure necessitating intubation and mechanical ventilation. Due to poor oxygenation (pO2 44 mmHg; FiO2 100%) emergent veno-venous ECMO was instituted. After one hour her blood pressure increased to 104/50 mmHg (pulse 80, pO2 75 mmHg), and continued so until weaning from ECMO and ventilation. Conclusion: Acute respiratory distress syndrome can be a major life threating complication following ILE; venovenous ECMO is suggested for its treatment.
钙通道阻滞剂(CCB)过量是一种潜在的致命中毒。静脉脂质乳剂(ILE)治疗CCB中毒在过去几年出现。2017年,美国医学毒理学学院发布了在这些病例中使用ILE复苏的临时指南。我们报告一个不常见的ILE并发症,急性呼吸窘迫综合征,用静脉-静脉体外膜氧合(ECMO)治疗。病例报告:一名40岁高血压女性在自杀企图中摄入4800 mg维拉帕米缓释和1500 mcg可乐定后出现休克(血压62/34 mmHg,脉搏86/ min)。患者给予葡萄糖酸钙、碳酸氢钠、静脉注射大剂量胰岛素、静脉注射胰高血糖素、心胺和血管加压药物治疗,无反应(血压69/37 mmHg,脉数78/min)。术后2小时,患者出现急性呼吸衰竭,需要插管和机械通气。由于氧合不良(pO2 44 mmHg;FiO2 100%)急诊静脉-静脉ECMO。1小时后,她的血压升高到104/50 mmHg(脉搏80,pO2 75 mmHg),并一直持续到脱离ECMO和通气。结论:急性呼吸窘迫综合征是ILE患者的主要并发症;建议采用静脉-静脉ECMO治疗。
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引用次数: 2
Researching Prospect of Correspondence between Prescription and Syndromes on the Pathologic Basis of Yin Deficiency Syndrome of Liver and Kidney and Effective Mechanism of Decoction of Yiguan Jian 肝肾阴虚证病理基础方证对应研究展望及益官健汤作用机理
Pub Date : 2017-08-31 DOI: 10.4172/2329-6631.1000176
Yao Wl, Fan Ww, Chen Xl, S. My, Mu Yp, P. Liu, H. Zhang
The theory of correspondence between prescription and syndrome is an important starting point for studying modern TCM. Yin deficiency syndrome of liver and kidney is a common clinical syndrome found in many chronic diseases, and modern researches had found its pathobiological basis involving synthetic and metabolic disorders of the body material, chronic inflammation, and damage and apoptosis of cells, etc. Decoction of Yiguan Jian is an effective prescription for Yin deficiency syndrome of liver and kidney, commonly used in clinical treatment of a variety of chronic diseases. Based on summarizing studies on pathobiological basis of Yin deficiency syndrome of liver and kidney and clinical effects of Decoction of Yiguan Jian, this article has discussed the meaning of correspondence between prescription and syndrome in the treatment of Yin deficiency syndrome of liver and kidney with decoction of Yiguan Jian, demonstrated the practical values and developing prospects, and provided new ideas for the study of correlation of syndrome and treatment.
方证对应理论是研究现代中医的重要起点。肝肾阴虚证是许多慢性疾病的临床常见证候,现代研究发现其病理生物学基础涉及机体物质合成代谢紊乱、慢性炎症、细胞损伤凋亡等。益官健汤是治疗肝肾阴虚证的有效方剂,临床常用于治疗多种慢性疾病。本文在总结肝肾阴虚证病理生物学基础及益官健汤临床疗效研究的基础上,探讨了益官健汤治疗肝肾阴虚证方证对应的意义,论证了其实用价值和发展前景,为证治相关性研究提供了新的思路。
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引用次数: 1
Coin Image of Action of Atropa belladonna in Crude and in Homoeopathic Potentised Form 颠茄粗品和顺势电位形态作用的硬币图像
Pub Date : 2017-08-22 DOI: 10.4172/2329-6631.1000175
Neeta Chavan
Atropa belladonna is a bifurcating herbaceous plant from Solanaceae natural order. Germination of seeds is difficult. Plant contains various alkaloids with various percentage in plant parts. Alkaloids are as Belladonnaare Atropine, Hyoscine (scopolamine), Hyoscyamine, and Belladonine having anticholinergic properties. They act through parasympathetic and sympathetic nervous system. Hyoscyamine is an antagonist of muscarinic acetylcholine receptors. Atropine and Hyoscine having anticholinergic properties. By combine action they produce stimulation of higher centers of brain initially and then motor centers. Atropa belladonna is recommended in various pharmacological doses for various health disorders. According to Homeopathic fundamental principles homeopathic remedy Belladonna is prepared using entire Belladonna plant and its medication is used to cure a number of health conditions, particularly unexpected onset of infections with inflammation and intense heat. The Belladonna plant is highly noxious. But when is given as a homeopathic medication, it does not preserve the slightest trace of toxicity and become safe for human consumption along with its different indications. Homeopathic Belladonna is completely safe and effective for many health concerns and has different indications than pharmacological suggestions.
颠茄是茄科自然目的一种分生草本植物。种子很难发芽。植物中含有不同比例的生物碱。生物碱有颠茄碱、阿托品、莨菪碱、莨菪碱和颠茄碱等具有抗胆碱能特性。它们通过副交感神经和交感神经系统起作用。莨菪碱是毒蕈碱类乙酰胆碱受体的拮抗剂。阿托品和海莨菪碱具有抗胆碱能特性。通过联合作用,它们首先刺激大脑的高级中枢,然后是运动中枢。颠茄被推荐以不同的药理学剂量治疗各种健康疾病。根据顺势疗法的基本原理,顺势疗法的药物颠茄是用整个颠茄植物制备的,它的药物被用来治疗许多健康状况,特别是意想不到的感染,炎症和高温。颠茄是剧毒植物。但是,当作为顺势疗法药物给予时,它不会保留丝毫的毒性痕迹,并且随着其不同的适应症,人类消费变得安全。顺势疗法颠茄对许多健康问题是完全安全有效的,有不同的适应症,而不是药理学建议。
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引用次数: 0
Mesoporous Silica Nanoparticles: A Review 介孔二氧化硅纳米颗粒研究进展
Pub Date : 2017-08-16 DOI: 10.4172/2329-6631.1000174
Asad Mehmood, H. Ghafar, Samiya Yaqoob, Umar Farooq Gohar, B. Ahmad
One of the greatest challenges in the field of medicine is the effective and efficient drug delivery to the defected cells or tumor cells with minimal toxic side effects. Due to lacking properties like specification and solubility of drug molecule, patient requires high doses of the drug to attain the desired therapeutic effect for the disease treatment. To overcome this problem various drug carriers are available in the pharmaceutical field, which help in delivering the therapeutic drug/ gene to the target site. For this purpose, mesoporous silica nanoparticles (MSNs) are found to be biocompatible, chemically and thermally stable nanoparticles. Their unique structural properties facilitate the loading of drug/gene and subsequent controlled delivery of drug to the target site. During recent years research on MSNs has been extensively increase. Since 2001, when MCM-41 was first proposed and later on SBA-15 and MCM-48 as drug carrier for controlled delivery system. Morphological characteristics like pore size, pore volume, particle size, surface area, pH and loading capacity of drug are widely effects the MSNs, when altered. Meanwhile, functionalization of MSNs using organic and inorganic group elaborates the delivery of drug to targeted site. This review article also deals with the recent research on synthesis methods of MSNs and their applications in the field of medicine, imaging, diagnosis, cellular uptake, target drug delivery, cell tracing and bio-sensing.
如何以最小的毒副作用将药物有效、高效地输送到有缺陷的细胞或肿瘤细胞,是医学领域面临的最大挑战之一。由于缺乏药物分子的规格和溶解度等特性,患者需要高剂量的药物才能达到所需的治疗效果。为了克服这一问题,制药领域出现了各种各样的药物载体,它们有助于将治疗药物/基因运送到靶点。为此,介孔二氧化硅纳米颗粒(MSNs)被发现具有生物相容性、化学稳定性和热稳定性。它们独特的结构特性有助于药物/基因的装载和随后的药物控制递送到靶点。近年来,对微微网络的研究得到了广泛的发展。自2001年以来,MCM-41首次被提出,后来SBA-15和MCM-48作为受控给药系统的药物载体。孔径、孔体积、粒径、比表面积、pH值和药物负载能力等形态特征在改变后会对微孔微球产生广泛的影响。同时,利用有机和无机基团对msn进行功能化,阐述了药物向目标部位的传递。本文综述了近年来纳米微球的合成方法及其在医学、影像、诊断、细胞摄取、靶向药物传递、细胞示踪和生物传感等领域的应用。
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引用次数: 94
期刊
Journal of Developing Drugs
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