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Highlights on polymeric micelles as versatile nanocarriers for drug transporting 高分子胶束作为药物运输的多用途纳米载体
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i2.806
Hussein A. Abdul Hussein, Nidhal K. Maraie
Polymeric micelles are nanoscale core-shell structures formed by amphiphilic (block or graft) copolymers, that can self-aggregate in an aqueous medium. PMs characterized by small size, spherical shape, lower critical micellar concentration, which gave higher stability for PMs over conventional surfactant micelles. The core/shell structure permits polymeric micelle to entrap poor soluble drugs and can improve their solubility and permeability. The preparation of PMs tends to be relatively easy as compared to other novel drug delivery systems. This review focus on the general properties, types, types of copolymer utilized, formation mechanism, preparation methods, characterization techniques, and the applications on PMs.
聚合物胶束是由两亲(嵌段或接枝)共聚物形成的纳米级核壳结构,可在水介质中自聚集。其具有体积小、球形、临界胶束浓度低的特点,与传统表面活性剂胶束相比具有更高的稳定性。核/壳结构允许聚合物胶束捕获难溶性药物,提高其溶解度和渗透性。与其他新型给药系统相比,pmms的制备相对容易。本文综述了共聚物的一般性质、类型、共聚物类型、形成机理、制备方法、表征技术及其在高分子材料中的应用。
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引用次数: 1
Protective Effect of Co Q10 and Candesartan on Bleomyycin Induced Lung Fibrosis in Rats coq10和坎地沙坦对博莱霉素诱导大鼠肺纤维化的保护作用
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i1.787
Fatima Mohammad Saeed Mahdi, M. G. Alabbassi, Muthanna Ibrahim, Al-Ezzi
Fibrosis of the lungs is the final phase of many lung illnesses. Its characterized by excessive matrix production leading to the normal lung architecture destruction and eventually death. CoQ10 is an essential constituent of membrane oxidoreductase System. It is an intracellularly localized antioxidant   enzyme that is endogenously synthesized in humans. CoQ10 protects cellular components from destruction by free radical-induced oxidative damage. candesartan is a selective antagonist of angiotensin II type 1 receptor (AT1) and is widely employed for treatment of hypertension. Most up to date research shows angiotensin II close involvement with damage and fibrosis process in tissues of organs of circulation. Objective: This animal study was designed to investigate the effect of Co Q10 and candesartan as antifibrotic agents against pulmonary fibrosis focusing on selected markers involved in pulmonary fibrosis. Materials and Method: 48 rats divided randomly into four groups, each consisting of 12 male rats. Group I: (Control group), the rats in this group received single injection of 0.2 ml normal saline via intratracheal route. Group II: (The BLM group), received BLM (8.3 U/kg) as a single dose via the intratracheal rout. Group III: (BLM+CoQ10 group) rats receive BLM (8.3 U/kg) as sulfate salt dissolved in 0.1 ml of normal saline via the intratracheal instillation concomitant with 100 mg/kg co Q 10 per day orally for 5 days before and 10 days after BLM injection. Group IV: (BLM+ candesartan group) rats receive BLM (8.3 U/kg) as sulfate salt dissolved in 0.1 ml of normal saline via the intratracheal instillation concomitant with (10 mg/kg) candesartan per day orally for 5 days before and 10 days after BLM injection. The studied serum biomarkers were glutathione, arachidonate 5 lipoxygenase in addition to histopathological examination using trichrome stain.  Results: serum GSH concentration was lower in BLM group in comparison with the control group and the (BLM+ CoQ10) but this difference is not statistically significant. The serum GSH levels showed a significant(P<0.05) elevation in (BLM+ Candesartan) group when compared with the levels in the BLM group. The serum ALOX5 concentration was significantly elevated in BLM group in comparison with the control group (P < 0.05). The serum ALOX5 levels were highly significantly lower in (BLM +CoQ10) (P < 0.01) and very highly significantly lower in the (BLM+ Candesartan) group (P < 0.001) when comparing it with the levels in the BLM group. furthermore, histologically CoQ10 and candesartan showed reduction in the numbers of inflammation cells and a decrease in the damage to the lung architecture and fibrosis induced by bleomycin. Conclusion: CoQ10 and candesartan decrease pulmonary fibrosis induced by bleomycin in male rats.
肺纤维化是许多肺部疾病的最后阶段。其特点是基质产生过多,导致正常肺结构破坏,最终死亡。辅酶q10是膜氧化还原酶系统的重要组成部分。它是一种细胞内定位的抗氧化酶,在人体内内源性合成。辅酶q10保护细胞成分免受自由基诱导的氧化损伤的破坏。坎地沙坦是血管紧张素II型1受体(AT1)的选择性拮抗剂,广泛用于治疗高血压。最新研究表明血管紧张素II与循环器官组织的损伤和纤维化过程密切相关。目的:本动物研究旨在探讨Co Q10和坎地沙坦作为抗纤维化药物对肺纤维化的作用,重点关注与肺纤维化有关的选定标志物。材料与方法:48只大鼠随机分为4组,每组12只雄性大鼠。第一组:(对照组)经气管内注射生理盐水0.2 ml单次。第二组(BLM组),经气管内给药,给药剂量为8.3 U/kg。第三组(BLM+CoQ10组)大鼠给予BLM (8.3 U/kg)硫酸盐溶解于0.1 ml生理盐水中,气管内滴注,同时每天口服100mg /kg CoQ10,连续注射BLM前5天,注射后10天。IV组(BLM+坎地沙坦组)大鼠给予BLM (8.3 U/kg)硫酸盐溶解于0.1 ml生理盐水中,经气管内滴注,同时每日口服(10 mg/kg)坎地沙坦,连续注射BLM前5天、注射后10天。血清生物标志物为谷胱甘肽、花生四烯酸脂氧合酶,并进行三色染色组织病理学检查。结果:与对照组和(BLM+ CoQ10)相比,BLM组血清GSH浓度较低,但差异无统计学意义。与BLM组相比,(BLM+坎地沙坦)组血清GSH水平显著升高(P<0.05)。与对照组相比,BLM组血清ALOX5浓度显著升高(P < 0.05)。血清ALOX5水平(BLM+ CoQ10)极显著低于BLM组(P < 0.01), (BLM+坎地沙坦)组极显著低于BLM组(P < 0.001)。此外,组织学上,CoQ10和坎地沙坦显示炎症细胞数量减少,博来霉素引起的肺结构损伤和纤维化减少。结论:CoQ10和坎地沙坦可降低博来霉素诱导的雄性大鼠肺纤维化。
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引用次数: 3
Effects of Saw Palmetto Therapy on some Inflammatory Biomarkers in a Sample of Iraqi Male with Symptomatic Benign Prostatic Hyperplasia 锯棕榈治疗对伊拉克男性症状性前列腺增生一些炎症生物标志物的影响
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i1.774
Mazin Abdulridha Ateyah, Manal Khalid Abdulridha, Munaim Jumaa Alkabee
Background Saw palmetto contains powerful anti-inflammatory components commonly used in Benign prostatic hyperplasia (BPH) patients with symptoms. The current study was designed to assess the effectiveness of saw palmetto alone or supplementation   therapy with tamsulosin via measurement of some inflammatory biomarker in male with lower urinary tract symptoms (LUTS) consistent with (BPH). Methods The present study is an interventional prospective randomized enrolled newly diagnosed patients with moderate to severe symptomatic BPH. The eligible 60 patients were allocated into (3) groups, each group with (20) patients; Group (1) treated with Saw palmetto cap (320 mg); Group (2) treated with  Saw palmetto cap (320 mg) and tamsulosin (0.4mg); Group (3) treated with tamsulosin (0.4mg), protocols to be given once daily for 12 weeks. Measurement of prostate specific antigen (PSA), C-reactive protein (CRP), and interleukin 6 (IL-6) was done. Results There was significant decrease in the serum PSA, CRP and IL-6 level (P<0.01) in group1 and 2 patients only after treatment when compared to pretreatment.  Patients on combination therapy presented with high percent of change compared to other groups. No change in CRP and IL-6 level in patients on tamsulosin alone. Conclusion From the findings of the present study, phytotherapy with Saw Palmetto alone or as supplement produced significant 3 months drop in both inflammatory markers, the total CRP level and IL-6 level. Also produced significant decrease in PSA level, and may substitute the conventional therapy in mild disease status.
背景锯棕榈含有强效抗炎成分,常用于有症状的良性前列腺增生(BPH)患者。目前的研究旨在通过测量与BPH一致的下尿路症状(LUTS)男性的一些炎症生物标志物来评估锯棕榈单独或坦索罗辛补充治疗的有效性。方法本研究是一项介入前瞻性随机入组的新诊断的中重度BPH症状患者。将符合条件的60例患者分为3组,每组20例;组(1)用锯棕榈帽(320 mg)处理;组(2)用锯棕榈帽(320 mg)和坦索罗辛(0.4mg)处理;3组给予坦索罗辛(0.4mg),每日1次,连用12周。检测前列腺特异性抗原(PSA)、c反应蛋白(CRP)、白细胞介素6 (IL-6)。结果1、2组患者治疗后血清PSA、CRP、IL-6水平均较治疗前显著降低(P<0.01)。与其他组相比,接受联合治疗的患者表现出较高的变化百分比。单独使用坦索罗辛组CRP和IL-6水平无变化。结论从本研究的结果来看,锯棕榈单独或作为补充剂的植物治疗在3个月的时间里,炎症标志物、总CRP水平和IL-6水平都有显著下降。同时也能显著降低PSA水平,在轻症状态下可替代常规治疗。
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引用次数: 1
Prognostic factor of serum carcinoembryonic antigen in colorectal cancer patients: a follow up study 结直肠癌患者血清癌胚抗原影响预后的随访研究
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i3.791
Taha HT Al-Saigh, Shatha A Abdulmawjood, Faris A Ahmed
Colorectal cancer is a serious cancer with high mortality. Most of the recurrence usually occurred within two years after surgery. This study was conducted in Nineveh Medical Center and Al-Jammhorri Hospital to evaluate colorectal cancer patients in a follow up study for two years. Serum carcinoembryonic antigen, colonoscopy, ultrasound of the abdomen, and chest X rays were used for evaluation. One hundred and ninety-four patients with colorectal cancer were included in the study. The patients were diagnosed colorectal adenocarcinomas by histopathology and staged according to Duke’s classification. The patients were undergone surgical removal of the cancer. Chemotherapy was started to the patient after two weeks of the surgery. Blood samples were taken one week before and one week after surgery. Other blood samples were taken after chemotherapy and then every six months for two years. The blood samples were analyzed for serum carcinoembryonic antigen. The patients were also checked by colonoscopy, ultrasound for abdomen, and chest X ray every six months. Serum carcinoembryonic antigen in colorectal patients was higher than 5 ng/mL and decreased significantly after surgery but still higher than 5 ng/mL. After chemotherapy serum decreased significantly compared with that after surgery. During the two-year period serum carcinoembryonic antigen was not significantly different from that in patients after chemotherapy. Twenty-one patients died after two years of the study Serum carcinoembryonic antigen in the dead patients was much significantly higher than 5 ng/mL before surgery and decreased significantly after operation and after chemotherapy but still higher than 5 ng/mL. In conclusion, colorectal cancer is a significant disease in Iraq. The mortality rate is high due to lack of education of the community to that disease. Carcinoembryonic antigen marker is still acceptable test but should be used with other clinical assessments
结直肠癌是一种严重的癌症,死亡率高。大多数复发通常发生在术后两年内。本研究在尼尼微医学中心和Al-Jammhorri医院进行,对结直肠癌患者进行为期两年的随访研究。血清癌胚抗原、结肠镜检查、腹部超声和胸部X线检查进行评估。194名结直肠癌患者参与了这项研究。经组织病理学诊断为结肠腺癌,并按Duke分类法进行分期。这些病人接受了手术切除肿瘤。手术两周后,病人开始接受化疗。手术前一周和手术后一周分别取血样。化疗后采集其他血液样本,然后每六个月采集一次,持续两年。对血样进行血清癌胚抗原分析。每6个月对患者进行结肠镜检查、腹部超声检查和胸部X光检查。结直肠患者血清癌胚抗原高于5 ng/mL,术后明显下降,但仍高于5 ng/mL。化疗后血清水平较手术后明显下降。两年内血清癌胚抗原与化疗后无明显差异。研究2年后死亡21例,死亡患者血清癌胚抗原显著高于术前5 ng/mL,术后和化疗后显著降低,但仍高于5 ng/mL。总之,结直肠癌是伊拉克的一种重要疾病。由于社区缺乏对这种疾病的教育,死亡率很高。癌胚抗原标记仍然是可接受的测试,但应与其他临床评估一起使用
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引用次数: 0
Nuclear Factor Erythroid-2 Linked Factor (Nrf2) as a Potential Mediator of Hepatotoxicity 核因子-红细胞-2相关因子(Nrf2)作为肝毒性的潜在介质
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i4.796
Inam Sameh Arif, Israa Burhan Raoof, Hayder Hussein Luaibi
Hepatotoxicity is a term used to describe serious health complications of liver disease caused by a variety of factors. Nuclear factor erythroid-2 linked factor (Nrf2) as a potential mediator of hepatotoxicity via inflammatory and induction of oxidative stress, oxidation produces more toxic compounds caused more pathogenic cases; therefore, to maintain sufficient homeostasis, involve antioxidant materials and detoxification factors. Controlling cytokine activity in normal cells is a useful way to regulate the signaling pathway of Nrf2. Recent studies found a relation between each Nrf2 and NF-κB activation and drug-induced liver injury.  This review presents a detailed and conformation update of Nrf2 roles in hepatotoxicity which considers that drug-induced liver injury is the main problem to draw attention in medical clinics and to develop new drugs with less harmful to the liver. In addition to that. Kept each of normal oxidation and cytokines levels is crucial responses for cells alteration and remaining to survive.
肝毒性是一个术语,用于描述由多种因素引起的肝脏疾病的严重健康并发症。核因子-红细胞-2相关因子(Nrf2)作为肝毒性的潜在介质,通过炎症和诱导氧化应激,氧化产生的毒性化合物较多,引起的致病性病例较多;因此,维持足够的体内平衡,涉及抗氧化物质和解毒因子。调控正常细胞的细胞因子活性是调控Nrf2信号通路的有效途径。近年来研究发现Nrf2和NF-κB活化与药物性肝损伤有关。本文综述了Nrf2在肝毒性中的作用,认为药物性肝损伤是目前临床需要关注的主要问题,并开发对肝脏危害较小的新药。除此之外。维持正常的氧化和细胞因子水平是细胞改变和存活的关键反应。
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引用次数: 1
Design, Molecular Docking, Synthesis of Aromatic Amino Acids Linked to Cephalexin. 设计,分子对接,合成与头孢氨苄连接的芳香氨基酸。
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i3.794
Yasir F. Muhsin, Shakir M. Alwan, Ayad Kareem Khan
Infections caused by bacteria have a significant impact on public health. Chemical synthesis of new derivatives of cephalexin inked to amino acid (tryptophan or histidine) through an amide bond at the acyl side chain is achieved. This is a new approach of incorporating, tryptophan and histidine into the the primary amino group of cephalexin, in order to provide a bulky group very close to the β-lactam ring. This chemical addition act as isosteric group to the alkoximino that protect beta lactam ring from bacterial beta lactamase enzyme. The new derivatives may show resistance to β-lactamases, improve activity and pharmacokinetic properties and may give new life for old drugs that are susceptible to hydrolysis by most β-lactamases. The chemical structures of these derivatives were confirmed by: FTIR, 1H-NMR spectroscopy, elemental micro analysis and some physical properties. Molecular docking on serine beta lactamase and prediction of ADME parameters were recorded using GOLD suite and Swiss ADME software respectively. Docking scores of the new derivatives of Cephalexin on β-lactamases were higher than those of Cephalexin, which may indicate better activity
细菌引起的感染对公众健康有重大影响。通过酰基侧链上的酰胺键,实现了头孢氨苄与氨基酸(色氨酸或组氨酸)连接的新衍生物的化学合成。这是一种新的方法,将色氨酸和组氨酸结合到头孢氨苄的初级氨基中,以提供一个非常接近β-内酰胺环的庞大基团。这种化学加成物作为烷氧亚胺的等构基团,保护内酰胺环免受细菌内酰胺酶的侵害。新的衍生物可能对β-内酰胺酶产生抗性,提高活性和药代动力学性质,并可能使易被大多数β-内酰胺酶水解的旧药物获得新的生命。通过FTIR、1H-NMR、微量元素分析和一些物理性质证实了这些衍生物的化学结构。分别使用GOLD suite和Swiss ADME软件记录丝氨酸β内酰胺酶的分子对接和ADME参数的预测。头孢氨苄新衍生物与β-内酰胺酶的对接分数高于头孢氨苄,可能具有更好的活性
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引用次数: 6
Nrf2 as a modulator of oxidative stress Nrf2作为氧化应激的调节剂
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i4.798
Inam Sameh Arif, Yassir Mustafa Kamal, Israa Burhan Raoof
Nrf2 is active protein presents in the cytoplasm in the cells of the body. In the presence of an activators, Nrf2 can enter the nucleus which bind to Antioxidant Responses Elements (ARE) or otherwise named human ARE (hARE) which control the whole antioxidants activity in human cell. Many factors may contribute to defective or overwhelmed cellular antioxidants activities for instances aging and cellular damages. These cellular damages can be produced by free radicals or oxidative stress. In the mechanism, if Nrf2 activated in the nucleus, can caused the production of collaborative antioxidants enzymes especially: catalase, glutathione (GLT) and superoxide dismutase (SOD) as a responsible for detoxification of free radical inside the cells.
Nrf2是存在于机体细胞细胞质中的活性蛋白。在激活因子存在的情况下,Nrf2可以进入细胞核,与抗氧化反应元件(anti - oxide Responses Elements, ARE)结合,或称为人类抗氧化反应元件(human ARE, hARE),后者控制人类细胞的整个抗氧化活性。许多因素可能导致细胞抗氧化剂活性缺陷或过度,例如衰老和细胞损伤。这些细胞损伤可由自由基或氧化应激产生。在机制上,如果Nrf2在细胞核中被激活,可以引起协同抗氧化剂酶的产生,特别是过氧化氢酶、谷胱甘肽(GLT)和超氧化物歧化酶(SOD),这些酶负责细胞内自由基的解毒。
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引用次数: 3
Study the antibacterial effect of N_butanol extract of Urtica dioica 研究白荨麻疹正丁醇提取物的抑菌作用
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i1.800
Ahmed Abdulaziz Ahmed, Baydaa Hameed Abdulah, Yaser Mustafa Kamal
Since ancient times Urtica dioica has been used as an herbal medicine in Western Asia. The current study demonstrates the anti-bacterial effect of N_butanol extraction of Urtica dioica. The antibacterial effect was tested against some of gram-positive bacteria and gram-negative bacteria isolated   from hospitalized patients having urinary tract infection. Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia and Pseudomonas aeruginosa was used. Urticasea is a family of plant known for their medicinal activity from folk medicine. Urtica dioica is a member of urticasea and it is known for it is antibacterial effect. Methods The leaves of Urtica dioica were collected in Iraq from jisr dayla district in Baghdad province in april 2019.The N_butanol extraction was compared with the drug ciprofloxacin. Disc diffusion method was used to determine the sensitivity of the samples. Results The N_ butanol extract shows weak inhibitory effect on Escherichia coli while other strain does not affect by extract comparing with ciprofloxacin. Conclusion The N_butanol extract of urtica dioica have weak antibacterial effect when compared with ciproflxacine
自古以来,杜鹃花在西亚就被用作草药。本研究证实了荨麻疹正丁醇提取物的抑菌作用。对尿路感染住院患者分离的革兰氏阳性菌和革兰氏阴性菌进行抑菌试验。使用金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌。荨麻疹是一种以民间医学的药用活性而闻名的植物。荨麻疹是荨麻疹的一种,以其抗菌作用而闻名。方法2019年4月在伊拉克巴格达省jisr dayla地区采集菊苣叶。对正丁醇提取液与环丙沙星进行了比较。采用圆盘扩散法测定样品的灵敏度。结果与环丙沙星相比,正丁醇提取物对大肠埃希菌的抑制作用较弱,其他菌株的抑制作用不明显。结论与环丙沙星相比,白花荨麻疹n_丁醇提取物的抑菌作用较弱
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引用次数: 0
Misuse of antibiotics in Iraq: A review of Iraqi published studies 伊拉克滥用抗生素:伊拉克已发表研究综述
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i2.805
Khulood Saadoon Salim, Atheer S. Alsabah, Hassanian S. Taghi
Misuse of antibiotics is one of the health problems worldwide. In Iraq, prevalence of self- medication with antibiotics increases resistant organisms, this will lead to bad impacts on health and economic aspects in the future. Aim of study is to review the published articles on the antibiotics misuse in Iraq, in   addition to assess the level of the population’s knowledge towards   antibiotics misuse and the suggested recommendation to reduce this problem. Method: In this study 12 articles conducted in different regions of Iraq were reviewed to   assess antibiotic misuse in a period from 2014-2020.Results: The results demonstrated high prevalence of antibiotic misuse among Iraqi population ranging from (45%- 92%). In addition, poor knowledge among   population towards antibiotics misuse also reported. Bad attitudes of pharmacists and physicians regarding antibiotics prescribing and dispensing were registered. Conclusion:  The review focuses on important health issue in Iraq that effect on health & economic system. New legislations and restriction need to apply to limit this problem.
抗生素滥用是世界范围内的健康问题之一。在伊拉克,普遍使用抗生素自行用药增加了耐药生物体,这将在未来对健康和经济方面造成不良影响。本研究的目的是审查已发表的关于伊拉克抗生素滥用的文章,并评估伊拉克人民对抗生素滥用的认识水平和减少这一问题的建议。方法:回顾性分析2014-2020年伊拉克不同地区的12篇抗生素滥用文献。结果:结果表明,伊拉克人口中抗生素滥用的发生率很高,范围为(45%- 92%)。此外,还报告了人们对抗生素滥用的认识不足。药师和医师对抗生素处方和调剂的不良态度进行了登记。结论:综述了影响伊拉克卫生和经济系统的重要卫生问题。需要新的立法和限制来限制这一问题。
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引用次数: 0
Nano-carriers as a Selective Treatment for Cancer 纳米载体作为癌症的选择性治疗
Pub Date : 2022-04-19 DOI: 10.32947/ajps.v21i1.802
Ghaidaa S. Hameed, Methaq Hamad Sabar
Among many therapeutic treatments for cancer, nano-carriers are the focus of our review to illustrate the update usage of this drug delivery approach, the most likely side effects and the reality of their potential application with minimum adverse effects. Here, we demonstrate the types of these nano-carriers based on their nature with detailed recent studies about their use. The variation in the skeleton of these nanoparticles enable the selection of the suitable type with higher specifications than others.  However, the poor in vivo testing is the main stumbling block for completion of their manufacturing. This review will help the researchers to find the road map for further investigation to finally aid the pharmaceutical companies in manufacturing these nano-carriers in appropriate dosage forms to save the life of millions of people in the world.   
在许多癌症治疗方法中,纳米载体是我们综述的重点,以说明这种药物传递方法的最新用法,最可能的副作用以及它们潜在应用的现实,并且副作用最小。在这里,我们根据这些纳米载体的性质展示了它们的类型,并详细介绍了它们的用途。这些纳米颗粒骨架的变化使得选择合适的类型具有更高的规格。然而,较差的体内测试是完成其制造的主要障碍。这一综述将有助于研究人员找到进一步研究的路线图,最终帮助制药公司以适当的剂型制造这些纳米载体,以拯救世界上数百万人的生命。
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引用次数: 1
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Al Mustansiriyah Journal of Pharmaceutical Sciences
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