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Functionalization of Polymeric Nanoparticles for Drug Delivery Across the BloodâBrain Barrier 高分子纳米颗粒在血-脑屏障药物传递中的功能化
Pub Date : 2020-01-01 DOI: 10.21767/2321-547X.8.1.33
Jyoti Rawat
The blood–brain barrier (BBB) is made out of cerebrum endothelial cells, pericytes, and astrocytes, which assemble a tight cell obstruction. Restorative (macro)molecules can't travel through the BBB in their free structure. This constraint is skirted by apolipoprotein E (ApoE)‐functionalized polymeric nanoparticles (NPs) that can move drugs (e.g., dalargin, loperamide, doxorubicin, and nerve development factor) over the BBB by means of low density lipoprotein (LDL) receptor‐mediated transcytosis. Covering with polysorbate 80 or poloxamer 188 encourages ApoE adsorption onto polymeric NPs empowering acknowledgment by LDL receptors of cerebrum endothelial cells. This impact is even upgraded when NPs are legitimately covered with ApoE without surfactant grapple. Also, covalent coupling of ApoE to NPs that bear receptive gatherings on their surface prompts altogether improved cerebrum take-up while keeping away from the utilization of surfactants. In this Progress Report a few in vitro BBB models utilizing mind endothelial cells or cocultures with astrocytes/pericytes/glioma cells are portrayed, which give bits of knowledge in regards to the capacity of a m
血脑屏障(BBB)是由大脑内皮细胞、周细胞和星形胶质细胞组成的,它们组成了一个紧密的细胞屏障。恢复性(宏观)分子不能在其自由结构中穿过血脑屏障。载脂蛋白E (ApoE)â Â′功能化的聚合物纳米颗粒(NPs)可以通过低密度脂蛋白(LDL) receptorâ Â′介导的胞吞作用将药物(如dalargin、loperamide、阿霉素和神经发育因子)转移到血脑屏障上,从而绕过了这一限制。覆盖聚山梨酸酯80或poloxam188促进ApoE吸附到聚合物NPs上,增强LDL受体对大脑内皮细胞的识别。当NPs被ApoE合法覆盖而没有表面活性剂缠绕时,这种影响甚至会升级。此外,ApoE与在其表面承受受体聚集的NPs的共价偶联,在避免使用表面活性剂的同时,促进了大脑的吸收。在本进展报告中,描述了一些利用脑内皮细胞或与星形胶质细胞/周细胞/胶质瘤细胞共培养的体外血脑屏障模型,这些模型提供了有关脑脑屏障能力的一些知识
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引用次数: 0
Steroidal molecules as swiftly acting therapeutics 类固醇分子作为速效治疗药物
Pub Date : 2020-01-01 DOI: 10.21767/2321-547X.8.1.34
Jyoti Rawat
The A steroid is a sort of natural exacerbate that contains a features plan of four cycloalkane rings that are joined to one another. Steroid biosynthesis is an anabolic metabolic pathway that produces steroids from basic forerunners. Steroid, any of a class of regular or engineered natural mixes portrayed by a sub-atomic structure of 17 carbon particles orchestrated in four rings. Steroids are significant in science, science, and medication
甾体是一种天然的化合物,它包含四个环烷烃环相互连接的特征图。类固醇生物合成是一种合成代谢途径,从基本的前体产生类固醇。类固醇:由17个碳粒子组成的四个环的亚原子结构所描绘的一类规则的或经过改造的天然混合物。类固醇在科学、科学和医学上都很重要
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引用次数: 0
Development and Evaluation of a Shea Butter Based Cream Containing Essential Oils from the Leaves of Ocimum gratissimum Lamiaceae), a Plant with Antifungal Activity 具有抗真菌活性的木果油基乳木果油乳霜的研制与评价
Pub Date : 2020-01-01 DOI: 10.21767/2321-547X.8.1.30
Koffi
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引用次数: 0
Anti-cancer and Anti-oxidant Potencies of Cuscuta reflexa Roxb. Plant Extracts 菟丝子的抗癌和抗氧化作用。植物提取物
Pub Date : 2020-01-01 DOI: 10.36648/2321-547X.8.1.31
I. Ali, M. Suhail, Mohd Fazil, B. Ahmad, A. Sayeed, Mohd Farooq Naqshb, A. Azam
All around the world, the percentage of deaths due to cancer is continuously increasing-the greatest devastation of deaths. Among all medications, Unani medicines are boon for human beings to treat cancer with no or least side effects. About 80% rural population use natural products for primary health care. Cuscuta reflexa Roxb. (family Cuscutaceae) is utilized in traditional medicines for curing cancer and other diseases, and it is considered as the most significant plant in the Unani medicinal system. The extracts of Cuscuta reflexa Roxb. were obtained to measure the anticancer activity with H-1299 and MCF-7 cancer cell lines. Soxhlet extraction was utilized for stem and seeds. The anticancer activity of fractions of each extract obtained by using Flash chromatography was also checked. Besides, the antioxidant activity of each fraction was also checked. DNA binding study supported the results obtained during whole process. The cellular death was detected utilizing ELISA. The results indicated that extracts of Cuscuta reflexa Roxb. exhibited strong anticancer activities as compared to the fractions of each extract. Cuscuta reflexa Roxb. extracts indicated noteworthy cytotoxicity against human H-1299 and (lung cancer) MCF-7 cancer cells (breast cancer). The extract of this plant may be given to the patients having lung cancer and breast cancer.
在世界范围内,癌症导致的死亡比例持续上升,这是对死亡的最大破坏。在所有药物中,Unani药物是人类治疗癌症的福音,没有或几乎没有副作用。约80%的农村人口使用天然产品进行初级卫生保健。Cuscuta reflexia Roxb。(cuscutacaceae科)在传统医学中用于治疗癌症和其他疾病,它被认为是Unani医疗系统中最重要的植物。山茱萸提取物。测定其对H-1299和MCF-7癌细胞的抗癌活性。茎和种子采用索氏提取。用闪蒸色谱法测定了各萃取物的抗癌活性。此外,还测定了各组分的抗氧化活性。DNA结合研究支持了整个过程的结果。采用ELISA法检测细胞死亡情况。结果表明:菟丝子提取物具有明显的抗氧化活性。表现出较强的抗癌活性。Cuscuta reflexia Roxb。提取物对人H-1299和(肺癌)MCF-7癌细胞(乳腺癌)具有显著的细胞毒性。这种植物的提取物可用于肺癌和乳腺癌患者。
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引用次数: 4
Flakka: A Designer Drug with Deadly Consequences Flakka:一种具有致命后果的设计药物
Pub Date : 2018-01-01 DOI: 10.21767/2321-547X.1000021
L. Hendricks, R. Ashmore, Samuel K. Bore
Flakka, a new designer drug, is surging in popularity. The name comes from la flaca, a Spanish club-slang term for a beautiful skinny girl. This latest illegal substance of abuse is likened to other synthetic cathinone drugs popularly called “bath salts” and takes the form of a pink or white foul-smelling crystal that can be eaten, mixed in drinks, snorted, injected, vaporized, and some have even used it like a suppository. The khat plant found in the Middle East and Somalia is the source of natural cathinones; there, leaves are chewed on to gain a sense of euphoria2,3. Vaporization is also a craze, using the fairly new e-cigarettes, where inhalation increases the immediacy to the blood stream. The U.S. National Institute on Drug Abuse has warned that smoking Flakka not only sends the drug very quickly into the bloodstream, it makes it particularly easy to overdose4. Poison control centers in states including Florida, Alabama, Mississippi, and Texas are responding to an increasing number of incidents involving it5. The lone active ingredient, alpha-PVP, is a stimulant that was developed in the 60s.
一种名为Flakka的新型人造药物正在迅速流行起来。这个名字来自la flaca,一个西班牙俱乐部俚语,指的是漂亮而苗条的女孩。这种最新的非法滥用物质与其他被称为“浴盐”的合成卡西酮药物类似,呈粉红色或白色的恶臭晶体,可以食用、混合在饮料中、鼻吸、注射、蒸发,有些人甚至把它当作栓剂使用。在中东和索马里发现的阿拉伯植物是天然卡西酮的来源;在那里,人们咀嚼树叶以获得一种欣快感。汽化也是一种热潮,使用相当新的电子烟,吸入增加了对血液的即时性。美国国家药物滥用研究所警告说,吸食弗拉卡不仅使药物迅速进入血液,而且特别容易过量。佛罗里达州、阿拉巴马州、密西西比州和德克萨斯州等州的中毒控制中心正在对越来越多的涉及它的事件作出反应。唯一的有效成分,α - pvp,是一种兴奋剂,是在60年代开发的。
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引用次数: 0
Preparation and In vitro Evaluation of Enteric Coated Oral Vancomycin Hydrochloride Sustained Release Formulation with Mucoadhesive Properties 肠溶包衣口服盐酸万古霉素黏附缓释片的制备及体外评价
Pub Date : 2018-01-01 DOI: 10.21767/2321-547X.1000029
Lana Alsharkas, Vijayaraj Kumar Palanirajan, Y. Wei
Clostridium difficile is a species of gram-positive bacteria thought to infect patients with weakened immune response resulting in colitis. Oral vancomycin hydrochloride is given four times a day to treat Clostridium difficile colitis and is commercially available in the form of capsule and solution. Patient’s compliance is the main issue in this treatment due to the multiple dosing frequencies. Accordingly, replacement of such dose regimen with a once daily dosage will enhance patient compliance. In this study, mucoadhesive vancomycin hydrochloride tablets were prepared with the use of chitosan to exert a local effect in the colon. Sustained release property was also imparted by chitosan. Enteric coating with Eudragit® S 100 was applied to prevent the sticking of chitosan tablets in the stomach and small intestine and deliver the tablets intact to the colon. The prepared tablets were evaluated for In vitro drug release for 24 hours and compared with the marketed formulation. The formulation was found to release in a sustained manner in pH 7.4 buffer allowing the colon delivered oral vancomycin hydrochloride to be a promising formulation in the development of a once daily treatment for Clostridium difficile colitis.
艰难梭菌是一种革兰氏阳性细菌,被认为感染免疫反应减弱的患者,导致结肠炎。口服盐酸万古霉素每天四次用于治疗艰难梭菌结肠炎,市售胶囊和溶液形式。由于多次给药频率,患者的依从性是该治疗的主要问题。因此,用每日一次的剂量替代这种剂量方案将提高患者的依从性。本研究利用壳聚糖制备盐酸万古霉素黏附片,使其在结肠内发挥局部作用。壳聚糖还具有缓释性能。采用Eudragit®s100肠溶包衣,防止壳聚糖片剂在胃和小肠的粘附,并将片剂完整地输送到结肠。对所制片剂进行了24小时体外释药评价,并与市售制剂进行了比较。该制剂被发现在pH 7.4缓冲液中持续释放,允许结肠递送口服盐酸万古霉素,是一种有前景的制剂,用于开发每日一次治疗艰难梭菌结肠炎。
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引用次数: 2
A Critical Therapeutic Target to Inhibit Apoptosisin Relevant Heart Failure: An Overview 抑制凋亡相关心力衰竭的关键治疗靶点:综述
Pub Date : 2018-01-01 DOI: 10.21767/2321-547X.1000027
Akriti Nepala, Sufia Yasmeenb, Fahad Akhtarc, Nirmala Kojua, Qu Aina, Cao Teng-Lia, Zhang Xiu-Xiua, Li Qinga, Chen Ding-Dinga
Heart failure (HF) is the ultimate trail anteceded by different genetics and categorized by impaired cardiac remodeling where heart chambers gradually expand and contractile function declines. Apoptosis is a well-thought-out system that gestures cells to self-destruct for cell renewal or to switch abnormal cell growth. The stability of cardiomyocytes is acknowledged using an essential method for the advancement of HF. Apoptosis possibly will remain in control on behalf of a substantial quantity of cardiomyocytes death in the sequence of acute myocardial infarction (MI) as well as advanced damage of persisting cells among the failing hearts. Indicating that distinctive apoptosis and the prospective ability knows how to remain lured in cardiomyocytes next to the investigational circumstances of beneficial mediation to inhibit apoptosis remnants as notorious. Promisingly apoptosis shows a starring protagonist in the reperfusion of tissue impairment, which has prophylactic, pathological and useful inferences. Numerous studies concluded that the progression of HF along with the apoptotic inhibitor is cardio protective and can prevent HF. This review article aims to deliberate lessons mainly to identify potential therapeutic targets in the cardiac muscles, as well as mechanisms of apoptosis in MI which is primarily intended for the upcoming treatment and inhibition of HF.
心力衰竭(HF)是由不同的基因导致的最终结局,并以心脏重构受损为分类,即心室逐渐扩张和收缩功能下降。细胞凋亡是一个经过深思熟虑的系统,它指示细胞自我毁灭以进行细胞更新或转换异常细胞生长。心肌细胞的稳定性被公认为是推进心衰的重要方法。在急性心肌梗死(MI)的序列中,细胞凋亡可能会代表大量心肌细胞死亡以及衰竭心脏中持续细胞的晚期损伤而受到控制。表明独特的细胞凋亡和潜在的能力知道如何在心肌细胞旁边保持引诱,有益的调解,以抑制细胞凋亡的残余作为臭名昭著的研究情况。令人鼓舞的是,细胞凋亡在组织损伤的再灌注中起主要作用,具有预防、病理和有用的推论。大量研究表明,心衰与凋亡抑制剂一起发展具有心脏保护作用,可以预防心衰。这篇综述文章旨在总结经验教训,主要是为了确定心肌的潜在治疗靶点,以及心肌梗死的细胞凋亡机制,这主要是为了即将到来的心衰治疗和抑制。
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引用次数: 0
Artificial T Cell Mimetics to Combat Melanoma Tumor Growth. 人工 T 细胞模拟物对抗黑色素瘤肿瘤生长
Shilpaa Mukundan, Dongli Guan, Amy Singleton, Yunlong Yang, Matthew Li, Biju Parekkadan

Despite recent breakthroughs in melanoma treatment with anti-PD-1 immunotherapy, innovative approaches are needed to improve off-target effects. In this study, we report a T cell mimetic microparticle delivery of soluble PD1 aiming at providing a carrier substrate for future combinatorial and targeting efforts. Microparticles of sizes varying from (5 μm to-7 μm) were conjugated with soluble mouse or human PD-1 through nearly irreversible binding between streptavidin and biotin. PD-1 conjugated microparticles (PDMPs) suppressed 3-dimensional tumor growth of human A375 and mouse B16-F10 melanoma cells compared to control microparticles conjugated with the Fc portion of human IgG1 (IgG1MPs). This can be attributed to competitive inhibition by PDMPs on a melanoma cell-intrinsic PD-1/PD-L1 pathway. A single, local administration of mPDMPs in a B16-F10 mouse melanoma model inhibited tumor growth significantly compared to control IgMPs at the same dose. CD45+ immune cells were found to infiltrate tumors treated with mPDMPs as a mechanism for tumor control. These results collectively suggest that PDMPs can target the melanoma cell-intrinsic PD-1/PD-L1 pathway and that these artificial T cell mimetics can be the scaffold for further improvements in anti-tumor immunotherapy.

尽管最近抗 PD-1 免疫疗法在黑色素瘤治疗中取得了突破性进展,但仍需要创新方法来改善脱靶效应。在这项研究中,我们报告了一种可溶性 PD1 的 T 细胞模拟微颗粒递送方法,旨在为未来的组合和靶向治疗提供载体基质。通过链霉亲和素和生物素之间近乎不可逆的结合,可溶性小鼠或人类 PD-1 与大小不等(5 μm 至 7 μm)的微颗粒共轭。与用人 IgG1 的 Fc 部分共轭的对照微颗粒(IgG1MPs)相比,PD-1 共轭微颗粒(PDMPs)抑制了人 A375 和小鼠 B16-F10 黑色素瘤细胞的三维肿瘤生长。这可归因于 PDMPs 对黑色素瘤细胞内在 PD-1/PD-L1 通路的竞争性抑制。与相同剂量的对照 IgMPs 相比,在 B16-F10 小鼠黑色素瘤模型中单次局部给药 mPDMPs 能显著抑制肿瘤生长。研究发现,CD45+免疫细胞浸润接受 mPDMPs 治疗的肿瘤是肿瘤控制的一种机制。这些结果共同表明,PDMPs 可以靶向黑色素瘤细胞内在的 PD-1/PD-L1 通路,这些人工 T 细胞模拟物可以成为进一步改善抗肿瘤免疫疗法的支架。
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引用次数: 0
Quercetin Loaded Nanostructured Lipid Carriers for Nose to Brain Delivery: In Vitro and In Vivo Studies 槲皮素负载的纳米结构脂质载体用于鼻到脑输送:体外和体内研究
Pub Date : 2018-01-01 DOI: 10.21767/2321-547X.1000022
N. L. Patil, H. Mahajan
The main objective of the study was to utilize potential of nanostructured lipid carriers of the quercetin for direct nose to brain delivery of drug as tool for the targeted delivery. The aim of this study was to prepare and characterize quercetin loaded NLC and to study its brain distribution. Novel QUE-NLCs were formulated. NLC Formulation was evaluated for various physicochemical properties such as particle size, zeta potential, drug loading, percent entrapment efficiency, morphology, in vitro drug release, and histopathology. The size of the QUE-NLC was about 118.2nm with poly dispersity index of 0.220 and zeta potential of -20.1 mV. Nose to brain distribution studies were performed using wistar rats.QUE-NLC exhibited sustained delivery of drug. Significant targeting to brain was achieved when compare to quercetin.The result showed that NLCs might be the promising approach for the nose to brain delivery of quercetin.
本研究的主要目的是利用槲皮素的纳米结构脂质载体的潜力,将药物作为靶向给药的工具,直接通过鼻子到大脑给药。本研究的目的是制备和表征槲皮素负载的NLC,并研究其脑内分布。研制了新型QUE-NLCs。评估了NLC制剂的各种物理化学性质,如粒径、zeta电位、载药量、包封率、形态、体外药物释放和组织病理学。QUE-NLC的尺寸约为118.2nm,多分散性指数为0.220,zeta电位为-20.1 mV。使用wistar大鼠进行鼻到脑分布研究。QUE-NLC表现出持续给药的特性。与槲皮素相比,实现了对大脑的显著靶向作用。结果表明,NLCs可能是一种很有前途的通过鼻向脑传递槲皮素的方法。
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引用次数: 10
Effect of Progesterone with Vitamin E on Pregnancy in Young Rabbit Does 黄体酮与维生素E对幼兔妊娠的影响
Pub Date : 2018-01-01 DOI: 10.21767/2321-547X.1000028
A. Salem, H. A. Hussein, Y. Gomaa, F. Allam
Progesterone (P4) and vitamin E (Vitamin E) are important in early stage of pregnancy especially in young does. The goal was to investigate effect of injection of P4, Vitamin E and their integration on pregnancy enhancement, embryo dimensions and P4 concentration in young does. 24 animals were divided into 4 equal groups: control group, P4 group (each doe was injected i.m with single dose of 1.0 mg long-acting P4 two days post-mating), Vitamin E group (each doe was injected i.m with 20 IU Vitamin E/kg BW every 3 days from mating to mid-pregnancy and P4+Vitamin E group. All does were ultrasono-graphically examined at days 7,10,12,14,16,18,20 and 22 of pregnancy. Results revealed that P4 and P4+Vitamin E treatment facilitated establishment of pregnancy on day 7 of pregnancy more than the control and Vitamin E alone. Amniotic vesicles diameters on day 12 and fetal length on days 14 and 16 were greater (P<0.05) in P4 and P4+Vitamin E groups. On days 18-22, fetus length was significantly larger in P4 group. P4 concentrations at first week and mid-pregnancy were significantly greater in P4 group followed by P4+Vitamin E. Conclusion: P4 and P4+Vitamin E enhanced the early stage of pregnancy during the first parity of rabbit does.
黄体酮(P4)和维生素E(维生素E)在怀孕早期很重要,尤其是对幼犬。目的是研究P4和维生素E注射及其整合对幼龄公羊促孕、胚胎尺寸和P4浓度的影响。将24只动物随机分为4组:对照组、P4组(交配后2 d每只母鹿注射单剂量长效P4 1.0 mg)、维生素E组(交配至妊娠中期每3 d每只母鹿注射20 IU维生素E/kg BW)和P4+维生素E组。在妊娠第7、10、12、14、16、18、20、22天均行超声检查。结果显示,P4和P4+维生素E治疗比对照组和单独维生素E治疗更容易在妊娠第7天建立妊娠。P4和P4+维生素E组第12天羊膜囊直径和第14、16天胎儿长度显著增加(P<0.05)。第18 ~ 22天,P4组胎长显著增大。P4组妊娠第1周和妊娠中期P4浓度显著高于对照组,P4+维生素E组次之。结论:P4和P4+维生素E对兔第一胎妊娠早期有促进作用。
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引用次数: 0
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American Journal of Advanced Drug Delivery
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