• 【脂质体中链激酶的负载量,用于血管靶向的纳米药物应用:包封效率和加工效果。】 复制标题 收藏 收藏
    DOI:10.1177/0885328210374778 复制DOI
    作者列表:Holt B,Gupta AS
    BACKGROUND & AIMS: :Vascular diseases leading to thrombo-occlusion are the leading cause of morbidity and mortality worldwide. Revascularization and restoration of antegrade blood flow is critical for tissue survival and patient health. In this aspect, systemic administration of thrombolytics (e.g., streptokinase) to dissolve occlusive thrombi is a clinically established strategy. However, this strategy typically necessitates the administration of large doses, leading to a high incidence of hemorrhagic complications due to systemic side effects. To minimize this risk, liposomes specifically targeted to the site of thrombo-occlusion have been bioengineered by exploiting ligand-receptor relationships pertinent to thrombus-associated cell phenotypes. This study focuses on encapsulating streptokinase within these liposomes, specifically regarding the effect of liposome processing conditions on streptokinase encapsulation and activity. Theoretical calculations of encapsulation capacity agreed well with that reported in the literature. The experimental encapsulation efficiency values are 45.9 ± 34.0% (n = 9 ± SD) and 21.6 ± 30.0% (n = 6 ± SD), using two different methods. The liposome processing conditions are found to decrease streptokinase activity; however, over 30% remain active after processing, maintaining enough activity to be therapeutic especially when protected inside a vehicle targeted to the site of thrombo-occlusion. The insight gained from the research reported here would enable refining the design and the processing conditions of liposomal formulations of fibrinolytics to yield reduced variability in encapsulation efficiency and streptokinase activity. The design of a thrombus-targeted 'stealth' liposome reported earlier and the current findings of fibrinolytics' encapsulation and activity in such liposomes can be efficiently integrated to develop an efficient strategy for vascular nanomedicine.
    背景与目标: :导致血栓闭塞的血管疾病是全球发病率和死亡率的主要原因。血运重建和顺行血流的恢复对于组织存活和患者健康至关重要。在这方面,溶栓剂(例如,链激酶)的全身给药以溶解闭塞性血栓是临床上确立的策略。但是,该策略通常需要大剂量给药,由于全身性副作用,导致出血并发症的发生率很高。为了使这种风险最小化,已经通过利用与血栓相关的细胞表型有关的配体-受体关系,生物工程化了专门针对血栓闭塞部位的脂质体。这项研究的重点是将链激酶包封在这些脂质体内,特别是关于脂质体加工条件对链激酶包封和活性的影响。封装能力的理论计算与文献报道的结果非常吻合。使用两种不同的方法,实验的包封效率值为45.9±34.0%(n = 9±SD)和21.6±30.0%(n = 6±SD)。发现脂质体加工条件降低了链激酶的活性。但是,加工后仍有超过30%的活性保持,保持足够的活性以进行治疗,尤其是在针对血栓闭塞部位的媒介物内部进行保护时。从这里报道的研究中获得的见识将有助于完善纤维蛋白溶解剂脂质体制剂的设计和加工条件,从而降低包封效率和链激酶活性的可变性。血栓靶向的“隐身”脂质体的设计已在较早前报道,纤维蛋白溶解剂在此类脂质体中的包封和活性的最新发现可有效整合,以开发出有效的血管纳米药物策略。
  • 【通过细乳液合成高负载量和高封装效率的紫杉醇负载型聚氰基丙烯酸正丁酯纳米粒子。】 复制标题 收藏 收藏
    DOI:10.1016/j.ijpharm.2007.01.052 复制DOI
    作者列表:Huang CY,Chen CM,Lee YD
    BACKGROUND & AIMS: :The manufacture of stable paclitaxel-loaded poly(n-butyl cyanoacrylate) (PBCA) nanoparticles containing high loading and encapsulation efficiency simultaneously were achieved in the presence of pluronic F127 via miniemulsion. It was found that both drug loading and encapsulation efficiencies of PBCA nanoparticles prepared by miniemulsion were higher (approximately three times) than those obtained by emulsion with similar paclitaxel content in the feed monomer (1%, w/w). Furthermore, the loading and encapsulation efficiencies increased concurrently (to a maximum of 4 and 80%, respectively) with increasing paclitaxel content and these nanoparticles were spherical in shape and with size near 100 nm. XRD patterns revealed that paclitaxel in particles was distributed in the molecular or amorphous state or in the form of small crystals. The in vitro drug release profile of drug-loaded PBCA nanoparticles prepared from miniemulsion exhibited a gradual release; more than 80% (w/w) of the paclitaxel was released after 96 h.
    背景与目标: :在普卢尼克F127的存在下,通过细乳液实现了稳定的负载紫杉醇的聚氰基丙烯酸正丁酯(PBCA)纳米粒子的制备,该纳米粒子同时具有高负载和包封效率。发现通过细乳液制备的PBCA纳米颗粒的载药量和包封效率均比通过进料单体中紫杉醇含量相似(1%,w / w)的乳液获得的载药量和包封效率更高(约三倍)。此外,随着紫杉醇含量的增加,加载和包封效率同时提高(分别达到最大4%和80%),并且这些纳米颗粒呈球形,尺寸接近100 nm。 XRD图谱表明,紫杉醇在颗粒中以分子或非晶态或小晶体形式分布。由细乳液制备的载有药物的PBCA纳米颗粒的体外药物释放曲线显示出逐渐释放; 96小时后释放出超过80%(w / w)的紫杉醇。
  • 【聚醚-共聚酯树状聚合物的分子结构对甲氨蝶呤包封和释放的影响。】 复制标题 收藏 收藏
    DOI:10.1016/j.biomaterials.2007.03.012 复制DOI
    作者列表:Dhanikula RS,Hildgen P
    BACKGROUND & AIMS: :In the present study, effects of alterations in the chemical structure of polyester-co-polyether (PEPE) dendrimers on the encapsulation and release of methotrexate (MTX) was investigated. A series of PEPE dendrimers of different architecture were synthesized. Biocompatibility of the resulting dendrimers was evaluated in vitro by assessing their cytotoxicity on RAW 264.7 cells using lactate dehydrogenase (LDH) assay. Dendrimers caused no cell death even at the concentration of 250 microg/mL, suggesting that they are acceptable for pharmaceutical applications. They also showed good capacity to encapsulate MTX, with loading as high as 24.5% w/w. Increase in the number of branches and the size of internal voids were shown to enhance the encapsulation. On the other hand, absence of aromatic rings as branching units drastically reduced the loading capacity. Physical entrapment, weak hydrogen bonding and hydrophobic interactions were established to be the mechanisms of encapsulation. Release of MTX was biphasic, which included a burst release in 6h followed by a slower release over a period of 50 or 168 h. Increase in the number of branches profoundly decreased this initial burst release; in contrast, absence of aromatic rings in the dendritic structure resulted in a very rapid release.
    背景与目标: :在本研究中,研究了聚酯-共聚醚(PEPE)树状聚合物的化学结构变化对甲氨蝶呤(MTX)包封和释放的影响。合成了一系列不同结构的PEPE树枝状聚合物。通过使用乳酸脱氢酶(LDH)分析评估它们对RAW 264.7细胞的细胞毒性,在体外评估了所得树状聚合物的生物相容性。树枝状大分子即使在250微克/毫升的浓度下也不会引起细胞死亡,这表明它们对于药物应用是可以接受的。他们还表现出了很好的封装MTX的能力,负载高达24.5%w / w。分支数目的增加和内部空隙的大小显示出增强封装的作用。另一方面,不存在芳环作为分支单元会大大降低其负载能力。物理包封,弱氢键和疏水相互作用被确定为封装的机制。 MTX的释放是双相的,包括在6小时内突然释放,然后在50或168小时内缓慢释放。分支数量的增加极大地减少了最初的爆发释放;相反,在树枝状结构中不存在芳环导致非常快速的释放。
  • 【新型脂质纳米粒脂质体黄嘌呤封装的亚马逊产品。】 复制标题 收藏 收藏
    DOI:10.1208/s12249-019-1601-y 复制DOI
    作者列表:Cordenonsi LM,Santer A,Sponchiado RM,Wingert NR,Raffin RP,Schapoval EES
    BACKGROUND & AIMS: :Lipid nanoparticles (LNs) are traditional systems able to effectively increase skin hydration. However, due to its reduced viscosity, LNs suspensions are less attractive for skin administration. To overcome this disadvantage, the LN were incorporated in the semi-solid formulation is easy manipulation. This study demonstrated that it is possible to obtain novel LN-loaded fucoxanthin (LN-FUCO) for topical administration containing a combination of bacuri butter and tucumã oil prepared by high shear homogenization for improved stability. The particle size was found to be 243.0 nm and the entrapment efficiency up to 98% of FUCO was incorporated and achieved the suitability of formula. The LN-FUCO hydrogel characteristics of slight acidity, drug content near 100%, and nanometric mean size assure to this formulation high compatibility to dermal application. Photostability assay by UVA, LN-FUCO, and LN-FUCO hydrogel improved photostability and conferred greater protection against FUCO degradation. The results obtained from in vitro skin permeation studies presented a significant difference between LN-FUCO hydrogel and FUCO (p < 0.05), with no detection of the drug in the receptor medium. Therefore, high shear homogenization is demonstrated to be a simple, available, and effective method to prepare high-quality LN-FUCO hydrogel for topical application.
    背景与目标: :脂质纳米颗粒(LNs)是能够有效增加皮肤水分的传统系统。然而,由于其粘度降低,LNs悬浮液对于皮肤给药的吸引力较小。为了克服该缺点,将LN掺入半固体制剂中易于操作。这项研究表明,有可能获得新型的局部装载LN的岩藻黄质(LN-FUCO),其中包含通过高剪切均质化制备的bacuri黄油和tucumã油的组合,以提高稳定性。发现粒径为243.0 nm,并结合了高达98%FUCO的包封率并达到了配方的适用性。 LN-FUCO水凝胶具有弱酸性,药物含量接近100%和纳米平均大小的特性,从而确保了该制剂与皮肤应用的高度相容性。通过UVA,LN-FUCO和LN-FUCO水凝胶进行的光稳定性测定提高了光稳定性,并提供了针对FUCO降解的更大保护。从体外皮肤渗透研究获得的结果表明,LN-FUCO水凝胶和FUCO之间存在显着差异(p <0.05),而在受体介质中未检测到药物。因此,高剪切均质化被证明是制备用于局部应用的高质量LN-FUCO水凝胶的简单,可用和有效的方法。
  • 【冷冻保存的龙胆植物离体芽的冷冻保存:玻璃化和包囊玻璃化方案的比较。】 复制标题 收藏 收藏
    DOI: 复制DOI
    作者列表:Tanaka D,Niino T,Isuzugawa K,Hikage T,Uemura M
    BACKGROUND & AIMS: :Using vitrification and encapsulation-vitrification protocols, we successfully cryopreserved shoot apices from in-vitro plants of different Gentiana cultivars (lines). Although both protocols gave high survival percentages after storage in liquid nitrogen, the encapsulation-vitrification protocol had several distinct advantages over the vitrification protocol: (i) survival was higher under optimal conditions, (ii) the range of optimal exposure periods to the plant vitrification solution 2 (PVS2) was broader, and (iii) regrowth of cryopreserved shoot apices was apparently more vigorous and faster. Shoot apices from ten cultivars/lines of three Gentiana species (G. scabra, G. triflora, and G. pneumonanthe) were successfully cryopreserved using the two protocols with average survival of 49.0 percent and 73.7 percent for vitrification and encapsulation-vitrification, respectively. These results indicate that the two protocols optimized in the present study are promising for cryopreservation of a wide range of Gentiana genetic resources.
    背景与目标: :使用玻璃化和包囊玻璃化方案,我们成功地冷冻了不同龙胆属植物(系)体外植物的芽尖。尽管两种方案在液氮中保存后均具有较高的存活率,但与玻璃化方案相比,封装玻璃化方案具有几个明显的优势:(i)在最佳条件下的存活率更高;(ii)植物玻璃化的最佳暴露时间范围溶液2(PVS2)的范围更广,并且(iii)低温保存的芽尖的再生显然更旺盛且更快。使用这两种方案成功地冷冻保存了三种龙胆属植物(G. scabra,G。triflora和G. pneumonanthe)的十个品种/品系的芽尖,玻璃化和包封玻璃化的平均存活率分别为49.0%和73.7%。这些结果表明,在本研究中优化的两种方案有望用于冷冻保存多种龙胆的遗传资源。
  • 【由聚[(环氧乙烷)-共缩水甘油]与油-水界面处的多个疏水亚油酸酯制备液核纳米胶囊及其its的包封。】 复制标题 收藏 收藏
    DOI:10.1021/bm0701797 复制DOI
    作者列表:Ren Y,Wang G,Huang J
    BACKGROUND & AIMS: :A convenient approach is provided to prepare liquid-core nanocapsules by cross-linking an amphiphilic copolymer at an oil-water interface. The hydrophilic copolymer poly[(ethylene oxide)-co-glycidol] was prepared by anionic polymerization of ethylene oxide and ethoxyethyl glycidyl ether first, then the hydroxyl groups on the backbone were recovered after hydrolysis and partly modified by hydrophobic conjugated linoleic acid. The copolymer with multiple linoleate pendants was absorbed at an oil-water interface and then cross-linked to form stable nanocapsules. The mean diameter of the nanocapsule was below 350 nm, and the size distribution was relatively narrow (<0.2) at low concentrations of oil in acetone (<10 mg/mL). The particle size could be tuned easily by variation of the emulsification conditions. The nanocapsule was stable in water for at least 5 months, and the shell maintained its integrity after removal of the oily core by solvent. Pyrene was encapsulated in these nanocapsules, and a loading efficiency as high as 94% was measured by UV spectroscopy.
    背景与目标: :提供了一种方便的方法,通过在油水界面交联两亲共聚物来制备液核纳米胶囊。首先通过环氧乙烷与乙氧基乙基缩水甘油醚的阴离子聚合反应制备亲水共聚物聚[(环氧乙烷)-共-缩水甘油],然后水解后回收骨架上的羟基,并通过疏水性共轭亚油酸进行部分改性。具有多个亚油酸酯侧基的共聚物在油-水界面处吸收,然后交联形成稳定的纳米胶囊。纳米胶囊的平均直径低于350 nm,并且在丙酮中的油浓度较低(<10 mg / mL)时,尺寸分布相对较窄(<0.2)。通过改变乳化条件,可以容易地调节粒径。纳米胶囊在水中至少稳定5个月,在通过溶剂除去油性核后,壳保持其完整性。 these被包封在这些纳米胶囊中,并且通过UV光谱法测得的负载效率高达94%。
  • 【GRM2细菌微隔室颗粒的包封机制和结构研究。】 复制标题 收藏 收藏
    DOI:10.1038/s41467-019-14205-y 复制DOI
    作者列表:Kalnins G,Cesle EE,Jansons J,Liepins J,Filimonenko A,Tars K
    BACKGROUND & AIMS: :Bacterial microcompartments (BMCs) are prokaryotic organelles consisting of a protein shell and an encapsulated enzymatic core. BMCs are involved in several biochemical processes, such as choline, glycerol and ethanolamine degradation and carbon fixation. Since non-native enzymes can also be encapsulated in BMCs, an improved understanding of BMC shell assembly and encapsulation processes could be useful for synthetic biology applications. Here we report the isolation and recombinant expression of BMC structural genes from the Klebsiella pneumoniae GRM2 locus, the investigation of mechanisms behind encapsulation of the core enzymes, and the characterization of shell particles by cryo-EM. We conclude that the enzymatic core is encapsulated in a hierarchical manner and that the CutC choline lyase may play a secondary role as an adaptor protein. We also present a cryo-EM structure of a pT = 4 quasi-symmetric icosahedral shell particle at 3.3 Å resolution, and demonstrate variability among the minor shell forms.
    背景与目标: :细菌微区室(BMCs)是由蛋白质壳和封装的酶核心组成的原核细胞器。 BMC涉及多个生化过程,例如胆碱,甘油和乙醇胺的降解和碳固定。由于非天然酶也可以封装在BMC中,因此对BMC壳组装和封装过程的更好理解对于合成生物学应用可能是有用的。在这里,我们报道了肺炎克雷伯氏菌GRM2基因座中BMC结构基因的分离和重组表达,核心酶包封背后的机制研究以及冷冻EM对壳颗粒的表征。我们得出的结论是,酶核心以分级方式被封装,并且CutC胆碱裂解酶可能作为衔接蛋白发挥辅助作用。我们还提出了一个低温电磁结构的pT = 4准对称二十面体壳颗粒,分辨率为3.3Å,并证明了次要壳形之间的差异。
  • 【基于电喷雾乳清蛋白的纳米胶囊,用于β-胡萝卜素的包封。】 复制标题 收藏 收藏
    DOI:10.1016/j.foodchem.2019.126157 复制DOI
    作者列表:Rodrigues RM,Ramos PE,Cerqueira MF,Teixeira JA,Vicente AA,Pastrana LM,Pereira RN,Cerqueira MA
    BACKGROUND & AIMS: :In this work an electrohydrodynamic process (electrospray) was used to produce β-carotene loaded nanocapsules based on whey protein isolate (WPI). WPI solutions were prepared in aqueous solutions with different concentrations of ethanol (5, 10 and 15%) which were used for β-carotene solubilization. Different electrospray conditions were tested and the morphology and molecular organization of the nanocapsules were studied on dried and hydrated state. The size of the dried nanocapsules ranged between 227 and 283 nm. After hydration, there was a significant increase in the mean size of the nanocapsules, being the sizes higher for nanocapsules produced with increasing concentrations of ethanol. Results, obtained from the reactivity of free sulfhydryl groups and fluorescence analysis, showed that the increase of ethanol concentration had a destabilizing effect on the protein unfolding. Electrosprayed WPI-based nanocapsules can be used for the encapsulation of β-carotene answering the industrial demand for novel encapsulation technologies to protect sensitive bioactive compounds.
    背景与目标: :在这项工作中,基于乳清蛋白分离物(WPI),使用电动流体动力学过程(电喷雾)制备了负载β-胡萝卜素的纳米胶囊。 WPI溶液是在具有不同浓度乙醇(5%,10%和15%)的水溶液中制备的,用于溶解β-胡萝卜素。测试了不同的电喷雾条件,并研究了纳米胶囊在干燥和水合状态下的形态和分子组织。干燥的纳米胶囊的大小在227至283 nm之间。水合后,纳米胶囊的平均尺寸显着增加,这是随着乙醇浓度增加而生产的纳米胶囊的尺寸更大。从游离巯基的反应性和荧光分析获得的结果表明,乙醇浓度的增加对蛋白质的展开具有去稳定作用。电喷雾的基于WPI的纳米胶囊可用于β-胡萝卜素的封装,从而满足工业上对保护敏感的生物活性化合物的新型封装技术的需求。
  • 【Piceatannol的白蛋白纳米封装通过下调核p65和HIF-1α增强结肠癌的抗癌能力。】 复制标题 收藏 收藏
    DOI:10.3390/cancers12010113 复制DOI
    作者列表:
    BACKGROUND & AIMS: :Piceatannol (PIC) is known to have anticancer activity, which has been attributed to its ability to block the proliferation of cancer cells via suppression of the NF-kB signaling pathway. However, its effect on hypoxia-inducible factor (HIF) is not well known in cancer. In this study, PIC was loaded into bovine serum albumin (BSA) by desolvation method as PIC-BSA nanoparticles (NPs). These PIC-BSA nanoparticles were assessed for in vitro cytotoxicity, migration, invasion, and colony formation studies and levels of p65 and HIF-1α. Our results indicate that PIC-BSA NPs were more effective in downregulating the expression of nuclear p65 and HIF-1α in colon cancer cells as compared to free PIC. We also observed a significant reduction in inflammation induced by chemical colitis in mice by PIC-BSA NPs. Furthermore, a significant reduction in tumor size and number of colon tumors was also observed in the murine model of colitis-associated colorectal cancer, when treated with PIC-BSA NPs as compared to free PIC. The overall results indicate that PIC, when formulated as PIC-BSA NPs, enhances its therpautice potential. Our work could prompt further research in using natural anticancer agents as nanoparticels with possiable human clinical trails. This could lead to the development of a new line of safe and effective therapeutics for cancer patients.
    背景与目标: :哌替卡诺醇(PIC)已知具有抗癌活性,这归因于其通过抑制NF-kB信号通路来阻止癌细胞增殖的能力。然而,其对缺氧诱导因子(HIF)的作用在癌症中尚不为人所知。在这项研究中,通过去溶剂化方法将PIC作为PIC-BSA纳米颗粒(NPs)加载到牛血清白蛋白(BSA)中。评估了这些PIC-BSA纳米粒子的体外细胞毒性,迁移,侵袭和集落形成研究以及p65和HIF-1α的水平。我们的结果表明,与游离PIC相比,PIC-BSA NPs在下调结肠癌细胞中核p65和HIF-1α的表达方面更有效。我们还观察到由PIC-BSA NPs引起的化学性结肠炎在小鼠中引起的炎症显着减少。此外,与游离PIC相比,当用PIC-BSA NPs治疗时,在结肠炎相关大肠癌的鼠模型中,还观察到肿瘤大小和结肠肿瘤数量的显着减少。总体结果表明,当PIC配制成PIC-BSA NP时,可以增强其治疗潜力。我们的工作可能会促使人们进一步研究将天然抗癌药用作可能与人类临床试验结合使用的纳米颗粒。这可能会导致开发出针对癌症患者的安全有效的新疗法系列。
  • 【用于减少中枢神经系统组织封装的神经探针设计。】 复制标题 收藏 收藏
    DOI:10.1016/j.biomaterials.2007.03.024 复制DOI
    作者列表:Seymour JP,Kipke DR
    BACKGROUND & AIMS: :This study investigated relationships between a microscale neural probe's size and shape and its chronic reactive tissue response. Parylene-based probes were microfabricated with a thick shank (48 microm by 68 microm) and an integrated thin lateral platform (5 microm by 100 microm, either solid or one of three lattice sizes). Devices were implanted in rat cerebral cortex for 4 weeks before immunostaining for neurons, astrocytes, microglia, fibronectin, laminin, and neurofilament. While nonneuronal density (NND) generally increased and neuronal density decreased within 75 microm of a probe interface compared to unimplanted control regions, there were significant differential tissue responses within 25 microm of the platform's lateral edge compared to the shank. The NND in this region of the lateral edge was less than one-third of the corresponding region of the shank (129% and 425% increase, respectively). Moreover, neuronal density around the platform lateral edge was about one-third higher than at the shank (0.70 and 0.52 relative to control, respectively). Also, microglia reactivity and extracellular protein deposition was reduced at the lateral edge. There were no significant differences among platform designs. These results suggest that neural probe geometry is an important parameter for reducing chronic tissue encapsulation.
    背景与目标: :这项研究调查了微型神经探针的大小和形状与其慢性反应性组织反应之间的关系。使用厚柄(48微米乘68微米)和集成的薄侧平台(5微米乘100微米,实心或三个晶格大小之一)进行微加工,以聚对二甲苯为基础的探针。在对神经元,星形胶质细胞,小胶质细胞,纤连蛋白,层粘连蛋白和神经丝进行免疫染色之前,将装置植入大鼠大脑皮层4周。尽管与未植入的对照区域相比,非神经密度(NND)通常在探针界面的75微米之内增加而神经元密度降低,但与小腿相比,在平台侧边缘的25微米之内有明显的差异组织反应。在侧边缘的此区域中的NND小于柄的相应区域的三分之一(分别增加129%和425%)。此外,平台侧边缘周围的神经元密度比小腿高约三分之一(相对于对照分别为0.70和0.52)。同样,小胶质细胞反应性和细胞外蛋白质沉积在侧边缘减少。平台设计之间没有显着差异。这些结果表明,神经探针的几何形状是减少慢性组织包膜的重要参数。
  • 【紫杉醇在大分子纳米壳中的包封。】 复制标题 收藏 收藏
    DOI:10.1021/bm070177m 复制DOI
    作者列表:Zahr AS,Pishko MV
    BACKGROUND & AIMS: :An electrostatic layer-by-layer self-assembly technique was used to encapsulate solid core paclitaxel nanoparticles within a polymeric nanometer-scale shell. This approach provides a new strategy for the development of polymeric vehicles that control drug release and target diseased tissues and cells specific to the ailment, such as breast cancer. Core paclitaxel nanoparticles, 153 +/- 28 nm in diameter, were prepared using a modified nanoprecipitation technique. A nanoshell composed of multilayered polyelectrolytes, poly(allylamine hydrochloride) and poly(styrene-4-sulfonate) was assembled stepwise onto core charged drug nanoparticles. In vitro studies were performed to determine the anticancer activity of paclitaxel core-shell nanoparticles. Paclitaxel core-shell nanoparticles induced cell cycle arrest in the G2/M phase after 24 and 48 h of incubation with a human breast carcinoma cell line, MCF-7. Changes in MCF-7 cell morphology, fragmentation of the nucleus, and loss of cell-cell contacts indicated that the cells responded to paclitaxel core nanoparticles upon treatment for 24 and 48 h. Cells arrested in G2/M phase illustrated abnormal microtubule and actin cytoskeleton morphology. The core-shell drug nanoparticles fabricated using this procedure provide a new approach in the delivery of paclitaxel devoid of Cremophor EL, a solvent that causes adverse side effects in patients undergoing chemotherapy for treatment of metastasized mammary cancers.
    背景与目标: :静电逐层自组装技术用于将固体核紫杉醇纳米颗粒包裹在聚合物纳米级壳中。该方法为开发控制药物释放并靶向特定于疾病的患病组织和细胞(例如乳腺癌)的聚合物载体提供了新的策略。使用改良的纳米沉淀技术制备了直径153 /-28 nm的核心紫杉醇纳米颗粒。将由多层聚电解质,聚(烯丙胺盐酸盐)和聚(苯乙烯-4-磺酸盐)组成的纳米壳逐步组装到带核电荷的药物纳米颗粒上。进行了体外研究以确定紫杉醇核-壳纳米颗粒的抗癌活性。与人乳腺癌细胞系MCF-7孵育24和48小时后,紫杉醇核-壳纳米颗粒诱导了G2 / M期的细胞周期停滞。 MCF-7细胞形态的变化,细胞核的碎裂以及细胞与细胞之间的接触损失表明,处理24小时和48小时后,细胞对紫杉醇核心纳米颗粒有反应。在G2 / M期停滞的细胞说明微管和肌动蛋白细胞骨架形态异常。使用该程序制备的核-壳药物纳米颗粒为不含紫杉醇的紫杉醇的递送提供了一种新方法,紫杉醇不含Cremophor EL,该溶剂在接受化疗的转移性乳腺癌患者中引起不良副作用。
  • 【用复合生物聚合物稳定的W / O / W乳剂中葡萄籽富酚提取物的封装:评价其稳定性和释放性。】 复制标题 收藏 收藏
    DOI:10.1016/j.foodchem.2018.07.217 复制DOI
    作者列表:Estévez M,Güell C,De Lamo-Castellví S,Ferrando M
    BACKGROUND & AIMS: :The ability of electrostatic complexes made up of sodium caseinate (NaCAS) and a polysaccharide, carboxymethyl cellulose (CMC) or gum Arabic (GA), to retain polyphenols from grape seed extract when encapsulated in W1/O/W2 emulsions was compared to that of the single NaCAS (1%). Both electrostatic complexes (0.5% NaCAS - 0.375% CMC and 0.5% NaCAS - 0.5%GA at pH 5.6) used as hydrophilic emulsifiers in W1/O/W2 were able to stabilize the O/W2 interface for 14 days, even though their protein content was reduced by a 50% regarding that of the emulsions only stabilized with NaCAS. Moreover, interfacial adsorption did not show significant differences between NaCAS-polysaccharide electrostatic complexes and the single NaCAS. In terms of interfacial barrier properties, the rate of polyphenol release during storage was not affected by the type of hydrophilic emulsifier. Since polyphenol transport in W1/O/W2 emulsions was diffusion controlled, interfacial adsorption was considered the main factor limiting polyphenol retention.
    背景与目标: 相比之下,由酪蛋白酸钠(NaCAS)和多糖,羧甲基纤维素(CMC)或阿拉伯树胶(GA)组成的静电复合物被封装在W1 / O / W2乳液中时,能够保留葡萄籽提取物中的多酚。单个NaCAS的比例(1%)。在W1 / O / W2中用作亲水性乳化剂的两种静电复合物(0.5%NaCAS-0.375%CMC和0.5%NaCAS-0.5%GA)在W1 / O / W2中均能稳定O / W2界面14天,即使它们的蛋白质相对于仅用NaCAS稳定的乳液,其含量降低了50%。而且,界面吸附在NaCAS-多糖静电复合物和单个NaCAS之间没有显示出显着差异。就界面阻隔性能而言,在储存期间多酚的释放速率不受亲水性乳化剂类型的影响。由于多酚在W1 / O / W2乳液中的传输受扩散控制,因此界面吸附被认为是限制多酚保留的主要因素。
  • 【透明质酸/明胶-BCP水凝胶中富含血小板的血浆包封,用于在BCP海绵支架中递送生长因子以进行骨再生。】 复制标题 收藏 收藏
    DOI:10.1177/0885328214551373 复制DOI
    作者列表:Son SR,Sarkar SK,Nguyen-Thuy BL,Padalhin AR,Kim BR,Jung HI,Lee BT
    BACKGROUND & AIMS: :Microporous calcium phosphate based synthetic bone substitutes are used for bone defect healing. Different growth factor loading has been investigated for enhanced bone regeneration. The platelet is a cellular component of blood which naturally contains a pool of necessary growth factors that mediate initiation, continuation, and completion of cellular mechanism of healing. In this work, we have investigated the encapsulation and immobilization of platelet-rich plasma (PRP) with natural polymers like hyaluronic acid (HA) and gelatin (Gel) and loading them in a biphasic calcium phosphate (BCP) scaffold, for a synthetic-allologous hybrid scaffold. Effect of PRP addition in small doses was evaluated for osteogenic potential in vitro and in vivo. BCP (10%) mixed HA-Gel hydrogel with or without PRP, was loaded into a BCP sponge scaffold. We investigated the hydrogel-induced improvement in mechanical property and PRP-mediated enhancement in biocompatibility. In vitro studies for cytotoxicity, cell attachment, and proliferation were carried out using MC3T3-E1 pre-osteoblast cells. In in vitro studies, the cell count, cell proliferation, and cell survival were higher in the scaffold with PRP loading than without PRP. However, in the in vivo studies using a rat model, the PRP scaffold was not superior to the scaffold without PRP. This discrepancy was investigated in terms of the interaction of PRP in the in vivo environment.
    背景与目标: :基于微孔磷酸钙的合成骨替代品可用于骨缺损愈合。已经研究了不同的生长因子负荷以增强骨骼再生。血小板是血液的细胞成分,自然包含一系列必需的生长因子,这些因子介导愈合的细胞机制的启动,持续和完成。在这项工作中,我们研究了透明质酸(HA)和明胶(Gel)等天然聚合物对富含血小板的血浆(PRP)的包封和固定化作用,并将它们装入双相磷酸钙(BCP)支架中,以制备异源杂种支架。评估了小剂量添加PRP的体外和体内成骨潜力。将具有或不具有PRP的BCP(10%)混合HA-Gel水凝胶装入BCP海绵支架中。我们调查了水凝胶诱导的机械性能的改善和PRP介导的生物相容性的增强。在体外研究中,使用MC3T3-E1前成骨细胞进行了细胞毒性,细胞附着和增殖的研究。在体外研究中,装有PRP的支架的细胞计数,细胞增殖和细胞存活率高于没有PRP的支架。但是,在使用大鼠模型的体内研究中,PRP支架并不优于没有PRP的支架。根据体内环境中PRP的相互作用研究了这种差异。
  • 【通过链激酶的脂质体包裹,在心肌梗塞的犬模型中加速溶栓和再灌注。】 复制标题 收藏 收藏
    DOI:10.1161/01.res.66.3.875 复制DOI
    作者列表:Nguyen PD,O'Rear EA,Johnson AE,Patterson E,Whitsett TL,Bhakta R
    BACKGROUND & AIMS: :The aim of thrombolytic therapy for acute myocardial infarction with plasminogen activators such as streptokinase is to lyse the coronary thrombus and reestablish blood flow as quickly as possible so that heart tissue loss is minimized and mortality rates are improved. Streptokinase has been encapsulated in large unilamellar phospholipid vesicles and tested in an animal model of acute myocardial infarction. The time required to restore vessel patency has been reduced more than 50% when compared with findings for free streptokinase. The total dosage of streptokinase required was lower, and smaller remnant thrombi were observed with the encapsulated agent. Results from this initial unoptimized study may have significant implications for further reduction in mortality from heart attacks by therapy with plasminogen activators.
    背景与目标: :使用纤溶酶原激活剂(例如链激酶)对急性心肌梗塞进行溶栓治疗的目的是裂解冠状动脉血栓并尽快恢复血流,从而最大程度地减少心脏组织损失并提高死亡率。链激酶已封装在大的单层磷脂囊泡中,并在急性心肌梗塞的动物模型中进行了测试。与游离链激酶的发现相比,恢复血管通畅所需的时间减少了50%以上。所需要的链激酶的总剂量较低,并且用包囊剂观察到较小的残留血栓。最初未经优化的研究结果可能对通过使用纤溶酶原激活剂治疗进一步降低心脏病发作的死亡率具有重要意义。
  • 【将葡萄籽提取物封装在聚乳酸微囊中,以在牙科材料应用中实现持续的生物活性和时间依赖性释放。】 复制标题 收藏 收藏
    DOI:10.1016/j.dental.2017.03.009 复制DOI
    作者列表:Yourdkhani M,Leme-Kraus AA,Aydin B,Bedran-Russo AK,White SR
    BACKGROUND & AIMS: OBJECTIVE:To sustain the bioactivity of proanthocyanidins-rich plant-derived extracts via encapsulation within biodegradable polymer microcapsules. METHODS:Polylactide microcapsules containing grape seed extract (GSE) were manufactured using a combination of double emulsion and solvent evaporation techniques. Microcapsule morphology, size distribution, and cross-section were examined via scanning electron microscopy. UV-vis measurements were carried out to evaluate the core loading and encapsulation efficiency of microcapsules. The bioactivity of extracts was evaluated after extraction from capsules via solvent partitioning one week or one year post-encapsulation process. Fifteen human molars were cut into 7mm×1.7mm×0.5mm thick mid-coronal dentin beams, demineralized, and treated with either encapsulated GSE, pristine GSE, or left untreated. The elastic modulus of dentin specimens was measured based on three-point bending experiments as an indirect assessment of the bioactivity of grape seed extracts. The effects of the encapsulation process and storage time on the bioactivity of extracts were analyzed. RESULTS:Polynuclear microcapsules with average diameter of 1.38μm and core loading of up to 38wt% were successfully manufactured. There were no statistically significant differences in the mean fold increase of elastic modulus values among the samples treated with encapsulated or pristine GSE (p=0.333), or the storage time (one week versus one year storage at room temperature, p=0.967). SIGNIFICANCE:Polynuclear microcapsules containing proanthocyanidins-rich plant-derived extracts were prepared. The bioactivity of extracts was preserved after microencapsulation.
    背景与目标: 目的:通过包封在可生物降解的聚合物微胶囊中,维持富含原花青素的植物提取物的生物活性。
    方法:采用双重乳化和溶剂蒸发技术相结合的方法,制备了含有葡萄籽提取物(GSE)的聚乳酸微胶囊。通过扫描电子显微镜检查微胶囊的形态,大小分布和横截面。进行UV-vis测量以评估微胶囊的核心负载和包封效率。从胶囊中提取后,通过包封后一周或一年的溶剂分配对提取物的生物活性进行评估。将15颗人类臼齿切成7mm×1.7mm×0.5mm厚的冠状中牙本质横梁,进行脱矿质,然后用​​封装的GSE,原始GSE进行处理,或不进行处理。基于三点弯曲实验测量牙本质样品的弹性模量,作为对葡萄籽提取物生物活性的间接评估。分析了包封过程和保存时间对提取物生物活性的影响。
    结果:成功制备了平均直径为1.38μm,核心负载量高达38wt%的多核微囊。在用胶囊化或原始GSE处理的样品中,弹性模量值的平均倍数增加(p = 0.333)或保存时间(在室温下保存一周与一年,p = 0.967)之间没有统计学上的显着差异。
    意义:制备了富含原花青素的植物提取物的多核微胶囊。微囊化后保留提取物的生物活性。

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