• 【海藻酸盐/乳糖修饰的壳聚糖水凝胶:用于软骨细胞封装的生物活性生物材料。】 复制标题 收藏 收藏
    DOI:10.1002/jbm.a.31307 复制DOI
    作者列表:Marsich E,Borgogna M,Donati I,Mozetic P,Strand BL,Salvador SG,Vittur F,Paoletti S
    BACKGROUND & AIMS: :A new bioactive scaffold was prepared from a binary polysaccharide mixture composed of a polyanion (alginate) and a polycation (a lactose-modified chitosan, chitlac). Its potential use for articular chondrocytes encapsulation and cartilage reconstructive surgery applications has been studied. The hydrogel combines the ability of alginate to act as a 3D supporting structure with the capability of the second component (chitlac) to provide interactions with porcine articular chondrocytes. Physico-chemical characterization of the scaffold was accomplished by gel kinetics and compression measurements and demonstrated that alginate-chitlac mixture (AC-mixture) hydrogels exhibit better mechanical properties when compared with sole alginate hydrogels. Furthermore, biochemical and biological studies showed that these 3D scaffolds are able to maintain chondrocyte phenotype and particularly to significantly stimulate and promote chondrocyte growth and proliferation. In conclusion, the present study can be considered as a first step towards an engineered, biologically active scaffold for chondrocyte in vitro cultivation, expansion, and cell delivery.
    背景与目标: :一种新的生物活性支架是由由聚阴离子(藻酸盐)和聚阳离子(乳糖修饰的壳聚糖,Chitlac)组成的二元多糖混合物制备的。研究了其在关节软骨细胞封装和软骨重建手术中的潜在用途。水凝胶将藻酸盐充当3D支持结构的能力与第二组分(chitlac)提供与猪关节软骨细胞相互作用的能力相结合。支架的理化特性通过凝胶动力学和压缩测量完成,并证明与单独的藻酸盐水凝胶相比,藻酸盐-壳聚糖混合物(AC混合物)水凝胶具有更好的机械性能。此外,生化和生物学研究表明,这些3D支架能够维持软骨细胞表型,特别是显着刺激和促进软骨细胞的生长和增殖。总之,本研究可被视为迈向工程化,具有生物学活性的软骨细胞体外培养,扩增和细胞递送支架的第一步。
  • 【基于泊洛沙姆的依托泊苷可注射热敏性水凝胶的高包封效率。】 复制标题 收藏 收藏
    DOI:10.3109/10837450.2013.819014 复制DOI
    作者列表:Soni G,Yadav KS
    BACKGROUND & AIMS: CONTEXT:Hydrogels are promising polymeric network capable of sustaining the release of drug but have a major limitation for encapsulation of hydrophobic drugs. OBJECTIVE:This study was undertaken to encapsulate etoposide in poloxamer 407-based thermosensitive hydrogels with an aim to sustain its release. MATERIALS AND METHODS:Etoposide-loaded hydrogels were prepared by the cold method and optimized for encapsulation efficiency (EE) by a 3(2) factorial design. Poloxamer 407-poloxamer 188 hydrogel (E-P407-P188) and poloxamer 407-poly(ethylene glycol) (E-P407-PEG) hydrogel were characterized for SEM, swelling, sol-gel phase transition and injectability study. RESULTS AND DISCUSSION:In E-P407-P188 hydrogel the EE of 75% could be obtained and in E-P407-PEG hydrogels the EE was 84%. The SEM images showed a porous structure. The release of ETO was sustained up to 48 h by E-P407-PEG hydrogel and 24 h by E-P407-P188 hydrogel. The drug release was governed by first-order kinetics and followed Fickian diffusion mechanism in both the cases. CONCLUSION:Such injectable thermosensitive hydrogel of etoposide could be effectively used for continuous release of drug to the tumor and surrounding tissues.
    背景与目标: 背景:水凝胶是一种有前途的聚合物网络,能够维持药物的释放,但对疏水性药物的封装有主要限制。
    目的:本研究旨在将依托泊苷包封在基于泊洛沙姆407的热敏水凝胶中,以维持其释放。
    材料与方法:依托泊苷负载的水凝胶通过冷法制备,并通过3(2)析因设计优化了包封效率(EE)。表征了泊洛沙姆407-泊洛沙姆188水凝胶(E-P407-P188)和泊洛沙姆407-聚乙二醇(E-P407-PEG)水凝胶的SEM,溶胀,溶胶-凝胶相变和可注射性研究。
    结果与讨论:在E-P407-P188水凝胶中,EE可达到75%;在E-P407-PEG水凝胶中,EE可达到84%。 SEM图像显示出多孔结构。 E-P407-PEG水凝胶将ETO的释放持续至48 h,E-P407-P188水凝胶将ETO的释放持续至24 h。在这两种情况下,药物的释放均由一阶动力学控制,并遵循菲克扩散机制。
    结论:这种可注射的依托泊苷热敏性水凝胶可有效地将药物连续释放至肿瘤和周围组织。
  • 【芝麻酚在磷脂酰胆碱胶束中的包裹:增强的生物利用度和抗炎活性。】 复制标题 收藏 收藏
    DOI:10.1016/j.foodchem.2017.02.002 复制DOI
    作者列表:Yashaswini PS,Kurrey NK,Singh SA
    BACKGROUND & AIMS: :Sesamol, the phenolic degradation product of sesamolin, although recognised for its anti-inflammatory effects, has low bioavailability. In this manuscript, we attempted to improve its bioavailability by encapsulation in mixed phosphatidylcholine micelles. Sesamol could be solubilised and entrapped in phosphatidylcholine mixed micelles (PCS) with 96.8% efficiency (particle size 3.0±0.06nm). Fluorescence spectra of PCS revealed lower relative fluorescence intensity (RFI 112) compared to 'free' sesamol (FS) (RFI 271). The bioaccessibility, transport across a monolayer of cells and cellular uptake of PCS was 8.58%, 1.5-fold and 1.2-fold better, respectively, compared to FS. The anti-inflammatory effects of FS and PCS were compared using LPS treated RAW 264.7 cell line and lipoxygenase inhibition. PCS effected downregulation of iNOS protein expression (27%), NO production (20%), ROS (32%) and lipoxygenase inhibition (IC50=31.24μM) compared to FS.
    背景与目标: :芝麻素酚,芝麻素酚的酚类降解产物,尽管其具有抗炎作用,但其生物利用度较低。在本手稿中,我们试图通过封装在混合的磷脂酰胆碱胶束中来提高其生物利用度。芝麻酚可以以96.8%的效率(粒径3.0±0.06nm)溶解并截留在磷脂酰胆碱混合胶束(PCS)中。与“游离”芝麻酚(FS)(RFI 271)相比,PCS的荧光光谱显示较低的相对荧光强度(RFI 112)。与FS相比,其生物可及性,单层细胞转运和PCS的细胞吸收分别好8.58%,1.5倍和1.2倍。使用LPS处理的RAW 264.7细胞系和脂氧合酶抑制作用比较了FS和PCS的抗炎作用。与FS相比,PCS对iNOS蛋白表达(27%),NO产生(20%),ROS(32%)和脂氧合酶抑制(IC50 =31.24μM)的下调。
  • 【通过封装对治疗性细胞移植的免疫保护。】 复制标题 收藏 收藏
    DOI:10.1016/0167-7799(96)10020-2 复制DOI
    作者列表:Morris PJ
    BACKGROUND & AIMS: The inflammatory response to an allogeneic or xenogeneic tissue transplant by the recipient is complex and includes both the specific immune response, and the non-specific response resulting from damage during implantation, ischaemic reperfusion injury and partial necrosis of the transplanted tissue. Transplantation of allogeneic or xenogeneic tissue within a biomembrane requires that the biomembrane be biologically inert, and that the mean pore size is adequate to allow the passage of oxygen and nutrition of the enclosed tissues, egress of the desired hormone or growth factor, while protecting the enclosed tissue from both the specific and non-specific responses of the host.

    背景与目标: 受者对同种异体或异种组织移植的炎性反应是复杂的,既包括特异性免疫反应,又包括植入过程中的损伤,缺血再灌注损伤和移植组织的部分坏死所引起的非特异性反应。将异基因或异种组织移植到生物膜中需要生物膜具有生物惰性,并且平均孔径要足以允许氧气和封闭组织的营养通过,所需激素或生长因子的流出,同时保护细胞膜。从宿主的特异性和非特异性反应中封闭组织。

  • 【离子和酶可交联的藻酸盐-酪胺共轭物均用作细胞包封的材料。】 复制标题 收藏 收藏
    DOI:10.1002/jbm.a.31299 复制DOI
    作者列表:Sakai S,Kawakami K
    BACKGROUND & AIMS: :The swelling behavior of the structural material of cell-enclosing capsules is a key factor for the successful transplantation of these capsules in the treatment of diseases. The present study aimed to develop cell-enclosing capsules displaying minimal swelling under physiological conditions. We investigated the use of an alginate-tyramine conjugate synthesized by a carbodiimide/active-ester coupling reaction. The conjugate gel crosslinked by calcium ions and peroxidase-catalyzed oxidative coupling of phenols swelled less in saline than in unmodified alginate. The degree of swelling could be controlled by conjugate preparation conditions. The conjugate gel showed no obvious cytotoxicity for cells, including the process of oxidative coupling generation. Further, encapsulated cells could be cultured for up to 2 months and achieve approximately 5.2-fold greater mitochondrial activity after 51 days of encapsulation than after 1 day. These results show that this alginate-tyramine conjugate is a promising material for use in cell-enclosing capsules for cell therapy.
    背景与目标: :封闭细胞的胶囊的结构材料的溶胀行为是这些胶囊在疾病治疗中成功移植的关键因素。本研究旨在开发在生理条件下显示最小溶胀的封闭细胞的胶囊。我们研究了通过碳二亚胺/活性酯偶联反应合成的藻酸盐-酪胺共轭物的使用。通过钙离子交联的共轭凝胶和过氧化物酶催化的酚氧化偶联在盐水中的溶胀少于未改性藻酸盐中的溶胀。溶胀度可以通过结合物的制备条件来控制。共轭凝胶对细胞没有明显的细胞毒性,包括氧化偶合过程。此外,被包封的细胞可以培养长达2个月,并且在包封51天后的线粒体活性比在1天后提高约5.2倍。这些结果表明,该藻酸盐-酪胺结合物是用于细胞治疗细胞的封闭胶囊中的有前途的材料。
  • 【蓝细菌的硅胶溶胶-凝胶封装:学术和应用研究的课程。】 复制标题 收藏 收藏
    DOI:10.1007/s00253-012-4686-8 复制DOI
    作者列表:Dickson DJ,Ely RL
    BACKGROUND & AIMS: :Cyanobacteria inhabit nearly every ecosystem on earth, play a vital role in nutrient cycling, and are useful as model organisms for fundamental research in photosynthesis and carbon and nitrogen fixation. In addition, they are important for several established biotechnologies for producing food additives, nutritional and pharmaceutical compounds, and pigments, as well as emerging biotechnologies for biofuels and other products. Encapsulation of living cyanobacteria into a porous silica gel matrix is a recent approach that may dramatically improve the efficiency of certain production processes by retaining the biomass within the reactor and modifying cellular metabolism in helpful ways. Although encapsulation has been explored empirically in the last two decades for a variety of cell types, many challenges remain to achieving optimal encapsulation of cyanobacteria in silica gel. Recent evidence with Synechocystis sp. PCC 6803, for example, suggests that several unknown or uncharacterized proteins are dramatically upregulated as a result of encapsulation. Also, additives commonly used to ease stresses of encapsulating living cells, such as glycerol, have detrimental impacts on photosynthesis in cyanobacteria. This mini-review is intended to address the current status of research on silica sol-gel encapsulation of cyanobacteria and research areas that may further the development of this approach for biotechnology applications.
    背景与目标: :蓝藻几乎生活在地球上的每个生态系统中,在养分循环中起着至关重要的作用,并且可以作为模型生物用于光合作用和碳氮固定的基础研究。此外,它们对于生产食品添加剂,营养和药物化合物以及色素的几种已确立的生物技术以及用于生物燃料和其他产品的新兴生物技术也很重要。将活性蓝细菌封装到多孔硅胶基质中是一种最近的方法,该方法可以通过将生物质保留在反应器中并以有用的方式修饰细胞代谢来显着提高某些生产过程的效率。尽管在过去的二十年中对各种细胞类型进行了封装研究,但是在硅胶中实现蓝细菌的最佳封装仍然存在许多挑战。最近的证据与集胞藻。例如,PCC 6803建议,由于封装,几种未知或未表征的蛋白质会显着上调。而且,通常用于减轻封装活细胞的压力的添加剂,例如甘油,对蓝细菌的光合作用具有有害影响。这份小型综述旨在解决蓝藻细菌二氧化硅溶胶-凝胶封装的研究现状以及可能会进一步发展该方法用于生物技术应用的研究领域。
  • 【将酪蛋白酸中的阿魏酸乙酯包封以抑制UHT奶中异味的形成。】 复制标题 收藏 收藏
    DOI:10.1016/j.foodchem.2017.05.140 复制DOI
    作者列表:Guan Y,Zhong Q
    BACKGROUND & AIMS: :Phenolic compounds can principally suppress the off-flavor development in ultrahigh temperature (UHT) treated milk, but little has been studied for lipophilic phenolic compounds that are to be encapsulated for even distribution in milk. The objective of this work was to study physicochemical properties of ferulic acid ethyl ester (FAEE) encapsulated in sodium caseinate and the inhibition of volatile formation after UHT processing. The capsules had an average hydrodynamic diameter of 246.2±10.9nm, a polydispersity index of 0.26±0.01, and a zeta-potential of -31.72±0.74mV. The capsules and the encapsulated FAEE were stable after heating at 138°C for 16min and UV radiation at 365nm for 32h. The encapsulated FAEE at a level of 0.18-1.42mg/mL suppressed the formation of 2-acetyl-2-thiazoline in model UHT milk by 32.8-63.2% after 30-day storage at 30°C. Therefore, FAEE encapsulated in caseinate can be potentially used to improve the quality of UHT milk.
    背景与目标: :酚类化合物主要可抑制超高温(UHT)处理的牛奶中异味的产生,但对于将其封装以均匀分布在牛奶中的亲脂性酚类化合物的研究很少。这项工作的目的是研究酪蛋白酸钠中包裹的阿魏酸乙酯(FAEE)的理化性质以及超高温处理后对挥发物形成的抑制作用。所述胶囊的平均流体力学直径为246.2±10.9nm,多分散指数为0.26±0.01,并且ζ电位为-31.72±0.74mV。胶囊和封装的FAEE在138°C加热16分钟并在365nm的UV辐射下32h后是稳定的。在30°C下储存30天后,FAEE封装的0.18-1.42mg / mL的水平可将UHT牛奶中2-乙酰基-2-噻唑啉的形成抑制32.8-63.2%。因此,封装在酪蛋白酸盐中的FAEE可以潜在地用于提高UHT牛奶的质量。
  • 【脂质中的羟丙基-β-环糊精中的药物S /胆固醇脂质体:香精油成分的特性对其封装和释放的影响。】 复制标题 收藏 收藏
    DOI:10.1016/j.ijpharm.2020.119151 复制DOI
    作者列表:Hammoud Z,Gharib R,Fourmentin S,Elaissari A,Greige-Gerges H
    BACKGROUND & AIMS: :Drug-in-cyclodextrin-in-liposome (DCL) represents a very promising approach for preserving essential oil (EO) components, thereby extending their shelf life and activity. In this study, we examined the effect of chemical structure, octanol/water partition coefficient (log P), and Henry's law constant (Hc) on the encapsulation and the release of monoterpenes (eucalyptol, pulegone, terpineol, and thymol) and phenylpropenes (estragole and isoeugenol) from DCLs. Hydroxypropyl-β-cyclodextrin/EO component (HP-β-CD/EO component) inclusion complexes were prepared in aqueous solution and loaded into liposomes by the ethanol injection method. The phospholipid:cholesterol:EO component molar ratio determined for DCL structures was affected by characteristics of EO components. The presence of a propenyl tail or a hydroxyl group in the structure of EO component may improve its loading into DCLs. Furthermore, low encapsulation efficiency (EE) was obtained for DCLs exhibiting high cholesterol membrane content. In addition, a positive linear relationship was found between the loading ratio of monoterpenes into DCLs and their hydrophobic character expressed as log P. The release of components from DCLs was influenced by their EE into the formulations. Finally, DCL formulations retain considerable amounts of EO components after 10 months.
    背景与目标: :脂质环糊精中的药物(DCL)代表了一种非常有希望的方法来保存精油(EO)成分,从而延长了它们的保质期和活性。在这项研究中,我们研究了化学结构,辛醇/水分配系数(log P)和亨利定律常数(Hc)对单萜类化合物(桉油醇,普来高通,松油醇和百里酚)和苯丙烯(雌二醇和异丁香酚)。在水溶液中制备羟丙基-β-环糊精/ EO组分(HP-β-CD/ EO组分)包合物,并通过乙醇注射法将其加载到脂质体中。对于DCL结构确定的磷脂:胆固醇:EO组分的摩尔比受EO组分的特性影响。 EO组分结构中丙烯基尾巴或羟基的存在可以改善其装入DCL的能力。此外,对于表现出高胆固醇膜含量的DCL,获得了低封装效率(EE)。另外,在单萜类到DCL中的负载率和它们的疏水特性表示为log P之间发现正线性关系。从DCL中释放组分受其EE对制剂的影响。最后,DCL制剂在10个月后保留了大量的EO成分。
  • 【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。

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