liposome

脂质体
  • 文章类型: Journal Article
    皮肤癌构成了一个重要的全球健康问题,需要创新的治疗方法。这篇综述探讨了掺入EA(边缘激活剂)的囊泡纳米制剂克服皮肤癌治疗障碍的潜力。皮肤固有的保护机制,特别是称为角质层和动脉网络的最外层,阻碍药物的渗透。富含磷脂的基于EA的纳米制剂通过增强药物通过皮肤屏障的渗透提供了有希望的解决方案。EAs如Span80、Span20、Tween20和胆酸钠等。,增强囊泡可变形性,影响药物渗透。本文综述了局部应用治疗皮肤癌的药物,强调与常规脂质体相关的挑战以及使用基于EA的纳米制剂克服这些挑战的重要性。此外,它提供了对各种EA特性的见解,批判性见解,临床试验,和专利。该评论还提供了一个简洁的组成概述,制备技术,以及基于EA的纳米制剂如传递体的应用,脂质体,跨丝小体,和用于递送治疗皮肤癌的药物的转niosomes。总的来说,这项审查旨在加速结合EA的配方的开发,这将进一步改善局部药物递送并提高皮肤癌治疗的治疗效果。
    Skin cancer poses a significant global health concern necessitating innovative treatment approaches. This review explores the potential of vesicle nanoformulation incorporating EA (edge activators) to overcome barriers in skin cancer management. The skin\'s inherent protective mechanisms, specifically the outermost layer called the stratum corneum and the network of blood arteries, impede the permeation of drugs. Phospholipid-enriched EA based nanoformulation offer a promising solution by enhancing drug penetration through skin barriers. EAs like Span 80, Span 20, Tween 20, and sodium cholate etc., enhance vesicles deformability, influencing drug permeation. This review discusses topical application of drugs treat skin cancer, highlighting challenges connected with the conventional liposome and the significance of using EA-based nanoformulation in overcoming these challenges. Furthermore, it provides insights into various EA characteristics, critical insights, clinical trials, and patents. The review also offers a concise overview of composition, preparation techniques, and the application of EA-based nanoformulation such as transfersomes, transliposomes, transethosomes, and transniosomes for delivering drugs to treat skin cancer. Overall, this review intends to accelerate the development of formulations that incorporate EA, which would further improve topical drug delivery and enhance therapeutic outcomes in skin cancer treatment.
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  • 文章类型: Journal Article
    目前,化疗联合光动力疗法在肿瘤治疗中取得了满意的疗效。Chloine6(Ce6)是一种光敏剂,具有高效和低暗毒性。同时,榄香烯(ELE)含有高效低毒的抗癌活性成分,能有效穿透肿瘤组织并抑制其恢复和增殖。由于这两种药物的水溶性差,我们制备了ELE/Ce6共负载脂质体(Lipo-ELE/Ce6)以提高其水溶性,从而增强抗肿瘤作用。Lipo-ELE/Ce6的表征表明Lipo-ELE/Ce6具有合适的包封率(EE),颗粒大小,多分散性(PDI),zeta电位,和良好的光控释放性能。体外,Lipo-ELE/Ce6能有效抑制T24细胞的生长并诱导细胞凋亡,更重要的是,体内实验表明Lipo-ELE/Ce6具有显著的抗肿瘤作用,明显优于免费药物。以上结果表明Lipo-ELE/Ce6可以通过光控释放和ROS反应显著增强非肌层浸润性膀胱癌(NMIBC)细胞凋亡的诱导。
    At present, chemotherapy combined with photodynamic therapy is exerting satisfactory therapeutic effects in the treatment of tumors. Chlorin e6 (Ce6) is a photosensitizer with high efficiency and low dark toxicity. At the same time, elemene (ELE) contains high-efficiency and low-toxicity anti-cancer active ingredients, which can effectively penetrate tumor tissue and inhibit its recovery and proliferation. Due to the poor water solubility of these two drugs, we prepared ELE/Ce6 co-loaded liposomes (Lipo-ELE/Ce6) to improve their water solubility, thereby enhancing the anti-tumor effect. The characterization of Lipo-ELE/Ce6 showed that Lipo-ELE/Ce6 had suitable encapsulation efficiency (EE), particle size, polydispersity (PDI), zeta potential, and good photo-controlled release properties. In vitro, Lipo-ELE/Ce6 effectively inhibited the growth of T24 cells and induced apoptosis, and more importantly, in vivo experiments showed that Lipo-ELE/Ce6 had significant anti-tumor effects, which was significantly better than free drugs. The above results suggest that Lipo-ELE/Ce6 can significantly enhance the induction of apoptosis of non-muscle invasive bladder cancer (NMIBC) by light-controlled release and ROS response.
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  • 文章类型: Journal Article
    基因治疗为治疗缺血性疾病提供了一个有希望的途径,然而,其临床疗效受到单一基因疗法的局限性和这种疾病的高氧化应激微环境特征的阻碍。脂质-聚合物杂合载体代表了一种通过利用脂质和聚合物的组合优势来增强基因治疗有效性的新方法。在这项研究中,我们设计了具有定制结构修饰的脂质-聚合物杂化纳米载体,以创建针对基因递送优化的多功能膜融合脂质-核靶向聚合物纳米递送系统(FLNP).我们的结果表明,FLNPs通过膜融合促进有效的细胞摄取和基因转染,溶酶体回避,和核瞄准机制。在封装肝细胞生长因子质粒(pHGF)和过氧化氢酶质粒(pCAT)后,制备HGF/CAT-FLNP,显著增强了C2C12细胞对H2O2诱导的体外损伤的抗性。体内研究进一步表明,HGF/CAT-FLNPs能有效缓解后肢缺血引起的坏疽,恢复电机功能,促进小鼠血液灌注恢复。代谢组学分析表明,FLNPs在基因转染过程中不会引起代谢紊乱。总之,FLNPs代表了多维辅助基因传递的通用平台,显着提高基因传递的效率,并有望使用pHGF和pCAT有效协同治疗下肢缺血。
    Gene therapy offers a promising avenue for treating ischemic diseases, yet its clinical efficacy is hindered by the limitations of single gene therapy and the high oxidative stress microenvironment characteristic of such conditions. Lipid-polymer hybrid vectors represent a novel approach to enhance the effectiveness of gene therapy by harnessing the combined advantages of lipids and polymers. In this study, we engineered lipid-polymer hybrid nanocarriers with tailored structural modifications to create a versatile membrane fusion lipid-nuclear targeted polymer nanodelivery system (FLNPs) optimized for gene delivery. Our results demonstrate that FLNPs facilitate efficient cellular uptake and gene transfection via membrane fusion, lysosome avoidance, and nuclear targeting mechanisms. Upon encapsulating Hepatocyte Growth Factor plasmid (pHGF) and Catalase plasmid (pCAT), HGF/CAT-FLNPs were prepared, which significantly enhanced the resistance of C2C12 cells to H2O2-induced injury in vitro. In vivo studies further revealed that HGF/CAT-FLNPs effectively alleviated hindlimb ischemia-induced gangrene, restored motor function, and promoted blood perfusion recovery in mice. Metabolomics analysis indicated that FLNPs didn\'t induce metabolic disturbances during gene transfection. In conclusion, FLNPs represent a versatile platform for multi-dimensional assisted gene delivery, significantly improving the efficiency of gene delivery and holding promise for effective synergistic treatment of lower limb ischemia using pHGF and pCAT.
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  • 文章类型: Journal Article
    背景:荷叶碱(NUC),从荷叶中提取的天然化合物,已被证明具有抗肥胖作用。然而,NUC作为抗肥胖药物在犬中的开发和应用由于其水溶性差和低生物利用度而受到阻碍。
    目的:为促进NUC相关产品的开发,本研究将NUC制备成脂质体制剂并评价其特性,在狗中的药代动力学,和对高脂肪饮食犬的抗肥胖作用。
    方法:采用乙醇注射法制备NUC脂质体,使用NUC,鸡蛋卵磷脂,和β-谷甾醇为原料。通过粒度分析仪和透析法评价脂质体的特性和体外释放度,分别。通过高效液相色谱(HPLC)方法进行口服NUC-脂质体后狗的药代动力学。此外,我们研究了NUC-脂质体对高脂饮食喂养的肥胖犬的抗肥胖作用.
    结果:NUC脂质体制备成功,EE为(79.31±1.06)%,粒径为(81.25±3.14)nm,zeta电位为(-18.75±0.23)mV,PDI为0.175±0.031。NUC从NUC-脂质体中的体外累积释放速率比NUC慢。NUC-脂质体在狗体内的T1/2和相对生物利用度增加,与NUC相比,CL降低。此外,NUC-脂质体对高脂饮食犬肥胖的预防作用强于NUC。
    结论:NUC脂质体制剂有利于提高其在犬体内的相对生物利用度和抗肥胖作用。
    BACKGROUND: Nuciferine (NUC), a natural compound extracted from lotus leaves, has been proven to have anti-obesity effects. However, the development and application of NUC as an anti-obesity drug in dogs are hindered due to its poor water solubility and low bioavailability.
    OBJECTIVE: To promote the development of NUC-related products for anti-obesity in dogs, this study prepared NUC into a liposome formulation and evaluated its characteristics, pharmacokinetics in dogs, and anti-obesity effects on high-fat diet dogs.
    METHODS: NUC liposomes were prepared by the ethanol injection method, using NUC, egg lecithin, and β-sitosterol as raw materials. The characteristics and release rate in vitro of liposomes were evaluated by particle size analyser and dialysis method, respectively. The pharmacokinetics in dogs after oral administration of NUC-liposomes was carried out by the high-performance liquid chromatography (HPLC) method. Moreover, we investigated the anti-obesity effect of NUC-liposomes on obese dogs fed with a high-fat diet.
    RESULTS: NUC-liposome was successfully prepared, with an EE of (79.31 ± 1.06)%, a particle size of (81.25 ± 3.14) nm, a zeta potential of (-18.75 ± 0.23) mV, and a PDI of 0.175 ± 0.031. The cumulative release rate in vitro of NUC from NUC-liposomes was slower than that of NUC. The T1/2 and relative bioavailability of NUC-liposomes in dogs increased, and CL reduced compared with NUC. In addition, the preventive effect of NUC-liposomes on obesity in high-fat diet dogs is stronger than that of NUC.
    CONCLUSIONS: The liposome formulation of NUC was conducive to improve its relative bioavailability and anti-obesity effect in dogs.
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  • 文章类型: Journal Article
    目的:L-抗坏血酸(维生素C)是一种必需的水溶性维生素,在各种生理功能中起着重要作用,包括免疫健康。维生素C在胃肠道中的稳定性其生物利用度是有限的。本研究旨在研究与标准维生素C相比,脂质体形式的维生素C是否可以增加吸收。
    方法:在随机分组中,双盲,安慰剂对照,跨界时尚,男性19例,女性8例(n=27;36.0±5.1岁,165.0±6.9cm,70.6±7.1kg)摄入单剂量安慰剂(PLA),500毫克维生素C(VITC),和500毫克脂质体维生素C(LV-VITC,LipoVantage®,Specnova,LLC,泰森角,VA,美国)。收集静脉血样0,0.5-,1-,1.5-,2-,3-,4-,6-,8-,12-,和摄入后24小时,并分析血浆和白细胞维生素C浓度。
    结果:与安慰剂相比,VITC和LV-VITC在血浆和白细胞中显示出明显更大的Cmax和AUC0-24(p<0.001)。此外,LV-VITC具有显著较高的Cmax(血浆+27%,白细胞+20%,p<0.001)和AUC0-24(血浆+21%,白细胞+8%,与VITC相比,p<0.001)值。
    结论:维生素C的脂质体制剂增加了血浆和白细胞的吸收。
    背景:临床试验注册-印度(CTRI/2023/04/051789)。
    OBJECTIVE: L-Ascorbic acid (vitamin C) is an essential water-soluble vitamin that plays an important role in various physiological functions, including immune health. The stability of vitamin C in the gastrointestinal tract its bioavailability is limited. This study aimed to investigate if a liposomal form of vitamin C can increase absorption compared to standard vitamin C.
    METHODS: In a randomized, double-blind, placebo-controlled, crossover fashion, 19 males and 8 females (n = 27; 36.0 ± 5.1 years, 165.0 ± 6.9 cm, 70.6 ± 7.1 kg) ingested a single-dose of placebo (PLA), 500 mg vitamin C (VIT C), and 500 mg liposomal vitamin C (LV-VIT C, LipoVantage®, Specnova, LLC, Tyson Corner, VA, USA). Venous blood samples were collected 0, 0.5-, 1-, 1.5-, 2-, 3-, 4-, 6-, 8-, 12-, and 24-hours after ingestion and were analyzed for plasma and leukocyte vitamin C concentration.
    RESULTS: VIT C and LV-VIT C demonstrated significantly greater Cmax and AUC0 - 24 in plasma and in leukocytes compared to placebo (p < 0.001). Additionally, LV-VIT C had significantly higher Cmax (plasma + 27%, leukocytes + 20%, p < 0.001) and AUC0 - 24 (plasma + 21%, leukocytes + 8%, p < 0.001) values as compared to VIT C.
    CONCLUSIONS: Liposomal formulation of vitamin C increases absorption into plasma and leukocytes.
    BACKGROUND: Clinical Trials Registry - India (CTRI/2023/04/051789).
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  • 文章类型: Journal Article
    敷料应该保护伤口,促进愈合,吸收液体,保持水分。细菌纤维素是一种生物聚合物,由于其在多种应用中的高生物相容性而在生物材料中脱颖而出。在敷料领域,它已经作为传统敷料的替代品销售。然而,它缺乏任何内在活动;其中,在感染的伤口中需要抗菌活性。我们通过用1-(5-羧基戊基)吡啶-1-溴化铵改性纤维素来开发阳离子纤维素膜,增强其润湿性(接触角:26.6°)和保水能力(2714.37%)。与未改性的对照相比,该改性的膜有效地保留了苯唑西林。脂质体包封进一步延长苯唑西林释放长达11天。负载苯唑西林的薄膜和脂质体制剂均表现出对金黄色葡萄球菌的抗微生物活性。我们的发现证明了化学修饰的纤维素作为伤口护理中受控阴离子抗生素和/或其制剂递送的平台的潜力。
    Dressings should protect wounds, promote healing, absorb fluids, and maintain moisture. Bacterial cellulose is a biopolymer that stands out in biomaterials due to its high biocompatibility in several applications. In the area of dressings, it is already marketed as an alternative to traditional dressings. However, it lacks any intrinsic activity; among these, the need for antimicrobial activity in infected wounds stands out. We developed a cationic cellulose film by modifying cellulose with 1-(5-carboxypentyl)pyridin-1-ium bromide, enhancing its wettability (contact angle: 26.6°) and water retention capacity (2714.37 %). This modified film effectively retained oxacillin compared to the unmodified control. Liposomal encapsulation further prolonged oxacillin release up to 11 days. Both oxacillin-loaded films and liposomal formulations demonstrated antimicrobial activity against Staphylococcus aureus. Our findings demonstrate the potential of chemically modified cellulose as a platform for controlled anionic antibiotics and/or their formulations delivery in wound care.
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  • 文章类型: Journal Article
    脂质体作为代表性的药物递送载体应用于各种抗癌治疗。然而,脂质体没有自己的靶向特性;因此,给特定组织或细胞的药物递送存在局限性。药物递送中的高靶向性是提高生物利用度和药物功效以及减少副作用的重要因素;最近的研究已经被积极地研究以修饰脂质体的表面以赋予它们特定的功能。在这项研究中,我们研究了一种通过与脂质体表面外泌体融合增强靶向能力的抗癌药物递送系统。我们设计了载有吉西他滨前药的外泌体-脂质体混合纳米颗粒作为胰腺导管腺癌(PDAC)的治疗方法。与外泌体的膜融合由于固有的靶向能力和巨细胞胞吞作用途径的扩展而显示出对胰腺癌细胞的优异靶向能力。
    Liposomes are applied to various anticancer treatments as representative drug delivery carriers. However, liposomes do not have their own targeting properties; therefore, there are limitations in drug delivery to specific tissues or cells. High targetability in drug delivery is an important factor in improving bioavailability and drug efficacy and reducing side effects; recent research has been actively investigated to modify the surface of liposomes to give them specific functions. In this study, we studied a drug delivery system for anticancer treatment that enhances targeting ability through fusion with exosomes on the surface of liposomes. We designed exosome-liposome hybrid nanoparticles loaded with a gemcitabine prodrug as a treatment for pancreatic ductal adenocarcinoma (PDAC). Membrane fusion with exosomes shows excellent targeting ability to pancreatic cancer cells due to intrinsic targeting ability and expansion of the macropinocytosis pathway.
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  • 文章类型: Journal Article
    脓肿分枝杆菌(Mab)是一种机会性非结核分枝杆菌,可导致易感患者难以治疗的肺部感染。例如患有囊性纤维化(CF)的患者,它是发病率和死亡率的主要原因。此外,由于该物种表现出的内在广泛的抗菌素耐药谱以及一些可用抗生素的副作用,此类感染的治疗管理仍然极其困难。在本研究中,我们表明,磷脂酰丝氨酸脂质体(PS-L)增强细胞内分枝杆菌杀死单克隆抗体感染的人巨噬细胞与功能或药理学抑制囊性纤维化电导调节因子(CFTR),通过涉及吞噬体酸化和活性氧(ROS)产生的机制。此外,PS-L在NF-kB激活和TNF-α产生方面显着降低Mab感染的巨噬细胞的促炎反应,与CFTR抑制无关。总之,这些结果证明了PS-L作为治疗难以治疗的单克隆抗体感染的治疗策略的可能未来发展的概念。
    Mycobacterium abscessus (Mab) is an opportunistic nontuberculous mycobacterium responsible of difficult-to-treat pulmonary infections in vulnerable patients, such as those suffering from Cystic Fibrosis (CF), where it represents a major cause of morbidity and mortality. Additionally, due to the intrinsic extensive antimicrobial resistance spectrum displayed by this species and the side effects reported for some available antibiotics, the therapeutic management of such infections remains extremely difficult. In the present study, we show that phosphatidylserine liposomes (PS-L) enhance intracellular mycobacterial killing of Mab infected human macrophages with functional or pharmacologically inhibited cystic fibrosis conductance regulator (CFTR), by a mechanism involving phagosome acidification and reactive oxygen species (ROS) production. Additionally, PS-L significantly reduce proinflammatory response of Mab infected macrophages in terms of NF-kB activation and TNF-α production, irrespective of CFTR inhibition. Altogether, these results represent the proof of concept for a possible future development of PS-L as a therapeutic strategy against difficult-to-treat Mab infection.
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  • 文章类型: Journal Article
    微米和纳米封装技术,如微流化,喷雾干燥,和离心挤压,已广泛应用于各个行业,包括药品,食物,化妆品,农业,为了提高稳定性,保质期,和活性成分的生物利用度,例如维生素A。基于乳液的递送平台为保护提供了可行和适当的替代方案,封装,和运输生物活性化合物。因此,有必要丰富我们的基本饮食,以防止人群中的维生素A缺乏症。这篇综述的重点是解决维生素A短缺的问题,用于改善重要维生素A的递送及其食品应用的封装技术。此外,需要更多的研究来保证纳米递送策略的安全性,随着它们在食品和饮料行业的扩散。
    Micro- and nano-encapsulation techniques, such as microfluidization, spray drying, and centrifugal extrusion, have been widely utilized in various industries, including pharmaceuticals, food, cosmetics, and agriculture, to improve the stability, shelf life, and bioavailability of active ingredients, such as vitamin A. Emulsion-based delivery platforms offer feasible and appropriate alternatives for safeguarding, encapsulating, and transporting bioactive compounds. Therefore, there is a need to enrich our basic diet to prevent vitamin A deficiency within a population. This review focused on addressing vitamin A shortages, encapsulation techniques for improving the delivery of vital vitamins A and their food applications. Additionally, more studies are required to guarantee the security of nano-delivery strategies, as they proliferate in the food and beverage sector.
    UNASSIGNED:
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  • 文章类型: Journal Article
    硼中子俘获疗法(BNCT)有望成为一种有前途的下一代癌症治疗方法。2020年,日本这导致了对这种治疗方式的研究,是世界上第一个批准BNCT的国家。已在BNCT中临床应用的硼试剂包括笼状硼化合物(巯基十一氢十二硼酸酯:BSH)和含硼氨基酸(对硼苯丙氨酸:BPA)。特别是,BPA制剂Steboronine®是BNCT唯一批准的药物。然而,BPA的问题是它在肿瘤中的保留率很低,并且在水中的溶解度非常低。对于BNCT来说,这一点不容忽视,这需要肿瘤中大量的硼。高剂量体积,伴随着低肿瘤保留,导致治疗效果降低和患者身体负担增加。在BSH的情况下,它对肿瘤的渗透不足是有问题的。基于药物输送系统(DDS)技术,我们开发了优于Steboronine®的下一代硼药物。我们的方法涉及使用创新的离子液体配方技术重新开发BPA。这里,我们描述了以前的硼试剂,并介绍了我们最近在开发硼化合物方面的努力。
    Boron neutron capture therapy (BNCT) is expected to be a promising next-generation cancer treatment. In 2020, Japan, which has led the research on this treatment modality, was the first country in the world to approve BNCT. The boron agents that have been clinically applied in BNCT include a caged boron compound (mercaptoundecahydrododecaborate: BSH) and a boron-containing amino acid (p-boronophenylalanine: BPA). In particular, the BPA preparation Steboronine® is the only approved drug for BNCT. However, the problem with BPA is that it is poorly retained in the tumor and has very low solubility in water. This cannot be overlooked for BNCT, which requires large amounts of boron in the tumor. The high dosage volume, together with low tumor retention, leads to reduced therapeutic efficacy and increased physical burden on the patient. In the case of BSH, its insufficient penetration into the tumor is problematic. Based on drug delivery system (DDS) technology, we have developed a next-generation boron pharmaceutical superior to Steboronine®. Our approach involves the redevelopment of BPA using innovative ionic liquid formulation technology. Here, we describe previous boron agents and introduce our recent efforts in the development of boron compounds.
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