Nanostructured lipid carriers

纳米结构脂质载体
  • 文章类型: Journal Article
    由于在作用部位的可用性有限,目前用于伤口愈合的治疗仍然表现出缺点。易于降解,立即释放药物,所有这些在慢性病中都是有害的。纳米改性策略,提供各种优势,可以增强药物的物理化学性质,已被用于努力使伤口愈合药物的功效最大化。如今,纳米结构脂质载体(NLC)提供药物递送能力,可以保护活性化合物免受环境影响并实现受控释放曲线。因此,NLC被认为是解决伤口治疗中遇到的挑战的替代疗法。本文综述了NLCs在伤口愈合给药中的应用。包括关于他们组成的讨论,制备方法,以及它们对治疗效果的影响。使用相对简单的技术,例如基于压力的过程,可以促进将药物修改到NLC模型中。乳化技术,溶剂利用方法,或相位反转。此外,具有最少材料组成的NLC生产可以适应单一和组合药物递送。通过体外,在体内,和临床研究,已经证实,NLC可以增强各种药物类型在伤口愈合治疗中的治疗潜力。NLC通过减少活性物质颗粒大小来增强功效,增加溶解度和生物利用度,延长药物释放,确保慢性伤口在伤口部位的持续剂量。总之,NLC代表用于在伤口愈合的情况下优化活性药理成分的生物利用度的有效纳米载体系统。
    The current treatments for wound healing still exhibit drawbacks due to limited availability at the action sites, susceptibility to degradation, and immediate drug release, all of which are detrimental in chronic conditions. Nano-modification strategies, offering various advantages that can enhance the physicochemical properties of drugs, have been employed in efforts to maximize the efficacy of wound healing medications. Nowadays, nanostructured lipid carriers (NLCs) provide drug delivery capabilities that can safeguard active compounds from environmental influences and enable controlled release profiles. Consequently, NLCs are considered an alternative therapy to address the challenges encountered in wound treatment. This review delves into the application of NLCs in drug delivery for wound healing, encompassing discussions on their composition, preparation methods, and their impact on treatment effectiveness. The modification of drugs into the NLC model can be facilitated using relatively straightforward technologies such as pressure-based processes, emulsification techniques, solvent utilization methods, or phase inversion. Moreover, NLC production with minimal material compositions can accommodate both single and combination drug delivery. Through in vitro, in vivo, and clinical studies, it has been substantiated that NLCs can enhance the therapeutic potential of various drug types in wound healing treatments. NLCs enhance efficacy by reducing the active substance particle size, increasing solubility and bioavailability, and prolonging drug release, ensuring sustained dosage at the wound site for chronic wounds. In summary, NLCs represent an effective nanocarrier system for optimizing the bioavailability of active pharmacological ingredients in the context of wound healing.
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  • 文章类型: Journal Article
    多形性胶质母细胞瘤(GBM)难以治愈和复发率高的主要原因包括:1.化疗药物难以穿透血脑屏障(BBB)靶向肿瘤细胞;2.神经胶质瘤干细胞(GSC)的存在导致化疗耐药。因此,突破BBB的局限性和克服GSCs引起的耐药性是解决这一问题的主要策略。这项研究提出了我们关于开发乳铁蛋白/CD133抗体缀合的纳米结构脂质载体(Lf/CD133-NLCS)以同时靶向BBB和GSC的结果。替莫唑胺(TMZ)负载的Lf/CD133-NLCS(Lf/CD133-NLCS-TMZ)对恶性神经胶质瘤细胞(U87-MG)和GSCs具有高效的体外抗肿瘤作用,同时证明在浓度低于200μg/mL时对人正常巨噬细胞和L929细胞无明显毒性。体外靶向GBM研究的结果表明,与NLCS-TMZ相比,U87-MG细胞和GSC中Lf/CD133-NLCS-TMZ的细胞摄取明显更高。这表明在Lf/CD133修饰后GBM的主动靶向增强。此外,在体外和体内,与NLCS-TMZ相比,Lf/CD133-NLCS-TMZ的BBB通透性增加。把结果放在一起,Lf/CD133-NLCS-TMZ对BBB和GSCs的双重靶向显示出巨大的潜力,以及基于此策略的GBM治疗。 .
    The main reasons for the difficulty in curing and high recurrence rate of glioblastoma multiforme (GBM) include: 1. The difficulty of chemotherapy drugs in penetrating the blood-brain barrier (BBB) to target tumor cells; 2. The presence of glioma stem cells (GSCs) leading to chemotherapy resistance. Therefore, breaking through the limitations of the BBB and overcoming the drug resistance caused by GSCs are the main strategies to address this problem. This study presents our results on the development of lactoferrin/CD133 antibody conjugated nanostructured lipid carriers (Lf/CD133-NLCS) for simultaneously targeting BBB and GSCs. Temozolomide (TMZ) loaded Lf/CD133-NLCS (Lf/CD133-NLCS-TMZ) exhibited high-efficiency in vitro anti-tumor effects toward malignant glioma cells (U87-MG) and GSCs, while demonstrating no significant toxicity to human normal macrophages and L929 cells at concentrations lower than 200 μg/mL. The results of the in vitro targeting GBM study revealed a notably higher cellular uptake of Lf/CD133-NLCS-TMZ in U87-MG cells and GSCs in comparison to NLCS-TMZ. This suggests that the active targeting of GBM was enhanced following Lf/CD133 modification. In addition, increased BBB permeability were confirmed for Lf/CD133-NLCS-TMZ compared to NLCS-TMZ both in vitro and in vivo. Taking the results together, Lf/CD133-NLCS-TMZ show great potential for dual targeting of BBB and GSCs, as well as GBM therapy based on this strategy. .
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  • 文章类型: Journal Article
    口服药物是最常见和最方便的途径,提供良好的患者依从性,但药物溶解度限制口服应用。塞来昔布,一种不溶性药物,需要连续高剂量口服给药,这可能会增加心血管风险。由药物和脂质辅料制备的纳米结构脂质载体可以有效提高药物的生物利用度,减少药物剂量,降低不良反应的风险。
    在这项研究中,我们制备了透明质酸修饰的塞来昔布纳米结构脂质载体(HA-NLCs),以提高塞来昔布的生物利用度,减少或预防药物不良反应。同时,我们成功构建了一套符合FDA标准的生物样本测试方法来研究HA-NLCs在大鼠体内的药代动力学。
    药代动力学分析证实HA-NLCs显著增强药物吸收,导致AUC0-t比参考制剂(Celebrex®)高1.54倍。此外,与未修饰的纳米结构脂质载体(CXB-NLCs)相比,HA-NLCs可增加药物的保留时间并改善其体内半衰期。
    HA-NLC显著增加塞来昔布的生物利用度。添加透明质酸延长了药物的体内作用持续时间,并降低了与频繁口服塞来昔布相关的心血管不良反应的风险。
    UNASSIGNED: Oral drug administration is the most common and convenient route, offering good patient compliance but drug solubility limits oral applications. Celecoxib, an insoluble drug, requires continuous high-dose oral administration, which may increase cardiovascular risk. The nanostructured lipid carriers prepared from drugs and lipid excipients can effectively improve drug bioavailability, reduce drug dosage, and lower the risk of adverse reactions.
    UNASSIGNED: In this study, we prepared hyaluronic acid-modified celecoxib nanostructured lipid carriers (HA-NLCs) to improve the bioavailability of celecoxib and reduce or prevent adverse drug reactions. Meanwhile, we successfully constructed a set of FDA-compliant biological sample test methods to investigate the pharmacokinetics of HA-NLCs in rats.
    UNASSIGNED: The pharmacokinetic analysis confirmed that HA-NLCs significantly enhanced drug absorption, resulting in an AUC0-t 1.54 times higher than the reference formulation (Celebrex®). Moreover, compared with unmodified nanostructured lipid carriers (CXB-NLCs), HA-NLCs enhance the retention time and improve the drug\'s half-life in vivo.
    UNASSIGNED: HA-NLCs significantly increased the bioavailability of celecoxib. The addition of hyaluronic acid prolonged the drug\'s in vivo duration of action and reduced the risk of cardiovascular adverse effects associated with the frequent administration of oral celecoxib.
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  • 文章类型: Journal Article
    目的:癌症是全球第二大死亡原因,常规疗法受限于明显的副作用。褪黑素(MEL),一种具有抗肿瘤特性的天然化合物,具有不稳定性和低溶解度。为了克服这些问题,将MEL包封到含有玫瑰果油的纳米结构脂质载体(MEL-NLC)中以增强稳定性并增强其抗肿瘤活性。方法:通过实验设计方法对MEL-NLC进行优化,并对其理化性质进行表征。评估了稳定性和生物制药行为,以及对各种癌细胞系的相互作用研究和体外抗肿瘤功效。结果:优化的MEL-NLC表现出理想的物理化学特性,包括小粒径和持续的MEL释放,长期稳定。体外研究表明,MEL-NLC在几种癌细胞系中选择性诱导细胞毒性,同时保留健康细胞。结论:MEL-NLC是一种有希望的癌症替代方案,结合增强的稳定性和靶向抗肿瘤活性,有可能克服常规治疗的局限性。
    尽管目前取得了进展,癌症是全球第二大死因,但是常规疗法有副作用和有限的疗效。自然疗法正在成为合适的替代品,其中,褪黑素是一种众所周知的具有抗肿瘤特性的化合物。然而,它被光降解,降低其治疗活性。为了有效地将褪黑素传递到癌细胞中,它已经被封装在含有玫瑰果油的可生物降解的纳米粒子中,这可能会增强抗肿瘤特性。这些纳米粒子已经过优化,显示小尺寸和高褪黑素封装,药物持续释放,稳定性好。此外,体外研究证明了对几种癌细胞系的抗肿瘤活性,也显示出它们内部的高度内化。此外,使用鸡胚鸡蛋进行的研究,表明纳米粒子是无毒的,从而证实了其有希望的治疗应用。
    Aim: Cancer constitutes the second leading cause of death worldwide, with conventional therapies limited by significant side effects. Melatonin (MEL), a natural compound with antitumoral properties, suffers from instability and low solubility. To overcome these issues, MEL was encapsulated into nanostructured lipid carriers (MEL-NLC) containing rosehip oil to enhance stability and boost its antitumoral activity. Methods: MEL-NLC were optimized by a design of experiments approach and characterized for their physicochemical properties. Stability and biopharmaceutical behavior were assessed, along with interaction studies and in vitro antitumoral efficacy against various cancer cell lines. Results: Optimized MEL-NLC exhibited desirable physicochemical characteristics, including small particle size and sustained MEL release, along with long-term stability. In vitro studies demonstrated that MEL-NLC selectively induced cytotoxicity in several cancer cell lines while sparing healthy cells. Conclusion: MEL-NLC represent a promising alternative for cancer, combining enhanced stability and targeted antitumoral activity, potentially overcoming the limitations of conventional treatments.
    Despite current advances, cancer is the second cause of death worldwide, but conventional therapies have side effects and limited efficacy. Natural therapies are emerging as suitable alternatives and, among them, Melatonin is a well-known compound with antitumoral properties. However, it is degraded by light, decreasing its therapeutical activity. In order to effectively deliver Melatonin into cancer cells, it has been encapsulated into biodegradable nanoparticles containing rosehip oil, which may boost the antitumoral properties. These nanoparticles have been optimized, showing a small size and a high Melatonin encapsulation, sustained drug release and good stability. Furthermore, in vitro studies demonstrated antitumoral activity against several cancer cell lines, also showing a high internalization inside them. Moreover, studies conducted using chicken embryonated eggs, showed that nanoparticles were non-toxic, thus confirming its promising therapeutical applications.
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  • 文章类型: Journal Article
    这篇综述旨在评估纳米材料的潜力,特别是纳米结构脂质载体(NLCs),在缓解与炎症相关疾病相关的挑战方面,特别强调慢性疾病,如关节炎。跨越WebofScience的综合综合评论,PubMed,以及2000年至2023年的其他学术存储库。文章是根据他们对NLC和炎症管理的关注来选择的,利用关键词,如“纳米材料,\"\"靶向给药,“和”关节炎。“排除标准涉及非英语学习或缺乏关于NLC的足够细节的学习。综合数据概述了优点,挑战,以及NLC在解决慢性炎症性疾病方面的前景。这篇综述还探讨了纳米技术的治疗应用,包括靶向药物递送和组织工程,特别关注慢性炎症中复杂的生物反应,通常涉及非甾体抗炎药(NSAIDs)。此外,探索倾向于局部给药方法,以加强对药物浓度的控制,随着脂质纳米粒的回顾,如脂质体和固体脂质纳米颗粒,强调它们在增加药物渗透方面的潜力,同时解决药物负荷不足等挑战。NLC已经成为克服药物输送挑战的有希望的候选人,特别是在关节炎治疗中,重点关注它们在不同脂质组合物中的优势。该综述强调了通过NLC利用在炎症管理方面取得的重大进展,提供对未来研究方向的见解。此外,它有助于纳米医学的不断进步,强调NLC在开发炎症相关疾病的创新治疗方法中的关键作用,特别是关节炎。NLC代表了有效干预的有希望的途径,纳米技术疗法的信号进展。
    This review seeks to assess the potential of nanomaterials, specifically Nano-struc-tured Lipid Carriers (NLCs), in mitigating challenges associated with inflammation-related disorders, with a particular emphasis on chronic ailments like arthritis. A comprehensive lit-erature review spanning Web of Science, PubMed, and other scholarly repositories from 2000 to 2023 is conducted. Articles are selected based on their focus on NLCs and inflammation management, utilizing keywords, such as \"nanomaterials,\" \"targeted drug delivery,\" and \"ar-thritis.\" Exclusion criteria involve non-English studies or those lacking adequate detail on NLCs. Synthesized data provide an overview of the advantages, challenges, and prospects of NLCs in addressing chronic inflammatory disorders. This review also examines the therapeu-tic applications of nanotechnology, including targeted drug delivery and tissue engineering, particularly focusing on the intricate biological responses in chronic inflammation, often in-volving Non-Steroidal Anti-Inflammatory Drugs (NSAIDs). Moreover, the exploration ex-tends to topical delivery methods to enhance control over medication concentration, with a review of lipid nanoparticles, such as liposomes and solid-lipid nanoparticles, highlighting their potential in augmenting drug permeation while addressing challenges like inadequate drug loading. NLCs have emerged as promising candidates for overcoming drug delivery challenges, par-ticularly in arthritis treatment, with a focus on their advantages across diverse lipid composi-tions. The review underscores significant strides in inflammation management through NLC utilization, offering insights into future research directions. Moreover, it contributes to ongoing advancements in nanomedicine, emphasizing the pivotal role of NLCs in developing innovative therapeutic approaches for inflammation-related dis-orders, particularly arthritis. NLCs represent a promising avenue for effective interventions, signaling progress in nanotechnology-enabled therapeutics.
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  • 文章类型: Journal Article
    纳米结构脂质载体(NLC)已成为创新的药物递送系统,与其他基于脂质的载体相比,具有明显的优势,如脂质体和固体脂质纳米颗粒。苯佐卡因(BZC),使用中最古老的局部麻醉剂,通过假胆碱酯酶进行代谢,导致对氨基苯甲酸的形成,与长期使用BZC相关的过敏反应的病原体。为了减轻不良反应和提高生物利用度,BZC封装在NLC内。利用23阶乘设计,包含棕榈酸鲸蜡酯(固体脂质)的制剂,丙二醇单辛酸酯(液体脂质),并系统地制备了以PluronicF68为表面活性剂,随着固体/液体脂质质量比(60:40-80:20%)的变化,总脂质含量(15-25%),和BZC浓度(1-3%)。通过动态光散射对优化的配方进行表征,差示扫描量热法,拉曼成像,X射线衍射,小角度中子散射,纳米裂纹分析,透射电子显微镜(TEM)/低温TEM,提供对纳米颗粒结构和BZC掺入其脂质基质的见解。NLCBZC表现出显著的包封效率(%EE=96%)和在25°C下储存时的1年稳定性。在小鼠中进行的体外动力学研究和体内镇痛试验表明,NLCBZC有效地持续药物释放超过20小时,并将BZC的麻醉效果延长至18小时。因此,我们建议使用NLCBZC来减少苯佐卡因的有效麻醉浓度(从20到3%或更低),从而最大程度地减少局部施用这种麻醉剂后的过敏反应,潜在的,为疼痛管理中BZC给药的新途径铺平了道路。
    Nanostructured lipid carriers (NLC) have emerged as innovative drug delivery systems, offering distinct advantages over other lipid-based carriers, such as liposomes and solid lipid nanoparticles. Benzocaine (BZC), the oldest topical local anesthetic in use, undergoes metabolism by pseudocholinesterase, leading to the formation of p-aminobenzoic acid, a causative agent for allergic reactions associated with prolonged BZC usage. In order to mitigate adverse effects and enhance bioavailability, BZC was encapsulated within NLC. Utilizing a 23 factorial design, formulations comprising cetyl palmitate (solid lipid), propylene glycol monocaprylate (liquid lipid), and Pluronic F68 as surfactants were systematically prepared, with variations in the solid/liquid lipid mass ratios (60:40-80:20%), total lipid contents (15-25%), and BZC concentrations (1-3%). The optimized formulation underwent characterization by dynamic light scattering, differential scanning calorimetry, Raman imaging, X-ray diffraction, small-angle neutron scattering, nanotracking analysis, and transmission electron microscopy (TEM)/cryo-TEM, providing insights into the nanoparticle structure and the incorporation of BZC into its lipid matrix. NLCBZC exhibited a noteworthy encapsulation efficiency (%EE = 96%) and a 1 year stability when stored at 25 °C. In vitro kinetic studies and in vivo antinociceptive tests conducted in mice revealed that NLCBZC effectively sustained drug release for over 20 h and prolonged the anesthetic effect of BZC for up to 18 h. We therefore propose the use of NLCBZC to diminish the effective anesthetic concentration of benzocaine (from 20 to 3% or less), thus minimizing allergic reactions that follow the topical administration of this anesthetic and, potentially, paving the way for new routes of BZC administration in pain management.
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  • 文章类型: Journal Article
    本研究探索了使用纳米结构脂质载体(NLC)的多西他赛(DOC)和厄洛替尼(ERL)的联合给药,与叶酸(FA)缀合以增强其对抗三阴性乳腺癌的协同抗癌功效。NLC是通过热熔均质化-超声分散开发的,并通过使用Plackett-Burman设计和Box-Behnken设计的按设计质量(QbD)方法进行优化。基于最大可取性生成图。球形,观察到zeta电位在-16.4至-14.15mV范围内的纳米尺寸分散体(<200nm)。这些纳米制剂表现出~95%的包封效率和约5%的载药量。稳定性测试表明,NLC在4°C的储存条件下保持稳定6个月。体外释放研究表明持续释放超过24小时,遵循Higuchi和Korsmeyer-Peppas模型的NLC和FANLC,分别。此外,与载药悬浮液相比,体外pH-stat脂解模型的生物可及性增加近5倍.装载DOC-ERL的制剂表现出剂量和时间依赖性的细胞毒性,在MDA-MB-231和4T1细胞中以1:3的摩尔比显示协同作用,组合指数分别为0.35和0.37。与负载DOC-ERL的FANLC的共治疗在各种体外测定中显示出协同抗癌作用。
    This study explored the combined administration of docetaxel (DOC) and erlotinib (ERL) using nanostructured lipid carriers (NLCs), with folic acid (FA) conjugation to enhance their synergistic anticancer efficacy against triple-negative breast cancer. NLCs were developed through hot melt homogenization-ultrasound dispersion, and optimized by a quality-by-design (QbD) approach using Plackett-Burman design and Box-Behnken design. Plots were generated based on maximum desirability. Spherical, nanosized dispersions (<200 nm) with zeta potential ranging from -16.4 to -14.15 mV were observed. These nanoformulations demonstrated ~95% entrapment efficiency with around 5% drug loading. Stability tests revealed that the NLCs remained stable for 6 months under storage conditions at 4 °C. In vitro release studies indicated sustained release over 24 h, following Higuchi and Korsmeyer-Peppas models for NLCs and FA NLCs, respectively. Additionally, an in vitro pH-stat lipolysis model exhibited a nearly fivefold increase in bioaccessibility compared to drug-loaded suspensions. The DOC-ERL-loaded formulations exhibited dose- and time-dependent cytotoxicity, revealing synergism at a 1:3 molar ratio in MDA-MB-231 and 4T1 cells, with combination indices of 0.35 and 0.37, respectively. Co-treatment with DOC-ERL-loaded FA NLCs demonstrated synergistic anticancer effects in various in vitro assays.
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  • 文章类型: Journal Article
    纳米结构脂质载体(NLC)代表了第二代纳米颗粒,提供了许多优于传统的输送系统。这些包括提高稳定性,增强的药物装载能力,和受控释放曲线,使他们成为一个广泛的治疗应用极具吸引力的候选人。它们适用于疏水性药物,如泰国的传统药用植物,如丁香油和α-mangostin。我们研究了载有Alpha-Mangostin和丁香油(NLC-AMCO)的纳米结构脂质载体的物理化学和生物学特性,以鉴定具有最高治疗功效的制剂。颗粒大小,charge,多分散指数,并记录其他特征。使用犬牙龈组织探索实时离体渗透。通过HPLC评估药物持续释放。此外,采用常规方法进行抗菌性能测试。NLC-AMCO可以在高达40°C下储存60天,而颗粒特性没有任何改变。与未包封的对应物相比,牙龈组织渗透和药物持续释放优于未包封的对应物。它在抑制细菌生长方面比测试的抗生素更有效,特别是对来自狗口腔的细菌。因此,这种替代治疗方法为宠物主人提供了成本效益和给药便利,并减少了动物在约束期间的不适.
    Nanostructured lipid carriers (NLC) represent the second generation of nanoparticles, offering numerous advantages over conventional delivery systems. These include improved stability, enhanced drug-loading capacity, and controlled release profiles, making them highly attractive candidates for a wide range of therapeutic applications. Their suitability for hydrophobic drugs like a traditional medicinal plant of Thailand as clove oil and alpha-mangostin. We investigated into nanostructured lipid carriers loaded with Alpha-Mangostin and clove oil (NLC-AMCO) into the physicochemical and biological characteristics to identify the formulation with the highest efficacy for treatment. The particle size, charge, polydispersity index, and other characterizations were recorded. The realtime ex vivo penetration was explored using canine gingival tissue. Drug sustained release was assessed by HPLC. Moreover, the antibacterial properties were tested by conventional methods. The NLC-AMCO can be stored at up to 40 °C for 60 days without any alterations in particle characteristics. Gingival tissue penetration and sustained drug release were superior compared to unencapsulated counterparts. It exhibited greater effectiveness in inhibiting bacterial growth than the antibiotics tested, particularly against bacteria from the oral cavities of dogs. Therefore, this alternative treatment approach offers cost-effectiveness and ease of administration for pet owners and reduces discomfort for the animals during restraint.
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  • 文章类型: Journal Article
    在这项研究中,开发了一种基于功能性纳米结构脂质载体(NLC)的水凝胶来修复受损的表皮皮肤屏障。NLC是通过高能方法制备的,使用摩洛哥坚果油和蜂蜡作为液体和固体脂质,分别,并以生理相关比例加载神经酰胺和胆固醇,作为结构和功能化合物。使用一系列表面活性剂并优化制备条件,获得215.5±0.9nm大小的NLC和-42.7±0.9的负ζ电位,表现出可接受的物理和微生物稳定性。通过差示扫描量热法和X射线粉末衍射进行的固态表征表明,形成了不完善的NLC型晶体。将优化的NLC分散体加载到基于透明质酸钠和黄原胶的凝胶中。获得的凝胶表现出剪切稀化和触变行为,适用于皮肤应用。掺入NLC增强了流变学,粘弹性,和所形成的凝胶的质地性质,同时保持舒适施用和患者依从性所需的合适铺展性。负载NLC的凝胶在体外表现出明显的闭塞效应。它在离体猪耳模型上提供了比无NLC凝胶高2.8倍的皮肤水合水平,显示出修复受损的表皮屏障和积极滋养皮肤的潜力。
    In this study, a functional nanostructured lipid carriers (NLCs)-based hydrogel was developed to repair the damaged epidermal skin barrier. NLCs were prepared via a high-energy approach, using argan oil and beeswax as liquid and solid lipids, respectively, and were loaded with ceramides and cholesterol at a physiologically relevant ratio, acting as structural and functional compounds. Employing a series of surfactants and optimizing the preparation conditions, NLCs of 215.5 ± 0.9 nm in size and a negative zeta potential of -42.7 ± 0.9 were obtained, showing acceptable physical and microbial stability. Solid state characterization by differential scanning calorimetry and X-ray powder diffraction revealed the formation of imperfect crystal NLC-type. The optimized NLC dispersion was loaded into the gel based on sodium hyaluronate and xanthan gum. The gels obtained presented a shear thinning and thixotropic behavior, which is suitable for dermal application. Incorporating NLCs enhanced the rheological, viscoelastic, and textural properties of the gel formed while retaining the suitable spreadability required for comfortable application and patient compliance. The NLC-loaded gel presented a noticeable occlusion effect in vitro. It provided 2.8-fold higher skin hydration levels on the ex vivo porcine ear model than the NLC-free gel, showing a potential to repair the damaged epidermal barrier and nourish the skin actively.
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  • 文章类型: Journal Article
    慢性阻塞性肺疾病(COPD)是一种以气流阻塞为特征的常见肺部疾病,残疾,和高死亡率。厚朴酚(MA),以其抗炎和抗氧化特性而闻名,具有缓解COPD症状的潜力。然而,MA面临诸如水溶性差和生物利用度低的挑战。本文中,使用乳化和溶剂蒸发制备负载MA的纳米结构脂质载体(MA-NLC)。这些载体的粒径为(19.67±0.36)nm,多分散指数为(0.21±0.01),zeta电位为(-5.18±0.69)mV。MA-NLC的细颗粒分数为(68.90±0.07)%,表明最小的肺部刺激和增强的安全性。通过雾化吸入器肺部给药MA-NLC主动靶向病变的肺组织,促进缓慢释放,并克服了与MA相关的低口服吸收和生物利用度的挑战。该制剂延长了MA的停留时间并优化了其在肺组织中的治疗效果。肺部给药后,MA-NLC在COPD模型中有效调节炎症和氧化应激标志物,展示了其作为COPD管理的有前途的治疗平台的潜力。
    Chronic obstructive pulmonary disease (COPD) is a prevalent lung condition characterized by airflow obstruction, disability, and high mortality rates. Magnolol (MA), known for its anti-inflammatory and antioxidant properties, holds the potential for alleviating COPD symptoms. However, MA faces challenges like poor aqueous solubility and low bioavailability. Herein MA-loaded nanostructured lipid carriers (MA-NLC) were prepared using emulsification and solvent evaporation. These carriers exhibited a particle size of (19.67 ± 0.36) nm, a polydispersity index of (0.21 ± 0.01), and a zeta potential of (-5.18 ± 0.69) mV. The fine particle fraction of MA-NLC was (68.90 ± 0.07)%, indicating minimal lung irritation and enhanced safety. Pulmonary delivery of MA-NLC via nebulizer actively targeted the diseased lung tissues, facilitated slow release, and overcame the challenges of low oral absorption and bioavailability associated with MA. This formulation prolonged the residence time of MA and optimized its therapeutic effect in pulmonary tissues. Upon pulmonary administration, MA-NLC effectively regulated inflammatory and oxidative stress markers in COPD models, demonstrating its potential as a promising therapeutic platform for COPD management.
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