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Application of modern analytical techniques in the analysis of complex matrices of natural origin on the example of honeybee venom 现代分析技术在复杂天然基质分析中的应用——以蜂毒为例
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-06-29 DOI: 10.32383/appdr/161914
Eliza Matuszewska, Agnieszka Klupczyńska-Gabryszak, Szymon Plewa, Natalia Rzetecka, Kacper Packi, H. Mohd, B. Michniak-Kohn, J. Matysiak
Honeybee venom (HBV) is a product of natural origin with an extremely complex composition. It exhibits several beneficial pharmacological properties, for example anti-inflammatory, antimicrobial, antidiabetic, anti-arthritic, and anti-tumour activities. On the other hand, HBV contains highly allergenic components, including melittin, which makes up more than 50% of its dry weight. Despite many studies conducted, HBV's components and mechanism of action are not yet fully known and understood. Therefore, to enhance the safety of its therapeutical applications, it is essential to establish HBV's composition and biological properties. Many analytical techniques and methods have been reported as potentially useful for the determination of new HBV constituents. Studies focus mainly on the analyses of the HBV proteome and metabolome. Also, properties of its components when applied to the skin, as well as its allergenicity, are being studied. Currently, the most commonly used methods for HBV analysis include high-performance liquid chromatography and mass spectrometry. Choosing the correct and most applicable method for HBV analysis is of great importance in order to obtain in-depth results crucial for the understanding of its mechanism of biological action. The diversity of chemical compounds in HBV also entails an appropriate sample preparation at the pre-analytical stage. In order to summarise the latest knowledge on techniques for the analysis of complex natural products, on the example of HBV, this review paper discusses the modern analytical tools of HBV characterisation, focusing on metabolomic and proteomic studies, topical applications, investigation of venom allergies, and the prospects for future research.
蜂毒(HBV)是一种天然产物,其成分极其复杂。它具有多种有益的药理特性,例如抗炎、抗菌、抗糖尿病、抗关节炎和抗肿瘤活性。另一方面,HBV含有高致敏成分,包括蜂毒肽,它占其干重的50%以上。尽管进行了许多研究,但HBV的成分和作用机制尚不完全清楚。因此,为了提高其治疗应用的安全性,有必要确定HBV的组成和生物学特性。据报道,许多分析技术和方法有可能用于测定新的HBV成分。研究主要集中在HBV蛋白质组和代谢组的分析上。此外,正在研究其成分在皮肤上的特性以及致敏性。目前,最常用的HBV分析方法包括高效液相色谱法和质谱法。选择正确和最适用的HBV分析方法对于获得深入的结果至关重要,这对于理解其生物学作用机制至关重要。HBV中化合物的多样性也需要在分析前阶段进行适当的样品制备。为了总结复杂天然产物分析技术的最新知识,以HBV为例,本文讨论了HBV特征的现代分析工具,重点是代谢组学和蛋白质组学研究、局部应用、毒液过敏的研究以及未来研究的前景。
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引用次数: 0
Participation of quetiapine in oxidative stress and inflammation status in the treatment of drug overdose 喹硫平在药物过量治疗中氧化应激和炎症状态的参与
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-06-29 DOI: 10.32383/appdr/165999
Karina Sommerfeld-Klatta, Magdalena Łukasik-Głębocka, E. Krawczak, Anna Stodolska, B. Zielińska-Psuja
Quetiapine (QT) belongs to the second generation of antipsychotics. It is mostly used to treat depression, bipolar disorder, and schizophrenia. During biotransformation via myeloperoxidase (MPO) QT is oxidized to quinoneimine and a reactive radical, which may contribute to the development of oxidative stress during intoxication. The coexisting inflammation may also significantly contribute to the disturbances in the course of QT poisoning. In this study, twenty-one patients poisoned with quetiapine were examined. The study aimed to assess the correlation between blood QT concentration and selected oxidative stress as well as inflammation biomarkers, such as MPO and C-reactive protein (CRP) levels in the serum of poisoned patients. The obtained results were related to the values of the control group consisting of 21 healthy people, untreated and not poisoned with the drug. In patients with a toxic QT concentration in the blood (3.15 ± 2.11 μg/mL), the activity of MPO and CRP serum level were significantly higher in comparison to the control group. The mean level of CRP in the study group was 76.74 mg/L, while in the control group only 1.86 mg/L. The increase in MPO activity and CRP blood level in patients after QT overdose may confirm the hypothesis of oxidative disorders arising during its biotransformation and concomitant inflammation. Statistically significant relationships between selected biomarkers and blood QT concentration, the patient's clinical condition and the type of therapy were demonstrated.
喹硫平(QT)属于第二代抗精神病药物。它主要用于治疗抑郁症、双相情感障碍和精神分裂症。在通过髓过氧化物酶(MPO)的生物转化过程中,QT被氧化为喹啉和一种反应性自由基,这可能有助于中毒期间氧化应激的发展。共存的炎症也可能对QT中毒过程中的紊乱有显著影响。本研究对21例喹硫平中毒患者进行了检查。该研究旨在评估血液QT浓度与中毒患者血清中选定的氧化应激以及炎症生物标志物(如MPO和C反应蛋白(CRP)水平)之间的相关性。所获得的结果与由21名健康人组成的对照组的值有关,这些健康人未经治疗且未被药物中毒。血液中QT毒性浓度(3.15±2.11μg/mL)的患者血清MPO活性和CRP水平明显高于对照组。研究组的CRP平均水平为76.74 mg/L,而对照组仅为1.86 mg/L。QT过量后患者MPO活性和CRP血液水平的增加可能证实了其生物转化过程中产生的氧化障碍和伴随炎症的假设。证明了所选生物标志物与血液QT浓度、患者的临床状况和治疗类型之间具有统计学意义的关系。
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引用次数: 0
Potential drug-drug interactions in hospitalized patients with COVID-19. COVID-19住院患者的潜在药物相互作用
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-06-29 DOI: 10.32383/appdr/162213
Danuta Szkutnik-Fiedler, Filip Kwiatkowski, Monika Chomej, D. Kołodziej, M. Michalak, E. Grześkowiak, E. Szałek
Most hospitalized patients with COVID-19 require complex pharmacotherapy due to underlying diseases, and polypharmacy may significantly increase the risk of drug-drug interactions (DDIs) and, in consequence, trigger adverse effects. The aim of this study was to assess the risk of potential DDIs during hospitalization in COVID-19 patients. A retrospective analysis of pharmacotherapy in 75 patients (age, Mean±SD, 63.6±14.9) with a proven diagnosis of SARS-CoV-2 infection was conducted. The analysis included drugs administered to treat comorbidities and the COVID-19 treatment. 524 moderate and 112 major interaction cases were revealed in the analyzed COVID-19 patients, and 84% of the patients were exposed to at least one major DDI. Drugs that caused the most frequently observed DDIs include macrolides, low molecular weight heparins, glucocorticosteroids, quinolones, and antihypertensive drugs. Most COVID-19 patients have comorbidities requiring polypharmacy, which increases the risk of DDIs. Therefore, additional monitoring should be considered due to potential adverse effects, drug conversion, and deprescription.
大多数COVID-19住院患者由于基础疾病需要复杂的药物治疗,多种药物治疗可能显著增加药物相互作用(ddi)的风险,从而引发不良反应。本研究的目的是评估COVID-19患者住院期间潜在ddi的风险。回顾性分析75例确诊为SARS-CoV-2感染的患者(年龄,Mean±SD, 63.6±14.9)的药物治疗情况。该分析包括用于治疗合并症和COVID-19治疗的药物。分析的COVID-19患者中发现中度交互作用病例524例,重度交互作用病例112例,84%的患者至少暴露于一种重度DDI。引起ddi最常见的药物包括大环内酯类药物、低分子肝素、糖皮质激素、喹诺酮类药物和降压药。大多数COVID-19患者有合并症,需要多重用药,这增加了ddi的风险。因此,由于潜在的不良反应、药物转化和取消处方,应考虑额外的监测。
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引用次数: 0
Stability of furosemide and torasemide in parenteral nutrition admixture 速尿和托拉塞胺在肠外营养混合物中的稳定性
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-06-29 DOI: 10.32383/appdr/168629
Szymon Tomczak, A. Jelińska, Jan Kościński
Furosemide and torasemide (loop diuretics) are used to treat hypertension or pulmonary edema. They are often administered in the parenteral route. In critically ill patients, there is a problem of a limited number of venous accesses, which complicates the polytherapy. Drugs of unknown compatibility must be administered separately, and the problem increases in patients receiving parenteral nutrition. Lipid emulsions have been introduced into clinical practice as a high-calorie, non-glucose source of energy for parenteral administration, but they can also be used as lipophilic drug carriers. In this paper, the parenteral nutrition admixture (PNA) Nutriflex Lipid special was used as a drug carrier for furosemide and torasemide. For this purpose, drug stability tests (HPLC method) were carried out in various light and temperature conditions, imitating clinical conditions, and the parameters of the lipid emulsion (pH, zeta potential, the size of the emulsion droplets and polpolydispersity) were tested. Furosemide and torasemide added to Nutriflex Lipid special did not cause significant changes in the physicochemical properties of PNA. Changes in pH and MDD were within acceptable limits. Both drugs when added to Nutriflex Lipid special were degraded, dependent on the storage conditions and the chemical structure.
速尿和托拉塞米(环状利尿剂)用于治疗高血压或肺水肿。它们通常以肠外途径给药。在危重患者中,存在静脉通路数量有限的问题,这使综合治疗复杂化。配伍不明的药物必须单独给药,而接受肠外营养的患者的问题更严重。脂质乳剂作为一种高热量、非葡萄糖的肠外给药能量来源已被引入临床实践,但它们也可以用作亲脂性药物载体。本研究采用肠外营养混合物(PNA) Nutriflex脂质特种作为呋塞米和托拉塞米的药物载体。为此,模拟临床条件,在各种光照和温度条件下进行药物稳定性试验(HPLC法),并测试脂质乳的参数(pH、zeta电位、乳滴大小和聚多分散性)。在Nutriflex脂质特种中加入速尿和托拉塞米对PNA的理化性质没有明显的影响。pH和MDD的变化在可接受范围内。这两种药物在加入Nutriflex脂质特殊液时,根据储存条件和化学结构的不同而降解。
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引用次数: 0
Physical compatibility of ibuprofen and selected parenteral drugs during simulated y-site administration 模拟y位点给药过程中布洛芬与选定的肠外药物的物理相容性
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-06-29 DOI: 10.32383/appdr/167804
K. Dettlaff, K. Dominiak, Marta Klimaszewska, A. Gostyńska
Intravenous ibuprofen (IBF) is indicated for short-term acute moderate pain and fever management. Limited data concerning the compatibility of intravenous IBF and other parenteral medications makes it inconvenient to use in polypharmacy-required patients. The simultaneous administration of two incompatible drugs is a health- or even life-threatening medical error. This study was performed to evaluate the physical compatibility of two intravenous IBF doses (600 mg/100 mL, 400 mg/100 mL) during Y-site administration with common parenteral medications. Eight infusion fluids, seven ready-to-use solutions for infusion, and thirty concentrates or powders for solutions for infusion were examined. All these drugs, if relevant, were reconstituted and diluted following the manufacturer's instructions to achieve concentrations found most commonly in clinical practice. Samples were prepared by mixing IBFs and selected drug product solutions at the 1:1 volume ratio. All samples underwent visual inspection and determination of pH and turbidity before combining with IBF and in time points (0, 30, 60, and 120 minutes) after simulated Y-site administration with IBF. In the case of propofol, which is an emulsion for infusion, lipid droplet size, zeta potential, and polydispersity index were also determined. The incompatibilities were observed for IBF combinations with amiodarone, ciprofloxacin, clemastine, gentamicin, vinpocetine, and calcium chloride.
静脉注射布洛芬(IBF)适用于短期急性中度疼痛和发烧治疗。关于静脉注射IBF和其他胃肠外药物的兼容性的有限数据使得在需要多药治疗的患者中使用不方便。同时服用两种不相容的药物是一种健康甚至危及生命的医疗错误。本研究旨在评估Y位给药期间两种静脉注射IBF剂量(600 mg/100 mL、400 mg/100 mL)与普通胃肠外药物的物理兼容性。检查了8种输液、7种用于输液的即用溶液和30种用于输液溶液的浓缩物或粉末。所有这些药物,如果相关的话,按照制造商的说明进行重组和稀释,以达到临床实践中最常见的浓度。通过将IBF和选定的药物产品溶液以1:1的体积比混合来制备样品。所有样品在与IBF联合用药前以及在模拟Y位点IBF给药后的时间点(0、30、60和120分钟)进行目视检查并测定pH和浊度。在丙泊酚(一种用于输注的乳液)的情况下,还测定了脂滴大小、ζ电位和多分散指数。观察到IBF与胺碘酮、环丙沙星、氯马汀、庆大霉素、长春西汀和氯化钙的组合存在不相容性。
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引用次数: 0
Preparation and characterization of pH-responsive Zein-ZnPc-PDA/HA nanoparticles intended for tumor therapy ph响应型玉米蛋白-锌npc - pda /HA纳米颗粒的制备与表征
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-05-04 DOI: 10.32383/appdr/163050
Huixiang Lu, Ming Yang, Xueying Tian, Xianhui He, Yujun Lu, Qian-rong Peng
Photodynamic therapy (PDT) has emerged as a non-invasive modality where photosensitizer (PS) plays an indispensable role for treating tumors. This study proposes a novel Zein nanoparticle (ZP) encapsulating Zinc phthalocyanine (ZnPc) that targets tumor through intravenous delivery. The ZPs were prepared by phase separation process. Modification of ZPs were realized through encapsulation of polydopamine (PDA) and hyaluronic acid (HA) in order to maintain photothermal, pH-responsive, and tumor-targeting properties. The physiochemical properties, in vitro release, and in vitro evaluation of photothermal and photodynamic effects were studied. The biosafety was analyzed through cytotoxicity assay using human lung cancer cell line A549 as model. The excellent biosafety and significant anti-tumor effect demonstrated that the novel ZPs can be potential candidates for the alternative treatment of cancer.
光动力疗法(PDT)已成为一种非侵入性治疗方式,光敏剂(PS)在治疗肿瘤中发挥着不可或缺的作用。本研究提出了一种新型的Zein纳米粒子(ZP),该纳米粒子包封酞菁锌(ZnPc),通过静脉递送靶向肿瘤。ZPs是通过相分离工艺制备的。ZPs的改性是通过包封聚多巴胺(PDA)和透明质酸(HA)来实现的,以保持光热、pH响应性和肿瘤靶向性。研究了光热和光动力效应的理化性质、体外释放和体外评价。以人癌症细胞株A549为模型,通过细胞毒性试验分析其生物安全性。优良的生物安全性和显著的抗肿瘤效果表明,新型ZPs可作为癌症替代治疗的潜在候选药物。
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引用次数: 0
Design, synthesis and antitumor activity of coumarin, isoxazole, pyrazole, pyridine and pyrimidine compounds: 3β-hydroxypregn-5-ene-20-one derivatives 香豆素、异恶唑、吡唑、吡啶和嘧啶类化合物:3β-羟基孕酮-5-烯-20- 1衍生物的设计、合成及其抗肿瘤活性
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-05-04 DOI: 10.32383/appdr/161430
K. El-Sharkawy, H. Alhazmi, A. Najmi, M. Albratty, A. Khalid, R. Hassani, S. Javed
In continuation of our reserach for synthesizing heterocyclic derivatives with a broad range of biological activities, the current research was performed to synthesize 3β-hydroxypregn-5-ene-20-one derivatives of coumarin, isoxazole, pyrazole, pyridine and pyrimidine and screen for antitumor activity. Synthesis of amino-thiopephen derivatives (1a-1b) was performed through reaction of 3β-hydroxypregn-5-ene-20-one with ethyl cyanoacetate or malononitrile and sulphur. 3β-Hydroxypregn-5-ene-20-one was reacted with ethyl cyanoacetate in the presence of hydrazine, urea or thiourea to obtain aminopyrazole (3), aminopyrimidine (4a-4b) derivatives, respectively. The amino-thiophene derivatives (1a-1b) further reacted with either phenylisothiocyanate or benzoylisothiocyanate to form fused thienopyrimidine derivatives (5a-5d). The products 1a and 1b were also treated with ethyl cyanoacetate to afford cyanoacetamidothiophene derivatives (6a-6b) which were converted to fused thienopyridone derivatives (7a-7b) through cyclization reaction. The compounds 6a and 6b were allowed to react with different carbonyl compounds including salicyaldehyde, cyclopentanone-sulphur mixture, acetylacetone and malonaldehyde to prepare coumarin (8a-8b), cyclopentylthiophene (9a-9b) and 2-pyridinone (10a-10d) derivatives respectively. Furthermore, the reactions of hydroxylamine hydrochloride and benzoylacetonitrile with the compounds 6a-6b separately afforded new aminoisoxazole (12a-12b) and phenylpyridone (14a-14b) derivatives, respectively. The structures of new products were established through IR, 1H NMR, 13C NMR spectroscopic and mass spectrometric analysis. The synthesized compounds (1a-1b to 14a-14b) displayed in-vitro antitumor activity against human cell-lines, including MCF-7 (breast adenocarcinoma), SF-268 (CNS cancer) and NCI-H460 (non-small lung cancer cell). The results suggested that all the screened products exhibited cell growth inhibitory activity in a dose-dependents manner. However, the compound 12a showed highest level of inhibition against all three cell-lines.
为了继续我们对具有广泛生物活性的杂环衍生物的合成研究,本研究对香豆素、异恶唑、吡唑、吡啶和嘧啶的3 - β-羟基孕酮-5-烯-20- 1衍生物进行了合成并进行了抗肿瘤活性筛选。通过3β-羟基孕酮-5-烯-20-酮与氰乙酸乙酯或丙二腈和硫的反应,合成了氨基噻吩衍生物(1a-1b)。3β-羟孕酮-5-烯-20- 1在肼、尿素或硫脲存在下与氰乙酸乙酯反应,分别得到氨基吡唑(3)、氨基嘧啶(4a-4b)衍生物。氨基噻吩衍生物(1a-1b)进一步与苯基异硫氰酸酯或苯甲酰异硫氰酸酯反应形成融合的噻吩嘧啶衍生物(5a-5d)。产物1a和1b也用氰乙酸乙酯处理得到氰乙酰氨基噻吩衍生物(6a-6b),并通过环化反应转化为熔融噻吩衍生物(7a-7b)。化合物6a和6b分别与水杨醛、环戊酮-硫混合物、乙酰丙酮和丙二醛等羰基化合物反应,分别制得香豆素(8a-8b)、环戊基噻吩(9a-9b)和2-吡啶酮(10a-10d)衍生物。此外,盐酸羟胺和苯甲酰乙腈分别与化合物6a-6b反应得到新的氨基异恶唑(12a-12b)和苯基吡酮(14a-14b)衍生物。通过IR、1H NMR、13C NMR和质谱分析确定了新产物的结构。合成的化合物(1a-1b至14a-14b)对人类细胞系,包括MCF-7(乳腺腺癌),SF-268(中枢神经系统癌)和NCI-H460(非小肺癌细胞)显示出体外抗肿瘤活性。结果表明,所有筛选的产物均表现出剂量依赖性的细胞生长抑制活性。然而,化合物12a对三种细胞系的抑制作用最高。
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引用次数: 0
Apigenin targets protein and lipids of HeLa cells and exhibits protective efficacy against oxidative stress 芹菜素靶向HeLa细胞的蛋白质和脂质,对氧化应激具有保护作用
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-05-04 DOI: 10.32383/appdr/163049
B. Pawlikowska-Pawlęga, J. Kapral-Piotrowska, A. Jarosz-Wilkołazka, B. Chudzik, R. Paduch, J. Jakubowicz-Gil, A. Wawrzyniak, I. Łuszczewska-Sierakowska, A. Sławińska-Brych, B. Zdzisińska, E. Reszczyńska, K. Trebacz, W. Gruszecki
Apigenin, non-toxic and non-mutagenic flavonoid, is an alternative to classical drugs that interact with membranes. Hence, the objects of the study were to examine its effects on liposomes made of egg yolk phosphatidylcholine (EYPC) with the use of 1H NMR, four-electrode BLM and EPR techniques, and determine its activity on lipids and proteins of human cervix carcinoma (HeLa) cells. In addition its protective efficacy against H2O2- induced oxidative shock was investigated. FTIR spectroscopy was applied to study molecular interactions with membrane lipids and proteins of HeLa cells. Microscopic techniques (SEM, light, and fluorescence), flow cytometer analysis, and NR assays were employed to reveal apigenin involvement in apoptosis in different cell conditions. Apigenin affected mainly the region of choline head groups and the hydrophobic core below this area. Simultaneously, the ordering effect was shown. The fingerprint region of lipids in the HeLa cells was found as a target for apigenin. Furthermore, in the amide I and amide II regions, a decrease in β-sheets and an increase in turns, loops, and unordered structures were noted. Apigenin reduced viability of cells and induced apoptosis. SEM observations revealed characteristic changes in morphology of the examined cells. Pretreatment of HeLa cells with apigenin protected them against H2O2-induced oxidative stress by the increase in glutathione content as well as superoxide dismutase and catalase levels. The consequences of molecular changes related to membranes and cancer cells make apigenin a unique and very interesting bio-compound with great significance for medical and biological applications.
芹菜素是一种无毒、非诱变的类黄酮,是与膜相互作用的经典药物的替代品。因此,本研究的目的是利用1H NMR、四电极BLM和EPR技术研究其对蛋黄磷脂酰胆碱(EYPC)脂质体的影响,并测定其对人宫颈癌(HeLa)细胞脂质和蛋白质的活性。此外,还研究了其对H2O2诱导的氧化休克的保护作用。利用FTIR光谱研究了HeLa细胞与膜脂和蛋白的相互作用。显微技术(扫描电镜、光和荧光)、流式细胞仪分析和NR分析揭示了芹菜素在不同细胞条件下参与凋亡的作用。芹菜素主要影响胆碱头基团区域及其以下疏水核。同时,还显示了排序效应。在HeLa细胞中发现脂质指纹区是芹菜素的靶点。此外,在酰胺I和酰胺II区,β-片减少,匝、环和无序结构增加。芹菜素降低细胞活力,诱导细胞凋亡。扫描电镜观察显示所检查细胞的形态学特征变化。芹菜素预处理HeLa细胞可通过提高谷胱甘肽含量、超氧化物歧化酶和过氧化氢酶水平,保护HeLa细胞免受h2o2诱导的氧化应激。与细胞膜和癌细胞相关的分子变化的后果使芹菜素成为一种独特而非常有趣的生物化合物,具有重要的医学和生物学应用意义。
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引用次数: 0
Acknowledgement to Reviewers 2022 审稿人致谢
4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-05-04 DOI: 10.32383/appdr/164727
Michał Tomczyk
We would like to take this opportunity to thank you for the effort and expertise that you contribute to reviewing, without which it would be impossible to maintain the high editorial standards of Acta Poloniae Pharmaceutica – Drug Research.
我们想借此机会感谢您在审稿过程中所付出的努力和专业知识,没有这些,我们就不可能保持Acta Poloniae Pharmaceutica - Drug Research的高编辑标准。
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引用次数: 0
Development and optimization of TPGS/P84 mixed polymeric micelles: enhanced stability and anticancer effect of paclitaxel against tumor therapy TPGS/P84混合聚合物胶束的开发与优化:紫杉醇抗肿瘤的稳定性和抗癌作用的增强
IF 0.4 4区 医学 Q4 PHARMACOLOGY & PHARMACY Pub Date : 2023-05-04 DOI: 10.32383/appdr/161587
Qi Huang, Yingli Zhao, Xing Fang, J. Liu, Quan Xia, Chao Tan, Yao Peng, Jingjing Wu
Mixed micelles (MMs), as a new targeted drug delivery system with high adjustability, have been widely studied in biomedicines. In order to study whether mixtures containing two different molecules have excellent targeted anti-tumor effect, MMs based on D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and triblock copolymer P84 were prepared, and the characterization, cell endocytosis, and exocytosis of P84/TPGS MMs were observed. Paclitaxel (PTX), a classical anti-tumor drug, was selected as a model compound to explore its anti-tumor effect in vivo. The results showed that P84/TPGS MMs had better stability, suitably distributed particle size, good cell endocytosis, and tumor sphere permeability, which could improve the permeability of PTX in the tumor site and effectively inhibit the growth of H22 tumor in mice. In conclusion, P84/TPGS MMs is a potential micelle carrier system of cancer targeting, needing further investigation.
混合胶束作为一种具有高度可调节性的新型靶向给药系统,在生物医学领域得到了广泛的研究。为了研究含有两种不同分子的混合物是否具有良好的靶向抗肿瘤作用,我们制备了基于D-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)和三嵌段共聚物P84的mm,并观察了P84/TPGS mm的表征、细胞内吞和胞外分泌情况。选择经典抗肿瘤药物紫杉醇(Paclitaxel, PTX)作为模型化合物,探讨其体内抗肿瘤作用。结果表明,P84/TPGS mm具有较好的稳定性、粒径分布适宜、良好的细胞内吞作用和肿瘤球通透性,可提高肿瘤部位PTX的通透性,有效抑制小鼠H22肿瘤的生长。综上所述,P84/TPGS mm是一种潜在的靶向癌症的胶束载体系统,有待进一步研究。
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引用次数: 0
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