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Image Analysis: A Novel Method in the Assessment of Pharmaceutical Foams 图像分析:一种评价药物泡沫的新方法
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.204-205
D. Farkas, Nikolett Kállai-Szabó, I. Antal
For almost half a century foams have been present in the pharmaceutical markets worldwide. Generally, they can be defined as thin liquid or solid film separated gas bubble agglomerations, but the pharmacopoeial monograph of medicated foams recognizes only the aforementioned 1,2. Pharmaceutical foams offer an outstanding alternative to conventional dosage forms in topical treatment. Apart from the satisfactory drug delivery ability, the ease and convenience of application contributes to the high acceptance and excellent patient compliance of this dosage form. Despite the growing interest for foams, the current pharmacopoeial examinations are not sufficient for the description of their unique nature and virtue. Although image analysis can not provide an exhaustive overview on foams, it offers a great complementary method for their assessment 3,4. This research aims to demonstrate the extensive applicability of image analysis in the evaluation process of pharmaceutical foams. It also aims to make assumptions on important foam characteristics based on the composition and the microand macroscopic properties of foams.
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引用次数: 0
Study on Drug Release from Oleogel Carriers 油凝胶载体药物释放的研究
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.328-329
Zsófia Vilimi, M. Hajdú, Nikolett Kállai-Szabó, I. Antal
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引用次数: 0
Lipopeptide Nanoparticulate Vaccine Candidates for the Induction of Protective Immune Responses 诱导保护性免疫反应的脂肽纳米颗粒疫苗候选物
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.124-125
I. Toth, M. Skwarczynski
The development of an effective vaccine for group A streptococci (GAS) has been challenged by the induced autoimmunity of epitopes derived from the C-repeat regions. Additionally, there are B-cell epitopes that have been shown to react with human heart tissue. Shorter safe B-cell epitopes, show little or no immunogenicity unless bound to a delivery platform including the conjugation to an inbuilt adjuvant. Self-adjuvanting lipid core peptide (LCP) systems where the antigen(s), carrier and adjuvant were within the same molecular entity has been developed. The LCP amphiphilic construct was incorporated into liposomes to produce particles with the desired size. The construct alone elicited high-levels of antibody titers comparable to that of the positive control (J8 + Complete Freund’s adjuvant). The developed strategy to produce nanoparticles, consisting of a peripheral antigenic epitope layer conjugated to a dendrimer core, which is both self-adjuvanting and produces a strong immune response to the GAS M-protein, offers an attractive alternative to conventional vaccine approaches. The greatest advantage of this system being the generation of protective immune response after oral administration. Our dendrimer-nanoparticles vaccine approach should be readily acquiescent to other pathogenic organisms in addition to GAS, and may prove particularly useful for the design of vaccines against infection deceases know to stimulate autoimmune response in a host.
A群链球菌(GAS)有效疫苗的开发一直受到来自C-repeat区域的表位诱导自身免疫的挑战。此外,有b细胞表位已被证明与人类心脏组织发生反应。较短的安全b细胞表位,显示很少或没有免疫原性,除非结合到递送平台,包括与内建佐剂的结合。抗原、载体和佐剂位于同一分子实体内的自佐剂脂质核心肽(LCP)系统已经被开发出来。LCP两亲性结构被纳入脂质体以产生所需大小的颗粒。该构建体单独引发了与阳性对照(J8 +完全弗氏佐剂)相当的高水平抗体滴度。开发出的生产纳米颗粒的策略提供了一种有吸引力的替代方法,这种纳米颗粒由外周抗原表位层偶联到树突核心组成,既具有自我佐剂作用,又能对GAS m蛋白产生强烈的免疫反应。该系统最大的优点是口服后产生保护性免疫反应。我们的树突-纳米颗粒疫苗方法应该可以很容易地对除GAS之外的其他病原生物默认,并且可能被证明对设计已知可刺激宿主自身免疫反应的感染死亡疫苗特别有用。
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引用次数: 0
Space Chemistry Realization via SpaceMedChem 通过SpaceMedChem实现空间化学
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.274-275
B. Buchholcz, G. Mezőhegyi, F. Darvas
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引用次数: 0
Structural Analysis of Human Glycoproteins by Tandem Mass Spectrometry 串联质谱法分析人糖蛋白结构
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.163-164
A. Ács, Dániel Szabó, K. Vékey, G. Sármay, L. Drahos, Lilla Turiák
The process of glycosylation is a highly conserved mechanism among species. The enzymatic addition of oligosaccharide chain to the protein significantly changes the physicochemical properties and protein-protein interactions. Therefore glycosylation considered as a CQA (Critical Quality Attribute) for biopharmaceutical products. At this point there is no routinely used, widespread analytical method to determine glycosylation. This may derive from the fact that the term glycosylation summarizes various features. The most often examined feature is the relative abundance of glycoforms. The position of different sugar residues within the oligosaccharide chain has been less frequently analyzed. In this study we have developed a method which, in addition to the commonly investigated features, determines the structural position of the fucose residue. We have examined glycosylation of three proteins: AGP (alpha-1-acid glycoprotein), PSA (Prostate Specific Antigen) and IgG (Immunoglobulin G).
糖基化过程是物种间高度保守的机制。低聚糖链的酶加作用显著地改变了蛋白质的理化性质和蛋白质间的相互作用。因此,糖基化被认为是生物制药产品的关键质量属性。在这一点上,没有常规使用的,广泛的分析方法来确定糖基化。这可能源于糖基化一词概括了各种特征。最常检查的特征是糖型的相对丰度。对低聚糖链中不同糖残基的位置分析较少。在这项研究中,我们开发了一种方法,除了通常调查的特征,确定焦残的结构位置。我们检测了三种蛋白的糖基化:AGP (α -1-酸性糖蛋白)、PSA(前列腺特异性抗原)和IgG(免疫球蛋白G)。
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引用次数: 0
Berberine-loaded Nano-Liposomes Generated with Ethanol-Injection and Thin-film Hydration Methods 乙醇注射与薄膜水合法制备小檗碱纳米脂质体
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.293-295
Duong Thi Thuan, A. Isomäki, Urve Paaver, Ivo Laidmäe, A. Tõnisoo, Tran Thi Hai Yen, Karin Kogermann, A. Raal, J. Heinämäki, Pham Thi Minh Hue
The poor solubility in water is very often a problem for active pharmaceutical substances of plant origin. The formulation of such drugs as liposomal preparations enables to improve the bioavailability of these drugs. Berberine (BBR) is a quaternary isoquinoline alkaloid derived from many native plant species (Coptis spp., Berberis spp., Hydrastis canadensis etc.). BBR has been traditionally used for the treatment of different disorders including hyper-cholesterolemia and cardiovascular diseases [1,2]. BBR has a strong antimicrobial activity enabling the use of it as an anti-diarrheal, anti-protozoal, fungal, candida, yeast, and parasitic intestinal active ingredient [3]. In addition, BBR has shown an anti-inflammatory, anti-diabetic, lipid peroxidation, and neuroprotective activity [3,4]. Unfortunaterly, BBR is poorly soluble in water and has a low bioavailability (<10%) due to the induced activity of multidrug efflux transporter Pglycoprotein (P-gp) in the intestine itself [2]. Such limitations associated with a poor oral bioavailability of BBR could be overcome by nanoformulating BBR to liposomes. Pharmaceutical liposomes can be fabricated by ethanol-injection and thin-film hydration methods. The lamellarity, size, shape and ultra-structure of liposomes can be determined by using different advanced techniques, such as cryogenic electron microscopy (Cryo-EM), dynamic light scattering (DLS), size-exclusion chromatography (SEC), and atomic force microscopy (AFM) [5]. Confocal laser scanning microscopy (CLSM) has been also used for such imaging [6]. The aim of our study is to investigate ethanolinjection and film hydration methods for generating BBR-loaded liposomes and to study the structure, size, size distribution and entrapment efficiency of the liposomes. The liposomes are ultimately intended for the oral treatment of hypercholesterolemia.
植物原料药在水中的溶解度差是一个非常常见的问题。这类药物如脂质体制剂的制剂能够提高这些药物的生物利用度。小檗碱(Berberine, BBR)是从许多本土植物(黄连、小檗、加拿大Hydrastis canadensis等)中提取的季际异喹啉类生物碱。BBR传统上被用于治疗不同的疾病,包括高胆固醇血症和心血管疾病[1,2]。BBR具有很强的抗菌活性,可作为抗腹泻、抗原虫、真菌、念珠菌、酵母菌和寄生虫的肠道活性成分[3]。此外,BBR还具有抗炎、抗糖尿病、脂质过氧化和神经保护活性[3,4]。不幸的是,由于多药外排转运体糖蛋白(P-gp)在肠道内的诱导活性,BBR难溶于水,生物利用度低(<10%)[2]。这些与BBR的口服生物利用度差相关的限制可以通过纳米配方BBR脂质体来克服。采用乙醇注射法和薄膜水化法制备药用脂质体。脂质体的层状、大小、形状和超结构可以通过使用不同的先进技术来确定,如低温电子显微镜(cro - em)、动态光散射(DLS)、尺寸排除色谱(SEC)和原子力显微镜(AFM)[5]。共聚焦激光扫描显微镜(CLSM)也被用于此类成像[6]。本研究的目的是研究乙醇注射和膜水化制备载bbr脂质体的方法,并研究脂质体的结构、大小、大小分布和包封效率。脂质体最终用于口服治疗高胆固醇血症。
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引用次数: 0
Interfacial Properties of Biodegradable Drug Carrier Nanoparticles 可生物降解药物载体纳米颗粒的界面性质
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.218-219
Dániel Fülöp, É. Kiss, Gergő Gyula
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引用次数: 0
High-Throughput Screening for Bioactive Natural Compounds from Plant Extracts by HPTLC Hyphenations 高效薄层色谱法筛选植物提取物中生物活性天然化合物
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.276-277
Á. Móricz, D. Krüzselyi, Maryam Jamshidi-Aidji, P. Ott, G. Morlock
In the last decade, effect-directed analysis (EDA) gave new impetus for the discovery of new potential drug compounds from natural sources. Highperformance thin-layer chromatography (HPTLC) was established as a high-throughput and reliable separation technique that is frequently utilized for screening of highly complex samples, such as crude plant extracts. HPTLC combined with biological and biochemical assays and high-resolution mass spectrometry (HRMS) followed by bioassay-guided isolation and NMR was demonstrated as a straightforward strategy for bioanalysis of natural products [1,2]. Diabetes and Alzheimer’s disease (AD) represent two of the global health issues. Type 2 diabetic patients, the majority of the people with diabetes, suffer from the hyperglycemia. The salivary and pancreatic α-amylases and αand β-glucosidases are involved in the degradation and digestion of polyand oligosaccharides to glucose, hence, glucosidase and amylase inhibitors are of therapeutic interest in type 2 diabetes as well as overweight and obesity [3,4]. AD is associated with the loss of cholinergic neurons in the brain and decrease in the neurotransmitter acetylcholine. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are crucially involved in the hydrolysis of the acetylcholine into choline. Hence, AChE-selective and dual AChE/BChE inhibitors represented the first generation of medicines for the decrease of the AD progression rate [5]. The fight against infectious diseases, a major global public hazard, is also a challenge due to the increase in the emergence of the (multi)drug-resistant microorganisms [6]. In this study (HP)TLC combined with direct αand β-glucosidase, α-amylase and antimicrobial assays will be demonstrated for the comparison of the bio-profiles (the enzyme inhibitory and antibacterial potentials) of invasive goldenrod species.
在过去的十年中,效应导向分析(EDA)为从天然来源发现新的潜在药物化合物提供了新的动力。高效薄层色谱(HPTLC)是一种高通量、可靠的分离技术,经常用于筛选高度复杂的样品,如植物粗提取物。HPTLC结合生物和生化分析和高分辨率质谱(HRMS),然后是生物测定引导分离和核磁共振被证明是天然产物生物分析的直接策略[1,2]。糖尿病和阿尔茨海默病(AD)是两个全球性的健康问题。2型糖尿病患者,占糖尿病患者的大多数,患有高血糖症。唾液和胰腺的α-淀粉酶以及α和β-葡萄糖苷酶参与多聚糖和低聚糖的降解和消化,因此,葡萄糖苷酶和淀粉酶抑制剂对2型糖尿病以及超重和肥胖具有治疗意义[3,4]。阿尔茨海默病与大脑胆碱能神经元的丧失和神经递质乙酰胆碱的减少有关。乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BChE)在乙酰胆碱水解成胆碱的过程中起关键作用。因此,AChE选择性和双重AChE/BChE抑制剂代表了第一代降低AD进展率的药物[5]。传染病是一项重大的全球公害,由于(多重)耐药微生物的出现增加,抗击传染病也是一项挑战[6]。在本研究中,(HP)TLC联合α和β-葡萄糖苷酶、α-淀粉酶和抗菌检测将用于比较入侵性黄花属植物的生物特征(酶抑制和抗菌潜力)。
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引用次数: 0
Comparative Dissolution Study of Coated Pellets Containing Microcrystalline Cellulose and Lactose As Core Materials 以微晶纤维素和乳糖为核心材料包被微球的溶解比较研究
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.177-178
Á. Barna, K. Sántha, Nikolett Kállai-Szabó, E. Balogh, Bálint Basa, G. Jakab, I. Antal
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引用次数: 0
Formulation and Complex Morphological Characterization of Core-Shell Fibrous Mats for Chronic Wound Healing 用于慢性伤口愈合的核-壳纤维垫的配方和复杂形态表征
Pub Date : 2021-11-15 DOI: 10.33892/aph.2021.91.247-248
Adrienn Kazsoki, A. Farkas, Diána Balogh‐Weiser, E. Mancuso, P. Sharma, D. Lamprou, R. Zelkó
In the recent past, one of the major challenges of the pharmaceutical industry was to overcome the poor aqueous solubility and permeability of new drug candidates, leading to their low bioavailability [1]. To solve these problems, novel structures were developed involving the polymer-based nanofibrous drug delivery systems [2,3]. The unique properties of the nanofibers as the high porosity with interconnected pore network and the increased surface area of the fibrous sheets, together with the active pharmaceutical ingredients can be embedded into the polymeric matrix carrier in an amorphous state, could lead to an increased dissolution and thus the bioavailability of drugs with a lower solubility [4,5]. Due to their structure, the formulation of nanofibrous materials loaded with different drugs have been widely used as drug delivery systems, scaffolds for tissue engineering and wound bandage. Electrospinning is a well controllable, simple and cost-effective technique for preparing matrices with nanometer-sized fibers with similar features and morphologies to the extracellular matrix (ECM) [6]. The ECM is the non-cellular component presents within all tissues and organs and plays a vital role in the wound healing process [7]. Therefore from those materials which can mimic their structure are believed to stimulate cell proliferation and could help the wound healing [6]. The diverse field of application of the nanofibrous materials required adequate functionalityrelated characteristics. One of the emerging improvements is the development of a bi-component core-shell fiber structure [8], which can offer several benefits for these samples: the core polymer/ composite can provide the required mechanical, physicochemical properties, and can control the release of the incorporated drug(s). The shell materials could preserve the unstable active pharmaceutical ingredients embedded into the core from the unfavorable environmental effect, which can increase the hydrophilicity and the biocompatibility of the fibrous samples. Besides that, one of the significant advantages of this core-shell nanostructures lies in the potential to tailor release properties of the incorporated drug and combine features of different polymers to achieve the required functionality-related characteristic and mechanical properties also [5].
近年来,制药行业面临的主要挑战之一是克服新候选药物的水溶性和渗透性差,导致其生物利用度低[1]。为了解决这些问题,聚合物基纳米纤维给药系统的新结构被开发出来[2,3]。纳米纤维的独特特性是具有相互连接的孔网络的高孔隙率和纤维片表面积的增加,以及活性药物成分可以以无定形嵌入聚合物基质载体中,从而增加溶解性,从而提高溶解度较低的药物的生物利用度[4,5]。纳米纤维材料由于其独特的结构特点,在药物递送系统、组织工程支架和创面绷带等方面得到了广泛的应用。静电纺丝是一种可控、简单、经济的技术,用于制备具有与细胞外基质(ECM)相似特征和形态的纳米级纤维基质[6]。外基质是存在于所有组织和器官中的非细胞成分,在伤口愈合过程中起着至关重要的作用[7]。因此,那些可以模仿其结构的材料被认为可以刺激细胞增殖并有助于伤口愈合[6]。纳米纤维材料的不同应用领域需要充分的功能相关特性。新出现的改进之一是双组分核-壳纤维结构的发展[8],它可以为这些样品提供几个好处:核心聚合物/复合材料可以提供所需的机械、物理化学性能,并且可以控制掺入药物的释放。壳材料可以保护嵌入芯内的不稳定活性药物成分不受不利环境影响,从而提高纤维样品的亲水性和生物相容性。除此之外,这种核壳纳米结构的一个显著优势在于,它有可能调整掺入药物的释放特性,并结合不同聚合物的特征,以实现所需的功能相关特性和力学性能[5]。
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引用次数: 0
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Acta pharmaceutica Hungarica
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