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1.
Braz. j. biol ; 83: e247604, 2023. tab, graf
Article in English | MEDLINE, LILACS, VETINDEX | ID: biblio-1339370

ABSTRACT

Abstract In the current report, we studied the possible inhibitors of COVID-19 from bioactive constituents of Centaurea jacea using a threefold approach consisting of quantum chemical, molecular docking and molecular dynamic techniques. Centaurea jacea is a perennial herb often used in folk medicines of dermatological complaints and fever. Moreover, anticancer, antioxidant, antibacterial and antiviral properties of its bioactive compounds are also reported. The Mpro (Main proteases) was docked with different compounds of Centaurea jacea through molecular docking. All the studied compounds including apigenin, axillarin, Centaureidin, Cirsiliol, Eupatorin and Isokaempferide, show suitable binding affinities to the binding site of SARS-CoV-2 main protease with their binding energies -6.7 kcal/mol, -7.4 kcal/mol, -7.0 kcal/mol, -5.8 kcal/mol, -6.2 kcal/mol and -6.8 kcal/mol, respectively. Among all studied compounds, axillarin was found to have maximum inhibitor efficiency followed by Centaureidin, Isokaempferide, Apigenin, Eupatorin and Cirsiliol. Our results suggested that axillarin binds with the most crucial catalytic residues CYS145 and HIS41 of the Mpro, moreover axillarin shows 5 hydrogen bond interactions and 5 hydrophobic interactions with various residues of Mpro. Furthermore, the molecular dynamic calculations over 60 ns (6×106 femtosecond) time scale also shown significant insights into the binding effects of axillarin with Mpro of SARS-CoV-2 by imitating protein like aqueous environment. From molecular dynamic calculations, the RMSD and RMSF computations indicate the stability and dynamics of the best docked complex in aqueous environment. The ADME properties and toxicity prediction analysis of axillarin also recommended it as safe drug candidate. Further, in vivo and in vitro investigations are essential to ensure the anti SARS-CoV-2 activity of all bioactive compounds particularly axillarin to encourage preventive use of Centaurea jacea against COVID-19 infections.


Resumo No presente relatório, estudamos os possíveis inibidores de Covid-19 de constituintes bioativos de Centaurea jacea usando uma abordagem tripla que consiste em técnicas de química quântica, docking molecular e dinâmica molecular. Centaurea jacea é uma erva perene frequentemente usada em remédios populares de doenças dermatológicas e febre. Além disso, as propriedades anticâncer, antioxidante, antibacteriana e antiviral de seus compostos bioativos também são relatadas. A Mpro (proteases principais) foi acoplada a diferentes compostos de Centaurea jacea por meio de docking molecular. Todos os compostos estudados, incluindo apigenina, axilarina, Centaureidina, Cirsiliol, Eupatorina e Isokaempferide, mostram afinidades de ligação adequadas ao sítio de ligação da protease principal SARS-CoV-2 com suas energias de ligação -6,7 kcal / mol, -7,4 kcal / mol, - 7,0 kcal / mol, -5,8 kcal / mol, -6,2 kcal / mol e -6,8 kcal / mol, respectivamente. Dentre todos os compostos estudados, a axilarina apresentou eficiência máxima de inibidor, seguida pela Centaureidina, Isokaempferida, Apigenina, Eupatorina e Cirsiliol. Nossos resultados sugeriram que a axilarina se liga aos resíduos catalíticos mais cruciais CYS145 e HIS41 do Mpro, além disso a axilarina mostra 5 interações de ligações de hidrogênio e 5 interações hidrofóbicas com vários resíduos de Mpro. Além disso, os cálculos de dinâmica molecular em uma escala de tempo de 60 ns (6 × 106 femtossegundos) também mostraram percepções significativas sobre os efeitos de ligação da axilarina com Mpro de SARS-CoV-2 por imitação de proteínas como o ambiente aquoso. A partir de cálculos de dinâmica molecular, os cálculos RMSD e RMSF indicam a estabilidade e dinâmica do melhor complexo ancorado em ambiente aquoso. As propriedades ADME e a análise de previsão de toxicidade da axilarina também a recomendaram como um candidato a medicamento seguro. Além disso, as investigações in vivo e in vitro são essenciais para garantir a atividade anti-SARS-CoV-2 de todos os compostos bioativos, particularmente a axilarina, para encorajar o uso preventivo de Centaurea jacea contra infecções por Covid-19.


Subject(s)
Humans , Pharmaceutical Preparations , Centaurea , COVID-19 , Protease Inhibitors , Molecular Dynamics Simulation , Molecular Docking Simulation , SARS-CoV-2
2.
Biochem J ; 479(12): 1337-1359, 2022 Jun 30.
Article in English | MEDLINE | ID: mdl-35748702

ABSTRACT

Some of the most threatening human diseases are due to a blockage of the mitochondrial electron transport chain (ETC). In a variety of plants, fungi, and prokaryotes, there is a naturally evolved mechanism for such threats to viability, namely a bypassing of the blocked portion of the ETC by alternative enzymes of the respiratory chain. One such enzyme is the alternative oxidase (AOX). When AOX is expressed, it enables its host to survive life-threatening conditions or, as in parasites, to evade host defenses. In vertebrates, this mechanism has been lost during evolution. However, we and others have shown that transfer of AOX into the genome of the fruit fly and mouse results in a catalytically engaged AOX. This implies that not only is the AOX a promising target for combating human or agricultural pathogens but also a novel approach to elucidate disease mechanisms or, in several cases, potentially a therapeutic cure for human diseases. In this review, we highlight the varying functions of AOX in their natural hosts and upon xenotopic expression, and discuss the resulting need to develop species-specific AOX inhibitors.


Subject(s)
Agrochemicals , Mitochondrial Proteins , Agrochemicals/pharmacology , Animals , Drosophila/metabolism , Food Security , Humans , Mice , Mitochondrial Proteins/genetics , Mitochondrial Proteins/metabolism , Oxidoreductases , Pharmaceutical Preparations , Plant Proteins/genetics , Plant Proteins/metabolism
3.
PLoS One ; 17(6): e0270271, 2022.
Article in English | MEDLINE | ID: mdl-35731793

ABSTRACT

PURPOSE: The science and technology (S&T) innovation in China's pharmaceutical industry has entered a bottleneck. The choice between external and internal research and development (R&D) has become a significant challenge for S&T development. To provide scientific suggestions for companies to choose an R&D strategy and enhance S&T development, we analyzed and compared the impacts of two R&D strategies on S&T output. METHODS: We selected the data related to China's pharmaceutical manufacturing industry from 2000 to 2019, established regression equations by the E-G two-step method, and used the VAR model for impulse responses and variance decompositions to research the relationship between two R&D strategies and S&T output. RESULTS: There is a stable long-term equilibrium relationship between two R&D strategies, including external and internal R&D, and S&T output in China's pharmaceutical manufacturing industry. When internal R&D increases by 1%, S&T output increases by 0.7382% with a 5-year lag. When S&T output increases by 1%, external R&D increases by 2.0749% with a 2-year lag. CONCLUSION: Compared with external R&D, internal R&D can boost S&T output.


Subject(s)
Drug Industry , Manufacturing Industry , China , Pharmaceutical Preparations , Research
5.
Front Public Health ; 10: 864506, 2022.
Article in English | MEDLINE | ID: mdl-35719658

ABSTRACT

Background: The emergence of SARS-CoV-2 triggered a chain of public health responses that radically changed our way of living and working. Non-healthcare sectors, such as the logistics sector, play a key role in such responses. This research aims to qualitatively evaluate the non-pharmaceutical interventions (NPIs) implemented in the UK logistics sector during the COVID-19 pandemic. Methods: We conducted nine semi-structured interviews in July-August 2020 and May-June 2021. In total 11 interviewees represented six companies occupying a range of positions in the UK's logistics sector, including takeaway food delivery, large and small goods delivery and home appliance installation, and logistics technology providers. Thematic analysis was completed using NVivo12. Codes relevant to NPIs were grouped into themes and mapped deductively onto an adapted Hierarchy of Control (HoC) framework, focusing on delivery workers. Codes relevant to the implementation process of NPIs were grouped into themes/subthemes to identify key characteristics of rapid responses, and barriers and facilitators. Results: HoC analysis suggests the sector has implemented a wide range of risk mitigation measures, with each company developing their own portfolio of measures. Contact-free delivery was the most commonly implemented measure and perceived effective. The other implemented measures included social distancing, internal contact tracing, communication and collaboration with other key stakeholders of the sector. Process evaluation identified facilitators of rapid responses including capacity to develop interventions internally, localized government support, strong external mandates, effective communication, leadership support and financial support for self-isolation, while barriers included unclear government guidance, shortage of testing capacity and supply, high costs and diversified language and cultural backgrounds. Main sustainability issues included compliance fatigue, and the possible mental health impacts of a prolonged rapid response. Conclusions: This research identified drivers and obstacles of rapid implementation of NPIs in response to a respiratory infection pandemic. Existing implementation process models do not consider speed to respond and the absence or lack of guidance in emergency situations such as the COVID-19. We recommend the development of a rapid response model to inform the design of effective and sustainable infection prevention and control policies and to focus future research priorities.


Subject(s)
COVID-19 , COVID-19/epidemiology , COVID-19/prevention & control , Humans , Pandemics/prevention & control , Pharmaceutical Preparations , SARS-CoV-2 , United Kingdom
6.
Anal Chem ; 94(23): 8241-8248, 2022 Jun 14.
Article in English | MEDLINE | ID: mdl-35647784

ABSTRACT

In an earlier investigation, low-frequency Raman (LFR) spectroscopy was shown to detect the transition temperature of the ß-relaxation (Tß) in both amorphous celecoxib and various celecoxib amorphous solid dispersions [Be̅rzins, K. Mol. Pharmaceutics 2021, 18(10), 3882-3893]. In this study, we further investigated the application of this technique to determine Tß, an important parameter for estimating crystallization potency of amorphous drugs. Alongside commercially available amorphous drugs (zafirlukast and valsartan disodium salt), differently melt-quenched samples of cimetidine were also analyzed. Overall, the variable-temperature LFR measurements allowed for an easy access to the desired information, including the even lesser transition of the tertiary relaxation motions (Tγ). Thus, the obtained results not only highlighted the sensitivity, but also the practical usefulness of this technique to elucidate (subtle) changes in molecular dynamics within amorphous pharmaceutical systems.


Subject(s)
Celecoxib/chemistry , Spectrum Analysis, Raman , Calorimetry, Differential Scanning , Cimetidine/chemistry , Indoles/chemistry , Pharmaceutical Preparations , Phenylcarbamates/chemistry , Sensitivity and Specificity , Sulfonamides/chemistry , Temperature , Transition Temperature , Valsartan/chemistry
7.
Chemosphere ; 303(Pt 2): 135176, 2022 Sep.
Article in English | MEDLINE | ID: mdl-35654238

ABSTRACT

The occurrences of pharmaceutical and personal care products (PPCPs) in both freshwater and sea have been widely reported. However, pollution control requires further information on riverine discharges with influence of land-based activities and associated risks to estuarine ecosystems. This study investigated the spatial occurrences and the relationship to sociodemographic parameters of 30 PPCPs in 67 rivers along the Bohai coastal region. The results showed that PPCPs were mainly deposited in aquatic phase, and the partitioning coefficient between water and sediment was highly determined by chemical properties. The levels of 30 PPCPs in rivers ranged from 8.33 to 894.48 ng/L, showing a large variance among regions. Caffeine, sulfamethoxazole, sulfamethazine, ofloxacin, anhydro-erythromycin, and trimethoprim were found to be the major pollutants. Multivariable analysis method was used to assess the correlation of PPCPs markers to socio-economic parameters. The results indicated that domestic emissions contributed most to the occurrences of PPCPs in the riverine water. Risk assessment result indicated that sulfamethoxazole, caffeine, tetracycline, and carbamazepine ranked top four with the highest risks to the most sensitive aquatic organisms. The results identified caffeine and carbamazepine with high detection frequency and concentration as the priority chemicals, while sulfamethoxazole and erythromycin should also be concerned due to their potential threats in specific rivers. This study provides valuable information for pollution control over PPCPs riverine discharges in estuarine regions.


Subject(s)
Cosmetics , Water Pollutants, Chemical , Caffeine/analysis , Carbamazepine/analysis , China , Cosmetics/analysis , Ecosystem , Environmental Monitoring/methods , Erythromycin , Pharmaceutical Preparations , Risk Assessment , Rivers/chemistry , Sulfamethoxazole , Water/analysis , Water Pollutants, Chemical/analysis
8.
Environ Pollut ; 307: 119568, 2022 Aug 15.
Article in English | MEDLINE | ID: mdl-35661806

ABSTRACT

Modelling natural attenuation is crucial to managing pharmaceuticals. However, little is known about the mechanism behind their in-stream sorption. To better understand the in-stream attenuation of the highly sorptive antibiotics azithromycin (AZM) and levofloxacin (LVF), we monitored them in a 2.1-km stretch of the Asano River under diverse flow conditions. This stretch receives effluent directly from a sewage treatment plant (STP), which was a dominant source of the pharmaceuticals. Average distribution coefficients between dissolved and particulate phases (Kd,SPM) in the outflow river water were 6.3×105 L/kg for AZM and 7.5×104 L/kg for LVF, while those in the STP effluent were 1-2 orders of magnitude lower. Mass balances in the river stretch calculated by considering only dissolved phase (MBw) and both dissolved and particulate phases (MBs) were 8%-52% and 58%-102%, respectively, for AZM, and 58%-71% and 60%-105% for LVF. MBw

Subject(s)
Rivers , Water Pollutants, Chemical , Azithromycin , Environmental Monitoring/methods , Geologic Sediments , Levofloxacin , Particulate Matter/analysis , Pharmaceutical Preparations , Sewage , Water , Water Pollutants, Chemical/analysis
9.
Phytomedicine ; 103: 154196, 2022 Aug.
Article in English | MEDLINE | ID: mdl-35667259

ABSTRACT

BACKGROUND: Edible fungi resources have good application prospects in the research and development of food, medicine, and health products. Polyporus umbellatus (Pers.) Fries, as a precious edible and medicinal fungus, has long been used by Chinese medicine to treat urinary systems and related kidney diseases. PURPOSE: In recent years, researchers have discovered and isolated a variety of active compounds from P. umbellatus. Modern phytochemical and pharmacological experiments showed that the crude extract of P. umbellatus had many biological functions and could be widely used in the fields of food, pharmaceutical and cosmetics. This paper summarizes the active components of P. umbellatus, through elaborating its mechanism of action, further clarify the action substances, in order to improve the utilization rate of P. umbellatus, promote the development and application of P. umbellatus in food, pharmaceutical and cosmetics industry. METHODS: In this paper, the literatures related to P. umbellatus were summarized and classified by "China National Knowledge Instructure (CNKI)", "Google Scholar" and "Web of Science". Compared with other articles, this work systematically sorted out all the active substances with clear structures in P. umbellatus. On this basis, combined with the chemical composition of P. umbellatus, its functional efficacy was expounded, and the effects of different types of active substances in P. umbellatus were further presented. RESULTS: The main chemical constituents of P. umbellatus include polysaccharide and sterol, and the secondary compounds include fatty acids, phenols and other small molecules. These active substances endowed P. umbellatus anti-cancer, antibacterial, diuretic, antioxidant, enhance immune system, promote hair growth and other pharmacological activities, which has been verified many times in vivo and in vitro experiments. CONCLUSION: Modern in vitro or in vivo pharmacological experiments and clinical practice for the efficacy of P. umbellatus provides a strong support, and the separation of compounds in P. umbellatus has also deepened people's understanding of this traditional Chinese medicine, greatly promoted the development and application of P. umbellatus. However, the complex active substances of poring also hinder the research of P. umbellatus to some extent, and the mechanism of action and potential synergistic or antagonistic effect of the mixture of various active ingredients have not been clearly analyzed. How to use the bioactivity-guided separation strategy to identify more bioactive components and analyze the molecular mechanism of the main active components have become the main problems of P. umbellatus research, but also provides a direction for the further study of it.


Subject(s)
Polyporus , Diuretics/pharmacology , Ethnopharmacology , Humans , Medicine, Chinese Traditional , Pharmaceutical Preparations , Phytochemicals/pharmacology , Polyporus/chemistry
10.
Chemosphere ; 303(Pt 3): 135227, 2022 Sep.
Article in English | MEDLINE | ID: mdl-35671817

ABSTRACT

Single-use plastics (SUPs) have become an essential constituent of our daily life. It is being exploited in numerous pharmaceutical and healthcare applications. Despite their advantages and widespread use in the pharma and medical sectors, the potential clinical problems of plastics, especially the release of micro-nanoplastics (MNPs) and additives from medical plastics (e.g. bags, containers, and administrative sets) and sorption of drugs remain understudied. Certainly, the MNPs are multifaceted stressors that cause detrimental effects to the ecosystem and human health. The origin and persistence of MNPs in pharmaceutical products, their administration to humans, endurance and possible health implication, translocation, and excretion have not been reviewed in detail. The prime focus of this article is to conduct a systematic review on the leaching of MNPs and additives from pharmaceutical containers/administrative sets and their interaction with the pharmaceutical constituents. This review also explores the primary and secondary routes of MNPs entry from healthcare plastic products and their potential health hazards to humans. Furthermore, the fate of plastic waste generated in hospitals, their disposal, and associated MNPs release to the environment, along with preventive, and alternative measures are discussed herein.


Subject(s)
Plastics , Water Pollutants, Chemical , Ecosystem , Humans , Pharmaceutical Preparations , Water Pollutants, Chemical/analysis
11.
Biomolecules ; 12(6)2022 Jun 04.
Article in English | MEDLINE | ID: mdl-35740909

ABSTRACT

Cancer is one of the main causes of death worldwide. To date, and despite the advances in conventional treatment options, therapy in cancer is still far from optimal due to the non-specific systemic biodistribution of antitumor agents. The inadequate drug concentrations at the tumor site led to an increased incidence of multiple drug resistance and the appearance of many severe undesirable side effects. Nanotechnology, through the development of nanoscale-based pharmaceuticals, has emerged to provide new and innovative drugs to overcome these limitations. In this review, we provide an overview of the approved nanomedicine for cancer treatment and the rationale behind their designs and applications. We also highlight the new approaches that are currently under investigation and the perspectives and challenges for nanopharmaceuticals, focusing on the tumor microenvironment and tumor disseminate cells as the most attractive and effective strategies for cancer treatments.


Subject(s)
Antineoplastic Agents , Neoplasms , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Humans , Nanomedicine , Neoplasms/drug therapy , Neoplasms/pathology , Pharmaceutical Preparations , Tissue Distribution , Tumor Microenvironment
12.
BMC Bioinformatics ; 23(1): 218, 2022 Jun 07.
Article in English | MEDLINE | ID: mdl-35672685

ABSTRACT

BACKGROUND: Due to their diverse bioactivity, natural product (NP)s have been developed as commercial products in the pharmaceutical, food and cosmetic sectors as natural compound (NC)s and in the form of extracts. Following administration, NCs typically interact with multiple target proteins to elicit their effects. Various machine learning models have been developed to predict multi-target modulating NCs with desired physiological effects. However, due to deficiencies with existing chemical-protein interaction datasets, which are mostly single-labeled and limited, the existing models struggle to predict new chemical-protein interactions. New techniques are needed to overcome these limitations. RESULTS: We propose a novel NC discovery model called OptNCMiner that offers various advantages. The model is trained via end-to-end learning with a feature extraction step implemented, and it predicts multi-target modulating NCs through multi-label learning. In addition, it offers a few-shot learning approach to predict NC-protein interactions using a small training dataset. OptNCMiner achieved better prediction performance in terms of recall than conventional classification models. It was tested for the prediction of NC-protein interactions using small datasets and for a use case scenario to identify multi-target modulating NCs for type 2 diabetes mellitus complications. CONCLUSIONS: OptNCMiner identifies NCs that modulate multiple target proteins, which facilitates the discovery and the understanding of biological activity of novel NCs with desirable health benefits.


Subject(s)
Deep Learning , Diabetes Mellitus, Type 2 , Humans , Machine Learning , Pharmaceutical Preparations , Proteins
13.
Article in Russian | MEDLINE | ID: mdl-35670410

ABSTRACT

The third report, which is a continuation of article on the Russian pharmaceutical branch in the 1990s, analyses corresponding conceptions of internal observers (participators of production and distribution of medications), including their assessments of normality of emerging market. The conclusion is made that the Russian pharmaceutical market grew from chaos that resulted from wreckage of the Soviet medication supply system in 1994-1998. The general dominance of generics over patented medications, distributors over manufacturers, weak interest of state authorities to long-term cooperation with pharmaceutics for the sake of development of own national production, low legal culture were generic characteristics of its infrastructure.


Subject(s)
Drug Industry , Pharmaceutical Preparations , Russia
14.
Int J Mol Sci ; 23(11)2022 May 25.
Article in English | MEDLINE | ID: mdl-35682643

ABSTRACT

The prevalence of Alzheimer's disease (AD) has been a major health concern for a long time. Despite recent progress, there is still a strong need to develop effective disease-modifying therapies. Several drugs have already been approved to retard the progression of AD-related symptoms; however, there is a need to develop an effective carrier system for the delivery of drugs to combat such diseases. In recent years, various biological macromolecules, including proteins, have been used as carriers for drug delivery. Irisin is a beneficial hormone in such diseases, including AD and related pathologies. Herein, the interaction mechanism of irisin with AD drugs such as memantine, galantamine, and fluoxetine is investigated. Fluorescence studies revealed that the above drugs bind to irisin with significant affinity, with fluoxetine having the highest binding affinity. Isothermal titration calorimetry (ITC) complemented the spontaneous binding of these drugs with irisin, delineating various associated thermodynamic and binding parameters. Molecular docking further validated the fluorescence and ITC results and unfolded the mechanism that hydrogen bonding governs the binding of fluoxetine to irisin with a significant binding score, i.e., -6.3 kcal/mol. We believe that these findings provide a promising solution to fight against AD as well as a platform for further research to utilize irisin in the drug-delivery system for an effective therapeutic strategy.


Subject(s)
Alzheimer Disease , Fibronectins , Alzheimer Disease/drug therapy , Binding Sites , Calorimetry/methods , Fluoxetine , Humans , Molecular Docking Simulation , Pharmaceutical Preparations , Protein Binding , Spectrometry, Fluorescence , Thermodynamics
15.
Int J Mol Sci ; 23(11)2022 May 29.
Article in English | MEDLINE | ID: mdl-35682788

ABSTRACT

Element analysis in clinical or biological samples is important due to the essential role in clinical diagnostics, drug development, and drug-effect monitoring. Particularly, the specific forms of element binding, actual redox state, or their spatial distribution in tissue or in single cells are of interest in medical research. This review summarized exciting combinations of sophisticated sample delivery systems hyphenated to inductively coupled plasma-mass spectrometry (ICP-MS), enabling a broadening of information beyond the well-established outstanding detection capability. Deeper insights into pathological disease processes or intracellular distribution of active substances were provided, enabling a better understanding of biological processes and their dynamics. Examples were presented from spatial elemental mapping in tissue, cells, or spheroids, also considering elemental tagging. The use of natural or artificial tags for drug monitoring was shown. In the context of oxidative stress and ferroptosis iron, redox speciation gained importance. Quantification methods for Fe2+, Fe3+, and ferritin-bound iron were introduced. In Wilson's disease, free and exchangeable copper play decisive roles; the respective paragraph provided information about hyphenated Cu speciation techniques, which provide their fast and reliable quantification. Finally, single cell ICP-MS provides highly valuable information on cell-to-cell variance, insights into uptake of metal-containing drugs, and their accumulation and release on the single-cell level.


Subject(s)
Hepatolenticular Degeneration , Trace Elements , Humans , Iron , Mass Spectrometry/methods , Metals/analysis , Pharmaceutical Preparations , Trace Elements/analysis
16.
Molecules ; 27(11)2022 Jun 02.
Article in English | MEDLINE | ID: mdl-35684516

ABSTRACT

Yeast particles (YPs) are 3-5 µm hollow and porous microspheres, a byproduct of some food grade yeast (Saccharomyces cerevisiae) extract manufacturing processes. Terpenes can be efficiently encapsulated inside YPs by passive diffusion through the porous cell walls. As previously published, this YP terpene encapsulation approach has been successfully implemented (1) to develop and commercialize fungicide and nematicide products for agricultural applications, (2) to co-load high potency agrochemical actives dissolved in terpenes or suitable solvents, and (3) to identify YP terpenes with broad-acting anthelmintic activity for potential pharmaceutical applications. These first-generation YP terpene materials were developed with a <2:1 terpene: YP weight ratio. Here we report methods to increase the terpene loading capacity in YPs up to 5:1 terpene: YP weight ratio. Hyper-loaded YP terpenes extend the kinetics of payload release up to three-fold compared to the commercialized YP terpene formulations. Hyper-loaded YP-terpene compositions were further optimized to achieve high terpene storage encapsulation stability from -20 °C to 54 °C. The development of hyper-loaded YP terpenes has a wide range of potential agricultural and pharmaceutical applications with terpenes and other compatible active substances that could benefit from a delivery system with a high payload loading capacity combined with increased payload stability and sustained release properties.


Subject(s)
Disinfectants , Terpenes , Drug Compounding , Pharmaceutical Preparations/chemistry , Saccharomyces cerevisiae , Terpenes/chemistry
17.
Huan Jing Ke Xue ; 43(6): 2996-3004, 2022 Jun 08.
Article in Chinese | MEDLINE | ID: mdl-35686769

ABSTRACT

The seasonal variation and spatial distribution of pharmaceuticals in typical drinking water sources in the middle reaches of the Yangtze River were analyzed using the solid-phase extraction and high-performance liquid chromatography-tandem mass spectrometry methods. Combined with the risk entropy method, the corresponding ecological risks for aquatic organisms were evaluated. The results showed that 80% of the target pharmaceuticals were detected in the drinking water sources, with average concentrations of 0.07-13.00 ng·L-1. The concentrations of the target pharmaceuticals were lower than or comparable with those in other drinking water sources reported in China. The spatiotemporal distribution of different pharmaceuticals varied. Generally, the detection level in winter was higher than that in summer, and there was no significant difference between that upstream and that downstream. This might be mainly attributed to seasonal/regional use and emissions of the pharmaceuticals, the impact of flow rate on dilution, and the impact of temperature on biodegradation. Compared with those before the COVID-19 epidemic, the detection concentrations of the target pharmaceuticals were relatively low. The reason for this might be that the prevention and control of the epidemic reduced the use and emission of the pharmaceuticals to a certain extent, and the high rainfall and runoff strengthened the dilution of water flow. The target pharmaceuticals, especially antibiotics, posed medium or low risks to aquatic organisms (especially algae). Considering the ecological risks and genotoxicity of pharmaceuticals and the potential risks of antibiotic-resistant genes, it is suggested to strengthen the investigation, evaluation, treatment, and control of pharmaceuticals in the water environment.


Subject(s)
COVID-19 , Drinking Water , Water Pollutants, Chemical , Anti-Bacterial Agents/analysis , Aquatic Organisms , China , Drinking Water/analysis , Environmental Monitoring/methods , Humans , Pharmaceutical Preparations , Risk Assessment , Water Pollutants, Chemical/analysis
18.
J Invasive Cardiol ; 34(6): E469-E476, 2022 Jun.
Article in English | MEDLINE | ID: mdl-35652710

ABSTRACT

OBJECTIVE: The application of 2 distinct and simultaneously applied drug-delivery platforms for the treatment of peripheral artery disease (PAD) has not been studied. This study investigated the outcomes of femoropopliteal disease treated with drug-coated balloon (DCB) followed by placement of drug-eluting stent (DES) when a bail-out procedure is required. METHODS: This was a single-center, retrospective study enrolling 22 consecutive patients (23 limbs) treated with DCB + DES. Bail-out stenting was performed for flow-limiting postangioplasty dissections and/or suboptimal angiographic result, such as residual stenosis. Procedural success (<30% residual stenosis) and the incidence of major adverse limb event (MALE) during an average follow-up of 15.2 months were estimated. RESULTS: Among the 22 patients (23 limbs), 14 presented with claudication and 8 with critical limb ischemia. The majority of the lesions were Trans-Atlantic Inter-Society Consensus class C/D, with a mean lesion length of 321 ± 130 mm. DCB angioplasty was performed with Stellarex (Philips) in 6 cases and In.Pact DCB (Medtronic) in 16 cases. Eluvia DES (Boston Scientific) was used for bail-out stenting in all cases (in 10 limbs for flow-limiting dissection and in 13 limbs for suboptimal angiographic result due to significant residual stenosis and/or recoil). A single Eluvia DES was used in 15 cases, while multiple Eluvia DESs were used in 8 cases. Procedural success was achieved in all but 1 case where persistent recoil occurred in a heavily calcified lesion. During an average follow-up of 15 months, restenosis or reocclusion of the target vessel was observed in 6 cases (26.1%), although only 3 patients required repeat revascularization (13.0%). During follow-up, 1 death and 1 major amputation occurred, both in patients who had originally presented with critical limb ischemia. Additionally, on routine duplex ultrasound, there were no cases of aneurysm formation at the sites of Eluvia stent placement. CONCLUSION: DCB with provisional DES implantation could be a viable treatment option for cases of suboptimal DCB results, without apparent additional cardiovascular or limb-related risks. Additional studies are needed to determine the risks and benefits of double-dose paclitaxel approach, especially for those patients with significant residual stenosis after DCB.


Subject(s)
Angioplasty, Balloon , Drug-Eluting Stents , Angioplasty, Balloon/adverse effects , Constriction, Pathologic/diagnosis , Constriction, Pathologic/etiology , Humans , Paclitaxel/pharmacology , Pharmaceutical Preparations , Retrospective Studies
19.
Int J Pharm Compd ; 26(3): 201-209, 2022.
Article in English | MEDLINE | ID: mdl-35657743

ABSTRACT

An investigational drug study is a biomedical or health-related research study in humans or animals that follows a predefined protocol. Preclinical studies involve the testing of potential drugs in the laboratory setting or in animals and typically are conducted before a clinical study. In the medical and pharmaceutical literature, hundreds of clinical and investigational studies are reported annually comparing the effects of different drugs, dosage forms, and delivery systems. These studies may compare different products, or they may compare a product with a placebo. A compounding pharmacist is often the source of the products used in these drug studies.


Subject(s)
Pharmacy , Drug Compounding/methods , Humans , Pharmaceutical Preparations , Pharmacists
20.
Int J Pharm Compd ; 26(3): 214-217, 2022.
Article in English | MEDLINE | ID: mdl-35657745

ABSTRACT

Enteral feeding has increased in recent years along with the various methods and equipment utilized. Oftentimes, it is necessary to administer medications via enteral tubes, and care must be observed to maintain the proper flow through the tubes. This is done by proper maintenance to prevent clogging and even removing clogs if they occur. Proper choice of a vehicle to administer a drug is critical for the patient to receive the benefit of drug therapy and to properly maintain the usefulness of the enteral feeding.


Subject(s)
Enteral Nutrition , Intubation, Gastrointestinal , Excipients , Humans , Pharmaceutical Preparations
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