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1.
Luminescence ; 39(7): e4816, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38965898

RESUMO

Bilastine, a new second generation antihistaminic drug, has been widely used for relieving symptoms of allergic rhinitis and urticaria without a sedative effect. A simple, cost-effective, and highly sensitive fluorimetric method was developed for the estimation of bilastine in human plasma, in addition to its pure state and tablets. The suggested method depended on binary complex formation of eosin with bilastine in a buffered medium at pH 4.2. The formed complex resulted in quantitative quenching of eosin emission at 538 nm after excitation at 335 nm. This method demonstrates a broad range of linearity, spanning from 200 to 1000 ng/mL, and exhibits exceptional sensitivity, with a limit of detection and quantitation of 30.85 and 93.48 ng/mL, respectively. In addition, this spectrofluorimetric method may be employed to determine the amount of bilastine in human plasma and tablets with satisfactory accuracy and excellent precision. Furthermore, the content uniformity of bilastine in commercially available tablets was successfully tested by this approach. Compared with the reference method, there were no significant variations in terms of precision or accuracy. In conclusion, the proposed protocol is highly recommended to quantitatively estimate bilastine in different quality control settings.


Assuntos
Benzimidazóis , Piperidinas , Espectrometria de Fluorescência , Comprimidos , Humanos , Piperidinas/sangue , Piperidinas/química , Espectrometria de Fluorescência/métodos , Benzimidazóis/sangue , Benzimidazóis/química , Limite de Detecção , Azul de Eosina I/química , Concentração de Íons de Hidrogênio
2.
Front Pharmacol ; 15: 1389670, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38910880

RESUMO

Background: Acute pancreatitis (AP) is an inflammatory condition that resolves spontaneously, but occasionally, develops into systemic inflammation, organ failure and mortality. Oxidative stress and activation of inflammatory pathways represent major players in AP pathogenesis. Current management of AP relies on attenuating injuries to the pancreas and putting the inflammatory process under control. In this study, we investigated the role of sitagliptin in modulating L-arginine-induced AP in rats. Methods: Swiss rats were subdivided into a healthy control group, AP group (a single dose of L-arginine 250 mg/100 g, intraperitoneal), and sitagliptin + L-arginine-treated group (10 mg sitagliptin/kg body weight/day, orally). Sitagliptin treatment started 1 hour after L-arginine injection and continued for 3days. Biochemical and histopathological investigations were performed on serum and tissue samples collected from test animals. Results: L-arginine increased pancreatic meyloperoxidase and serum amylase- and lipase activities and serum levels of TNF-α, LT-α, IFN-γ, IL-1α/ß, IL-6, IL-10, IL-12, and IL-15. AP animals showed elevated MDA and NO and decreased GSH and serum calcium levels. Histopathological changes were observed by H&E staining. Sitagliptin treatment significantly ameliorated these biochemical and histological changes diminishing the signs of AP. Conclusion: Sitagliptin treatment was effective in ameliorating L-arginine-induced AP which can be regarded to its anti-inflammatory and antioxidant effect.

3.
Pathogens ; 12(6)2023 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-37375522

RESUMO

BACKGROUND: Helicobacter pylori (H. pylori) is significantly linked to various diseases that seriously impact human health, such as gastric ulcers, chronic gastritis and gastric adenocarcinoma. METHODS: The compositional shifts in bacterial communities of the orointestinal axis were surveyed pre/post-eradication of H. pylori. In total, 60 samples, including stool and salivary specimens, were collected from 15 H. pylori-positive individuals (HPP) before beginning and 2 months after receiving the eradication therapy. The V3-V4 regions of the 16S rRNA gene were sequenced using MiSeq. RESULTS: Overall, oral microbiomes were collectively more diverse than the gut microbiomes (Kruskal-Wallis; p = 3.69 × 10-5). Notably, the eradication of H. pylori was associated with a significant reduction in the bacterial diversity along the orointestinal axis (Wilcoxon rank sum test; p = 6.38 × 10-3). Interestingly, the oral microbiome of HPP showed a positive correlation between Proteobacteria and Fusobacteria, in addition to a significant predominance of Streptococcus, in addition to Eubacterium_eligens, Haemophilus, Ruminococcaceae, Actinomyces and Staphylococcus. On the other hand, Fusobacterium, Veillonella, Catenibacterium, Neisseria and Prevotella were significantly enriched upon eradication of H. pylori. Generally, Bacteroidetes and Fusobacteria positively coexisted during H. pylori infection along the orointestinal axis (r = 0.67; p = 0.0006). The eradication of H. pylori was positively linked to two distinctive orotypes (O3 and O4). Orotype O4 was characterized by a robust abundance of Veillonella and Fusobacteria. The gut microbiomes during H. pylori infection showed a remarkable predominance of Clostridium_sensu_stricto_1 and Escherichia_Shigella. Likewise, Bifidobacterium and Faecalibacterium were significantly enriched upon eradication of H. pylori. CONCLUSIONS: Finally, the impact of eradication therapy clearly existed on the representation of certain genera, especially in the oral microbiome, which requires particular concern in order to counteract and limit their subsequent threats.

4.
Trop Med Infect Dis ; 8(5)2023 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-37235301

RESUMO

Conventional scolicidal agents are still unsatisfactory in combating hydatid disease due to their low efficacy and increased drug side effects. Therefore, novel scolicides are required. This study aimed to evaluate the antihydatic and immunomodulatory effects of eugenol essential oil (Eug) and its nanoemulsion (Eug-NE) in cystic echinococcosis (CE). Eug and Eug-NE were administered orally to CE-infected rats and compared to albendazole (ABZ). Hydatid cyst development was assessed based on organ weight and hypertrophy indicators of the infected organs, along with a histopathological and histochemical evaluation of collagen content. The immunomodulatory effects of treatment on CE were evaluated by serum cytokine levels measurement of interferon-γ (IFN-γ) and interleukin (IL)-4 and immunohistochemical (IHC) analysis of signal transducer and activator of transcription 4 (STAT4) and GATA-binding protein 3 (GATA3) markers. Eug-NE was the most effective in reducing the cyst weights, organ weights, and hypertrophy indicators and improving histopathological lesions with reduced collagen content. Eug and Eug-NE significantly increased the IFN-γ levels and decreased the IL-4 levels, while IHC analysis demonstrated a significant reduction in STAT4 and GATA3 expression in all treated groups. Eug and Eug-NE demonstrated antihydatic and preventative effects, with a substantial decrease in liver fibrosis compared to that of ABZ. Besides their promising immunomodulatory effects, their good treatment response suggests their use as alternatives or complementary scolicidal agents in hydatid cyst treatment.

5.
Artigo em Inglês | MEDLINE | ID: mdl-36936543

RESUMO

BACKGROUND: Paracetamol (acetaminophen) is an over-the-counter non-steroidal anti-inflammatory drug that may cause acute toxic overdosage particularly in neuropsychiatric patients. Paracetamol is also very commonly prescribed as an analgesic and antipyretic agent. Paracetamol toxicity causes decreased reduced glutathione and oxidative tissue damage. Aleppo galls is a promising natural remedy exerting antioxidant and tissue-protective effects that may combat acetaminophen-induced oxidative tissue damage. METHODOLOGY: Biochemical and toxicological effects of a toxic dose of paracetamol (250 mg/kg) were investigated for three consecutive days versus the tissue-protective effects of Aleppo galls. Eighteen white albino mice were randomly allocated in this study and divided into three experimental groups (six mice per group): negative control (received intraperitoneal sterile water injection), paracetamol toxicity group (received intraperitoneal paracetamol injection) and the third group (received paracetamol injection at 250 mg/kg/day together with oral Aleppo galls treatment at 250 mg/kg/day for 3 consecutive days). All mice were sacrificed by the end of the study. RESULTS: Our data revealed that paracetamol toxicity exerted significant oxidative stress damaging effects (high serum malondialdehyde, decreased serum catalase and decreased total antioxidant capacity), and significant inflammatory effects (high serum IL-6) and significant tissue-damaging effects (high serum LDH). Aleppo galls treatment significantly protected against acetaminophen toxicity-induced oxidative stress effects (P<0.001), inflammatory effects (P<0.001) and tissue-damaging effects (P<0.001). CONCLUSION: Aleppo galls are promising for future drug therapeutics and for the synthesis of natural remedies for treating paracetamol toxicity. We recommend formulating Aleppo galls extract as a pharmaceutical nutrition and to be given to those who need to take large doses of paracetamol.

6.
Int J Biochem Mol Biol ; 14(1): 1-9, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36936610

RESUMO

BACKGROUND: Acute paracetamol toxicity is a common and potentially life-threatening emergency causing liver failure that may necessitate liver transplantation. Unfortunately, current therapies are still defective. OBJECTIVES: To investigate the protective effects exerted by Aleppo galls (Quercus infectoria Olivier) extract against acute paracetamol toxicity in mice. METHODOLOGY: Eighteen mice were divided into three experimental groups, each included six mice in each group. The groups included: negative control group, paracetamol toxicity group that received an acute toxic intraperitoneal dose of paracetamol (250 mg/kg) for four consecutive days, and treatment group (received 250 mg/kg paracetamol followed few hours later by Aleppo galls extract for the same duration). Animals were anaesthetized using ether anaesthesia. Animals were sacrificed by decapitation and blood samples were drawn. Paracetamol toxicity effects versus Aleppo galls protection were evaluated on liver function tests, liver histology, serum cholesterol and serum triglycerides. RESULTS: Acute paracetamol toxicity caused significantly elevated serum transaminases (ALT and AST), decreased serum albumin, and increased serum cholesterol and triglycerides. Aleppo galls extract exerted significant protective effects and restored near normal serum levels of the previously-mentioned parameters. Upon histopathological evaluation, mice in the control group showed normal hepatic architecture with preserved hepatic cords and sinuses. Acute paracetamol toxicity induced peripheral zonal degeneration with focal necrosis of the hepatic tissue. The hepatocytes showed cytoplasmic vacuolation with indistinct cell borders. Central hepatic venules were congested. Administration of Aleppo galls extract reduced the tissue damaging effects induced by paracetamol toxicity with only minimal residual degenerative changes that were observed with absent necrosis. CONCLUSION: Quercus infectoria Olivier (Aleppo galls) is a promising source of phytochemicals and future therapeutics.

7.
RSC Adv ; 12(52): 33559-33566, 2022 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-36505680

RESUMO

A new, cost-effective and sensitive spectroscopic assay for the quantification of Colistin Sulfate (CS) and its prodrug colistimethate sodium (CMS) has been developed and validated. The validated technique depends on the condensation of the studied drug with 2,2-dihydroxyindan-1,3-dione (ninhydrin) and phenylacetaldehyde using Teorell and Stenhagen buffer (pH = 6) to yield a fluorescent product that is estimated at emission wavelength (λ em = 474 nm) after excitation wavelength (λ ex = 390 nm). The reaction's affecting factors were carefully studied and adjusted accurately. Over the following range (0.4-2.4 µg mL-1), the produced calibration plot looked rectilinear, and the estimated limits of detection and quantification (LOD and LOQ) were 0.051 & 0.154 µg mL-1 respectively. The recommended approach was utilized to evaluate market products containing the investigated drug. Moreover, content uniformity testing was employed as a new procedure not found in the previously reported fluorimetric technique.

8.
Nutrients ; 14(24)2022 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-36558489

RESUMO

Vitamin D is among the increasingly consumed dietary supplements during the COVID-19 pandemic. It plays a regulatory role in the immune system and moderates the renin-angiotensin system, which is implicated in infection pathogenesis. However, the investigation of serum levels of vitamin D3 forms and their relative ratios in COVID-19 patients is worth investigation to understand the impacts of disease severity. Hence, we investigated the serum levels of vitamin D3 (cholecalciferol) and its metabolites (calcifediol and calcitriol), in addition to their relative ratios and correlations with angiotensin-converting enzyme 2 (ACE2), interleukin-6 (Il-6), and neutrophil-lymphocyte ratio (NLR) in COVID-19 patients compared with healthy controls. Oropharyngeal specimens were collected from the study subjects for polymerase chain reaction testing for COVID-19. Whole blood samples were obtained for blood count and NLR testing, and sera were used for the analysis of the levels of the vitamin and its metabolites, ACE2, and IL-6. We enrolled 103 patients and 50 controls. ACE2, Il-6, and NLR were significantly higher in the patients group (72.37 ± 18.67 vs. 32.36 ± 11.27 U/L, 95.84 ± 25.23 vs. 2.76 ± 0.62 pg/mL, and 1.61 ± 0.30 vs. 1.07 ± 0.16, respectively). Cholecalciferol, calcifediol, and calcitriol were significantly lower in patients (18.50 ± 5.36 vs. 29.13 ± 4.94 ng/mL, 14.60 ± 3.30 vs. 23.10 ± 3.02 ng/mL, and 42.90 ± 8.44 vs. 65.15 ± 7.11 pg/mL, respectively). However, their relative ratios were normal in both groups. Levels of the vitamin and metabolites were strongly positively, strongly negatively, and moderately negatively correlated with ACE2, Il-6, and NLR, respectively. COVID-19 infection severity is associated with a significant decrease in vitamin D3 and its metabolites in a parallel pattern, and with a significant increase in ACE2, Il-6, and NLR. Higher levels of vitamin D and its metabolites are potentially protective against severe infection.


Assuntos
COVID-19 , Colecalciferol , Humanos , Enzima de Conversão de Angiotensina 2 , Calcifediol , Calcitriol , Colecalciferol/sangue , COVID-19/diagnóstico , Teste para COVID-19 , Interleucina-6 , Pandemias , Gravidade do Paciente , Prognóstico , Vitamina D , Vitaminas
9.
Healthcare (Basel) ; 10(9)2022 Sep 10.
Artigo em Inglês | MEDLINE | ID: mdl-36141350

RESUMO

The present study was undertaken to assess the current supply chain system of pharmaceuticals and vaccines in Pakistan in terms of structure, process, and outcomes, as well as related barriers and solutions for an effective supply chain system. A qualitative study was designed to explore stakeholders' perceptions selected using the snowball sampling technique. A semi-structured interview guide was used to interview these respondents at a convenient time and place. After data collection, recorded interviews were transcribed verbatim and subjected to thematic analysis. The results highlighted that the standard operating procedures (SOPs), checklists, and government guidelines were available at different levels, except for community pharmacies. Timely delivery of quality products and services along with market reputation, experience, and authorization were the key criteria used for supplier selection and evaluation. Good inventory management, financial models, effective coordination, training, and skill development programs were identified as key factors responsible for an efficient supply chain process. Availability of vaccines, their appropriate temperature monitoring, and transportation are also highly compromised in Pakistan. The results of the present study concluded that the current supply chain system in Pakistan is not up to the mark; major factors include poor forecasting and inventory control, delayed order placement, lack of training, inadequate involvement of professionally qualified staff, inadequate financing and procurement processes, and poor coordination and integration among all stakeholders.

10.
Talanta ; 246: 123497, 2022 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-35487016

RESUMO

It is established that vitamin D deficiency is correlated with the disease severity in COVID-19 patients. However, the reliable and sensitive quantitation of vitamin D3 (D3) and its metabolites remains a difficult challenge. Herein, a novel ultrasensitive and reliable UHPLC-ESI-MS/MS method was developed and validated for the quantitation of D3 and its major metabolites in COVID-19 patients. The mass spectral sensitivity was augmented via controlled microwave-assisted derivatization reaction (CMDR) with 2-nitrosopyridine (Pyr-NO) at 65 °C for 2 min. CMDR hyphenation with UHPLC-MS/MS improves detection sensitivity while shortening separation and derivatization reaction times. The precursor to product ion transitions for D3, 25-hydroxy D3 (25(OH)D3), 1,25-dihydroxy D3 (1,25-(OH)2D3) and calcipotriol (CPT) as an internal standard were m/z 493.4 â†’ 231.3, m/z 509.4 â†’ 231.3, m/z 525.4 â†’ 247.3, and m/z 521.4 â†’ 247.3; respectively. The separation of the formed derivatives was conducted using a gradient elution mode with mobile phase A: formic acid (0.1%) in water and mobile phase B: formic acid (0.1%) in acetonitrile. The elution started with 40% (v/v) of B for 0.3 min then increased linearly to 90% (v/v) at 2 min on an Agilent EclipsePlus C18 (50 × 2.1 mm, 1.8 µm) column at a flow rate of 0.3 mL min-1. The method was validated using FDA standards for bioanalytical method validation over a concentration range of 0.02-50 ng mL-1 with correlation coefficient ≥0.9987 and the lower limit of quantitation (LLOQ) were 0.02-0.05 ng mL-1 in human plasma. The developed method has demonstrated excellent comparability to a well-established chemiluminescent immunoassay (CLIA) method for the analysis of D3 metabolites in human samples. The developed UHPLC-ESI-MS/MS method was implemented for routine and reliable quantitation of D3 and its major metabolites in COVID-19 patients.


Assuntos
COVID-19 , Espectrometria de Massas em Tandem , COVID-19/diagnóstico , Colecalciferol , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Micro-Ondas , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem/métodos
11.
Vasc Health Risk Manag ; 17: 471-480, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34408425

RESUMO

BACKGROUND: Vitamin D deficiency is considered an emerging health problem that affects at least one billion patients worldwide. Calcitriol 1,25(OH)2D3 has several systemic effects, including anti-inflammatory, anti-thrombotic and anti-atherosclerotic impacts that explain its cardioprotective effects. The precise association between vitamin D and its metabolites and the value of supplements in acute coronary syndrome (ACS) is still controversial. This study aims to search the association between vitamin D2, D3, and metabolites and ACS in patients undergoing coronary angiography. MATERIALS AND METHODS: This was a case-control study on 73 consecutive adult patients with ACS undergoing coronary angiography compared to 50 controls without coronary artery disease and matched for age and sex from June 2019 till July 2019. Echocardiography and coronary angiography were done for all cases. Plasma vitamin D and its metabolites were measured at admission for all participants along with chemistry profiles. RESULTS: Vitamin D and its metabolites were statistically significantly lower in ACS patients than the controls. Multivariate regression analysis revealed that low levels of 25-hydroxyvitamin D (25(OH)D) and 1,25-dihydroxyvitamin D (1,25(OH)2D) significantly predicted ACS occurrence; the other significant predictors were high systolic blood pressure (BP), high total cholesterol, and low high-density lipoprotein-cholesterol. Interestingly, vitamin D2 and D3 did not significantly predict ACS (p>0.05). We did not find a statistically significant association between the number of affected coronary vessels and vitamin D metabolites. Moreover, there was no statistically significant correlation between vitamin D and its metabolites and left ventricular ejection fraction measured by echocardiography. CONCLUSION: There was a strong association between vitamin D and all its metabolites with ACS. Significantly, low 25(OH)D and 1,25(OH)2D predicted ACS, but vitamin D2 and D3 did not. Large randomized controlled trials are needed to verify the beneficial values of vitamin D supplementation in ACS patients.


Assuntos
Síndrome Coronariana Aguda/diagnóstico por imagem , Angiografia Coronária/métodos , Doença da Artéria Coronariana/complicações , Deficiência de Vitamina D/epidemiologia , Vitamina D , Síndrome Coronariana Aguda/sangue , Síndrome Coronariana Aguda/epidemiologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Estudos de Casos e Controles , Colesterol , Doença da Artéria Coronariana/sangue , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Volume Sistólico , Função Ventricular Esquerda/fisiologia , Vitamina D/administração & dosagem , Vitamina D/análogos & derivados , Vitamina D/sangue , Deficiência de Vitamina D/sangue
12.
Pulm Pharmacol Ther ; 70: 102073, 2021 10.
Artigo em Inglês | MEDLINE | ID: mdl-34418538

RESUMO

Vitamin D affects innate and adaptive immunity processes that impact treatment, severity, and morbidity of acute asthma episodes. Several vitamin D forms may help modulate immunity, including vitamin D2 (D2), vitamin D3 (D3), 25-hydroxyvitamin D3 (25(OH)D3), and 1,25-dihydroxyvitamin D3 (1,25-(OH)2D3). This study assessed serum levels of vitamin D derivatives in bronchial asthma patients and their correlation with disease markers. One hundred thirteen subjects, divided into two groups, were enrolled. The first group included 73 asthmatic patients (57 males and 16 females), and the second included 40 healthy adults (31 males and 9 females) as a control group. All subjects were evaluated with a careful history and clinical examination, a chest X-ray with a posteroanterior view, routine laboratory examination, spirometry, and asthma control tests (ACT). Vitamin D serum levels were assessed using ultra-performance liquid chromatography (UPLC) with tandem mass spectrometry. Disease markers were assessed and correlated with serum levels of vitamin D forms. Markers included forced expiratory volume in 1 s (FEV1), forced vital capacity (FVC), FEV1/FVC%, peak expiratory flow (PEF), forced expiratory flow25-75% (FEF25-75%), eosinophilic blood count, and total immunoglobulin E (IgE). Asthmatic patients had significantly lower serum levels of vitamin D than healthy controls (p ≤ 0.001). Further, serum vitamin D levels decreased significantly in uncontrolled asthmatic patients than partially controlled and controlled patients. Correlations for 25(OH)D3 and 1,25-(OH) 2D3 were stronger than for D2 and D3. There were negative correlations for eosinophilic blood count, total IgE, and ACT. Serum levels of all vitamin D forms were reduced in asthmatic patients with moderate to strong correlations with disease severity. Vitamin D deficiency or even insufficiency may thus play a role in disease severity.


Assuntos
Asma , Calcifediol/uso terapêutico , Deficiência de Vitamina D , Vitamina D/uso terapêutico , Adulto , Asma/tratamento farmacológico , Feminino , Humanos , Masculino , Índice de Gravidade de Doença , Vitamina D/análogos & derivados , Vitaminas/uso terapêutico
13.
Pharmaceuticals (Basel) ; 14(4)2021 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-33915770

RESUMO

Diabetic neuropathic pain (DNP) is a common diabetic complication that currently lacks an efficient therapy. The aim of the current work was to uncover the anti-allodynic and neuroprotective effects of memantine in a model of mouse diabetic neuropathy and its ameliorative effect on the high-mobility group box-1 (HMGB1)/toll-like receptor 4 (TLR4)/nuclear factor-k B (NF-kB) inflammatory axis. Diabetes was prompted by an alloxan injection (180 mg/kg) to albino mice. On the ninth week after diabetes induction, DNP was confirmed. Diabetic mice were randomly allocated to two groups (six mice each); a diabetes mellitus (DM) group and DM+memantine group (10 mg/kg, daily) for five weeks. DNP-related behaviors were assessed in terms of thermal hyperalgesia and mechanical allodynia by hot-plate and von Frey filaments. Enzyme-linked immunosorbent assay (ELISA) kits were used to measure the spinal glutamate, interleukin-1 beta (IL-1ß), and tumor necrosis factor-α (TNF-α). The spinal levels of N-methyl-D-aspartate type 1 receptor (NMDAR1), HMGB1, TLR4, and phosphorylated NF-kB were assessed using Western blotting. Histopathological investigation of the spinal cord and sciatic nerves, together with the spinal cord ultrastructure, was employed for assessment of the neuroprotective effect. Memantine alleviated pain indicators in diabetic mice and suppressed excessive NMDAR1 activation, glutamate, and pro-inflammatory cytokine release in the spinal cord. The current study validated the ability of memantine to combat the HMGB1/TLR4/NF-kB axis and modulate overactive glutamate spinal transmission, corroborating memantine as an appealing therapeutic target in DNP.

14.
Int J Pharm ; 592: 120077, 2021 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-33246047

RESUMO

Despite the fact that atrovastatin (At) is being one of the bestselling statins used to prevent complicated cardiovascular diseases, its low oral bioavailability decreases its clinical relevance. Herein, incorporation of At into ethylcellulose nanoparticles (At-NPs) was executed to test if it would enhance its oral bioavailability. The emulsification-evaporation method was used to prepare the At-NPs. The prepared nanoparticles were characterized by measuring the particle size, zeta potential as well as using FTIR, DSC, and XRD examination. The entrapment efficiency, drug content, and the in vitro release behavior of At-NPs were also examined. The in vivo oral bioavailability of the selected At-NPs formula was tested after being given orally to New Zealand rabbits. The nanoparticles obtained had a high drug content and a distinct spherical shape but with varying sizes. No physical or chemical interactions were detected between At and the nanoparticles as confirmed by FTIR, DSC, and XRD. The in vitro release study of At from the prepared At-NPs has shown nanoparticles size-dependent release behavior. The in vivo oral absorption testing confirmed the bioavailability of the prepared At-NPs to be as follows: (Cmax = 940 ng/ml and AUC0-12 = 8759 ng.h/ml) > Lipitor® (Cmax = 635 ng/ml and AUC0-12 = 4367 ng.h/ml) > At (Cmax = 515 ng/ml and AUC0-12 = 2517 ng.h/ml). These results revealed that the oral formula of At-NPs increases the bioavailability of At 3.87 times. This makes ethylcellulose nanoparticles an esteemed candidate nano-vehicle for At, increasing its bioavailability and thus improving its clinical relevance.


Assuntos
Portadores de Fármacos , Nanopartículas , Administração Oral , Animais , Atorvastatina , Disponibilidade Biológica , Tamanho da Partícula , Coelhos
15.
J Appl Biomed ; 18(2-3): 80-86, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34907729

RESUMO

BACKGROUND: The liver is the main metabolic organ involved in disposal and detoxification of various molecules. Plantago psyllium L. seed has been reported to exert positive effects in some pathological conditions. The current study aims to assess the hepatoprotective effect of Plantago psyllium L. seed extract against carbon tetrachloride-induced hepatotoxicity. METHODS: Male albino Wistar rats were randomly divided into five groups of 10 rats each. Hepatotoxicity was induced by orally administered carbon tetrachloride (CCl4) for nine weeks with or without the different treatments which were utilized daily for the whole nine weeks. Serum and tissue samples were then withdrawn and different liver biomarkers were investigated. RESULTS: Treatment of rats with Psyllium seed ethanolic extract significantly alleviated the toxic effects of CCl4. This was evidenced by its ability to restore liver biomarkers levels. Moreover, treatment with Psyllium seed extract normalized levels of oxidative biomarkers such as lipid peroxidation, hepatic content of reduced glutathione and catalase activity, as well as the expression level of the inflammatory marker TNF-α. Histopathological examination reflected the protective effect of the extract on liver architecture and confirmed the observed biochemical data. CONCLUSIONS: The presented data demonstrates a potential hepatoprotective effect of Psyllium seed extract compared to the standard hepatoprotective drug silymarin. This effect can be attributed to the antioxidant and anti-inflammatory effects of Psyllium extract.


Assuntos
Doença Hepática Induzida por Substâncias e Drogas , Plantaginaceae , Plantago , Psyllium , Animais , Antioxidantes/farmacologia , Tetracloreto de Carbono/toxicidade , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico , Masculino , Extratos Vegetais/farmacologia , Psyllium/farmacologia , Ratos , Ratos Wistar , Sementes
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