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1.
Artigo em Inglês | MEDLINE | ID: mdl-38706354

RESUMO

The meninges serve as a protective layer, and the fluid around the brain and spinal cord can become inflamed, known as meningitis. Lipid-based pharmaceutical formulations, by their high lipophilicity, can negotiate the Blood-Brain Barrier (BBB). The current mode of treatment of meningitis is mainly through antibiotics, which, at best, is partially effective. The success of antibiotic therapy depends on several factors, for example, the difficulty of reaching the infection site, maintaining proper concentrations of the drug after crossing the BBB, and finally, its efficacy in preventing recurrent infection. In this context, interest has focused on organic and inorganic nanostructures for meningitis and transporting antibiotics to the selected region through the BBB. A focus has also been placed on several polymeric nanotechnology techniques for detecting various types of meningitis. This review focuses on nano interventions and their most recent meningitis treatments using nanotechnology.

2.
Heliyon ; 9(3): e14259, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36938401

RESUMO

Background: The combination of empagliflozin and sitagliptin to treat type-2 diabetes might be more economical and patient compliance with an additive improvement in glycemic control due to complementary modes of action. Aim of the study: To design, formulate and optimize an immediate tablet dosage form containing empagliflozin and sitagliptin utilizing statistically reliable study design followed by in-vitro and in-vivo testing. Method: ology: To determine the effects of copovidone (X1) and croscarmellose sodium (X2) amounts on the dependent variables of disintegration time and percent drug release, the formulation was developed using Design Expert Software v.13's direct compression method-based central composite design optimization study. The formulations' assay, dissolution, friability, hardness, weight variation, disintegration, and anti-diabetic effects were evaluated in comparison to the standard drug. The analysis included the use of high performance liquid chromatography (HPLC) assay methods. Mice were employed to investigate the efficacy of an anti-diabetic drug after they were administered a high-fat diet and two injections of streptozotocin at a dosage of 30 mg/kg BW each. Results: Formulation of F3 out of nine had all in-vitro parameters at the most satisfactory condition. It was found that assay of the best formulation is 100.99% and 100.19% for empagliflozin and sitagliptin respectively. The disintegration time of F3 was found at 5.32 min. Percentage release of empagliflozin in 30 min was found 89.05% while sitagliptin was with 93.76%. The results showed that administration of F3 significantly reduced FBG (68.61%, p < 0.0001), total cholesterol levels (70.29 ± 0.48; p < 0.0001), triglycerides (70.20 ± 0.40, p < 0.0001); HDL levels (52.50 ± 0.31; p < 0.0001), LDL levels (33.34 ± 0.28; p < 0.0001), compared to diabetic control, this effect was comparable to metformin treatment. Conclusion: The direct compression approach has been used to develop, and optimize a new combination tablet incorporating empagliflozin and sitagliptin with better dissolution rate and anti-diabetic action.

3.
Biomed Pharmacother ; 143: 112185, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34543985

RESUMO

Bauhinia scandens L. (Family, Fabaceae) is a medicinal plant used for conventional and societal medication in Ayurveda. The present study has been conducted to screen the chemical, pharmacological and biochemical potentiality of the methanol extracts of B. scandens stems (MEBS) along with its related fractions including carbon tetrachloride (CTBS), di-chloromethane (DMBS) and n-butanol (BTBS). UPLC-QTOF-MS has been implemented to analyze the chemical compounds of the methanol extracts of Bauhinia scandens stems. Additionally, antinociceptive and anti-inflammatory effects were performed by following the acetic acid-induced writhing test and formalin-mediated paw licking test in the mice model. The antipyretic investigation was performed by Brewer Yeast induced pyrexia method. The clot lysis method was implemented to screen the thrombolytic activity in human serum. Besides, the in silico study was performed for the five selected chemical compounds of Bauhinia scandens, found by UPLC-QTOF-MS By using Discover Studio 2020, UCSF Chimera, PyRx autodock vina and online tools. The MEBS and its fractions exhibited remarkable inhibition in dose dependant manner in the antinociceptive and antiinflammatory investigations. The antipyretic results of MEBS and DMBS were close to the standard drug indomethacin. Investigation of the thrombolytic effect of MEBS, CTBS, DMBS, and BTBS revealed notable clot-lytic potentials. Besides, the phenolic compounds of the plant extracts revealed strong binding affinity to the COX-1, COX-2, mPGES-1 and plasminogen activator enzymes. To recapitulate, based on the research work, Bauhinia scandens L. stem and its phytochemicals can be considered as prospective wellsprings for novel drug development and discovery by future researchers.


Assuntos
Analgésicos/farmacologia , Anti-Inflamatórios/farmacologia , Antipiréticos/farmacologia , Bauhinia , Fibrinolíticos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Analgésicos/isolamento & purificação , Analgésicos/metabolismo , Analgésicos/toxicidade , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/toxicidade , Antipiréticos/isolamento & purificação , Antipiréticos/metabolismo , Antipiréticos/toxicidade , Bauhinia/química , Coagulação Sanguínea/efeitos dos fármacos , Modelos Animais de Doenças , Feminino , Febre/metabolismo , Febre/microbiologia , Febre/prevenção & controle , Fibrinolíticos/isolamento & purificação , Fibrinolíticos/metabolismo , Fibrinolíticos/toxicidade , Humanos , Inflamação/induzido quimicamente , Inflamação/metabolismo , Inflamação/prevenção & controle , Masculino , Camundongos , Simulação de Acoplamento Molecular , Dor/induzido quimicamente , Dor/metabolismo , Dor/prevenção & controle , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/metabolismo , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/metabolismo , Extratos Vegetais/toxicidade , Caules de Planta , Ligação Proteica
4.
ACS Appl Bio Mater ; 4(4): 3089-3100, 2021 04 19.
Artigo em Inglês | MEDLINE | ID: mdl-35014397

RESUMO

Because of the emergence of multidrug-resistant pathogenic bacteria, there is a growing interest for the development of an efficient alternative to antibiotics. Gold nanoparticles (AuNPs) are promising candidates due to their inherent non-toxicity and can be used as effective carriers of drugs. Cholera caused by Gram-negative Vibrio cholerae is still a potential threat in many developing countries. Virstatin, a small molecule, has been reported to inhibit virulence regulation in V. cholerae. Herein, we report an efficient synthesis of virstatin-conjugated gold nanoparticles (VL-AuNPs) and their antibacterial efficacy against the El Tor biotype of V. cholerae (VcN16961). The spherical-shaped NPs have an average diameter of ∼17 nm. The uniqueness of VL-AuNPs relies in the enhanced antibacterial efficacy compared to virstatin, as evidenced from the inhibitory concentration obtained from growth kinetics, and attributed to the inhibition of ATPase activity and DNA damage. More importantly, the expression of cholera toxin, the most important virulence factor of V. cholera, is reduced to a far greater extent than by any of the component molecules. The effect of VL-AuNPs on VcN16961 was monitored using various assays such as confocal microscopy, FACS, fluorescence spectroscopy, and so on. Overall, VL-AuNPs could be a potential candidate for the use as an effective agent for combating diarrheal diseases caused by V. cholera.


Assuntos
Antibacterianos/farmacologia , Materiais Biocompatíveis/farmacologia , Butiratos/farmacologia , Ouro/farmacologia , Nanopartículas Metálicas/química , Naftalimidas/farmacologia , Vibrio cholerae O1/efeitos dos fármacos , Antibacterianos/síntese química , Antibacterianos/química , Materiais Biocompatíveis/síntese química , Materiais Biocompatíveis/química , Butiratos/química , Ouro/química , Cinética , Teste de Materiais , Testes de Sensibilidade Microbiana , Estrutura Molecular , Naftalimidas/química , Tamanho da Partícula , Vibrio cholerae O1/crescimento & desenvolvimento
20.
J Colloid Interface Sci ; 439: 54-61, 2015 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-25463175

RESUMO

HYPOTHESIS: Undoped TiO2 nanoparticles are considered as a poor photocatalytic candidate in visible light due to the wide band gap. Incorporation of Gd ions is expected to modulate the electronic structure of the material and thereby enhance the photocatalytic properties of the material. EXPERIMENTS: Gadolinium doped TiO2 nanoparticles were fabricated via a simple sol-gel method. FINDINGS: The surface area of Gd doped TiO2 (225m(2)/g) nanoparticles is much higher than that of undoped TiO2 (95m(2)/g). Doping of Gadolinium enhances the visible light absorption property of TiO2 nanoparticles. Photoluminescence intensity increases at 0.03 and 0.05mol and thereafter reduces at 0.07mol. The photocatalytic efficiency of these nanoparticles is evaluated by observing degradation of phenol in aqueous solution under visible light. The doped nanoparticles are found to exhibit better photocatalytic activity. This enhancement has been attributed to the introduction of the Gd 4f energy levels in the band gap of TiO2. The presence of these states has been further confirmed by theoretical study based on density functional theory (DFT). It is speculated that the 4f states of Gd act as efficient electron trap centers. These 4f states facilitate electron migration to the surface making available free carriers to take part in photocatalysis.

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