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•NR is neuroprotective, reduced infarction, improved motor and cognitive function.•NR ameliorated behavioral parameters, oxidative stress and neuroinflammatory markers.•Data indicate ...that NR has therapeutic potential against ischemic stroke in rat model.
Resveratrol is a nutraceutical compound that has exciting pharmacological potential in different diseases, including stroke. Due to its low bioavailability, the efficacy of resveratrol is minimal. Hence, the present study is aimed to synthesize and characterize nanoparticles of resveratrol (NR) followed by evaluating the neuroprotective role and elucidate the mechanism of NR in a rat model of middle cerebral artery occlusion (MCAO). Male Wistar rats (280–300 g) were pretreated with various doses (125 µg, 250 µg, and NR 500 µg; once daily, i.p.) of NR or vehicle (nanostructured lipid carriers) for 10 days. MCAO was performed for 2 h followed by reperfusion of 22 h. After 24 h of MCAO, animals were tested for the neurological outcome and were sacrificed for the analysis of infarct volume, oxidative, inflammatory, and apoptotic markers. NR-treated rats showed a substantial reduction in infarction compared to saline controls in parallel with improved motor and cognitive function. Further, NR pretreatment ameliorated oxidative stress markers and attenuated activities of antioxidant enzymes and Na+ K+ ATPase. The enhanced activities of caspases −3 and −9 and cytokines: interleukin-1β, and −6, and tumor necrosis factor-ɑ) in the MCAO group were significantly protected with the treatment of 500 µg of NR. Taken together, these data indicate that inhibition by NR has therapeutic potential in the ischemic stroke model. Further investigations into the therapeutic efficacy and post-treatment protocols are needed to confirm whether NR treatment could be a promising candidate for a stroke.
Strategy for effective brain drug delivery Alam, M. Intakhab; Beg, Sarwar; Samad, Abdus ...
European journal of pharmaceutical sciences,
08/2010, Letnik:
40, Številka:
5
Journal Article
Recenzirano
Blood–brain barrier (BBB) together with enzymes restricts the entry of substances for maintaining the internal milieu of the brain. Because of the presence of multiple endogenous transporters, BBB ...allows a selective entry of nutrients and minerals across it and limits the entry of foreign substances like drugs as well as neuropharmaceutical agents. This makes the CNS treatment ineffective. The conventional drug delivery systems which release drug into general circulation fail to deliver drugs effectively to brain and is therefore not very useful in treating certain diseases that affect CNS including Alzheimer's disease, dementia, Parkinson's disease, mood disorder, AIDS, viral and bacterial meningitis. Therefore there is a need to develop and design approaches which specifically target to brain in a better and effective way. The present review enlightens about several novel approaches including nanotechnology based approach like nanoparticles, liposomes, antibody mediated delivery approach and application of genomics in brain drug targeting that would give an insight to the researchers, academia and industrialists.
NLC containing Gefitinib (NANOGEF) was prepared using stearic acid, sesame oil and surfactants (sodium lauryl sulfate and tween 80). NANOGEFs were evaluated for particle size, polydispersity index ...(PdI), zeta potential, entrapment efficiency (EE), stability, release studies and cytotoxicity studies (MTT assay). The optimized NANOGEF exhibited particle size of 74.06 ± 9.73 d.nm, PdI of 0.339 ± 0.029 and EE of 99.76 ± 0.015%. The TEM study revealed spherical shape of NANOGEF formulations. The slow and sustained release behavior was exhibited by all NANOGEFs. The effects of surfactants were observed not only on particle size but also on zeta potential, entrapment efficiency, stability and release studies. The MTT assay revealed 4.5 times increase in cytotoxicity for optimized NANOGEF (IC
50
= 4.642 µM) when compared with Gefitinib alone (IC
50
= 20.88 µM in HCT-116 cells). Thus NANOGEF may be considered as a potential drug delivery system for the cure of colon cancer.
Celotno besedilo
Dostopno za:
DOBA, IZUM, KILJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
Ganoderma lucidum (G. lucidum) polysaccharides and triterpenoids are the major bioactive compounds and have been used as traditional medicine for ancient times. Massive demands of G. lucidum have ...fascinated the researchers towards its application as functional food, nutraceutical and modern medicine owing to wide range of application in various diseases include immunomodulators, anticancer, antiviral, antioxidant, cardioprotective, hepatoprotective. G. lucidum polysaccharides exhibit immunomodulatory properties through boosting the action of antigen-presenting cells, mononuclear phagocyte system, along with humoral and cellular immunity. β-Glucans isolated from G. lucidum are anticipated to produce an immune response through pathogen associated molecular patterns (PAMPs). β-Glucans after binding with dectin-1 receptor present on different cells include macrophages, monocytes, dendritic cells and neutrophils produce signal transduction that lead to trigger the mitogen-activated protein kinases (MAPKs), T cells and Nuclear factor-κB (NF-κB) that refer to cytokines production and contributing to immune response. While triterpenoids produce antiviral effects through inhibiting various enzymes like neuraminidase, HIV-protease, DENV2 NS2B-NS3 protease and HSV multiplication. Polysaccharides and triterpenoids adjunct to other drugs exhibit potential action in prevention and treatment of various diseases. Immunomodulators and antiviral properties of this mushroom could be a potential source to overcome this current pandemic outbreak.
The purpose of this study was to develop a novel nano antibacterial formulation of dextran sulfate sodium polymer. The dextran sulfate sodium (DSS) nanoparticles were formulated with gelation ...technique. The nanoparticles exhibited significant physicochemical and effective antibacterial properties, with zeta potential of - 35.2 mV, particle size of 69.3 z d nm, polydispersity index of 0.6, and percentage polydispersity of 77.8. The DSS nanoparticles were stable up to 102 °C. Differential scanning calorimetry revealed an endothermic peak at 165.77 °C in 12.46 min, while XRD analysis at 2θ depicted various peaks at 21.56°, 33.37°, 38.73°, 47.17°, 52.96°, and 58.42°, indicating discrete nanoparticle formation. Antibacterial studies showed that the DSS nanoparticles were effective against Gram-positive and Gram-negative bacteria. The minimum inhibitory concentrations of DSS nanoparticles for Bacillus subtilis (B. subtilis), Staphylococcus aureus (S. aureus), Streptococcus pyogenes (S. pyogenes), Escherichia coli (E. coli), Pseudomonas aeruginosa (P. aeruginosa), Klebsiella pneumoniae (K. pneumoniae) and Proteus vulgaris (P. vulgaris) were 150, 200, 250, 150, 200, 250, 250 µg/mL, respectively. The antibacterial effects of DSS nanoparticles were in the order E. coli (26 ± 1.2 mm) at 150 µg/mL > S. pyogenes (24.6 ± 0.8 mm) at 250 µg/mL > B. subtilis (23.5 ± 2 mm) at 150 µg/mL > K. pneumoniae (22 ± 2 mm) at 250 µg/mL > P. aeruginosa (21.8 ± 1 mm) at 200 µg/mL > S. aureus (20.8 ± 1 mm) at 200 µg/mL > P. vulgaris (20.5 ± 0.9 mm) at 250 µg/mL. These results demonstrate the antibacterial potency of DSS injectable nanoparticles.
Corona virus disease 2019 (COVID-19) outbreak has become a severe community health threat across the world. Covid-19 is a major illness, presently there is no as such any medicine and vaccine those ...can claim for complete treatment. It is spreading particularly in a feeble immune people and casualties are expanding abruptly and put the health system under strain. Among the strategic measures face mask is one of the most used measures to prevent spread of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Wearing a face mask possibly create a false sense of security lead to decline others measures. Face mask could be risk for the people of under lying medical conditions, old age group, outdoor exercise, acute and chronic respiratory disorders and feeble innate immune. Restrictive airflow due to face mask is the main cause of retention of CO2 called hypercapnia that can lead to respiratory failure with symptoms of tachycardia, flushed skin, dizziness, papilledema, seizure and depression. According to latest updates face shield and social distancing could be better substitute of face mask.
Abstract The present study was aimed to investigate and compare the efficacy of duloxetine (DLX) loaded nanostructured lipid carriers (NLC) with DLX solution pharmacodynamically following intranasal ...administration. The study was further conducted to estimate DLX concentration in brain and blood. DLX was administered to albino Wistar rats either intranasally or orally in solution form (DLX solution) or encapsulated in NLC (DLX–NLC). These were evaluated in-vivo for pharmacodynamic studies for depression by forced swimming test and locomotor activity test. Intranasal DLX–NLC treatment exhibited improved behavioural analysis results (swimming, climbing, and immobility) than the DLX solution after 24 h of study. Furthermore, DLX–NLC significantly increased the total swimming and climbing time when compared with control and significantly reduced the immobility period. The intranasal DLX–NLC demonstrated improved locomotor activity when compared with DLX solution. Amount of DLX was quantified in blood and brain after the forced swimming test. The intranasal DLX–NLC demonstrated higher concentration in brain compared with DLX solution. Thus, intranasal DLX–NLC was found to be a promising formulation for the treatment of depression.
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Efficacy of antidepressants relies upon their continued presence at the site of action (brain) over a prolonged period of time. The BBB restricts the access of antidepressants to the ...brain on oral as well as intravenous administration. Direct delivery (by-passing the BBB) of antidepressant drugs can increase the CSF concentration with concomitant reduction in dose and side effects. Intranasal administration of nanostructured lipid carriers (NLC) containing antidepressant drug circumvent the BBB and maintain the prolonged release at the site of action. The aim of the present study was to evaluate the enhancement in brain uptake of NLC containing duloxetine (DLX) after intranasal administration. Duloxetine loaded NLC (DLX-NLC) was evaluated pharmacoscintigraphically for drug targeting potential (DTP), drug targeting efficiency (DTE) and biodistribution studies in different organs including brain. The radiolabeling efficiency of DLX and DLX-NLC was found to be 98.41±0.96 and 98.87±0.82 after 30min, respectively. The biodistribution studies exhibited higher percentage of radioactivity/g for DLX-NLC formulations in brain as compared with the DLX. The higher DTP (86.80%) and DTE (757.74%) suggested that DLX-NLC formulation has a better brain targeting efficiency than DLX solution (DTP=65.12%; DTE=287.34%) when administered intranasally. Moreover, the intranasal administration exhibited about 8-times higher concentration of DLX in brain when compared with the intravenous administration of DLX solution. The intranasal NLC containing DLX can be employed as an effective method for the treatment of depression.
Acetaminophen (APAP) is a well-known antipyretic and analgesic medicine. It is safe at therapeutic suggested level while overdose initiates oxidative stress and inflammation mediated neurochemical ...alteration in the brain. The aim of this study was to investigate the role of cinnamon oil (CO), which possesses potent antioxidant and anti-inflammatory activities against an overdose of APAP that induced oxidative stress and inflammation in male albino rats. APAP treated rats showed significant elevation of thiobarbituric acid-reactive substances (TBARS) and decreased level of GSH in brain tissue, which is recognized as a biomarker of oxidative stress. Antioxidant enzymes GPx, GR, SOD, and CAT activity was depleted in APAP group along with neurotoxicity biomarkers such as Na
+
-K
+
-ATPase and increased activity of acetylcholinesterase (AchE), monoamine oxidase (MAO), and upregulated pro-inflammatory cytokine was observed. CO significantly protected the diminished activity of the antioxidant enzyme and suppressed the upregulated cytokines in brain tissue. CO also attenuated the activity of neurotoxicity biomarker enzyme, decreased TBARS content, and an increased level of GSH. The present findings perceptibly confirmed that the nutraceutical property of CO ameliorates APAP induced oxidative stress and inflammation. Therefore, our findings suggested that CO could be an alternative nutraceutical substitute in APAP overdose poisoning.
Celotno besedilo
Dostopno za:
DOBA, IJS, IZUM, KILJ, NUK, PILJ, PNG, SAZU, UILJ, UKNU, UL, UM, UPUK
Background: One of the imperative progressions within the pharmaceutical industry, especially drugs, is the expanded utilization of materials in order to enhance its dissolution, solubility and ...bioavailability. Planetary ball monomill approach can be the latest entrant to Green nanotechnology - being solvent-free, eco-friendly, cost-effective, and sustainable particle size reduction approach. Objectives: Salicylic acid nanopowder (SA-NP) was aimed to be prepared using planetary ball monomill by dry milling technique to enhance its solubility and bioavailability. Methods: Various milling parameters such as milling speed, milling time and number of balls was varied and their effect on dependent responses including size (nm) and polydispersity indices (PDI) were evaluated using a 3-Factorial-3-Level Box-Behnken statistical design. Particle size and PDI analysis was performed using light scattering technique. Results: The particle size of salicylic acid obtained by optimizing the dry milling parameters was Z-Average (d.nm): 776.3 nm and PDI: 0.600 up to Z-Average (d. nm): 205.0 nm and PDI: 0.383. Conclusions: Dry milling can be used for the preparation of nanopowders of drug candidates with poor water-solubility issues. Present day medications have nano-scaled active ingredients which are rapidly absorbed by the human body as compared to the conventional ones. Enlarged surface area increases the solubility of the drug, thereby improves its bioavailability.
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