scholarly journals Polylactide Nanocapsules Attenuate Adverse Cardiac Cellular Effects of Lyso-7, a Pan-PPAR Agonist/Anti-Inflammatory New Thiazolidinedione

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1521
Author(s):  
Giani M. Garcia ◽  
Jérôme Roy ◽  
Ivan R. Pitta ◽  
Dulcinéia S. P. Abdalla ◽  
Andrea Grabe-Guimarães ◽  
...  
Keyword(s):  
Drug Effects ◽  
Repeated Administration ◽  
Repeated Treatment ◽  
Decay Kinetics ◽  
Cell Contraction ◽  
Cellular Effects ◽  
Anti Inflammatory ◽  
High Concentrations

Lyso-7 is a novel synthetic thiazolidinedione, which is a receptor (pan) agonist of PPAR α,β/δ,γ with anti-inflammatory activity. We investigated the cardiotoxicity of free Lyso-7 in vitro (4.5–450 nM), and Lyso-7 loaded in polylactic acid nanocapsules (NC) in vivo (Lyso-7-NC, 1.6 mg/kg). In previous work, we characterized Lyso-7-NC. We administered intravenously Lyso-7, Lyso-7-NC, control, and blank-NC once a day for seven days in mice. We assessed cell contraction and intracellular Ca2+ transients on single mice cardiomyocytes enzymatically isolated. Lyso-7 reduced cell contraction and accelerated relaxation while lowering diastolic Ca2+ and reducing Ca2+ transient amplitude. Lyso-7 also promoted abnormal ectopic diastolic Ca2+ events, which isoproterenol dramatically enhanced. Incorporation of Lyso-7 in NC attenuated drug effects on cell contraction and prevented its impact on relaxation, diastolic Ca2+, Ca2+ transient amplitude, Ca2+ transient decay kinetics, and promotion of diastolic Ca2+ events. Acute effects of Lyso-7 on cardiomyocytes in vitro at high concentrations (450 nM) were globally similar to those observed after repeated administration in vivo. In conclusion, we show evidence for off-target effects of Lyso-7, seen during acute exposure of cardiomyocytes to high concentrations and after repeated treatment in mice. Nano-encapsulation of Lyso-7 in polymeric NC attenuated the unwanted effects, particularly ectopic Ca2+ events known to support life-threatening arrhythmias favored by stress or exercise.

scholarly journals Immunomodulatory Activities of Selected Essential Oils

Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1139 ◽  
Author(s):  
Georg Sandner ◽  
Mara Heckmann ◽  
Julian Weghuber
Keyword(s):  
Essential Oils ◽  
Study Data ◽  
In Vivo Studies ◽  
Immunomodulatory Effects ◽  
Regulatory Pathways ◽  
Cellular Effects ◽  
Anti Inflammatory ◽  
Toxic Potential

Recently, the application of herbal medicine for the prevention and treatment of diseases has gained increasing attention. Essential oils (EOs) are generally known to exert various pharmacological effects, such as antiallergic, anticancer, anti-inflammatory, and immunomodulatory effects. Current literature involving in vitro and in vivo studies indicates the potential of various herbal essential oils as suitable immunomodulators for the alternative treatment of infectious or immune diseases. This review highlights the cellular effects induced by EOs, as well as the molecular impacts of EOs on cytokines, immunoglobulins, or regulatory pathways. The results reviewed in this article revealed a significant reduction in relevant proinflammatory cytokines, as well as induction of anti-inflammatory markers. Remarkably, very little clinical study data involving the immunomodulatory effects of EOs are available. Furthermore, several studies led to contradictory results, emphasizing the need for a multiapproach system to better characterize EOs. While immunomodulatory effects were reported, the toxic potential of EOs must be clearly considered in order to secure future applications.

scholarly journals A Comparative Review of Autologous Conditioned Serum and Autologous Protein Solution for Treatment of Osteoarthritis in Horses

2021 ◽  
Vol 8 ◽  
Author(s):  
Livia Camargo Garbin ◽  
Michael J. Morris
Keyword(s):  
Interleukin 1 ◽  
Joint Inflammation ◽  
Clinical Results ◽  
Protein Solution ◽  
Autologous Conditioned Serum ◽  
Comparative Review ◽  
Anti Inflammatory ◽  
High Concentrations

Many alternative treatments aimed at modulating osteoarthritis (OA) progression have been developed in the past decades, including the use of cytokine inhibitors. IL-1β is considered one of the most impactful cytokines in OA disease and therefore, its blockage offers a promising approach for the modulation of OA. Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory protein belonging to the IL-1 family that competes with IL-1β for occupancy of its receptors, without triggering the same downstream inflammatory response. Because of its natural anti-inflammatory properties, different methods have been proposed to use IL-1Ra therapeutically in OA. Autologous conditioned serum (ACS) and autologous protein solution (APS) are blood-derived products produced with the use of specialized commercial kits. These processes result in hemoderivatives with high concentrations of IL-1Ra and other cytokines and growth factors with potential modulatory effects on OA progression. Several studies have demonstrated potential anti-inflammatory effect of these therapies with promising clinical results. However, as with any hemoderivatives, clinical outcomes may vary. For optimal therapeutic use, further research is warranted for a more comprehensive understanding of the product's composition and interaction of its components in joint inflammation. Additionally, differences between ACS and APS treatments may not be clear for many clients and clinicians. Thus, the objective of this narrative review is to guide the reader in important aspects of ACS and APS therapies, in vitro and in vivo applications and to compare the use of both treatments in OA.

scholarly journals Berberine-Loaded Carboxylmethyl Chitosan Nanoparticles Ameliorate DSS-Induced Colitis and Remodel Gut Microbiota in Mice

2021 ◽  
Vol 12 ◽  
Author(s):  
Luqing Zhao ◽  
Xueying Du ◽  
Jiaxin Tian ◽  
Xiuhong Kang ◽  
Yuxin Li ◽  
...  
Keyword(s):  
Gut Microbiota ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Triggered Release ◽  
Release Studies ◽  
Anti Inflammatory ◽  
High Concentrations ◽  
Recurrent Inflammation

Inflammatory bowel disease (IBD) is a refractory disorder characterized by chronic and recurrent inflammation. The progression and pathogenesis of IBD is closely related to oxidative stress and irregularly high concentrations of reactive oxygen species (ROS). A new oxidation-responsive nano prodrug was constructed from a phenylboronic esters-modified carboxylmethyl chitosan (OC-B) conjugated with berberine (BBR) that degrades selectively in response to ROS. The optimized micelles exhibited well-controlled physiochemical properties and stability in a physiological environment. OC-B-BBR micelles could effectively encapsulate the anti-inflammatory drug berberine and exhibit ideal H2O2-triggered release behavior as confirmed by in vitro drug loading and release studies. The in vivo anti-inflammatory effect and regulation of gut microbiota caused by it were explored in mice with colitis induced by dextran sodium sulfate (DSS). The results showed that OC-B-BBR significantly ameliorated colitis symptoms and colon damage by regulating the expression levels of IL-6 and remodeling gut microbiota. In summary, this study exhibited a novel BBR-loaded Carboxylmethyl Chitosan nano delivery system which may represent a promising approach for improving IBD treatment.

In vitro and in vivo evaluation of the anti-inflammatory effects of Arzanol from Helichrysum italicum

Planta Medica ◽  
2010 ◽  
Vol 76 (12) ◽  
Author(s):  
J Bauer ◽  
F Dehm ◽  
A Koeberle ◽  
F Pollastro ◽  
G Appendino ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Anti Inflammatory

Haemanthus coccineus extract shows profound anti-inflammatory actions in vitro and in vivo due to its main alkaloid narciclasine

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
S Fuchs ◽  
LT Hsieh ◽  
W Saarberg ◽  
CAJ Erdelmeier ◽  
TA Wichelhaus ◽  
...  
Keyword(s):  
Anti Inflammatory

Natural Anti-inflammatory compounds as Drug candidates in Alzheimer’s disease

2020 ◽  
Vol 27 ◽  
Author(s):  
Reyaz Hassan Mir ◽  
Abdul Jalil Shah ◽  
Roohi Mohi-ud-din ◽  
Faheem Hyder Potoo ◽  
Mohd. Akbar Dar ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Natural Products ◽  
Protective Action ◽  
New Drugs ◽  
Huperzine A ◽  
Brain Disorder ◽  
Anti Inflammatory

: Alzheimer's disease (AD) is a chronic neurodegenerative brain disorder characterized by memory impairment, dementia, oxidative stress in elderly people. Currently, only a few drugs are available in the market with various adverse effects. So to develop new drugs with protective action against the disease, research is turning to the identification of plant products as a remedy. Natural compounds with anti-inflammatory activity could be good candidates for developing effective therapeutic strategies. Phytochemicals including Curcumin, Resveratrol, Quercetin, Huperzine-A, Rosmarinic acid, genistein, obovatol, and Oxyresvertarol were reported molecules for the treatment of AD. Several alkaloids such as galantamine, oridonin, glaucocalyxin B, tetrandrine, berberine, anatabine have been shown anti-inflammatory effects in AD models in vitro as well as in-vivo. In conclusion, natural products from plants represent interesting candidates for the treatment of AD. This review highlights the potential of specific compounds from natural products along with their synthetic derivatives to counteract AD in the CNS.

In vivo Evaluation and Alzheimer’s Disease Treatment Outcome of siRNA Loaded Dual Targeting Drug Delivery System

2019 ◽  
Vol 20 (1) ◽  
pp. 56-62 ◽  
Author(s):  
Chi Zhang ◽  
Zhichun Gu ◽  
Long Shen ◽  
Xianyan Liu ◽  
Houwen Lin
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Treatment Outcome ◽  
Neuroprotective Effect ◽  
Sirna Delivery ◽  
Repeated Administration ◽  
Spatial Learning And Memory ◽  
In Vivo Evaluation

Background: To deliver drugs to treat Alzheimer’s Disease (AD), nanoparticles should firstly penetrate through blood brain barrier, and then target neurons. Methods: Recently, we developed an Apo A-I and NL4 dual modified nanoparticle (ANNP) to deliver beta-amyloid converting enzyme 1 (BACE1) siRNA. Although promising in vitro results were obtained, the in vivo performance was not clear. Therefore, in this study, we further evaluated the in vivo neuroprotective effect and toxicity of the ANNP/siRNA. The ANNP/siRNA was 80.6 nm with good stability when incubated with serum. In vivo, the treatment with ANNP/siRNA significantly improves the spatial learning and memory of APP/PS1 double transgenic mice, as determined by mean escape latency, times of crossing the platform area during the 60 s swimming and the percentage of the distance in the target quadrant. Results and Conclusion: After the treatment, BACE1 RNA level of ANNP/siRNA group was greatly reduced, which contributed a good AD treatment outcome. Finally, after repeated administration, the ANNP/siRNA did not lead to significant change as observed by HE staining of main organs, suggesting the good biocompatibility of ANNP/siRNA. These results demonstrated that the ANNP was a good candidate for AD targeting siRNA delivery.

Formulation and Evaluation of Atorvastatin Calcium-Poly-ε-Caprolactone Nanoparticles Loaded Ocular Inserts for Sustained Release and Antiinflammatory Efficacy

2020 ◽  
Vol 21 (15) ◽  
pp. 1688-1698
Author(s):  
Germeen N.S. Girgis
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
In Vivo Study ◽  
Average Weight ◽  
Drug Release Profile ◽  
Atorvastatin Calcium ◽  
Anti Inflammatory

Purpose: The work was performed to investigate the feasibility of preparing ocular inserts loaded with Poly-ε-Caprolactone (PCL) nanoparticles as a sustained ocular delivery system. Methods: First, Atorvastatin Calcium-Poly-ε-Caprolactone (ATC-PCL) nanoparticles were prepared and characterized. Then, the optimized nanoparticles were loaded within inserts formulated with Methylcellulose (MC) and Polyvinyl Alcohol (PVA) by a solvent casting technique and evaluated physically, for in-vitro drug release profile. Finally, an in-vivo study was performed on the selected formulation to prove non-irritability and sustained ocular anti-inflammatory efficacy compared with free drug-loaded ocuserts. Results: The results revealed (ATC-PCL) nanoparticles prepared with 0.5% pluronic F127 were optimized with 181.72±3.6 nm particle size, 0.12±0.02 (PDI) analysis, -27.4± 0.69 mV zeta potential and 62.41%±4.7% entrapment efficiency. Nanoparticles loaded ocuserts manifested compatibility between drug and formulation polymers. Moreover, formulations complied with average weight 0.055±0.002 to 0.143±0.023 mg, and accepted pH. ATC-PCL nanoparticles loaded inserts prepared by 5% MC showed more sustained, prolonged in-vitro release over 24h. In-vivo study emphasized non-irritability, ocular anti-inflammatory effectiveness represented by smaller lid closure scores, and statistically significant lowering in PMN count after 3h. Conclusion: These findings proposed a possibly simple, new and affordable price technique to prepare promising (ATC-PCL) nanoparticles loaded inserts to achieve sustained release with prolonged antiinflammatory efficacy.

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