scholarly journals Bioactive Compounds and Nanodelivery Perspectives for Treatment of Cardiovascular Diseases

2021 ◽  
Vol 11 (22) ◽  
pp. 11031
Author(s):  
Rakesh K. Sindhu ◽  
Annima Goyal ◽  
Evren Algın Yapar ◽  
Simona Cavalu

Bioactive compounds are comprised of small quantities of extra nutritional constituents providing both health benefits and enhanced nutritional value, based on their ability to modulate one or more metabolic processes. Plant-based diets are being thoroughly researched for their cardiovascular properties and effectiveness against cancer. Flavonoids, phytoestrogens, phenolic compounds, and carotenoids are some of the bioactive compounds that aim to work in prevention and treating the cardiovascular disease in a systemic manner, including hypertension, atherosclerosis, and heart failure. Their antioxidant and anti-inflammatory properties are the most important characteristics that make them favorable candidates for CVDs treatment. However, their low water solubility and stability results in low bioavailability, limited accessibility, and poor absorption. The oral delivery of bioactive compounds is constrained due to physiological barriers such as the pH, mucus layer, gastrointestinal enzymes, epithelium, etc. The present review aims to revise the main bioactive compounds with a significant role in CVDs in terms of preventive, diagnostic, and treatment measures. The advantages of nanoformulations and novel multifunctional nanomaterials development are described in order to overcome multiple obstacles, including the physiological ones, by summarizing the most recent preclinical data and clinical trials reported in the literature. Nanotechnologies will open a new window in the area of CVDs with the opportunity to achieve effective treatment, better prognosis, and less adverse effects on non-target tissues.

Nutrients ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 2147 ◽  
Author(s):  
Michele Dei Cas ◽  
Riccardo Ghidoni

The yellow pigment curcumin, extracted from turmeric, is a renowned polyphenol with a broad spectrum of health properties such as antioxidant, anti-inflammatory, anti-cancer, antidiabetic, hepatoprotective, anti-allergic, anti-dermatophyte, and neuroprotective. However, these properties are followed by a poor pharmacokinetic profile which compromises its therapeutic potential. The association of low absorption by the small intestine and the extensive reductive and conjugative metabolism in the liver dramatically weakens the oral bioavailability. Several strategies such as inhibition of curcumin metabolism with adjuvants as well as novel solid and liquid oral delivery systems have been tried to counteract curcumin poor absorption and rapid elimination from the body. Some of these drug deliveries can successfully enhance the solubility, extending the residence in plasma, improving the pharmacokinetic profile and the cellular uptake.


Molecules ◽  
2012 ◽  
Vol 17 (7) ◽  
pp. 8359-8377 ◽  
Author(s):  
Xesús Feás ◽  
M. Pilar Vázquez-Tato ◽  
Leticia Estevinho ◽  
Julio A. Seijas ◽  
Antonio Iglesias

Author(s):  
Himanshu Paliwal ◽  
Ram Singh Solanki ◽  
Chetan Singh Chauhan

The purpose of conducting this study was to prepare an oral microemulsion formulation of Rosuvastatin calcium (RC) to improve its water solubility. Oil in water microemulsion was formulated using Oleic acid, Tween 80 and Polyethylene Glycol-400(PEG-400) as oil, surfactant and co-surfactant, respectively. The ideal proportion of surfactant: co-surfactant (Smix) was chosen by constructing pseudoternary diagrams. The microemulsion formulations which proved to be stable after thermodynamic stability testing were further evaluated for physical characteristics. Selected formulations were evaluated for droplet size, zeta potential, polydispersity index, viscosity and % drug content. The results were suggestive that optimized microemulsion formulation (F2) was thermodynamically stable and clear having a droplet size of 74.29 nm and zeta potential of -18.44.  In vitro dissolution study for optimized microemulsion was performed using a dialysis bag method and cumulative % drug release was determined. The result from the release study was indicative of improved solubility of Rosuvastatin calcium which may serve to boost up the oral bioavailability of drug.


2021 ◽  
Vol 13 (2) ◽  
pp. 46-55
Author(s):  
Josemar Oliveira Filho ◽  
Ailton Lemes ◽  
Ricardo Cruz Filho ◽  
Rafaiane Guimarães ◽  
Kamylla Oliveira ◽  
...  

The objective of this study was to evaluate the partial replacement of wheat flour by beet flour (BF) in fresh pasta production, analyzing its chemical, technological, and sensorial characteristics. BF showed good water (4.2 g water/g flour) and oil absorption (2.2 g oil/g flour), water solubility (67.3%), and emulsifying properties (30.0%). The incorporation of BF in fresh pasta formulations improved the nutritional value of the pasta, increased the ash (1.65 to 2.16 g/100 g) and fiber contents (1.31 to 12.29 g/100 g) of the fresh pasta, and decreased the lipid contents (50.0% reduction), thereby causing changes in its cooking properties. The antioxidant capacity (0.5 to 4.76%) and the content of total phenolics (69.1 to 70.5 mg/100 g) and betalains (0.04 to 0.16 mg/100g) also increased with the addition of BF, improving the functional profile of the pasta. In the sensory profile, the pasta formulated with the highest concentrations of BF demonstrated the highest intensities for the sensory attributes among fresh pasta evaluated. In general, it was shown that BF represents a promising ingredient to produce new fresh pasta with functional characteristics.


2020 ◽  
Vol 0 (37) ◽  
pp. 0-0
Author(s):  
Pırıl Ayris GÜRSİLİ ◽  
Burcu YEŞİLKAYA

Aim: Life has changed very fast during last 10 years. The adaptation of sedentary life, changes of eating habbits and other negative environmental factors consisted of reactive oxygen species in the human body and causing immunity to weaken. The prevelance of chronic dieases are increased caused by this reason. To take precautions against increasing diseases and to stop their progress, too much medication usage has been observed. People who don’t want to use medicine, started to use natural herbal products. Herbals are essentials for life and diseases. Herbals have different and comlex compounds which can be a cure for a diease. It has been possible to benefit the body mechanism and diseases with antioxidant, anti-inflammatory and antifibrotic effects. Thistle is one of the major herbal that is used for both as a cure and a nutrient. Its nutritional value and the bioactive compounds are important for a human life. Method: Current studies reviewed to explain thistles with its nutritional value, bioactive compounds and effects on diseases. Result: The thistle has important role as a component of medicines and also the natural form itself has a huge nutritional value for health. Consclusion: thistle have a beneficial effect on human body to be treated naturally, and its benefits are focused on noncommunicable diseases. Treatment of most chronic diseases, they had the advantages to stop their healing, protection and progression against diseases. Many studies have had positive effects. however, more studies should be done.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 561 ◽  
Author(s):  
Maharjan ◽  
Kim ◽  
Jin ◽  
Ko ◽  
Song ◽  
...  

As a posterior ocular disease, wet age-related macular degeneration (WAMD) has been known to be related to vision loss, accompanying ocular complications. The intravitreous injection of VEGF antibodies has been reported to be an effective treatment to relieve symptoms of WAMD. However, the limitations of this treatment are high costs and invasiveness. For this reason, oral delivery route can be considered as a cost-effective way and the safest method to deliver drug molecules to the eyes. Accordingly, ursodeoxycholic acid (UDCA) was included in the oral formulation as the potential substance for the cure of WAMD in the animal model. Various pharmacological activities, such as antioxidant or anti-inflammatory effects, have been reported for UDCA and recent reports support the effects of UDCA in ocular treatment. However, due to poor water solubility and low pKa (around 5.0), it has been challenging to formulate aqueous solution of UDCA in the neutral pH range. In the present study, we confirmed the aqueous solubility of the oral UDCA formulation and performed a preclinical study, including pharmacokinetic profiling and WAMD model efficacy study in mice after oral administration of the drug solution. The results demonstrated that the formulation improved bioavailability of UDCA and efficiently delivered UDCA to the eye tissues after oral absorption. UDCA formulation was found to have inhibitory effects of choroidal neovascularization with a functional recovery in mice retinas. Taken together, our results suggest that the oral UDCA formulation could be used as a potent supplement for the cure of WAMD and related retinal diseases.


2016 ◽  
Vol 10 (1s) ◽  
pp. 65 ◽  
Author(s):  
Anna Rita Rivelli ◽  
Rosa Agneta ◽  
Christian Möllers ◽  
Susanna De Maria

Horseradish is grown for its enlarged taproot that is widely used as a dish condiment and as a source of horseradish peroxidase. Nowadays, the species is gaining great interest due to the richness in bioactive compounds that besides providing a high nutritional value are tested for innovative applications in different fields. Nevertheless, the effect of crop management on root yield and glucosinolates (GLS) biosynthesis is poorly documented. Aim of this study was to evaluate the root yield and GLS concentration of two field-grown horseradish accessions (Cor and Mon) grown with nitrogen (N) alone and both N and sulphur (S) (-N-S, +N-S and +N+S treatments) and harvested at different times [late autumn (LA), 2011 and 2012, early spring (ES), 2012]. Yield increased throughout the harvests up to 48% on average of the fertilised treatments and 25% in the unfertilised control. Conversely, root GLS concentration significantly declined in the unfertilised control throughout the harvests [from 7.6 in LA_2011 to 1.43 μmol/g dry matter (DM) in LA_2012] while it highly increased in plants grown with N alone and with both N and S by 46 and 98%, respectively, from LA_2011 to ES_2012 (up to 11.9 and 21.1 μmol/g DM, respectively); then it drastically decreased by 80% on average, in the next harvest. Among individual GLS, the concentration of sinigrin and nasturtin similarly varied as effect of the analysed factors, showing the highest values in Cor accession. The data show that although the level of GLS is highly dependent on genotype, fertilisation and harvesting date may play a primary role in determining the yield and GLS concentration in horseradish root.


2018 ◽  
Vol 38 (4) ◽  
pp. 629-638 ◽  
Author(s):  
Carline MARQUETTI ◽  
Tatiane Batista dos SANTOS ◽  
Kelen Fabiana Cavalli KAIPERS ◽  
Bruna Raquel BÖGER ◽  
Ivane Benedetti TONIAL ◽  
...  

Author(s):  
Manikandan P ◽  
Sundara Ganapathy R

The objective of this review is to focus the inferences of low/poor bioavailability and lack of dose proportionality for the oral delivery of drugs in prostatecancer therapy. To overcome such problems, various formulation strategies has been reported including various methods for the use of surfactants,cyclodextrins, solid dispersions, micronization, permeation enhancers, and lipids. Flutamide is an antiandrogen drug and used for the therapy of prostate cancer. The flutamide drug is having limited clinical application due to its poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. The lipid-based formulations such as nanoemulsion have been shown to improve the solubility and oral absorption of lipophilic drugs. To conclude, this article emphasizes the various approaches of nanoemulsion based formulation for prostate cancer therapy.Keywords: Nanoemulsion, Prostate cancer, Flutamide, Antiandrogen drug, Lipophilic drugs.


2020 ◽  
Vol 12 (22) ◽  
pp. 9424 ◽  
Author(s):  
Magdalena Wróbel-Kwiatkowska ◽  
Waldemar Turski ◽  
Piotr Juszczyk ◽  
Agnieszka Kita ◽  
Waldemar Rymowicz

Y. lipolytica remains a nonpathogenic, unconventional yeast, which can be applied for the production of bioactive compounds. Our previous study confirmed the ability of yeast Yarrowia lipolytica to produce kynurenic acid (KYNA). Here, we investigated the effectiveness of KYNA production in cultures cultivated in medium containing honey of various origin, used as a source of carbon and energy. It was evidenced that the highest content of KYNA in culture broth (68 mg/L) and yeast biomass (542 mg/kg) was obtained when chestnut honey was used. The content of lipids and amino acids composition in yeast biomass producing KYNA was also determined. It was found that the composition of both amino acids and lipids in yeast biomass depended on the honey type used as a component of the medium. This finding revealed that supplementation of medium broth with honey may significantly affect the nutritional value of yeast biomass. The practical applicability of this finding requires further study.


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