scholarly journals Performance of Choline Geranate Deep Eutectic Solvent as Transdermal Permeation Enhancer: An In Vitro Skin Histological Study

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 540
Author(s):  
Rodrigo Boscariol ◽  
Érika A. Caetano ◽  
Erica C. Silva ◽  
Thais J. Oliveira ◽  
Raquel M. Rosa-Castro ◽  
...  

In the present research work, we addressed the changes in skin by which deep eutectic solvents (DES) enhanced transdermal permeation of bioactive compounds and propose a rationale for this mechanism. Several studies showed that these unusual liquids were ideal solvents for transdermal delivery of biomolecules, but to date, no histological studies relating the action of DES to changes in the structure of the outer skin barrier have been reported. In the research effort described herein, we presented an in-depth analysis of the changes induced in the skin by choline geranate DES, a compound with proven capabilities of enhancing transdermal permeation without deleterious impacts on the cells. The results obtained showed that a low percentage of DES acted as a transient disruptor of the skin structure, facilitating the passage of bioactive compounds dissolved in it.

Author(s):  
Grazielle Oliveira ◽  
Caroline Marques ◽  
Anielle de Oliveira ◽  
Amanda de Almeida dos Santos ◽  
Wanderlei do Amaral ◽  
...  

2021 ◽  
Vol 23 (3) ◽  
pp. 1300-1311 ◽  
Author(s):  
Dasom Jung ◽  
Jae Back Jung ◽  
Seulgi Kang ◽  
Ke Li ◽  
Inseon Hwang ◽  
...  

The in vitro and in vivo studies suggest that choline chloride-based deep eutectic solvents may not be considered as pure, safe mixtures even if they consist of safe compounds.


2021 ◽  
Vol 11 (11) ◽  
pp. 4897
Author(s):  
Bárbara Socas-Rodríguez ◽  
M. Vanessa Torres-Cornejo ◽  
Gerardo Álvarez-Rivera ◽  
Jose A. Mendiola

In this work, a review about the applicability of eutectic solvents, mainly deep eutectic solvents (DES) and natural deep eutectic solvents (NADES), for the extraction of bioactive compounds from natural products has been carried out. These alternative solvents have shown not only to have high extraction yields but also to be environmentally friendly, exhibiting very low or almost no toxicity, compared to conventional organic solvents. The last trends and main extraction methods that have been most widely used in studies using these emerging solvents have been reviewed, as well as the varied natural sources in which they have been used, including agro-food by-products. Besides the toxicity, biodegradability of these solvents is reviewed. Likewise, different reported bioactivity tests have been included, in which extracts obtained with these ecological solvents have been tested from antioxidant activity analysis to in vivo studies with rats, through in vitro cytotoxicity tests.


2021 ◽  
Vol 12 ◽  
Author(s):  
Hafiz Ibtesam Ahmad ◽  
Muhammad Faisal Nadeem ◽  
Haji Muhammad Shoaib Khan ◽  
Muhammad Sarfraz ◽  
Hammad Saleem ◽  
...  

Sphaeranthus indicus L. is a medicinal herb having widespread traditional uses for treating common ailments. The present research work aims to explore the in-depth phytochemical composition and in vitro reactivity of six different polarity solvents (methanol, n-hexane, benzene, chloroform, ethyl acetate, and n-butanol) extracts/fractions of S. indicus flowers. The phytochemical composition was accomplished by determining total bioactive contents, HPLC-PDA polyphenolic quantification, and UHPLC-MS secondary metabolomics. The reactivity of the phenolic compounds was tested through the following biochemical assays: antioxidant (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation) and enzyme inhibition (AChE, BChE, α-glucosidase, α-amylase, urease, and tyrosinase) assays were performed. The methanol extract showed the highest values for phenolic (94.07 mg GAE/g extract) and flavonoid (78.7 mg QE/g extract) contents and was also the most active for α-glucosidase inhibition as well as radical scavenging and reducing power potential. HPLC-PDA analysis quantified rutin, naringenin, chlorogenic acid, 3-hydroxybenzoic acid, gallic acid, and epicatechin in a significant amount. UHPLC-MS analysis of methanol and ethyl acetate extracts revealed the presence of well-known phytocompounds; most of these were phenolic, flavonoid, and glycoside derivatives. The ethyl acetate fraction exhibited the highest inhibition against tyrosinase and urease, while the n-hexane fraction was most active for α-amylase. Moreover, principal component analysis highlighted the positive correlation between bioactive compounds and the tested extracts. Overall, S. indicus flower extracts were found to contain important phytochemicals, hence could be further explored to discover novel bioactive compounds that could be a valid starting point for future pharmaceutical and nutraceuticals applications.


Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2110 ◽  
Author(s):  
Xianchao Shang ◽  
Jia-Neng Tan ◽  
Yongmei Du ◽  
Xinmin Liu ◽  
Zhongfeng Zhang

Deep eutectic solvents (DESs) are commonly employed as environmentally-friendly solvents in numerous chemical applications owing to their unique physicochemical properties. In this study, a novel and environmentally-friendly extraction method based on ultrasound assisted-deep eutectic solvent extraction (UAE-DES) was investigated for the extraction of flavonoids from Cyclocarya paliurus (Batal.) Iljinskaja (C. paliurus) leaves, and the antioxidant activities of these flavonoids were evaluated. Nine different DES systems based on either two or three components were tested, and the choline chloride/1,4–butanediol system (1:5 molar ratio) was selected as the optimal system for maximizing the flavonoid extraction yields. Other extraction conditions required to achieve the maximum flavonoid extraction yields from the leaves of C. paliurus were as follows: DES water content (v/v), 30%; extraction time, 30 min; temperature, 60 °C; and solid-liquid ratio, 20 mg/mL. Liquid chromatography-mass spectrometry allowed the detection of five flavonoids in the extract, namely kaempferol-7-O-α-l-rhamnoside, kaempferol, quercetin, quercetin-3-O-β-d-glucuronide, and kaempferol-3-O-β-d-glucuronide. In vitro antioxidant tests revealed that the flavonoid-containing extract exhibited strong DPPH and ABTS radical-scavenging abilities. Results indicate that UAE-DES is a suitable approach for the selective extraction of flavonoids from C. paliurus leaves, and DESs can be employed as sustainable extraction media for other bioactive compounds.


Author(s):  
T. Raja Sekharan ◽  
R. Margret Chandira ◽  
S.C. Rajesh ◽  
Shunmugaperumal Tamilvanan ◽  
C.T. Vijayakumar ◽  
...  

Turmeric is a commonly known natural spice that contains many phytoconstituents. Among which Curcumin is a polyphenol present in turmeric responsible for many pharmacological actions. Curcumin is still used as a traditional medicine in fields such as Ayurvedic, Siddha, and Unani. Though Curcumin has a large number of activities, it has disadvantages, such as small shelf life due to poor chemical stability, poor absorption results in less bioavailability, less water solubility, rapid metabolism results in quick elimination from the systemic circulation. A Deep eutectic solvent (DES) is a new class of solvents. Hydrophobic DES can be used for dissolving water-insoluble compounds. DES can be prepared when two solid components mixed in a particular proportion are converted into liquid. DES can be used as a solvent for dissolving water-insoluble compounds and to increase the stability. In this work initially, curcumin linearity studies were conducted in different buffers. A buffer showing maximum absorbance was selected from the linearity studies. Then, DES was prepared by combining Camphor:Menthol (1:1) (CM-DES), Camphor:Thymol (1:1) (CT-DES) and, Menthol:Thymol (1:1) (MT-DES). The stability of curcumin in different DES was determined from the stock and working solutions in benchtop condition (room temperature) and, refrigerator condition (5±3°C). Only working solution stability was determined in the in vitro media temperature (37±2°C). From this study, it was concluded that 50 mM Sodium dihydrogen orthophosphate with 0.5% SLS at pH 5.5 showed maximum absorbance value compared with other buffers, so it was selected for further studies. From stability studies, it was found that curcumin in CM-DES was found to be stable in both stock and working solutions compared to the other two CT-DES and MT-DES.


Author(s):  
V. Ramadas ◽  
G. Chandralega

Sponges, exclusively are aquatic and mostly marine, are found from the deepest oceans to the edge of the sea. There are approximately 15,000 species of sponges in the world, of which, 150 occur in freshwater, but only about 17 are of commercial value. A total of 486 species of sponges have been identified in India. In the Gulf of Mannar and Palk Bay a maximum of 319 species of sponges have been recorded. It has been proved that marine organisms are excellent source of bioactive secondary metabolites and number of compounds of originated from marine organisms had been reported to possess in-vitro and in-vivo immuno stimulatory activity. Extracts from 20 sponge species were tested for bacterial symbionts and bioactive compounds were isolated from such associated bacterial species in the present study.


Author(s):  
Waras Nurcholis ◽  
Edy Djauhari Purwakusumah ◽  
Mono Rahardjo ◽  
Latifah K. Darusman

Temulawak (Curcuma  xanthorrhizaRoxb.) belongs to the family Zingiberaceae, has been empirically used as herbal medicines. The research was aimed to evaluate three promising lines of Temulawak based on their high bioactive contents (xanthorrhizol and curcuminoid) and its in vitro bioactivity (antioxidant and toxicity), and to obtain information on agrobiophysic environmental condition which produced high bioactive compounds. The xanthorrhizol and curcuminoid contents were measured by HPLC. In vitro antioxidant and toxicity were determined by DPPH (1,1-diphenyl-2-picryl-hydrazyl) method and BSLT (Brine Shrimp Lethality Test). The result showed that promising line A produced the highest yield of bioactive and bioactivity, i.e. 0.157 and 0.056 g plant-1of xanthorrizol and curcuminoid respectively. The IC50 of antioxidant activity was 65.09 mg L-1and LC50of toxicity was 69.05 mg L-1. In this study, Cipenjo had the best temulawak performance than two other locations. According to the agrobiophysic parameters, Cipenjo environmental condition was suitable for temulawak cultivation with temperature 28-34 ºC, rainfall ± 223.97 mm year-1 and sandy clay soil. Keywords: antioxidant, curcuminoid, promising lines, temulawak, xanthorrhizol


Author(s):  
Prakash Goudanavar ◽  
Ankit Acharya ◽  
Vinay C.H

Administration of an antiviral drug, acyclovir via the oral route leads to low and variable bioavailability (15-30%). Therefore, this research work was aimed to enhance bioavailability of acyclovir by nanocrystallization technique. The drug nanocrystals were prepared by anti-solvent precipitation method in which different stabilizers were used. The formed nanocrystals are subjected to biopharmaceutical characterization including solubility, particle size and in-vitro release. SEM studies showed nano-crystals were crystalline nature with sharp peaks. The formulated drug nanocrystals were found to be in the range of 600-900nm and formulations NC7 and NC8 showed marked improvement in dissolution velocity when compared to pure drug, thus providing greater bioavailability. FT-IR and DSC studies revealed the absence of any chemical interaction between drug and polymers used. 


2020 ◽  
Vol 26 ◽  
Author(s):  
Kondeti Ramudu Shanmugam ◽  
Bhasha Shanmugam ◽  
Gangigunta Venkatasubbaiah ◽  
Sahukari Ravi ◽  
Kesireddy Sathyavelu Reddy

Background : Diabetes is a major public health problem in the world. It affects each and every part of the human body and also leads to organ failure. Hence, great progress made in the field of herbal medicine and diabetic research. Objectives: Our review will focus on the effect of bioactive compounds of medicinal plants which are used to treat diabetes in India and other countries. Methods: Information regarding diabetes, oxidative stress, medicinal plants and bioactive compounds were collected from different search engines like Science direct, Springer, Wiley online library, Taylor and francis, Bentham Science, Pubmed and Google scholar. Data was analyzed and summarized in the review. Results and Conclusion: Anti-diabetic drugs that are in use have many side effects on vital organs like heart, liver, kidney and brain. There is an urgent need for alternative medicine to treat diabetes and their disorders. In India and other countries herbal medicine was used to treat diabetes. Many herbal plants have antidiabetic effects. The plants like ginger, phyllanthus, curcumin, aswagandha, aloe, hibiscus and curcuma showed significant anti-hyperglycemic activities in experimental models and humans. The bioactive compounds like Allicin, azadirachtin, cajanin, curcumin, querceitin, gingerol possesses anti-diabetic, antioxidant and other pharmacological properties. This review focuses on the role of bioactive compounds of medicinal plants in prevention and management of diabetes. Conclusion: Moreover, our review suggests that bioactive compounds have the potential therapeutic potential against diabetes. However, further in vitro and in vivo studies are needed to validate these findings.


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