Liposome‐encapsulated folic acid is incorporated into the films made from sodium carboxymethyl cellulose (CMC) (2 mas%) and a mixture of CMC and solagum (9:1 w/w) using the film‐forming cast solution ...method. Histidine is used to increase solubility for folic acid in liposomes (1–5 mg mL−1), and propylene glycol is used as a film plasticizer (2.6 mas%). The obtained films (50–60 µm tick) containing 3.12–20.19 mg of folic acid per gram of film are envisaged to be used as patches for transdermal delivery of folic acid. Therefore, some physical, mechanical, release and structural attributes of the films are scrutinized. Folic acid gives yellow color to the films and contributes to stronger chemical bonds which result in improved strength of the film. Liposomes prolong the release of folic acid from films to 24 h without adverse effects on mechanical properties of the films, but degrade homogeneity of the films, which can be ascribed to its agglomeration within the film matrix as revealed by atomic force microscopy. According to the release at pH 5.5, the film formulation based on a blend of CMC and solagum containing 3 mg mL−1 liposome‐encapsulated folic acid is recommended.
Practical Application: Folic acid is effective in reducing oxidative stress levels in the skin and neutralizing the harmful free radicals and is also essential for various metabolic reactions in the body. However, the limited solubility of folic acid linked with its poor absorption in an organism, low storage stability, short half‐life upon oral consumption, specific food preferences of some people, extensive liver metabolism, and pregnancy‐induced vomiting point to a large potential in transdermal usage of folic acid. This has motivated us to design new multicomponent polymer‐lipid systems as an alternative solution to overcome some of these drawbacks. The results obtained for these multicomponent films pointed to their potential for prolonged release of folic acid to 24 h, which can also be useful for scientists interested in encapsulating similar poorly soluble compounds in CMC patches. The finding can be also valuable information for pharmaceutical manufacturers and scientists worldwide.
The influence of folic acid‐loaded liposomes incorporated in the complex biopolymer film on the mechanical, release and morphological properties is investigated by the atomic force microscopy, in vitro diffusion tests and the technique which determines force‐displacement at the breaking point.
In this study, the petals collected from peony hybrid Paeonia lactiflora "Bowl of Beauty" and Calendula officinalis L. were extracted using an ethanol-water mixture assisted with microwave and ...ultrasonic treatment. The isolation of Calendula officinalis L. essential oil was done by hydrodistillation as well. The total phenolic and flavonoids content in the extracts and oil were determined and their antioxidant activity was evaluated. The highest total phenolic content was found for the extracts of hybrid P. lactiflora and C. officinalis L. obtained by ultrasound extraction (83.16 and 114.47 mg GA/g, respectively), while the flavonoid content obtained by microwave-assisted extraction was relatively high (123.48 and 65.29 mg QE/g, respectively). The highest antioxidant activity was obtained in DPPH• and ABTS•+ assay for the microwave-assisted extraction of hybrid P. lactiflora (79% and 83%) and ultrasound-assisted extraction of C. officinalis L. (45% and 49%), respectively. To improve antioxidant activity of both types of examined analytes (extracts and essential oil), the pectin biopolymer film (as a carrier) was prepared in the process of enzymatically assisted catalysis. Optical microscopy and FTIR spectroscopy were used for the characterization of obtained materials. The films, with essential oil of C. officinalis L. and gallic acid, showed significantly increased percentage inhibition in DPPH• and ABTS•+ test (91% and 95%, respectively) after 10 minutes. The results, also, showed that all formulations of pectin biopolymer film, modified with gallic acid, can be successfully applied as a carrier for both types of ingredients.
In this study, development of folic acid-loaded liposomes using a basic amino acid, histidine as a solubilizing agent for folic acid was presented, which tackled the poor solubility of this vitamin. ...The effect of the liposomal membrane modifiers, cholesterol and SPAN 20 on the characteristics of the final formulations was examined. Liposomes prepared from a commercially available purified soybean lecithin (Phospholipon 90G) by proliposome method were between 503 and 877 nm in average diameter, where cholesterol induced enlargement and SPAN.20 reduction of vesicles. High encapsulation efficiency of 84% and drug loading of 0.123 mg g−1 were achieved, irrespective to the composition. According to AFM images, folic acid-loaded liposomes of a fraction with a nano size were flattened compared to globular empty liposomes. FTIR analysis revealed possible interactions between phospholipids and histidine, while DSC study suggested interactions between folic acid and lipids during heating. Release study done by a Franz diffusion cell showed prolonged release of folic acid from liposomes and the release rate was determined by folic acid solubility.
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•Liposomes were used as a model system for encapsulation of folic acid.•A basic amino acid-histidine was used as a solubilizing agent for folic acid.•Interactions between folic acid and phospholipids were determined by DSC analysis.•Interactions between histidine and phospholipids were analyzed by ATR-IR.•Cholesterol and SPAN 20 did not contribute to the effect of prolonged release.
In order to gain further insight into how various extraction techniques (maceration, microwave-, and ultrasound-assisted extractions) affect the chemical profile and biological activities of leaf ...extracts from Paeonia tenuifolia L., Paeonia peregrina Mill., and Paeonia officinalis L., this research was performed. The targeted chemical characterization of the extracts was achieved using the Ultra-High-Performance-Liquid-Chromatography-Linear-Trap-Mass-Spectrometry OrbiTrap instrumental technique, while Fourier Transform Infrared Spectroscopy was conducted to investigate the structural properties of the examined leaf extracts. According to the results, the species P. officinalis, Božurna locality as the origin of the plant material, and microwave-assisted extraction produced the maximum polyphenol yield, (491.9 ± 2.7 mg gallic acid equivalent (GAE)/mL).
The ethanolic extracts exhibited moderate antioxidant activity as evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl) and phosphomolybdenum tests. With MIC values of 0.125 mg/mL, the leaf extracts produced by ultrasound-assisted extraction and maceration (Deliblato sands and Bogovo gumno) had the best antibacterial activity against Pseudomonas aeruginosa and Salmonella Typhimurium. Ultrasound-assisted extraction has proven to produce the most effective antimicrobial agents. Inhibitory potential towards glucosidase, amylase, cholinesterases, and tyrosinase was evaluated in enzyme inhibition assays and molecular docking simulations. Results show that leaves of P. tenuifolia L. obtained by ultrasound-assisted extraction had the highest acetylcholinesterase and butyrylcholinesterase inhibitory activity. Namely, the complexity of the polyphenol structures, the extraction method, the used locality, and the different mechanisms of the reactions between bioactives from leaf extracts and other components (free radicals, microorganisms, and enzymes) are the main factors that influence the results of the antioxidant tests, as well as the antibacterial and enzyme-inhibitory activities of the extracts. Hydroxymethyl-phenyl pentosyl-hexoside and acetyl-hydroxyphenyl-hexoside were the first time identified in the leaf extract of the Paeonia species. Due to their proven biological activities and the confirmed existence of bioactive compounds, leaf extracts may find use in foodstuffs, functional foods, and pharmaceutical products.
Without being aware of their chemical composition, many cultures have used herbaceous peony roots for medicinal purposes. Modern phytopreparations intended for use in human therapy require specific ...knowledge about the chemistry of peony roots and their biological activities. In this study, ethanol-water extracts were prepared by maceration and microwave- and ultrasound-assisted extractions (MAE and UAE, respectively) in order to obtain bioactive molecules from the roots of
L.,
Mill., and
L. wild growing in Serbia. Chemical characterization; polyphenol and flavonoid content; antioxidant, multianti-enzymatic, and antibacterial activities of extracts; and
gastrointestinal digestion (GID) of hot water extracts were performed. The strongest anti-cholinesterase activity was observed in PT extracts. The highest anti-ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical potential was observed in PP extracts, whereas against DPPH (2,2-diphenyl-1-picrylhydrazyl radicals), the best results were achieved with PO extracts. Regarding antibacterial activity, extracts were strongly potent against
A molecular docking simulation was conducted to gather insights into the binding affinity and interactions of polyphenols and other
-specific molecules in the active sites of tested enzymes.
GID of
teas showed a different recovery and behavior of the individual bioactives, with an increased recovery of methyl gallate and digallate and a decreased recovery of paeoniflorin and its derivatives. PT (Gulenovci) and PP (Pirot) extracts obtained by UAE and M were more efficient in the majority of the bioactivity assays. This study represents an initial step toward the possible application of
root extracts in pharmacy, medicine, and food technologies.
The presented study aimed to optimize polyphenol extraction from Satureja montana L. obtained from the experimental field of the Institute for Medicinal Plants Research ?Dr Josif Pancic?, Serbia, by ...varying the most important parameters for maceration, solid-to-solvent ratio, and extraction time. The obtained extracts were characterized regarding the total polyphenol content (TPC), total flavonoid content (TFC), antioxidant potential, extraction yield, conductivity, density, surface tension, and viscosity. The TPC and TFC were ~7 to 92 mg GAE (gallic acid equivalent)/g and 3.7 to 10.9 mg CE (catechin equivalent)/g, respectively. The highest extraction yield (86 %) as well as the highest antioxidant activities were obtained for the extracts prepared using a solid-to-solvent ratio of 1 g :50 cm3. On the other hand, the extraction time did not have a significant influence. The highest conductivity was measured in the extract prepared at a 1 g :10 cm3 ratio, while the highest density and surface tension were in the extract prepared at a 1 g :40 cm3 ratio (941 kg m-3 and 29.0 mN m-1, respectively). The highest viscosity was measured in the extract prepared at a 1 g : 20 cm3 ratio (2.89 mPa?s). Our study shows the possibilities for the production of polyphenol-rich extract of S. montana which might be used in pharmaceutical, food, or cosmetic products.
Vaccinium myrtillus L. (bilberry, Ericaceae), a perennial, wild, and small deciduous shrub that grows in the mountains and forests of Europe. The leaf extracts are widely used in traditional medicine ...due to their astringent, antiseptic, antioxidant, anti-inflammatory, hypolipidemic, and hypoglycemic activities. Microwave-assisted extraction provides various benefits, including reducing solvent consumption and extraction time and increasing extraction yield. In the present study, bilberry extracts were prepared using dried leaves, pure ethanol, or an ethanol-water mixture, and different temperatures in a microwave reactor (60, 100, and 160 ◦ C). The extracts were examined in terms of total polyphenol content (TPC) and antioxidant activity. The TPC of the 96% ethanol extracts rose with the increase of the extraction temperature; the extract obtained at 60 ◦ C (37.2 ± 0.5 mg gallic acid equivalents (GAE)/g of plant material)<the extract at 100 ◦ C (46.6 ± 0.3 GAE/g)<the extract at 160 ◦ C (55.1 ± 0.5 mg/g). The TPC of the 50% ethanol extract prepared at 60 ◦ C was significantly lower (54.9 ± 1.0 mg GAE/g) in comparison to the extracts obtained at 100 and 160 ◦C (58.3 ± 1.0 and 58.0 ± 1.5 mg GAE/g, respectively). ABTS antioxidant capacity was higher in the 50% ethanol extracts compared to 96% ethanol parallels, while in the DPPH assay, there was no statistically significant difference between the 50 and 96% ethanol extracts. Due to higher TPC and anti-ABTS activity and reduced consumption of organic solvent, a 50% ethanol extract of V. myrtillus was favored, while the optimal temperature was 60 ◦ C for the extract with the highest antioxidant capacity and 100 ◦ C for the extract with the highest amount of polyphenols.
Without being aware of their chemical composition, many cultures have used herbaceous peony roots for medicinal purposes. Modern phytopreparations intended for use in human therapy require specific ...knowledge about the chemistry of peony roots and their biological activities. In this study, ethanol–water extracts were prepared by maceration and microwave- and ultrasound-assisted extractions (MAE and UAE, respectively) in order to obtain bioactive molecules from the roots of Paeonia tenuifolia L., Paeonia peregrina Mill., and Paeonia officinalis L. wild growing in Serbia. Chemical characterization; polyphenol and flavonoid content; antioxidant, multianti-enzymatic, and antibacterial activities of extracts; and in vitro gastrointestinal digestion (GID) of hot water extracts were performed. The strongest anti-cholinesterase activity was observed in PT extracts. The highest anti-ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical potential was observed in PP extracts, whereas against DPPH (2,2-diphenyl-1-picrylhydrazyl radicals), the best results were achieved with PO extracts. Regarding antibacterial activity, extracts were strongly potent against Bacillus cereus. A molecular docking simulation was conducted to gather insights into the binding affinity and interactions of polyphenols and other Paeonia-specific molecules in the active sites of tested enzymes. In vitro GID of Paeonia teas showed a different recovery and behavior of the individual bioactives, with an increased recovery of methyl gallate and digallate and a decreased recovery of paeoniflorin and its derivatives. PT (Gulenovci) and PP (Pirot) extracts obtained by UAE and M were more efficient in the majority of the bioactivity assays. This study represents an initial step toward the possible application of Paeonia root extracts in pharmacy, medicine, and food technologies.
In the present study, basil (Ocimum basilicum L.) and lovage (Levisticum officinale Koch.) extracts were obtained using maceration, ultrasound- and microwave-assisted extractions (UAE and MAE, ...respectively). Varying the different extraction solvents, including water, methanol, acetone, and ethyl acetate, the analyses of total polyphenol and flavonoid contents (TPC and TFC, respectively), as well as antioxidant properties (DPPH radical scavenging and cupric ion reducing activities) were carried out for all obtained plants' extracts. The total amount of extractive substances of the selected extracts was also measured. The highest TPC was achieved in water basil extract obtained using UAE, while the highest TFC was determined in the basil extracts prepared using maceration and MAE. The highest level of DPPH radical neutralization was observed for methanol and acetone extracts obtained by maceration (for both plants) as well as UAE and MAE (for lovage). However, the obtained results did not exhibit statistically significant correlation with the TPC and TFC. The highest cupric ion-reducing capacity was measured in methanol lovage extract prepared using UAE and in methanol basil and lovage extracts from MAE. Interestingly, a significantly higher amount of the extractive substances was measured in all methanolic lovage extracts compared to basil parallels. Thus, it can be concluded that the selection of the extraction medium and extraction technique depends on the used plant species, as well as on the future application and purpose (or role) of the prepared extracts.
Even though Melissa officinalis L. (lemon balm, fam. Lamiaceae) is a well-known medicinal, aromatic, and spicy plant, and its physicochemical profile and biological activity have been investigated, ...there is no detailed research regarding the influence of solvent nature (polarity) on the extraction of active compounds (total polyphenols and total flavonoids) and antioxidant activities of the obtained extracts. Therefore, this study aimed to evaluate the polyphenol and flavonoid contents, as well as the antioxidant potential of lemon balm extracts obtained by varying the polarity of the extraction solvents (methyl alcohol, acetone, ethyl acetate, and deionized water) and using three extraction techniques (maceration-MAC, ultrasound-UAE, and microwave-assisted extraction-MAE). Two in vitro tests (ABTS and FRAP assays) were used to determine the antioxidant activity of the extracts. Total tannin and total protein contents, extraction yield, and physical properties of the selected extracts were measured as well. The highest content of polyphenols was found for the methanolic and water extracts obtained by all three extraction techniques, while the highest flavonoid yield was detected only in the mentioned methanolic extracts. The microwave reactor provided methanolic, ethyl acetate, and water extracts with the highest ABTS radical scavenging activity, while in the case of UAE, it was methanolic and water extracts, and in the case of MAC only water extracts. On the other hand, among lemon balm extracts from MAC, water extract possessed the highest ferric reducing power, whereas in UAE and MAE, it was ethyl acetate extract. Total tannin content determined in selected water extracts was 2.55, 4.53, and 1.83 mg tannic acid equivalent (TAE)/mL, while total proteins amounted to 1.34, 1.50, and 1.31 mg/mL using MAC, UAE, and MAE, respectively. The content of total extractive substances in the form of the extraction yield was also determined for selected water extracts and amounted to 12.6 % for MAC, 17.2 % for UAE, and 36.8 % for MAE. Further, this research has included the investigation of some physical properties of lemon balm water extracts, such as conductivity (3.68-4.14 mS/cm), pH (5.99-6.43), density (0.854-0.901 g/mL), surface tension (26.0-31.7 mN/m), and viscosity (1.18-1.21 mPa·s). This research represents the base for the future encapsulation of lemon balm extracts, enriched in polyphenol content, in a novel type of biofunctional carrier that potentially can be applied in the pharmacy, chemical industry, and biotechnics.
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