Diego Francisco Cortés-Rojas

Clove (Syzygium aromaticum): a precious spice

Clove (Syzygium aromaticum) is one of the most valuable spices that has been used for centuries as food preservative and for many medicinal purposes. Clove is native of Indonesia but nowadays is cultured in several parts of the world including Brazil in the state of Bahia. This plant represents one of the richest source of phenolic compounds such as eugenol, eugenol acetate and gallic acid and posses great potential for pharmaceutical, cosmetic, food and agricultural applications. This review includes the main studies reporting the biological activities of clove and eugenol. The antioxidant and antimicrobial activity of clove is higher than many fruits, vegetables and other spices and should deserve special attention. A new application of clove as larvicidal agent is an interesting strategy to combat dengue which is a serious health problem in Brazil and other tropical countries. Pharmacokinetics and toxicological studies were also mentioned. The different studies reviewed in this work confirm the traditional use of clove as food preservative and medicinal plant standing out the importance of this plant for different applications.

Physicochemical Properties of Phytopharmaceutical Preparations as Affected by Drying Methods and Carriers

This article reports a study of the effects of the drying methods and drying carriers on system performance and physicochemical properties of spray- and spouted bed–dried phytopharmaceutical preparations from Bidens pilosa L. Colloidal silicon dioxide, β-cyclodextrin, maltodextrin dextrose equivalent (DE) 10, and microcrystalline cellulose were used as drying carriers. The dried product was characterized by the particle size and morphology, total flavonoid content, solubility, flowability, and water activity. High-performance liquid chromatography (HPLC) was used to detect four marker compounds previously reported for this plant. Spray and spouted bed drying systems were compared through energetic efficiency, product recovery, elutriation, and product accumulation. The crystalline state of the powders was assessed by X-ray diffraction. Results showed high degradation rates for total flavonoid content and marker compounds during spouted bed drying. Depending on the drying carrier added to extractive solutions, different degrees of protection from degradation were conferred, and the physical characteristics of the product were changed accordingly. The lowest flavonoid degradation (8.6%) and the higher concentration of marker compounds were obtained using β-cyclodextrin as the drying carrier. Particle size was higher when a blend of Aerosil (Evonik Degussa, Hanau, Germany) and cellulose was employed as the drying carrier. A maximum product recovery of 86.9% was achieved by spray drying and 72.9% by spouted bed drying with the Aerosil : cellulose composition.

Bioactive compounds in Bidens pilosa L. populations: a key step in the standardization of phytopharmaceutical preparations

The total flavonoid content (TFC), total polyphenols content (TPC), and in vitro antioxidant activity (AA) of six Bidens pilosa L., Asteraceae, populations harvested from different localities were evaluated in this work. The plants were separated in roots, stems, and leaves/flowers, and the influence of extraction methods was investigated.Areversed-phase high-performance liquid chromatography method (HPLC) was developed and employed to obtain characteristic HPLC fingerprints of the bioactive compounds present in the extractive solutions, which were correlated with the TFC, TPC, and AA. Extractive solutions of leaves/flowers presented a higher AA when compared with those obtained from other parts of the plant (IC50 of 35.35±0.10 µg/mL). The stem extracts presented the lowest AA (IC50 117.2±1.96 µg/mL). A direct correlation of AA with TFC and TPC was evidenced. The highest AA was obtained by dynamic maceration and was statistically different from the AA presented by the extractive solutions obtained by other extraction methods. The results of this work evidenced differences that can be found at different stages of development of phytopharmaceutical preparations from B. pilosa and highlighted the importance of using the concentration of marker compounds as well as HPLC fingerprints as quality control parameters.

Surfactant Mediated Extraction of Antioxidants from Syzygium aromaticum

In the present study surfactant mediated extraction has been investigated for the extraction of antioxidants from clove flower buds (Syzygium aromaticum). The advantage of this technique is the replacement of organic solvents or other toxic substances by surfactants that could be part of a formulation. The influence of the Hydrophilic Lipophylic Balance (HLB) on extraction was examined in the range of 4.3 to 15 by the mixture of two commonly used surfactants in pharmaceutical and food applications (Tween 80 and Span 80). The effect of the surfactant concentration (2, 5, and 10%) was also evaluated. Results showed that higher HLB values improved eugenol and polyphenols extraction, which could be correlated with the in vitro antioxidant activity. Surfactant concentration of 5% (w/w) showed to be more effective than 2% and there were no significant differences between the results obtained at concentrations of 5 and 10%. The effect of the pH was also investigated on Tween 80 solutions and results showed that increases on the pH value improved the eugenol extraction.

Effects of lipid formulations on clove extract spray dried powders: comparison of physicochemical properties, storage stability and in vitro intestinal permeation

Abstract Clove is an aromatic plant spice with potent antioxidant and anti-inflammatory activity. Eugenol is the main compound which contributes to such medicinal and nutritional benefits. To date, the formulation of unstable, volatile and poorly water-soluble compounds remains a challenging task. Lipid formulations can be used to improve physicochemical and biopharmaceutical properties of poorly soluble compounds. The aim of this study is to investigate the effects of lipids, such as Gelucire and Compritol on physicochemical properties; stability and in vitro intestinal permeation of spray dried powdered formulations loaded with clove’s bioactive compounds. Results showed that eugenol retention in spray-dried powders could be correlated with antioxidant activity and with mass recovery after spray drying. Adding Gelucire but not Compritol to clove extract formulations, improved solubility of spray dried powders. Stability test in high humidity environment (63.5% RH) suggested that formulations including both Gelucire and Compritol were significantly more stable compared to the formulation without any lipid at the two tested temperatures (25 °C and 40 °C). This suggests that lipid additions to clove (Syzygium aromaticum) extract formulations provide protective effects for the spray dried powders in high-humidity environments. In addition, results from in vitro intestinal permeation studies suggested that eugenol uptake, was not being hindered by transporters nor was the absorption being affected by lipid formulations.