Natural products are considered an important source of the therapeutic arsenal currently available. Among these alternatives are the seeds of Ambrosia peruviana (altamisa), whose extract has shown an ...anti-inflammatory effect. The main objective of this work was to perform a preformulation study of Ambrosia peruviana seeds ethanolic extract, where the main factors that affect the physical, chemical, and pharmacological stability of the extract were evaluated, as well as a compatibility study by differential scanning calorimetry (DSC) analysis against different excipients. A dry extract was obtained by rotary evaporation of the seeds macerated with 96% ethanol. The anti-inflammatory activity was determined by measuring its effect on NO production in RAW 264.7 macrophages, stimulated with LPS. The results showed that the dry extract maintained its stability over time when stored at a temperature of 4 and 25ºC, demonstrating its biological activity, the content of phenolic compounds, and its physicochemical parameters remain practically invariable. However, when exposed to high temperatures (60 ºC) it was affected. The thermal analysis revelated that the behavior of most of the selected excipients and the dry extract was maintained, which indicates that it did not present incompatibilities, therefore they can be candidates for formulating a microemulsion.
This study investigated the inhibitory effects of Achyrocline satureioides extract (ASE) incorporated into a topical nanoemulsion on Herpes Simplex Virus type 1 (HSV-1/KOS strain) replication, as ...well as the distribution of the main ASE flavonoids (quercetin, luteolin, and 3-O-methylquercetin) in porcine skin and mucosa. The ASE-loaded nanoemulsion showed more pronounced effects against HSV-1 replication when compared to the ASE or pure quercetin, as determined by the viral plaque number reduction assay. All flavonoids were detected in the skin epidermis (2.2 µg/cm2) and the mucosa upper layers (3.0 µg/cm2) from ASE-loaded nanoemulsion until 8 h after topical application. A higher amount of flavonoids was detected when these tissues were impaired, especially in deeper mucosa layers (up to 7-fold). Flavonoids were detected in the receptor fluid only when the mucosa was injured. Such results were supported by confocal microscopy images. Overall, these findings suggest that the tested ASE-loaded nanoemulsion has potential to be used topically for herpes infections.
Isoflavones are polyphenol compounds found mainly in legumes such as soybeans (
Glycine max
(L.) Merrill). These compounds can be found in different chemical forms; however, the beneficial effects ...for skin care have been mainly credited to their free forms. This manuscript claims to review the main effects of isoflavone aglycones on the skin, the different techniques for obtaining bioactive forms from soybeans, and the interest in incorporating them into topical systems. The benefits of dermatological application of isoflavones, as anti-aging action, estrogenic activity, wound healing properties, and antiphotocarcinogenic effects are highlighted. Moreover, the advantages and drawbacks of the extraction techniques of soybeans, methods for converting glucosides into aglycones, and purification procedures are described. Different strategies to incorporate these poorly soluble compounds in conventional or nanostructured delivery systems are also discussed. Illustrative examples especially for genistein-loaded liposomes, nanoemulsions, nanocapsules and cyclodextrin complexation are reported.
Achyrocline satureioides (Lam.) DC Asteraceae extracts (ASEs) have been investigated for the treatment of various skin disorders. This study reports the effects of ASE-loaded nanoemulsions (NEASE) on ...the cellular viability, death by necrosis, and migration of immortalized human keratinocytes (HaCaT cell line), as well as the irritant potential through the hen’s egg chorioallantoic membrane test (HET-CAM). NEASE exhibited a polydispersity index above 0.12, with a droplet size of 300 nm, ζ-potential of −40 mV, and content of flavonoids close to 1 mg/mL. No cytotoxicity of the ASE was observed on HaCaT by MTT assay (up to 10 µg/mL). A significant increase of HaCaT viability was observed to NEASE (up to 5 μg/mL of flavonoids), compared to treatment with the ASE. The necrosis death evaluation demonstrated that only NEASE did not lead to cell death at all the tested concentrations. The scratch assay demonstrated that NEASE was able to increase the cell migration at low flavonoid concentrations. Finally, the HET-CAM test proved the non-irritative potential of NEASE. Overall, the results indicate the potential of the proposed formulations for topical use in wound healing, in view of their promising effects on proliferation and migration in keratinocytes, combined with an indication of the absence of cytotoxicity and non-irritating potential.
(Lam.) DC extract-loaded nanoemulsions have demonstrated potential for wound healing, with promising effects on keratinocyte proliferation. We carried out the first in vivo investigation of the wound ...healing activity of a hydrogel containing
extract-loaded nanoemulsions. We prepared hydrogels by adding the gelling agent (Carbopol
Ultrez) to extract-loaded nanoemulsions (~250 nm in diameter) obtained by spontaneous emulsification. The final flavonoid content in formulation was close to 1 mg/mL, as estimated by ultra-fast liquid chromatography. Permeation/retention studies using porcine ear skin showed that flavonoids reached deeper layers of pig ear skin when it was damaged (up to 3.2 µg/cm² in the dermis), but did not reach the Franz-type diffusion cell receptor fluid. For healing activity, we performed a dorsal wound model using Wistar rats, evaluating the lesion size, anti-inflammatory markers, oxidative damage, and histology. We found that extract-loaded formulations promoted wound healing by increasing angiogenesis by ~20%, reducing inflammation (tumor necrosis factor α) by ~35%, decreasing lipid damage, and improving the re-epithelialization process in lesions. In addition, there was an increase in the number of blood vessels and hair follicles for wounds treated with the formulation compared with the controls. Our findings indicate that the proposed formulation could be promising in the search for better quality healing and tissue reconstruction.
Background and Purpose
In cor pulmonale, the increased afterload imposed on the right ventricle (RV) generates a maladaptive response, impairing the contractile cardiac function. Oxidative mechanisms ...play an important role in the pathophysiology and progression of this disease. The administration of pterostilbene (PTS), a phytophenol with antioxidant potential, may represent a therapeutic option. In the present study, we evaluated the effect of PTS complexed with hydroxypropyl‐β‐cyclodextrin (HPβCD) on hypertrophy, contractile function and oxidative parameters in the RV of rats with pulmonary hypertension, induced by the administration of monocrotaline (MCT).
Experimental Approach
The rats received daily doses of the PTS : HPβCD complex at 25, 50 or 100 mg·kg−1, p.o., for 14 days. The diastolic function, E/A ratio, and systolic function, shortening fraction, fractional area change (FAC) and tricuspid annular plane systolic excursion (TAPSE) of the RV were determined by echocardiography.
Key Results
The PTS : HPβCD complex reduced the production of NADPH oxidase‐dependent superoxide anions and oxidative stress in the RV of MCT‐treated rats in a dose‐dependent manner. At higher doses it prevented the reduction in FAC and TAPSE in MCT‐treated animals.
Conclusions and Implications
The PTS : HPβCD complex prevented the maladaptative remodelling and protected systolic function in the RV of rats with pulmonary hypertension. These cardioprotective mechanisms may be related, in part, to the antioxidant potential of PTS, favoured by the increased p.o. bioavailability promoted by the presence of HPβCD in the complex.
The aim of this study was to optimize topical nanoemulsions containing genistein, by means of a 23 full factorial design based on physicochemical properties and skin retention. The experimental ...arrangement was constructed using oil type (isopropyl myristate or castor oil), phospholipid type (distearoylphosphatidylcholine DSPC or dioleylphosphaditylcholine DOPC), and ionic cosurfactant type (oleic acid or oleylamine) as independent variables. The analysis of variance showed effect of third order for particle size, polydispersity index, and skin retention of genistein. Nanoemulsions composed of isopropyl myristate/DOPC/oleylamine showed the smallest diameter and highest genistein amount in porcine ear skin whereas the formulation composed of isopropyl myristate/DSPC/oleylamine exhibited the lowest polydispersity index. Thus, these two formulations were selected for further studies. The formulations presented positive ζ potential values (>25 mV) and genistein content close to 100% (at 1 mg/mL). The incorporation of genistein in nanoemulsions significantly increased the retention of this isoflavone in epidermis and dermis, especially when the formulation composed by isopropyl myristate/DOPC/oleylamine was used. These results were supported by confocal images. Such formulations exhibited antiherpetic activity in vitro against herpes simplex virus 1 (strain KOS) and herpes simplex virus 22 (strain 333). Taken together, the results show that the genistein-loaded nanoemulsions developed in this study are promising options in herpes treatment.
The aim of this study was to develop a modified release system (MRS), hydrophilic matrix type, containing Physalis peruviana fruit extract as the active ingredient. For this purpose, a co-processing ...method via spray-drying was used, whose conditions were previously established, using in the formulation silicon dioxide as a drying aid and HPMC K15M as a polymer, to modulate the release of the extract. Four formulations were prepared, and pharmacotecnical properties and hypoglycemic in vitro assay were evaluated; in these formulations, the ratio of the polymer was changed to find the influence of this excipient on the release of the extract, from the hydrophilic matrices, under different pH conditions simulating the gastrointestinal tract. To selected formulation from this test, other assays were performed such as erosion studies, water uptake and movement fronts, which complemented the evaluation on the release mechanism. It was established that composition of the co-processed with and without polymer, presented good flow and compaction properties. The characterization of the MRS showed a modulated release of the extract, the concentration of the polymer was the main factor that affected its release rate. Formulation Ex: SiO2: HPMC-K15M (55.2%: 41.4%: 3.4%) was selected, among the formulations evaluated, because it presented adequate modulation of the extract release. The release mechanism was a combination of diffusion of the extract and erosion of the matrix. The in-vitro studies showed that the excipients and the process did not significantly influence the hypoglycemiant activity of the extract.
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•Co-processed material was elaborated from polymer and P. peruviana extract.•Co-processed material was characterized in its physical-mechanical properties.•A control release tablet from P. peruviana fruits extract was developed.•Its release was governed by combination of diffusion and erosion mechanisms.•The hypoglycemic activity remained after transformation to solid state.
Non-alcoholic steatohepatitis (NASH) is a frequent condition in obese patients that may progress to end-stage liver disease. This study was designed to evaluate the modulation of this condition by ...use of quercetin (Q), a flavonoid largely found in vegetable foods, with known anti-inflammatory and antioxidant properties, in the experimental model of non-alcoholic steatohepatitis (NASH) using a diet deficient in methionine and choline (MCD). Male C57BL6 mice were divided into four groups (n = 16): (i) Control plus vehicle (control ration plus carboxymethylcellulose 1% used as vehicle, CO + V); (ii) Control ration plus Q 50 mg/kg (CO + Q); (iii) MCD diet plus vehicle (NASH + V); and (iv) MCD diet plus Q (NASH + Q). Diets were administered for 4 weeks. At the end of the experimental period, liver alterations, bioindicators of oxidative stress and DNA damage were assessed. NASH was diagnosed in 100% of the mice that were fed the MCD diet. In addition, a significant increase in DNA damage in liver tissue from NASH + V group was observed in comparison with CO + V. The group NASH + Q showed a significant decrease in hepatic damage enzymes, lipoperoxidation, DNA damage and a lower degree of macrovesicular steatosis, ballooning and inflammatory process. These findings suggest that Q may have protective effects by improving liver integrity in NASH.
Lactobionic acid and sorbitol are produced from lactose and fructose in reactions catalyzed by glucose–fructose oxidoreductase and glucono-δ-lactonase, periplasmic enzymes present in
Zymomonas ...mobilis
cells. Considering the previously established laboratory-scale process parameters, the bioproduction of lactobionic acid was explored to enable the transfer of this technology to the productive sector. Aspects such as pH, temperature, reuse and storage conditions of Ca-alginate immobilized
Z. mobilis
cells, and large-scale bioconversion were assessed. Greatest catalyst performance was observed between pH range of 6.4 and 6.8 and from 39 to 43 °C. The immobilized biocatalyst was reused for twenty three 24-h batches preserving the enzymatic activity. The activity was maintained during biocatalyst storage for up to 120 days. Statistically similar results, approximately 510 mmol/L of lactobionic acid, were attained in bioconversion of 0.2 and 3.0 L, indicating the potential of this technique of lactobionic acid production to be scaled up to the industrial level.
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