Abstract We report on a systematic review of the efficacy of turmeric derivatives for the in vivo treatment of peripheral neuropathies. Our review protocol followed the PRISMA Statement. The Medline (PubMed), Web of Science, Scopus, and Scielo databases were used. The search strategy was (“neuropathy” OR “neuropathies” OR “nerve injury” OR “nerve injuries”) AND (“curcumin” OR “turmeric yellow” OR “yellow, turmeric” OR “diferuloylmethane”). Eligibility criteria were in vivo animal models, published in English, Portuguese, Spanish, or French, evaluating the efficacy of turmeric derivatives in the treatment of peripheral neuropathies. We have included 30 papers, and all consisted of pre-clinical trials with good methodological quality. Animals treated with turmeric derivatives (i.e., curcumin, curcumin by-products and curcumin loaded delivery systems) demonstrated remarkable amelioration in the injuries caused by diabetic and sciatic neuropathy, as well as for vincristine, cisplatin, and alcohol-induced neuropathy, especially with regards to the functional recovery of the affected nerve. Turmeric has great potential for the treatment of peripheral neuropathies, including those associated with diabetes mellitus. Clinical trials still need to be performed to assess the feasibility of human treatment as an alternative or adjuvant to existing pharmacological therapy.

Abstract The antinociceptive and anti-inflammatory activities of crude ethanolic extract of Celtis iguanaea leaves and their active fractions are reported. The oral treatment with crude ethanolic extract (CEE; 100, 300 or 1000 mg/Kg) inhibited the number of writhings in a dose-dependent manner. The intermediate dose also inhibited formalin-induced nociception in both phases. The oral treatment with dichloromethane fraction (DF; 9 mg/Kg) produced antinociceptive effect in both phases of formalin test; however, the treatment with ethyl acetate fraction (EAF; 16 mg/Kg) reduced pain only in the second phase of this test. The oral treatments with CEE (300 mg/Kg) or DF (9 mg/Kg) reduced the nociception induced by capsaicin and pre-treatment with naloxone did not change these effects. The oral administration of CEE (300 mg/Kg), DF (9 mg/Kg) or ethyl EAF (16 mg/Kg) reduced ear edema, leukocytes migration and myeloperoxidase activity. Furthermore, the oral treatment with CEE (300 mg/Kg) or EAF (16 mg/Kg) reduced the level of Tumor Necrosis Factor - Alpha (TNF-α) in the pleurisy test. In conclusion, the DF showed antinociceptive activity that involves the vanilloid system as well as anti-inflammatory effect and the EAF showed anti-inflammatory activity involving the reduction of TNF-α cytokine.

Abstract UVB-irradiation increases the risk of various skin disorders, therefore leading to inflammation and oxidative stress. In this sense, antioxidant-rich herbs such as Rosmarinus officinalis may be useful in minimizing the damage promoted by reactive oxygen species. In this work, we report the efficacy of a R. officinalis hydroethanolic extract (ROe)-loaded emulgel in preventing UVB-related skin damage. Total phenols were determined using Folin-Ciocalteu assay, and the main phytocomponents in the extract were identified by UHPLC-HRMS. Moreover, in vitro sun protection factor (SPF) value of ROe was also assessed, and we investigated the in vivo protective effect of an emulgel containing ROe against UVB-induced damage in an animal model. The ROe exhibited commercially viable SPF activity (7.56 ± 0.16) and remarkable polyphenolic content (24.15 ± 0.11 mg (Eq.GA)/g). HPLC-MS and UHPLC-HRMS results showcased that the main compounds in ROe were: rosmarinic acid, carnosic acid and carnosol. The evaluation of the in vitro antioxidant activity demonstrated a dose-dependent effect of ROe against several radicals and the capacity to reduce iron. Therefore, we demonstrated that topical application of the formulation containing ROe inhibited edema formation, myeloperoxidase activity, GSH depletion and maintained ferric reducing (FRAP) and ABTS scavenging abilities of the skin after UVB exposure.

ABSTRACT A 33 Box–Behnken design and Response Surface Methodology were performed to evaluate the influence of extract feed rate, drying air inlet temperature and spray nozzle airflow rate on the process yield, stability parameters (moisture content and water activity) and on several physicomechanical properties of spray-dried rosemary extracts. Powder yield ranged from 17.1 to 74.96%. The spray-dried rosemary extracts showed moisture content and water activity below 5% and 0.5%, respectively, which indicate their chemical and microbiological stabilities. Even without using drying aids, some sets of experimental conditions rendered dried products with suitable flowability and compressibility characteristics for direct preparation of solid dosage forms. Analysis of variance and Response Surface Methodology proved that studied factors significantly affected most of the spray-dried rosemary extract quality indicators at different levels. The main processing parameter affecting the spray-dried rosemary extract characteristics was inlet temperature. The best combination of parameters used to obtain a reasonable yield of stable dry rosemary extracts with adequate technological properties for pharmaceutical purpose involves an extract feed rate of 2 ml/min, 80 °C inlet temperature and 40 l/min SA. The design of experiments approach is an interesting strategy for engineering spray-dried rosemary extracts with improved characteristics for pharmaceutical industrial purpose.

Bioresorbable polymeric films were prepared by solvent casting using a tyrosine-derived polycarbonate and metronidazole (MDZ) as the model drug at 2.5%, 5% and 10% (w/w). Drug loading did not affect the water uptake, drug release, polymer degradation or erosion profiles. All devices released approximately 85% (w/w) of the drug within a 1.5 h period. This may be attributed to the rapid water uptake of the polymer. An increase in the water uptake correlated with a linear rate increase of the polymer degradation (0.968 ≤ R2 ≤ 0.999). Moreover, MDZ presented a remarkable plasticizing effect for the polymer and drug loading exerted a significant impact on the mechanical properties of the obtained films. The results obtained can be used to further the development of novel biocompatible and biodegradable polymeric platforms for the delivery of metronidazole and other drugs in a broad range of pharmaceutical applications.

A 2³ full factorial design was used to assess the impact of spraying air flow rate (30-50 L/min), drying air inlet temperature (90-150 ºC) and extract feed rate (4-6 g/min) on the quality of Eugenia dysenterica DC., Myrtaceae, spray-dried extracts. Response surface methodology (RSM) was applied to analyze the significance of the effects of process factors on product quality and to obtain fitted equations to predict dry powder properties. Powder yields were satisfactory, ranging from 34.64 to 63.92%. The dried products showed moisture contents and water activities below 5% and 0.5, respectively. The recuperation ratios of total polyphenols, tannins and flavonoids ranged from 88.66 to 99.07%, 70.38 to 81.87% and 74.51 to 98.68%, respectively. Additionally, in some conditions the parameters related to dry product’s flowability and compressibility varied over a range acceptable for pharmaceutical purposes. RSM proved that studied factors significantly affected most of the quality indicators at different levels. The spray drying technology is an attractive and promising alternative for the development of intermediate phytopharmaceutical products of E. dysenterica.

The aim of this work was to study the effect of dynamic maceration factors upon the curcumin content of Curcuma longa L., Zingiberaceae, extracts and to determine the optimum set of parameters for the extraction of curcumin using a 2(5) full factorial design and the response surface methodology. Under the established conditions, the content of soluble solids and curcumin in the extracts ranged from 0.8 to 3.4%, and from 0.1 to 1.8%, respectively. The most influential variable observed for the extraction was the ethanolic strength of the solvent. The optimized condition involves an extraction time of 12 h, agitation speed of 30 rpm, drug to solvent ratio of 1/6, extraction temperature of 80 ºC and the solvent with ethanolic strength of 70%. The data reported herein are useful for further developments of curcuma phytopharmaceutical intermediate products with optimized characteristics.

A new electroanalytical method coupling TLC-DPV in solid state was developed for quantitative determination of phytoantioxidants with medicinal purpose, e.g. rosmarinic acid (RA) in samples of phytopharmaceuticals, e.g. rosemary (Rosmarinus officinalis L.). The method showed to be feasible, presenting linearity in concentrations ranging from 0.694 x 10-3 to 9.526 x 10-3 mol L-1 (r = 0.9945), good sensibility, selectivity, reproducibility, repeatability, agility and affordable cost. The concentrations of RA in different extracts of rosemary ranged from 0.05 to 0.52 (% w/w), presenting high recovery levels when compared to HPLC.