Topical antifungal bigels: formulation, characterization and evaluation

Bigels with antifungal substances, ciclopirox olamine and terbinafine hydrochloride, were made of hydrogel (poloxamer 407 gel) and oleogel (polyethylene and liquid paraffin mixture). Prepared bigels were found physically stable at room temperature for six months and at least four months at 40 °C. Released amount of drug decreased when oleogel concentration in the formulation increased. Release test results depended on the insertion place of active substances. The amount of released substance was highest when ciclopirox olamine was incorporated in both phases in an equal quantity, and terbinafine hydrochloride in oleogel or in hydrogel. All formulations showed great inhibition of Microsporum canis. Thus, bigels with ciclopirox olamine and terbinafine hydrochloride are a promising dosage form for topical use

Propolis – quality analysis and use in topical formulations

The aim of this study was to produce propolis extracts, assess their quality and effect on skin cells and determine the penetration of active ingredients from designed semi-solid topical formulations. The use of higher-concentration ethanol and a larger amount of raw material allows extracting a larger quantity of active ingredients from raw propolis. In order to achieve effective extraction of compounds from raw materials, the use of ultrasound extraction is recommended for the production of aqueous extracts. Ultrasound extraction is an effective method for the production of aqueous extracts of propolis. The results show that depending on concentration, propolis extracts reduce the viability of keratinocytes. The phenolic compounds under observation penetrated the epidermis and dermis from designed formulations. The base of semi-solid formulation influences the efficacy of propolis preparations. The overall quantity of phenolic compounds that penetrated the skin was around 2 % from the ointment and 1.5 % from the cream

In vitro antiproliferative/cytotoxic activity on cancer cell lines of a cardanol and a cardol enriched from Thai Apis mellifera propolis

<p>Abstract</p> <p>Background</p> <p>Propolis is a complex resinous honeybee product. It is reported to display diverse bioactivities, such as antimicrobial, anti-inflammatory and anti-tumor properties, which are mainly due to phenolic compounds, and especially flavonoids. The diversity of bioactive compounds depends on the geography and climate, since these factors affect the floral diversity. Here, <it>Apis mellifera </it>propolis from Nan province, Thailand, was evaluated for potential anti-cancer activity.</p> <p>Methods</p> <p>Propolis was sequentially extracted with methanol, dichloromethane and hexane and the cytotoxic activity of each crude extract was assayed for antiproliferative/cytotoxic activity <it>in vitro </it>against five human cell lines derived from duet carcinoma (BT474), undifferentiated lung (Chaco), liver hepatoblastoma (Hep-G₂), gastric carcinoma (KATO-III) and colon adenocarcinoma (SW620) cancers. The human foreskin fibroblast cell line (Hs27) was used as a non-transformed control. Those crude extracts that displayed antiproliferative/cytotoxic activity were then further fractionated by column chromatography using TLC-pattern and MTT-cytotoxicity bioassay guided selection of the fractions. The chemical structure of each enriched bioactive compound was analyzed by nuclear magnetic resonance and mass spectroscopy.</p> <p>Results</p> <p>The crude hexane and dichloromethane extracts of propolis displayed antiproliferative/cytotoxic activities with IC₅₀values across the five cancer cell lines ranging from 41.3 to 52.4 μg/ml and from 43.8 to 53.5 μg/ml, respectively. Two main bioactive components were isolated, one cardanol and one cardol, with broadly similar <it>in vitro </it>antiproliferation/cytotoxicity IC₅₀values across the five cancer cell lines and the control Hs27 cell line, ranging from 10.8 to 29.3 μg/ml for the cardanol and < 3.13 to 5.97 μg/ml (6.82 - 13.0 μM) for the cardol. Moreover, both compounds induced cytotoxicity and cell death without DNA fragmentation in the cancer cells, but only an antiproliferation response in the control Hs27 cells However, these two compounds did not account for the net antiproliferation/cytotoxic activity of the crude extracts suggesting the existence of other potent compounds or synergistic interactions in the propolis extracts_.</p> <p>Conclusion</p> <p>This is the first report that Thai <it>A. mellifera </it>propolis contains at least two potentially new compounds (a cardanol and a cardol) with potential anti-cancer bioactivity. Both could be alternative antiproliferative agents for future development as anti-cancer drugs.</p

Sex- and age-related differences in the management and outcomes of chronic heart failure: an analysis of patients from the ESC HFA EORP Heart Failure Long-Term Registry

Aims: This study aimed to assess age- and sex-related differences in management and 1-year risk for all-cause mortality and hospitalization in chronic heart failure (HF) patients. Methods and results: Of 16 354 patients included in the European Society of Cardiology Heart Failure Long-Term Registry, 9428 chronic HF patients were analysed [median age: 66 years; 28.5% women; mean left ventricular ejection fraction (LVEF) 37%]. Rates of use of guideline-directed medical therapy (GDMT) were high (angiotensin-converting enzyme inhibitors/angiotensin receptor blockers, beta-blockers and mineralocorticoid receptor antagonists: 85.7%, 88.7% and 58.8%, respectively). Crude GDMT utilization rates were lower in women than in men (all differences: P\ua0 64 0.001), and GDMT use became lower with ageing in both sexes, at baseline and at 1-year follow-up. Sex was not an independent predictor of GDMT prescription; however, age >75 years was a significant predictor of GDMT underutilization. Rates of all-cause mortality were lower in women than in men (7.1% vs. 8.7%; P\ua0=\ua00.015), as were rates of all-cause hospitalization (21.9% vs. 27.3%; P\ua075 years. Conclusions: There was a decline in GDMT use with advanced age in both sexes. Sex was not an independent predictor of GDMT or adverse outcomes. However, age >75 years independently predicted lower GDMT use and higher all-cause mortality in patients with LVEF 6445%

Formulation of Gels and Emulgels with Malus domestica Borkh: Apple Extracts and Their Biopharmaceutical Evaluation In Vitro

Phenolic compounds that estimate apple extracts with multifaceted biological effects are potentially valuable for protection against skin disorders. The purpose of our research was to formulate gels and emulgels containing a complex of phenolic compounds of apple extracts and to perform a biopharmaceutical evaluation of semi-solid pharmaceutical forms, determining their antioxidant activity in vitro. HPLC analyses of phenolic compounds were performed. The total amount of phenolic compounds found in the sample of apples from the &lsquo;Paprastasis antaninis&rsquo; cultivar was 1455.5 &plusmn; 72.8 &micro;g/g. The release of phenolics from gels and emulgels was assessed by Franz-type diffusion cells. The in vitro release test revealed that phenolic compounds were released from the gel (G1&ndash;G6) formulations (70.6&ndash;73.8%) compared to the amounts (77.2&ndash;83.9%) released from the emulgel (E1&ndash;E6) formulations. The largest amount (83.9%) of phenolic compounds was released from the E5 formulation, while the smallest amounts (70.6%) were released from the formulations G3 and G5. The antioxidant activity evaluated by the DPPH and FRAP methods observed in all gel (G1&ndash;G6) and emulgel (E1&ndash;E6) formulations after 6 h were the strongest, compared to the activities observed in the formulations after 2 or 4 h. Gels and emulgels, which are rich in apple extracts, have strong antioxidant properties and may be promising choices for the development of new, innovative pharmaceutical forms or cosmetics

Correction: Stanciauskaite et al. Balsam Poplar Buds: Extraction of Potential Phenolic Compounds with Polyethylene Glycol Aqueous Solution, Thermal Sterilization of Extracts and Challenges to Their Application in Topical Ocular Formulations. <i>Antioxidants</i> 2022, <i>11</i>, 1771

In the original publication [...

Preparation of Ophthalmic Microemulsions Containing Lithuanian Royal Jelly and Their Biopharmaceutical Evaluation

Royal jelly is a natural substance secreted by worker honeybees that possesses antioxidant, anti-inflammatory, and other biological activities. The purpose of this study was to formulate microemulsions with incorporated Lithuanian royal jelly for possible ophthalmic delivery and to evaluate the quality of the microemulsions in vitro. The oil in water type microemulsions were prepared by the oil titration method, incorporating royal jelly, surfactant, co-surfactant, oil, and water. Physicochemical characteristics of the microemulsions and the quantity of 10-hydroxy-2-decenoic acid released in vitro were assessed. The in vitro assessment of prepared microemulsions formulations was performed with the Statens Seruminstitut rabbit cornea (SIRC) cell culture model. The results revealed that the droplet size of all microemulsion formulations was 67.88–124.2 nm and the polydispersity index was lower than 0.180. In the in vitro release study, the release of 10-hydroxy-2-decenoic acid depended on the amount of royal jelly incorporated and on the ratio of surfactant and co-surfactant in formulations. The in vitro tests with the SIRC cell culture line have shown that all formulations were found non-irritating

Rosmarinic Acid and Melissa officinalis Extracts Differently Affect Glioblastoma Cells

Lemon balm (Melissa officinalis L.) has many biological effects but especially important is its neuroprotective activity. The aim of the study is to produce different extracts of Melissa officinalis and analyse their chemical composition and biological properties on rat glioblastoma C6 cells. Results revealed that rosmarinic acid (RA) is the predominant compound of lemon balm extracts. RA has cytotoxic effect on glioblastoma cells (LC50 290.5 μM after the incubation of 24 h and LC50 171.3 μM after 48 h). RA at concentration 80–130 μM suppresses the cell proliferation and has an antioxidant effect. 200 μM and higher concentrations of RA have a prooxidant effect and initiate cell death through necrosis. The aqueous extract of lemon balm is also enriched in phenolic compounds: protocatechuic, caftaric, caffeic, ferulic, and cichoric acids and flavonoid luteolin-7-glucoside. This extract at concentrations 50 μM–200 μM RA has cytotoxic activity and initiates cell death through apoptosis. Extracts prepared with 70% ethanol contain the biggest amount of active compounds. These extracts have the highest cytotoxic activity on glioblastoma cells. They initiate generation of intracellular ROS and cell death through apoptosis and necrosis. Our data suggest that differently prepared lemon balm extracts differently affect glioblastoma cells and can be used as neuroprotective agents in several therapeutic strategies