Apples are an important source of biologically active compounds. Consequently, we decided to model hard gelatin capsules with lyophilized apple powder by using different excipients and to evaluate ...the release kinetics of phenolic compounds. The apple slices of "Ligol" cultivar were immediately frozen in a freezer (at -35°C) with air circulation and were lyophilized with a sublimator at the pressure of 0.01 mbar (condenser temperature, -85°C). Lyophilized apple powder was used as an active substance filled into hard gelatin capsules. We conducted capsule disintegration and dissolution tests to evaluate the quality of apple lyophilizate-containing capsules of different encapsulating content. Individual phenolic compounds can be arranged in the following descending order according to the amount released from the capsules of different compositions: chlorogenic acid > rutin > avicularin > hyperoside > phloridzin > quercitrin > (-)-epicatechin > isoquercitrin. Chlorogenic acid was the compound that was released in the highest amounts from capsules of different encapsulating content: its released amounts ranged from 68.4 to 640.3 μg/mL. According to the obtained data, when hypromellose content ranged from 29% to 41% of the capsule mass, the capsules disintegrated within less than 30 min, and such amounts of hypromellose did not prolong the release of phenolic compounds. Based on the results of the dissolution test, the capsules can be classified as fast-dissolving preparations, as more than 85% of the active substances were released within 30 min.
Bronchial asthma is one of the most common chronic respiratory diseases, and its care is often complex. In this research, we tested the proposal that participation of pharmacists in the management of ...bronchial asthma can improve patient outcomes. A two-stage study was constructed consisting of a training element and a service element, using the Asthma Control Test and a structured questionnaire about the patients’ disease condition (based on the results of a qualitative study). The study was conducted in 21 pharmacies in Lithuania and involved 338 asthmatic patients (age 18–88 years). It was found that before the pharmacy service was provided, the average number of mistakes patients made in administration of asthma medications was 2.03; this number decreased to 1.12 after the service was provided (p<0.05). Disease control paralleled the improvement in number of mistakes: 26.1% of patients who previously exerted no control over the disease symptoms began to exert sufficient control over their asthma symptoms (Asthma Control Test >20) after the service was provided (p<0.05). The reduced number of mistakes probably can be attributed to the positive effects of the provided services. By reducing the number of patient mistakes, pharmacists may improve the outcomes of asthmatic patients.
Resveratrol is well known for its antioxidant activity and susceptibility to ultraviolet radiation. Development of formulations providing improved stability and relevant drug delivery of resveratrol ...is still a challenging task. The aim of this study was to determine protective characteristics of formulated microemulsions by evaluating photoisomerization of resveratrol and to investigate the effects of resveratrol on human keratinocyte cells under oxidative stress caused by ultraviolet radiation. Incorporation of resveratrol into microemulsions resulted in increased photostability of active compounds and the results demonstrated that photodegradation of resveratrol was significantly delayed. Results of biopharmaceutical evaluation in vitro demonstrated that up to 60 % of resveratrol was released from microemulsions within 6 hours under a constant release rate profile. In vivo biological testing confirmed the ability of resveratrol to protect cells from oxidative stress and to increase cell viability. It was concluded that microemulsions might be considered in the development of UV light sensitive compounds.
Mitochondria are both the primary targets and mediators of ischaemic damage in brain cells. Insufficient oxygen causes reactive oxygen species that damage the mitochondria, leading to the loss of ...functionality and viability of highly energy-demanding neurons. We have recently found that aqueous (AqEP), polyethylene glycol-aqueous (Pg-AqEP) and ethanolic propolis extracts (EEP) can modulate mitochondria and ROS production in C6 cells of astrocytic origin. The aim of this study was to investigate the effect of the extracts on viability, mitochondrial efficiency and superoxide generation, and inflammatory cytokine release in primary rat cerebellar neuronal-glial cell cultures affected by ischaemia (mimicked by hypoxia +/- deoxyglucose). AqEP and Pg-AqEP (15-60 µg/mL of phenolic compounds, or PC) significantly increased neuronal viability in ischaemia-treated cultures, and this was accompanied by a reduction in mitochondrial superoxide levels. Less extended protection against ischaemia-induced superoxide production and death was exhibited by 2 to 4 µg/mL of PC EEP. Both Pg-AqEP and Ag-EP (but not EEP) significantly protected the cultures from hypoxia-induced elevation of TNF-α, IL-1β and IL-6. Only Pg-AqEP (but not AqEP or EEP) prevented hypoxia-induced loss of the mitochondrial basal and ATP-coupled respiration rate, and significantly increased the mitochondrial respiratory capacity. Summarising, the study revealed that hydrophilic propolis extracts might protect brain cells against ischaemic injury by decreasing the level of mitochondrial superoxide and preventing inflammatory cytokines, and, in the case of Pg-AqEP, by protecting mitochondrial function.
The aim of this study was to evaluate the release of rosmarinic acid (RA) from the experimental topical formulations with the Melissa officinalis L. extract and to evaluate its penetration through ...undamaged human skin ex vivo. The results of the in vitro release study showed that higher amounts of RA were released from the emulsion vehicle when lemon balm extract was added in its dry form. An inverse correlation was detected between the released amount of RA and the consistency index of the formulation. Different penetration of RA into the skin may be influenced by the characteristics of the vehicle as well as by the form of the extract. The results of penetration assessment showed that the intensity of RA penetration was influenced by its lipophilic properties: RA was accumulating in the epidermis, while the dermis served as a barrier, impeding its deeper penetration.
The objective of this study was to formulate optimal formulations of microemulsions (MEs) and evaluate their feasibility for delivery of resveratrol into human skin ex vivo. Oil-in-water MEs were ...formulated using surfactant (S) PEG-8 caprylic/capric glycerides and cosurfactant (CoS) polyglyceryl-6-isostearate. Ethyl oleate was used as an oily phase. MEs were formulated using 5 : 1, 6 : 1, and 7 : 1 surfactant and cosurfactant (S : CoS) weight ratios. Pseudoternary phase diagrams were constructed and optimal compositions of MEs were obtained using Design Expert software. Mean droplet size for optimized ME formulations was determined to be 68.54 ± 1.18 nm, 66.08 ± 0.16 nm, and 66.66 ± 0.56 nm for systems with S : CoS weight ratios 5 : 1, 6 : 1, and 7 : 1, respectively. Resveratrol loading resulted in mean droplet size increase. The distribution of droplet size between fractions changed during storage of formulated MEs. Results demonstrated the increase of number of droplets and relative surface area when S : CoS weight ratios were 6 : 1 and 7 : 1 and the decrease when S : CoS weight ratio was 5 : 1. The highest penetration of resveratrol into the skin ex vivo was determined from ME with S : CoS weight ratio 5 : 1. It was demonstrated that all MEs were similar in their ability to deliver resveratrol into the skin ex vivo.
Antioxidant and free radical scavenging effects are attributed to phenolic compounds present in propolis, and when delivered to the skin surface and following penetration into epidermis and dermis, ...they can contribute to skin protection from damaging action of free radicals that are formed under UV and premature skin aging. This study was designed to determine the penetration of phenolic acids and vanillin into the human skin in vitro from experimentally designed vehicles. Results of the study demonstrated the ability of propolis phenolic acids (vanillic, coumaric, caffeic, and ferulic acids) and vanillin to penetrate into skin epidermis and dermis. The rate of penetration and distribution is affected both by physicochemical characteristics of active substances and physical structure and chemical composition of semisolid vehicle. Vanillin and vanillic acid demonstrated relatively high penetration through epidermis into dermis where these compounds were concentrated, coumaric and ferulic acids were uniformly distributed between epidermis and dermis, and caffeic acid slowly penetrated into epidermis and was not determined in dermis. Further studies are deemed relevant for the development of semisolid topically applied systems designed for efficient delivery of propolis antioxidants into the skin.
The aim of the study was to design gels with lemon balm extract, assess their quality, and investigate the effect of rosmarinic acid on skin cells in normal conditions and under oxidative stress. ...Methods. The quantities of rosmarinic acid (RA) released from gels were evaluated by applying the HPLC technique. HaCaT cell viability was assessed by using the MTT method. ROS generation was measured using DCFH-DA dye. The results showed that the gelling material affected the release of RA content from gels. Lower and slower RA content release was determined in carbomer-based gels. After 6 hours of biopharmaceutical research in vitro, at least 4% of RA was released from the gel. The results of the biological studies on HaCaT cells demonstrated that, in the oxidative stress conditions, RA reduced intracellular ROS amounts to 28%; 0.25–0.5 mg/mL of RA increased cell viability by 10–24% and protected cells from the damage caused by H2O2. Conclusions. According to research results, it is appropriate to use a carbomer as the main gelling material, and its concentration should not exceed 1.0%. RA, depending on the concentration, reduces the amount of intracellular ROS and enhances cell viability in human keratinocytes in oxidative stress conditions.
Royal jelly is a bee product with a high commercial interest due to its exceptional biological properties and unique composition. In this study, we evaluated the quality of Lithuanian Royal jelly, ...including the water content, antioxidant activity, amount of polyphenolic compounds and pH. The results indicated that Lithuanian Royal jelly had the values of pH, water content as well as polyphenols that were comparable to the data already published. In the study, we also evaluated the impact of various solvents on the amount of 10-hydroxy-2-decenoic acid (10-HDA), the main fatty acid, naturally occurring only in Royal jelly and which is the quality marker, in solutions obtaining the amount using the HPLC method. According to solubility tests performed, 10-HDA from Royal jelly is best soluble in ethanol of various concentrations, yet in order to be used for exceptional Royal jelly antibacterial and many other biological properties it was important to increase the solubility in aqueous solutions. Addition of β-cyclodextrin has increased the amount of 10-HDA in solution up to the level of ethanol solutions. The antioxidant and antibacterial tests have demonstrated that Lithuanian Royal jelly exhibits positive effects against free radicals, as well as mostly occurring bacterial strains, such as Esherichia coli, Pseudomonas aeruginosa, Enterococcus faecalis and Staphylococcus aureus. As the conclusion of this study, we can assume that the quality assessment methods chosen for this study, are significant for standardizing the procedures for further studies.
Microemulsions (MEs) were formulated using PEG-8 caprylic/capric glycerides and ethanolic propolis extracts. Characterization of MEs was performed by determining mean droplet size, polydispersity ...index, stability under varying external factors, and formulation effect on delivery of phenolic compounds into the skin ex vivo. Essential oils were included into the formulations of MEs and their influence on physical characteristics of the nanostructured systems as well as penetration into epidermis and dermis were evaluated. The droplet size, their distribution, and stability of the formulated MEs were not affected. Presence of essential oils in the formulation increased penetration of phenolic compounds in general, but only the amount of ferulic acid increased significantly. Mean droplet size increased with increase of oily phase amount, suggesting that phenolic compounds and components of essential oils were not modifying the formation of the interphase film composition and/or structure. Phenolic compounds were predominantly located in the lipid phase of the MEs thus minimizing their availability at the surface of the skin.
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