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Sci. Pharm., Volume 89, Issue 3 (September 2021) – 5 articles

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Review
The Chemistry and Pharmacology of Fungal Genus Periconia: A Review
Sci. Pharm. 2021, 89(3), 34; https://doi.org/10.3390/scipharm89030034 - 29 Jul 2021
Viewed by 283
Abstract
Periconia is filamentous fungi belonging to the Periconiaceae family, and over the last 50 years, the genus has shown interest in natural product exploration for pharmacological purposes. Therefore, this study aims to analyze the different species of Periconia containing natural products such as [...] Read more.
Periconia is filamentous fungi belonging to the Periconiaceae family, and over the last 50 years, the genus has shown interest in natural product exploration for pharmacological purposes. Therefore, this study aims to analyze the different species of Periconia containing natural products such as terpenoids, polyketides, cytochalasan, macrosphelides, cyclopentenes, aromatic compounds, and carbohydrates carbasugar derivates. The isolated compound of this kind, which was reported in 1969, consisted of polyketide derivatives and their structures and was determined by chemical reaction and spectroscopic methods. After some years, 77 compounds isolated from endophytic fungus Periconia were associated with eight plant species, 28 compounds from sea hare Aplysia kurodai, and ten from endolichenic fungi Parmelia sp. The potent pharmacological agents from this genus are periconicin A, which acts as an antimicrobial, pericochlorosin B as an anti-human immunodeficiency virus (HIV), peribysin D, and pericosine A as cytotoxic agents, and periconianone A as an anti-inflammatory agent. Furthermore, information about taxol and piperine from Periconia producing species was also provided. Therefore, this study supports discovering new drugs produced by the Periconia species and compares them for future drug development. Full article
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Article
The Optimization of a Dimenhydrinate Transdermal Patch Formulation Based on the Quantitative Analysis of In Vitro Release Data by DDSolver through Skin Penetration Studies
Sci. Pharm. 2021, 89(3), 33; https://doi.org/10.3390/scipharm89030033 - 16 Jul 2021
Viewed by 548
Abstract
Dimenhydrinate is an over-the-counter medication that is used to relieve nausea, vomiting, and vertigo caused by motion sickness. It has a short elimination half-life, possibly due to its first-pass metabolism. The current study aimed to prepare and evaluate new transdermal formulations of dimenhydrinate [...] Read more.
Dimenhydrinate is an over-the-counter medication that is used to relieve nausea, vomiting, and vertigo caused by motion sickness. It has a short elimination half-life, possibly due to its first-pass metabolism. The current study aimed to prepare and evaluate new transdermal formulations of dimenhydrinate to prolong the drug’s release and improve its cutaneous permeation. First, the patches were fabricated and evaluated to determine their properties. The results were statistically investigated and considered significant at the p < 0.05 level. Additionally, the quantitative analysis of the drug-release data and kinetic modeling was performed by using the DDSolver software to decide the candidate formula dependably. The effect of the penetration enhancers on the permeability of dimenhydrinate from the selected patch was then studied ex vivo compared to the control sample, and the patch’s safety was evaluated in rabbits, using the skin-irritation test. Full article
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Article
Cumulative Risks of Excipients in Pediatric Phytomucolytic Syrups: The Implications for Pharmacy Practice
Sci. Pharm. 2021, 89(3), 32; https://doi.org/10.3390/scipharm89030032 - 05 Jul 2021
Viewed by 682
Abstract
Expectorant phytomucolytic syrups are widely used pediatric OTC-medicines. Physicians, pediatricians, and pharmacists are traditionally concerned with the efficacy of the active ingredients in cough syrups, and rarely consider the safety aspects of excipients that however are not absolutely “inactive” and are proved to [...] Read more.
Expectorant phytomucolytic syrups are widely used pediatric OTC-medicines. Physicians, pediatricians, and pharmacists are traditionally concerned with the efficacy of the active ingredients in cough syrups, and rarely consider the safety aspects of excipients that however are not absolutely “inactive” and are proved to initiate some negative reactions and interactions with other drugs. This paper presents a review, categorization, and comparative analysis of the safety profile of excipients contained in the 22 best-selling OTC pediatric phytomucolytic syrups available in pharmaceutical markets in Ukraine and Germany and proposes an approach to the consideration of the excipients’ safety risks for a pharmacist in the process of pharmaceutical care. The study has revealed that only one of the twenty-two analyzed syrups does not contain any potentially harmful excipients. The results of this analysis were used for developing a specific decision tool for pharmacists that can be used for minimizing excipient-initiated reactions when delivering OTC phytomucolytic syrups for children. Full article
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Article
Antibacterial, Antibiofilm, and Antischistosomal Activity of Montrichardia linifera (Arruda) Schott (Araceae) Leaf Extracts
Sci. Pharm. 2021, 89(3), 31; https://doi.org/10.3390/scipharm89030031 - 05 Jul 2021
Viewed by 609
Abstract
With a broad ethnopharmacological tradition in Brazil, Montrichardia linifera has been reported as a potent antirheumatic, antimicrobial, and antiprotozoan agent. However, there is a lack of studies on its effect on bacterial biofilm formation and Schistosoma mansoni worms. This study reports the effects [...] Read more.
With a broad ethnopharmacological tradition in Brazil, Montrichardia linifera has been reported as a potent antirheumatic, antimicrobial, and antiprotozoan agent. However, there is a lack of studies on its effect on bacterial biofilm formation and Schistosoma mansoni worms. This study reports the effects of antibacterial, antibiofilm, and antischistosomal properties of leaf extracts of M. linifera. Phytochemical screening and identification of the main compounds of the extracts were performed. All the extracts evaluated showed antibacterial activity at the concentrations tested. We checked for the presence of flavonoids and derivatives of phenolic acids by the presence of spectra with bands characteristic of these classes in the sample analyzed. The antibacterial assays showed that the best MICs corresponded to 125 µg/mL against Enterococcus faecalis ATCC 29212 in all fractions. The ethanolic and methanolic extracts showed the ability to inhibit biofilm of Staphylococcus aureus ATCC 25123. For the antischistosomal activity, only the acetone and ethyl acetate extracts had a significant effect against helminths, with potent activity at a concentration of 50 µg/mL, killing 100% of the worms after 72 h of incubation. The M. linifera leaf extracts showed antibacterial activity, biofilm inhibition capacity, and anthelmintic activity against S. mansoni. Full article
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Article
A Comprehensive Spectroscopic Analysis of the Ibuprofen Binding with Human Serum Albumin, Part II
Sci. Pharm. 2021, 89(3), 30; https://doi.org/10.3390/scipharm89030030 - 22 Jun 2021
Viewed by 738
Abstract
Human serum albumin (HSA) is the most abundant human plasma protein. HSA plays a crucial role in many binding endos- and exogenous substances, which affects their pharmacological effect. The innovative aspect of the study is not only the interaction of fatted (HSA) and [...] Read more.
Human serum albumin (HSA) is the most abundant human plasma protein. HSA plays a crucial role in many binding endos- and exogenous substances, which affects their pharmacological effect. The innovative aspect of the study is not only the interaction of fatted (HSA) and defatted (dHSA) human serum albumin with ibuprofen (IBU), but the analysis of the influence of temperature on the structural modifications of albumin and the interaction between the drug and proteins from the temperature characteristic of near hypothermia (308 K) to the temperature reflecting inflammation in the body (312 K and 314 K). Ibuprofen is a non-steroidal anti-inflammatory drug. IBU is used to relieve acute pain, inflammation, and fever. To determine ibuprofen’s binding site in the tertiary structure of HSA and dHSA, fluorescence spectroscopy was used. On its basis, the fluorescent emissive spectra of albumin (5 × 10−6 mol/dm3) without and with the presence of ibuprofen (1 × 10−5–1 × 10−4 mol/dm3) was recorded. The IBU-HSA complex’s fluorescence was excited by radiation of wavelengths of λex 275 nm and λex 295 nm. Spectrophotometric spectroscopy allowed for recording the absorbance spectra (zero-order and second derivative absorption spectra) of HSA and dHSA under the influence of ibuprofen (1 × 10−4 mol/dm3). To characterize the changes of albumin structure the presence of IBU, circular dichroism was used. The data obtained show that the presence of fatty acids and human serum albumin temperature influences the strength and type of interaction between serum albumin and drug. Ibuprofen binds more strongly to defatted human serum albumin than to albumin in the presence of fatty acids. Additionally, stronger complexes are formed with increasing temperatures. The competitive binding of ibuprofen and fatty acids to albumin may influence the concentration of free drug fraction and thus its therapeutic effect. Full article
(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
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