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Sci. Pharm., Volume 88, Issue 4 (December 2020) – 9 articles

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Open AccessArticle
Anti-Proliferative and Genotoxic Activities of the Helichrysum petiolare Hilliard & B.L. Burtt
Sci. Pharm. 2020, 88(4), 49; https://doi.org/10.3390/scipharm88040049 - 20 Oct 2020
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Abstract
Helichrysum petiolare (Asteraceae family) is part of the Helichrysum genus which comprises of an estimated 600 species. Several parts of the plant have been used traditionally for the treatment of various ailments, such as cough, infection, asthma, chest problems, diabetes and wounds. Given [...] Read more.
Helichrysum petiolare (Asteraceae family) is part of the Helichrysum genus which comprises of an estimated 600 species. Several parts of the plant have been used traditionally for the treatment of various ailments, such as cough, infection, asthma, chest problems, diabetes and wounds. Given its various chemical constituents with anticancer properties, there has been no scientific evidence of its usage for the treatment of cancer. This study aims to investigate the anti-proliferative and genotoxic activities of H. petiolare methanol extract. The cytotoxic effect and cell cycle analysis of mouse melanoma cells (B16F10) and human melanoma cells (MeWo) were assessed using the ImageXpress Micro XLS Widefield High-Content Analysis System. The genotoxic potential of the extract towards Vero cells was also assessed using the micronucleus assay. The extract displayed cytotoxicity towards B16F10 and MeWo skin melanoma cells, thereby showing a dose-dependent decrease in cell density. This was preceded by cell cycle arrest in B16F10 cells at the S phase and MeWo cell arrest at the early M phase with a significant increase in apoptosis in both cells. Furthermore, the extract displayed genotoxic potential at the tested concentrations (12.5–200 μg/mL). Overall, the results revealed that H. petiolare extract may have the potential to eradicate skin cancer. Full article
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Open AccessArticle
Prevalence of Drug Interaction in Severely Obese Individuals and Associated Factors: Baseline Results from a Clinical Trial
Sci. Pharm. 2020, 88(4), 48; https://doi.org/10.3390/scipharm88040048 - 20 Oct 2020
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Abstract
The prevalence of obesity is increasing worldwide and is commonly associated with comorbidities. The use of several drugs is often necessary, which leads to Potential Drug Interactions (PDI) that may increase the morbidity and mortality. This study aimed to analyze the prevalence of [...] Read more.
The prevalence of obesity is increasing worldwide and is commonly associated with comorbidities. The use of several drugs is often necessary, which leads to Potential Drug Interactions (PDI) that may increase the morbidity and mortality. This study aimed to analyze the prevalence of drug interaction and its association with socio-demographics, health status, and drug use in severely obese individuals. Baseline data from a randomized clinical trial registered at Clinicaltrial.gov (NCT02463435) were used. A total of 150 individuals aged 18–65 years with a body mass index of 35 kg/m2 were included. The outcome variable was the presence of PDI, and the explanatory variables were divided into the following four levels: socio-demographic, lifestyle, health, and medication use. The prevalence of PDI was 50% (n = 75) (95% CI 41–58). The variables associated with drug–drug interactions in the multiple analyses were arterial hypertension (PR 1.83, 95%, CI 1.10–3.04), polypharmacy (PR 3.12, 95%, CI 2.17–4.50), and diabetes mellitus (PR 0.60, 95%, CI 0.45–0.81). The risk factors for the occurrence of drug interaction were the presence of diabetes mellitus, hypertension, and polypharmacy. Full article
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Open AccessArticle
Nephroprotective Effect of the Herbal Composition BNO 2103 in Rats with Renal Failure
Sci. Pharm. 2020, 88(4), 47; https://doi.org/10.3390/scipharm88040047 - 14 Oct 2020
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Abstract
(1) Background: this research aims at studying the nephroprotective properties of BNO 2103 in a model of chromate-induced renal failure in rats and at proving the possibility of using BNO 2103 in clinical practice for the complex treatment of chronic kidney disease (CKD). [...] Read more.
(1) Background: this research aims at studying the nephroprotective properties of BNO 2103 in a model of chromate-induced renal failure in rats and at proving the possibility of using BNO 2103 in clinical practice for the complex treatment of chronic kidney disease (CKD). (2) Methods: fifty rats divided into five groups were studied. The drugs BNO 2103, Prednisolone and Lespephril were administered within 20 days. The excretory function and the functional state of kidneys, blood biochemical parameters and indicators of nitrogen metabolism were determined. (3) Results: under the influence of BNO 2103, there was a significant improvement in renal excretory function, in nitrogen metabolism and blood biochemical parameters compared with the control pathology group. BNO 2103 also outperformed the comparators in most indicators. (4) Conclusions: BNO 2103 has demonstrated nephroprotective, hypoazotemic and diuretic effects; and can be used to implement to the combined therapy of CKD. Full article
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Open AccessArticle
Voltammetric Behaviour of Drug Molecules as a Predictor of Metabolic Liabilities
Sci. Pharm. 2020, 88(4), 46; https://doi.org/10.3390/scipharm88040046 - 13 Oct 2020
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Abstract
Electron transfer plays a vital role in drug metabolism and underlying toxicity mechanisms. Currently, pharmaceutical research relies on pharmacokinetics (PK) and absorption, distribution, metabolism, elimination and toxicity (ADMET) measurements to understand and predict drug reactions in the body. Metabolic stability (and toxicity) prediction [...] Read more.
Electron transfer plays a vital role in drug metabolism and underlying toxicity mechanisms. Currently, pharmaceutical research relies on pharmacokinetics (PK) and absorption, distribution, metabolism, elimination and toxicity (ADMET) measurements to understand and predict drug reactions in the body. Metabolic stability (and toxicity) prediction in the early phases of the drug discovery and development process is key in identifying a suitable lead compound for optimisation. Voltammetric methods have the potential to overcome the significant barrier of new drug failure rates, by giving insight into phase I metabolism events which can have a direct bearing on the stability and toxicity of the parent drug being dosed. Herein, we report for the first time a data-mining investigation into the voltammetric behaviour of reported drug molecules and their correlation with metabolic stability (indirectly measured via t½), as a potential predictor of drug stability/toxicity in vivo. We observed an inverse relationship between oxidation potential and drug stability. Furthermore, we selected and prepared short- (<10 min) and longer-circulation (>2 h) drug molecules to prospectively survey the relationship between oxidation potential and stability. Full article
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Open AccessArticle
Preventive Effect of a Polyphenol-Rich Extract from Geranium sanguineum L. on Hepatic Drug Metabolism in Influenza Infected Mice
Sci. Pharm. 2020, 88(4), 45; https://doi.org/10.3390/scipharm88040045 - 12 Oct 2020
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Abstract
The decreased hepatic drug metabolism (predominately first phase) is one of the essential reasons for numerous side effects and for increased drug toxicity during influenza virus infection (IVI). The present study aims to investigate some mechanisms of the preventive effect of a standardized [...] Read more.
The decreased hepatic drug metabolism (predominately first phase) is one of the essential reasons for numerous side effects and for increased drug toxicity during influenza virus infection (IVI). The present study aims to investigate some mechanisms of the preventive effect of a standardized polyphenol complex from the medicinal plant Geranium sanguineum L. (PPhC) (10 mg/kg nasally). A verified experimental model of IVI A/Aichi/2/68 (H3N2) (4.5 lg LD50) in male ICR (Institute of Cancer Research, USA) mice was used. Changes in hepatic monooxygenase activities as well as nicotinamide adenine dinucleotide phosphate (NADPH)-cytochrome C reductase activity and cytochtome P450 content were studied on days 2, 6, 9, 21 of the infection together with thiobarbituric acid reactive substances in the liver supernatant. Our data clearly demonstrates that IVI affects all components of the electronic chain of cytochrome P-450. N-demethylases and hydroxylases as well as the activity of cytochrome C reductase and cytochtome P-450 content were decreased in the course of the virus infection. This implies that free radicals play an important role not only in the pathogenesis of IVI, but also in the modulation of the hepatic monooxygenase activity. This is also consistent with the established polyphenol complex PPhC from the medicinal plant Geranium sanguineum L. preventive effect against increased thiobarbituric acid reactive substances (TBARS)-levels. PPhC restored most of the monooxygenase activities that were inhibited in IVI animals, even over the control levels, probably via multiple mechanisms that may entail antioxidant activity and selective antiviral and protein-binding effects. In contrast to infected animals, in healthy mice, PPhC showed moderate reversible inhibitory effect on hepatic monooxygenase activities. Full article
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Open AccessArticle
Curcumin-Loaded Nanoemulsion for Better Cellular Permeation
Sci. Pharm. 2020, 88(4), 44; https://doi.org/10.3390/scipharm88040044 - 06 Oct 2020
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Abstract
Curcumin nanoemulsion was prepared using coconut oil, Tween 80 (surfactant) and polyethylene glycol (co-solvent) with the addition of honey and glycerol as additives. The nanoemulsion was optimized and systematically characterized for transdermal delivery. Small particle size (15.92 nm), low polydispersity index (0.17) and [...] Read more.
Curcumin nanoemulsion was prepared using coconut oil, Tween 80 (surfactant) and polyethylene glycol (co-solvent) with the addition of honey and glycerol as additives. The nanoemulsion was optimized and systematically characterized for transdermal delivery. Small particle size (15.92 nm), low polydispersity index (0.17) and slight acidic (pH 4.18) curcumin nanoemulsion was obtained without any chemical degradation based on the Fourier transform infrared (FTIR) spectrum. The incorporation of curcumin inside nanoglobul improved curcumin stability and skin permeability. Its high permeability can be seen from Nile dyed curcumin in different layers of skin through fluorescent imaging. The release kinetic of curcumin followed the Higuchi model, which explains why the skin permeation was a Fickian diffusion-controlled process because the Korsmeyer constant was proven to be 0.3 (<0.5). Nanoencapsulation slightly decreased the antioxidant capacity of curcumin for about 7.9% compared to its free counterpart. It showed low cytotoxicity (EC50 2.3552 µg/mL) to human skin fibroblasts. Cell death was noticed at a high concentration (2.5 µg/mL) of treatment. Curcumin was also found to promote wound closure at low concentration 0.1563 µg/mL and was comparable with the performance of ascorbic acid based on scratch assay. Therefore, this nutritious curcumin nanoemulsion is a promising transdermal delivery system for topical application. Full article
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Open AccessArticle
The Effect of Cladode Drying Techniques on the Prebiotic Potential and Molecular Characteristics of the Mucilage Extracted from Opuntia ficus-indica and Opuntia joconostle
Sci. Pharm. 2020, 88(4), 43; https://doi.org/10.3390/scipharm88040043 - 02 Oct 2020
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Abstract
The dry, powdered cladodes of Opuntia ficus-indica are often-used in over-the-counter (OTC) pharmaceutical formulations. Gentle drying techniques, such as lyophilization and vacuum drying are compared with convection drying for the cladodes and also compared with another species of economic importance, Opuntia joconostle. The [...] Read more.
The dry, powdered cladodes of Opuntia ficus-indica are often-used in over-the-counter (OTC) pharmaceutical formulations. Gentle drying techniques, such as lyophilization and vacuum drying are compared with convection drying for the cladodes and also compared with another species of economic importance, Opuntia joconostle. The heteropolysaccharide purified from the mucilage extracted from the dried powders were investigated in their monosaccharide composition (HPAEC-PAD, TLC), mineral and protein content, molecular dimensions (SEC) and fermentability by probiotic bacteria (Bioscreen technique) for evaluation of the prebiotic potential of the mucilage. The heteropolysaccharide is composed of galactose, arabinose, xylose, galacturonic acid and rhamnose. O. ficus-indica includes an additional 13% of glucose coming from an α-glucan. The content of Ca (0.3%) and Mg (0.4%) is relatively low in both species; the content of protein adds up to 1.5% in O. ficus-indica but is significantly lower in O. joconostle with 0.8%. The average molecular mass Mw of the extracted mucilage ranges from 3.7 to 4.7 × 105 g∙mol−1 for both species; only the mucilage from long-time convection drying (C2) delivers a lower average Mw of 2.6 × 105 g∙mol−1, due to partial breakdown of the mucilage matrix. All tested probiotic strains utilized the mucilage to some extent; C2 being the most active, and thus confirms the prebiotic potential of cladode’s powder and its derived products. In general, the molecular dimensions and prebiotic potential are not extremely sensitive to the drying treatment, yet temperature and drying time can modify the cladode’s powder to a profile with better prebiotic characteristics. Full article
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Open AccessReview
The Mechanism of Action of Cyclophosphamide and Its Consequences for the Development of a New Generation of Oxazaphosphorine Cytostatics
Sci. Pharm. 2020, 88(4), 42; https://doi.org/10.3390/scipharm88040042 - 28 Sep 2020
Viewed by 333
Abstract
Although cyclophosphamide (CP) has been used successfully in the clinic for over 50 years, it has so far not been possible to elucidate the mechanism of action and to use it for improvement. This was not possible because the basis of the mechanism [...] Read more.
Although cyclophosphamide (CP) has been used successfully in the clinic for over 50 years, it has so far not been possible to elucidate the mechanism of action and to use it for improvement. This was not possible because the basis of the mechanism of action of CP, which was found by lucky coincidence, is apoptosis, the discovery of which was honored with the Nobel Prize only in 2002. Another reason was that results from cell culture experiments were used to elucidate the mechanism of action, ignoring the fact that in vivo metabolism differs from in vitro conditions. In vitro, toxic acrolein is formed during the formation of the cytotoxic metabolite phosphoreamidemustard (PAM), whereas in vivo proapoptotic hydroxypropanal (HPA) is formed. The CP metabolites formed in sequence 4-hydroxycyclophosphamide (OHCP) are the main cause of toxicity, aldophosphamide (ALDO) is the pharmacologically active metabolite and HPA amplifies the cytotoxic apoptosis initiated by DNA alkylation by PAM. It is shown that toxicity is drastically reduced but anti-tumor activity strongly increased by the formation of ALDO bypassing OHCP. Furthermore, it is shown that the anti-tumor activity against advanced solid P388 tumors that grow on CD2F1 mice is increased by orders of magnitude if DNA damage caused by a modified PAM is poorly repairable. Full article
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Open AccessArticle
Prevalence of Adverse Drug Events in Severely Obese Adults and Associated Factors: Clinical Trial Baseline Results
Sci. Pharm. 2020, 88(4), 41; https://doi.org/10.3390/scipharm88040041 - 23 Sep 2020
Viewed by 364
Abstract
Drugs are the most widely used therapeutic tool for treatment of diseases. However, misuse can lead to an adverse drug event (ADE) in susceptible individuals such as those that are severely obese. This study aimed to describe the frequency of ADEs, the associations [...] Read more.
Drugs are the most widely used therapeutic tool for treatment of diseases. However, misuse can lead to an adverse drug event (ADE) in susceptible individuals such as those that are severely obese. This study aimed to describe the frequency of ADEs, the associations of ADEs with anatomical therapeutic chemical classes and their respective frequency, estimate the prevalence of ADEs, and analyse factors associated with ADE in adults with severe obesity. Cross-sectional analysis of baseline data from a randomized clinical trial in the central-western region of Brazil. A total of 150 individuals aged 18–65 years with a Body Mass Index of 35 kg/m2 were included. The outcome variable was the presence of ADE and the explanatory variables were socio-demographic factors, lifestyle, health, and medication use. ADEs were associated with use of drugs for the digestive tract and metabolism (p < 0.001) and the cardiovascular system (p < 0.001). The prevalence of ADEs was 32.67% (n = 49) and associated with the age range 40 to 49 years (p = 0.033), diabetes (p = 0.004), multimorbidities ≥ 4 (p = 0.009), self-medication (0.031), and presence of potential drug interactions (0.017). The prevalence of ADEs was high and was associated with drugs commonly used in treatment of obesity-related morbidities and self-medication. The introduction of a pharmacist to multi-professional teams can improve medication safety for severely obese patients. Full article
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