Scientia Pharmaceutica

11 pages, 1968 KiB

Open AccessArticle

Caesalpinia sappan L. Ameliorates Scopolamine-Induced Memory Deficits in Mice via the cAMP/PKA/CREB/BDNF Pathway

by Helmi Helmi, Nanang Fakhrudin, Arief Nurrochmad and Zullies Ikawati

Sci. Pharm. 2021, 89(2), 29; https://doi.org/10.3390/scipharm89020029 - 18 Jun 2021

Cited by 3 | Viewed by 3853

Memory is an essential aspect of human cognition. A decrease in this aspect is well associated with Alzheimer’s disease (AD). The development of a novel cognitive enhancer (CE) may help overcome AD-related problems. In this study, we evaluated the CE effect of Caesalpinia [...] Read more.

Memory is an essential aspect of human cognition. A decrease in this aspect is well associated with Alzheimer’s disease (AD). The development of a novel cognitive enhancer (CE) may help overcome AD-related problems. In this study, we evaluated the CE effect of Caesalpinia sappan L. (CS) in memory deficit mice. Administration of its ethanolic extract (250 and 500 mg/kg body weight (BW)) and brazilin (5 and 10 mg/kg BW) ameliorated the scopolamine-amnesic effect, as evidenced by significant decreases (p < 0.01, p < 0.05) in the escape latency time and increases (p < 0.01) in the percentage of time spent in the target quadrant of the Morris water maze test. We also examined the cyclic adenosine monophosphate (cAMP) level, protein kinase A (PKA) activity, and protein expression levels of phosphorylated cAMP response element binding (pCREB) and brain-derived neurotrophic factor (BDNF) in hippocampal tissues to elucidate the underlying molecular mechanism. Results showed that CS wood ethanolic extract and brazilin not only significantly increase (p < 0.01, p < 0.05) cAMP levels and PKA activity but also significantly enhance (p < 0.01, p < 0.05) the expression level of pCREB and BDNF in the hippocampus. These findings indicate that CS activates the cAMP/PKA/CREB/BDNF pathway. Taken together, our results demonstrate that CS is a promising herb that could be developed as a CE agent. Full article

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17 pages, 1093 KiB

Open AccessArticle

Characterization of Phytochemical Components of Crocus sativus Leaves: A New Attractive By-Product

by Olha Mykhailenko, Liudas Ivanauskas, Ivan Bezruk, Lyudmila Sidorenko, Roman Lesyk and Victoriya Georgiyants

Sci. Pharm. 2021, 89(2), 28; https://doi.org/10.3390/scipharm89020028 - 15 Jun 2021

Cited by 13 | Viewed by 5739

Abstract

Crocus sativus L. is one of the world’s most famous saffron production crops and its enormous by-products, such as leaves, are an excellent source of bioactive compounds with potential nutritional applications. The total phenolic content of Crocus leaves was 5.44 ± 0.01 mg [...] Read more.

Crocus sativus L. is one of the world’s most famous saffron production crops and its enormous by-products, such as leaves, are an excellent source of bioactive compounds with potential nutritional applications. The total phenolic content of Crocus leaves was 5.44 ± 0.01 mg GAE/g, and the total flavonoid content was 2.63 ± 0.05 mg RE/g, respectively. The main bioactive compounds in the leaves, such as polyphenols, flavonoids by HPLC and carboxylic acids, and amino acids, were also identified by GC-MS. HPLC analyses revealed mangiferin as a dominant constituent (1.26 ± 0.02 mg/g). C. sativus contains seven essential amino acids (ILE, LEU, LYS, MET, PHE, THR, TRP, VAL) in high concentration. Among them, isoleucine (7965 µg/g) was the dominant compound. In addition, the K and Ca concentrations in the leaves were significant (p < 0.05). The chemical composition revealed α-linolenic acid (22,490 µg/g) and linoelaidic acid (9880 µg/g) to be major constituents among all the acids found in the Crocus leaves. The extracts of C. sativus leaves showed the highest inhibitory activity for Gram-positive (B. subtilis and S. aureus) bacteria in the in vitro assay. The current results identify and underline the potential of natural products from C. sativus leaves that can add value to saffron production. Full article

(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)

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8 pages, 2940 KiB

Open AccessArticle

Antihyperuricemic, Anti-Inflammatory and Antihypertensive Effect of a Dry Extract from Solidago virgaurea L. (Asteraceae)

by Mircea Tămaş, Oliviu Vostinaru, Loredana Soran, Ildiko Lung, Ocsana Opris, Anca Toiu, Alexandru Gavan, Elena Dinte and Cristina Mogosan

Sci. Pharm. 2021, 89(2), 27; https://doi.org/10.3390/scipharm89020027 - 14 Jun 2021

Cited by 8 | Viewed by 4641

Abstract

Solidago virgaurea L. is a perennial plant used in European traditional medicine as a diuretic or a remedy for inflammatory conditions of the urinary tract but also for gout, especially in the Balkans. The present study was focused on a preclinical, in vivo [...] Read more.

Solidago virgaurea L. is a perennial plant used in European traditional medicine as a diuretic or a remedy for inflammatory conditions of the urinary tract but also for gout, especially in the Balkans. The present study was focused on a preclinical, in vivo evaluation of antihyperuricemic, anti-inflammatory, and antihypertensive effects of a dry extract from S. virgaurea L. (ESV). Colorimetric and HPLC–MS techniques were used to identify the main chemical constituents of ESV. Antihyperuricemic effect of ESV was assessed in a rat model of hyperuricemia induced by the administration of potassium oxonate. Antihypertensive effect of ESV was evaluated in hyperuricemic rats by monitoring systolic blood pressure with a non-invasive blood-pressure recording system. The anti-inflammatory effect of ESV was tested using a rat model of paw edema. The main chemical constituents of ESV were rutin and phenolic acids represented by chlorogenic and caffeic acid. ESV demonstrated significant antihyperuricemic effects in rats due to an uricosuric mechanism. Additionally, ESV reduced the progression of arterial hypertension in hyperuricemic rats and also showed anti-inflammatory properties slightly inferior to diclofenac. The results suggest that ESV could be a natural remedy for the treatment of gout and protection against endothelial dysfunction caused by hyperuricemia. Full article

(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)

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13 pages, 4022 KiB

Open AccessArticle

Exerting DNA Damaging Effects of the Ilimaquinones through the Active Hydroquinone Species

by Apisada Jiso, Laphatrada Yurasakpong, Sirorat Janta, Kulathida Chaithirayanon and Anuchit Plubrukarn

Sci. Pharm. 2021, 89(2), 26; https://doi.org/10.3390/scipharm89020026 - 03 Jun 2021

Cited by 1 | Viewed by 4009

Abstract

Possessing the quinone moiety, ilimaquinone (1), a sponge–derived sesquiterpene quinone, has been hypothesised to express its cytotoxicity through a redox cycling process, yielding active product(s) that can cause DNA damage. To determine the DNA damaging effects of 1 and examine whether [...] Read more.

Possessing the quinone moiety, ilimaquinone (1), a sponge–derived sesquiterpene quinone, has been hypothesised to express its cytotoxicity through a redox cycling process, yielding active product(s) that can cause DNA damage. To determine the DNA damaging effects of 1 and examine whether a redox transformation may participate in its functions, the DNA damaging properties of 1, the corresponding hydroquinone (2) and hydroquinone triacetates (3) and their 5-epimeric counterparts (4–6) were tested and compared. When incubated directly with plasmid DNA, the hydroquinones were the only active species capable of cleaving the DNA. In cell-based assays, however, the quinones and hydroquinone triacetates were active in the same range as that of the corresponding hydroquinones, and all damaged the cellular DNA in a similar manner. The in situ reduction of 1 and 4 were supported by the decreases in the cytotoxicity when cells were pre-exposed to dicoumarol, an NAD(P)H:quinone oxidoreductase 1 (NQO1) inhibitor. The results confirmed the DNA damaging activities of the ilimaquinones 1 and 4, and indicated the necessity to undergo an in-situ transformation into the active hydroquinones, thereby exerting the DNA damaging properties as parts of the cytotoxic mechanisms. Full article

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16 pages, 3434 KiB

Open AccessArticle

Olanzapine Loaded Nanostructured Lipid Carriers via High Shear Homogenization and Ultrasonication

by Adejumoke Lara Ajiboye, Uttom Nandi, Martin Galli and Vivek Trivedi

Sci. Pharm. 2021, 89(2), 25; https://doi.org/10.3390/scipharm89020025 - 27 May 2021

Cited by 14 | Viewed by 5701

Abstract

The aim of this study was to understand the effect of high shear homogenization (HSH) and ultrasonication (US) on the physicochemical properties of blank and olanzapine loaded nanostructured lipid carriers (NLCs) along with their drug loading potential and drug release profiles from formulated [...] Read more.

The aim of this study was to understand the effect of high shear homogenization (HSH) and ultrasonication (US) on the physicochemical properties of blank and olanzapine loaded nanostructured lipid carriers (NLCs) along with their drug loading potential and drug release profiles from formulated particles. NLCs were prepared with different ratios of Compritol and Miglyol as the solid and liquid lipids, respectively, under changing HSH and US times between 0 to 15 min. The surfactants (Poloxamer 188 (P188) and tween 80) and the drug content was kept constant in all formulations. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, drug crystallinity and chemical interactions between lipids and OLZ. The in-vitro drug release was performed using dialysis tube method in phosphate buffer solution (PBS) at pH 7.4. The formulated NLCs were negatively charged, spherically shaped and monodisperse, with particle sizes ranging from 112 to 191 nm. There was a significant influence of US time on the preparation of NLCs in comparison to HSH, where a significant reduction in the mean particle diameter was seen after 5 min of sonication. An increase of Miglyol content in NLCs led to an increase in particle size. In general, application of US led to decrease in particle size after HSH but an increase in particle diameter of low Miglyol containing preparation was also observed with longer sonication time. OLZ was successfully encapsulated in the NLCs and a total release of 89% was achieved in 24 h in PBS at pH 7.4. Full article

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10 pages, 1724 KiB

Open AccessArticle

Zolmitriptan Intranasal Spanlastics for Enhanced Migraine Treatment; Formulation Parameters Optimized via Quality by Design Approach

by Asmaa Saleh, Maha Khalifa, Seham Shawky, Amjaad Bani-Ali and Heba Eassa

Sci. Pharm. 2021, 89(2), 24; https://doi.org/10.3390/scipharm89020024 - 27 May 2021

Cited by 16 | Viewed by 5056

Abstract

Zolmitriptan is a potent second-generation triptan prescribed for migraine attacks. It suffers low bioavailability (40%) after oral administration due to the hepatic first-pass metabolism. Spanlastics are surfactant-based elastic vesicular drug carrier systems. This study aimed to design and optimize intranasal spanlastic formulations as [...] Read more.

Zolmitriptan is a potent second-generation triptan prescribed for migraine attacks. It suffers low bioavailability (40%) after oral administration due to the hepatic first-pass metabolism. Spanlastics are surfactant-based elastic vesicular drug carrier systems. This study aimed to design and optimize intranasal spanlastic formulations as an alternative approach that directly targets brain delivery, enhancing its bioavailability and avoiding the first-pass effect. The quality by design approach was applied to correlate the formulation parameters (Span 60 and Tween 80 concentrations) and critical quality attributes (entrapment efficiency (EE%) and particle size). Spanlastic formulations were designed based on response surface central composite design and prepared via an ethanol injection method. Designed formulations were characterized by EE% and particle size measurements to select the optimized formula (with a combination of small particle size and high EE%). The optimized formula was further subjected to transmission electron microscopy, zeta potential measurement and ex vivo permeation study. The optimized formulation showed a particle size of 117.5 nm and EE% of 45.65%, with a low percentage of error between the observed and predicted values. Seventy percent of zolmitriptan was permeated through the nasal membrane within 30 min, and it completely permeated within 2 h with a significantly higher steady-state flux compared to plain gel. This study introduced a successful and promising intranasal formulation suitable for further brain delivery analysis. Full article

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10 pages, 1351 KiB

Open AccessArticle

Quercetin Inhibits Colorectal Cancer Cells Induced-Angiogenesis in Both Colorectal Cancer Cell and Endothelial Cell through Downregulation of VEGF-A/VEGFR2

by Tamonwan Uttarawichien, Chantra Kamnerdnond, Tasanee Inwisai, Prasit Suwannalert, Nathawut Sibmooh and Witchuda Payuhakrit

Sci. Pharm. 2021, 89(2), 23; https://doi.org/10.3390/scipharm89020023 - 25 May 2021

Cited by 4 | Viewed by 5316

Abstract

Colorectal cancer (CRC) aggressiveness is caused by cancer angiogenesis which promotes the cancer growth and metastasis associated with poor prognosis and poor survival. The vascular endothelial growth factor-A (VEGF-A) and its receptor (VEGFR-2) form the major signaling pathway in cancer angiogenesis. This study [...] Read more.

Colorectal cancer (CRC) aggressiveness is caused by cancer angiogenesis which promotes the cancer growth and metastasis associated with poor prognosis and poor survival. The vascular endothelial growth factor-A (VEGF-A) and its receptor (VEGFR-2) form the major signaling pathway in cancer angiogenesis. This study aimed to investigate the anti-angiogenesis activity of quercetin in both colorectal cancer cells and endothelial cells. The tube formation of human vein endothelial cells (HUVECs) was determined by using conditioned media of HT-29 cells treated with quercetin co-cultured with HUVECs. The VEGF-A and NF-κB p65 protein expressions in the quercetin-treated HT-29 cells were determined by fluorescence assay and Western blot analysis. The VEGFR-2 protein expression in HUVECs was determined after they were co-cultured with the quercetin-treated HT-29 cells. Quercetin markedly decreased the HT-29 cell-induced angiogenesis in HUVECs. NF-κB p65 and VEGF-A protein expression were also inhibited by quercetin. Moreover, quercetin significantly inhibited VEGFR-2 expression and translocation in HUVECs after they were co-cultured with high dose quercetin-treated HT-29 cells. Taken together, quercetin had an anti-angiogenesis effect on VEGF-A inhibition related to the NF-κB signaling pathway in the HT-29 cells and reduced VEGFR-2 expression and translocation in HUVECs. Full article

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11 pages, 1469 KiB

Open AccessArticle

Docking-Based Virtual Screening and Molecular Dynamics Simulations of Quercetin Analogs as Enoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors of Mycobacterium tuberculosis

by Dian Ayu Eka Pitaloka, Dwi Syah Fitra Ramadhan, Arfan, Lidya Chaidir and Taufik Muhammad Fakih

Sci. Pharm. 2021, 89(2), 20; https://doi.org/10.3390/scipharm89020020 - 20 May 2021

Cited by 28 | Viewed by 5676

Abstract

The emergence of multidrug-resistant Mycobacterium tuberculosis (MTB) has become a major problem in treating tuberculosis (TB) and shows the need to develop new and efficient drugs for better TB control. This study aimed to use in silico techniques to discover potential inhibitors to [...] Read more.

The emergence of multidrug-resistant Mycobacterium tuberculosis (MTB) has become a major problem in treating tuberculosis (TB) and shows the need to develop new and efficient drugs for better TB control. This study aimed to use in silico techniques to discover potential inhibitors to the Enoyl-[acyl-carrier-protein] reductase (InhA), which controls mycobacterial cell wall construction. Initially, 391 quercetin analogs present in the KNApSAck_3D database were selected, filters were sequentially applied by docking-based virtual screening. After recategorizing the variables (bond energy prediction and molecular interaction, including hydrogen bond and hydrophobic bond), compounds C00013874, C00006532, and C00013887 were selected as hit ligands. These compounds showed great hydrophobic contributions, and for each hit ligand, 100 ns of molecular dynamic simulations were performed, and the binding free energy was calculated. C00013874 demonstrated the greatest capacity for the InhA enzyme inhibition with ΔGbind = −148.651 kcal/mol compare to NAD (native ligand) presented a ΔGbind = −87.570 kcal/mol. These data are preliminary studies and might be a suitable candidate for further experimental analysis. Full article

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10 pages, 1802 KiB

Open AccessArticle

Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues

by Mariia Mishchenko, Sergiy Shtrygol’, Andrii Lozynskyi, Semen Khomyak, Volodymyr Novikov, Olexandr Karpenko, Serhii Holota and Roman Lesyk

Sci. Pharm. 2021, 89(2), 22; https://doi.org/10.3390/scipharm89020022 - 19 May 2021

Cited by 5 | Viewed by 5178

Abstract

Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID [...] Read more.

Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID dual COX-2/5-LOX inhibitor darbufelone methanesulfonate using an scPTZ model in mice in dose 100 mg/kg is reported. Darbufelone possesses anticonvulsant properties in the scPTZ model and presents interest for in-depth studies as a possible anticonvulsant multi-target agent with anti-inflammatory activity. The series of 4-thiazolidinone derivatives have been synthesized following the analogue-based drug design and hybrid-pharmacophore approach using a darbufelone matrix. The synthesized derivatives showed a significant protection level for animals in the scPTZ model and are promising compounds for the design of potential anticonvulsants with satisfactory drug-like parameters. Full article

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11 pages, 1082 KiB

Open AccessArticle

Antiproliferative Activity of Triterpenoid and Steroid Compounds from Ethyl Acetate Extract of Calotropis gigantea Root Bark against P388 Murine Leukemia Cell Lines

by Kartini Hasballah, Murniana Sarong, Renzavaldy Rusly, Herdina Fitria, Dewi Rara Maida and Muhammad Iqhrammullah

Sci. Pharm. 2021, 89(2), 21; https://doi.org/10.3390/scipharm89020021 - 19 May 2021

Cited by 32 | Viewed by 5095

Abstract

Calotropis gigantea has been known to produce bioactive secondary metabolites with antiproliferative activities against cancer cells. Herein, we extracted the secondary metabolites using ethyl acetate from its root bark and further tested its antiproliferative activities against P388 murine leukemia cell lines. The subfractions [...] Read more.

Calotropis gigantea has been known to produce bioactive secondary metabolites with antiproliferative activities against cancer cells. Herein, we extracted the secondary metabolites using ethyl acetate from its root bark and further tested its antiproliferative activities against P388 murine leukemia cell lines. The subfractions from the ethyl acetate extract was obtained from Vacuum Liquid Column Chromatography (VLCC), and followed by Gravity Column Chromatography (GCC). The subfraction C₂ and D₁ were identified to contain triterpenoids and steroids with the most potent cytotoxicity against Brine Shrimp Lethality Test (BSLT). A 3-(4,5-dimethylthiazol-2-yl) -2-5 diphenyl tetrazolium bromide (MTT) assay suggested that ethyl acetate extract has the highest antiproliferative activities against P388 murine leukemia cell lines (IC₅₀ = 21.79 μg/mL), as opposed to subfraction C₂ (IC₅₀ = 50.64 µg/mL) and subfraction D₁ (IC₅₀ = 49.33 µg/mL). The compound identified in subfraction C₂ and D₁ are taraxerol acetate and calotropone, respectively. Though taraxerol acetate and calotropone were active in inhibiting the leukemic cell lines, their IC₅₀s were lower than the ethyl acetate extract, which is probably due to the synergism of the secondary metabolites. Full article

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18 pages, 400 KiB

Open AccessReview

Clofazimine as a Treatment for Multidrug-Resistant Tuberculosis: A Review

by Rhea Veda Nugraha, Vycke Yunivita, Prayudi Santoso, Rob E. Aarnoutse and Rovina Ruslami

Sci. Pharm. 2021, 89(2), 19; https://doi.org/10.3390/scipharm89020019 - 18 May 2021

Cited by 14 | Viewed by 9152

Abstract

Multidrug-resistant tuberculosis (MDR-TB) is an infectious disease caused by Mycobacterium tuberculosis which is resistant to at least isoniazid and rifampicin. This disease is a worldwide threat and complicates the control of tuberculosis (TB). Long treatment duration, a combination of several drugs, and the [...] Read more.

Multidrug-resistant tuberculosis (MDR-TB) is an infectious disease caused by Mycobacterium tuberculosis which is resistant to at least isoniazid and rifampicin. This disease is a worldwide threat and complicates the control of tuberculosis (TB). Long treatment duration, a combination of several drugs, and the adverse effects of these drugs are the factors that play a role in the poor outcomes of MDR-TB patients. There have been many studies with repurposed drugs to improve MDR-TB outcomes, including clofazimine. Clofazimine recently moved from group 5 to group B of drugs that are used to treat MDR-TB. This drug belongs to the riminophenazine class, which has lipophilic characteristics and was previously discovered to treat TB and approved for leprosy. This review discusses the role of clofazimine as a treatment component in patients with MDR-TB, and the drug’s properties. In addition, we discuss the efficacy, safety, and tolerability of clofazimine for treating MDR-TB. This study concludes that the clofazimine-containing regimen has better efficacy compared with the standard one and is also well-tolerated. Clofazimine has the potential to shorten the duration of MDR-TB treatment. Full article

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13 pages, 1507 KiB

Open AccessArticle

Liquid Chromatographic Fingerprints for the Characterization of Flavanol-Rich Nutraceuticals Based on 4-Dimethylaminocinnamaldehyde Precolumn Derivatization

by Oscar Vidal-Casanella, Oscar Nuñez and Javier Saurina

Sci. Pharm. 2021, 89(2), 18; https://doi.org/10.3390/scipharm89020018 - 06 May 2021

Cited by 2 | Viewed by 3873

Abstract

Flavanols consist of a great family of bioactive molecules displaying a wide range of health-promoting attributes for humans, including antioxidant, antimicrobial or anti-inflammatory effects. As a result, botanical species rich in this type of compound are often used to develop nutraceutical products or [...] Read more.

Flavanols consist of a great family of bioactive molecules displaying a wide range of health-promoting attributes for humans, including antioxidant, antimicrobial or anti-inflammatory effects. As a result, botanical species rich in this type of compound are often used to develop nutraceutical products or dietary supplements with recognized healthy attributes. This paper aims at characterizing nutraceutical products using liquid chromatographic fingerprints related to flavanol composition. Catechins and their oligomers were exploited to characterize and authenticate various commercial products prepared with extracts of red berries and medicinal plants. These compounds resulted in interesting descriptors of some fruits and vegetables, thus providing an additional perspective for the study of nutraceuticals. For such a purpose, a new method based on liquid chromatography with UV/Vis detection (HPLC–UV/Vis) with precolumn derivatization with 4-dimethylaminocinnamaldehyde was developed. Results indicated that the separation of flavanols was very complex due to the degradation of procyanidin derivatives. The resulting data sets were analyzed using chemometric methods such as principal component analysis and partial least square–discriminant analysis. Despite the complexity of chromatographic fingerprints, nutraceutical samples could be discriminated according to their main ingredients. In general, catechin and epicatechin were the most abundant compounds in the different samples, and procyanidin A₂ was highly specific to cranberry. Full article

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8 pages, 900 KiB

Open AccessCommunication

Preliminary Protocol Development of a HPLC-TBARS-EVSC (Ex Vivo Stratum Corneum) Assay for Skin Research: Application in a Sunscreen System

by Rafael Sauce, Claudinéia Aparecida Sales de Oliveira Pinto, Carmen Ayala-Jara, Zulita Adriana Prieto, Maria Valéria Robles Velasco and André Rolim Baby

Sci. Pharm. 2021, 89(2), 17; https://doi.org/10.3390/scipharm89020017 - 27 Apr 2021

Cited by 10 | Viewed by 5033

Abstract

Considering the importance of the cutaneous tissue investigation and the need for the development of new protocols to non-invasively establish the safety and efficacy of dermocosmetics and topical products, we aimed at developing an HPLC-TBARS-EVSC (high performance liquid chromatography–thiobarbituric acid reactive species–ex vivo [...] Read more.

Considering the importance of the cutaneous tissue investigation and the need for the development of new protocols to non-invasively establish the safety and efficacy of dermocosmetics and topical products, we aimed at developing an HPLC-TBARS-EVSC (high performance liquid chromatography–thiobarbituric acid reactive species–ex vivo stratum corneum) assay for the lipid peroxidation measurement on subjects’ stratum corneum (SC) obtained by tape stripping; additionally, we applied the HPLC-TBARS-EVSC assay in an emulsified sunscreen system containing ethylhexyl triazone and bemotrizinol as UV filters. HPLC analysis was performed in isocratic mode with 35% methanol/65% phosphate buffer (pH 7.0) as the mobile phase. The diode detector was set at 532 nm to quantify the malondialdehyde (MDA)-TBA adduct. An ex vivo tape stripping method was applied in 10 volunteers in three pre-defined regions of the volar forearms: the control; the irradiated; and the site containing the sunscreen (2.0 mg·cm⁻²). Ten adhesive tapes per region were used for SC removal. An exclusive ex vivo protocol to measure SC lipid peroxidation was preliminarily developed with linearity and selectivity. The protocol suggested the use of an artificial irradiation dose (5506 KJ·m⁻²) to improve the assay response from the SC. The sunscreen system had a significative decrease in SC lipoperoxidative damage compared to the control. Our protocol can aid in the efficacy establishment of anti-UV and antioxidant agents, for instance, in studies that aim at elucidating the level of SC lipid peroxidation and even in carrying out baseline investigations characterizing different ethnicities and genders. Full article

(This article belongs to the Special Issue Functional Ingredients in Topical and Transdermal Delivery Systems)

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15 pages, 2546 KiB

Open AccessArticle

Development of a Novel, Fast, Simple HPLC Method for Determination of Atorvastatin and its Impurities in Tablets

by Nataliia Shulyak, Marjan Piponski, Sergiy Kovalenko, Tanja Bakovska Stoimenova, Trajan Balkanov, Hussein I. El-Subbagh, Iryna Drapak, Joy Oluwatobiloba Omotosho and Liliya Logoyda

Sci. Pharm. 2021, 89(2), 16; https://doi.org/10.3390/scipharm89020016 - 05 Apr 2021

Cited by 10 | Viewed by 6946

Abstract

Our main target and concept was to develop a method for the determination of the most prescribed antilipemic drug, atorvastatin, together with its related substances, with a single sample preparation and during a single chromatographic run, in the shortest possible period of time, [...] Read more.

Our main target and concept was to develop a method for the determination of the most prescribed antilipemic drug, atorvastatin, together with its related substances, with a single sample preparation and during a single chromatographic run, in the shortest possible period of time, with the lowest possible mobile phase consumption. A new rapid, simple chromatographic method for the determination of atorvastatin and its main specified impurities was developed, using different chromatographic columns. With this new concept of a mobile phase and a powerful core–shell, or a superficially porous silica-based column, satisfactory results for targeted parameters, such as critical peak resolution, run time length, and column backpressure, were achieved. The analysis is performed within a run duration of less than 15 min, which is about six times shorter than the official European Pharmacopoeia method. The chromatogram performances suggests that the method limit of quantification (LOQ) can be about 7 times lower, and the limit of detection (LOD) about 20 times lower, using an injection volume of only 2 µl. This was confirmed by the performed method validation in accordance with the International Conference on Harmonization (ICH) guideline for the validation of analytical procedures Q2(R1), where the selectivity, linearity, accuracy, precision, limit of quantification, and limit of detection were tested and confirmed. Full article

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8 pages, 1324 KiB

Open AccessTechnical Note

Simple Equations Pertaining to the Particle Number and Surface Area of Metallic, Polymeric, Lipidic and Vesicular Nanocarriers

by M. R. Mozafari, E. Mazaheri and K. Dormiani

Sci. Pharm. 2021, 89(2), 15; https://doi.org/10.3390/scipharm89020015 - 29 Mar 2021

Cited by 18 | Viewed by 6555

Abstract

Introduction: Bioactive encapsulation and drug delivery systems have already found their way to the market as efficient therapeutics to combat infections, viral diseases and different types of cancer. The fields of food fortification, nutraceutical supplementation and cosmeceuticals have also been getting the benefit [...] Read more.

Introduction: Bioactive encapsulation and drug delivery systems have already found their way to the market as efficient therapeutics to combat infections, viral diseases and different types of cancer. The fields of food fortification, nutraceutical supplementation and cosmeceuticals have also been getting the benefit of encapsulation technologies. Aim: Successful formulation of such therapeutic and nutraceutical compounds requires thorough analysis and assessment of certain characteristics including particle number and surface area without the need to employ sophisticated analytical techniques. Solution: Here we present simple mathematical formulas and equations used in the research and development of drug delivery and controlled release systems employed for bioactive encapsulation and targeting the sites of infection and cancer in vitro and in vivo. Systems covered in this entry include lipidic vesicles, polymeric capsules, metallic particles as well as surfactant- and tocopherol-based micro- and nanocarriers. Full article

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Sci. Pharm., Volume 89, Issue 2 (June 2021) – 15 articles

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