Scientia Pharmaceutica

14 pages, 813 KiB

Open AccessArticle

Old Dogs with New Tricks: Antiparasitic Potential of Structurally Diverse 5-Nitrofuran and 5-Nitrothiophene Imines and Acyl Hydrazones

by Ibrahim S. Al Nasr, Waleed S. Koko, Tariq A. Khan, Rainer Schobert and Bernhard Biersack

Sci. Pharm. 2023, 91(3), 44; https://doi.org/10.3390/scipharm91030044 - 19 Sep 2023

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Abstract

Miscellaneous imines and acyl hydrazones were prepared from 5-nitrofuraldehyde and 5-nitrothiophene-2-carboxaldehyde. Their activities against Toxoplasma gondii and Leishmania major parasites were evaluated. Promising antiparasitic effects and selectivities were observed for certain acyl hydrazones and imines. Cobalt(II) and copper(II) complexes conserved the high anti-Toxoplasma activities [...] Read more.

Miscellaneous imines and acyl hydrazones were prepared from 5-nitrofuraldehyde and 5-nitrothiophene-2-carboxaldehyde. Their activities against Toxoplasma gondii and Leishmania major parasites were evaluated. Promising antiparasitic effects and selectivities were observed for certain acyl hydrazones and imines. Cobalt(II) and copper(II) complexes conserved the high anti-Toxoplasma activities of 3-hydroxy-2-naphthoic carboxyl hydrazone (2a). In addition, sound activities against L. major promastigotes were observed for various analogs of 2a (2b and 2i) and pyrid-2-ylpyrazole-based imines (3g and 3h). Relatively low toxicities to kidney cells and macrophages indicate promising selectivity profiles for these compounds. Full article

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14 pages, 1976 KiB

Open AccessReview

Ethnobotanical Review of Selected Medicinal Plants in Guam for the Treatment of Urinary Tract Ailments and Their Pharmacological Properties

by Sahena Ferdosh

Sci. Pharm. 2023, 91(3), 43; https://doi.org/10.3390/scipharm91030043 - 01 Sep 2023

Viewed by 4649

Abstract

The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which [...] Read more.

The Chamorro healers of Guam have more than a thousand years of history of using herbs and medicinal plants for the treatment of common ailments. The objective of this study is to review the bioactive compounds and pharmacological properties of medicinal plants which are used for urinary tract health by local healers. Literature searches were performed using Google Scholar, ScienceDirect, PubMed, and SpringerLink, by using several keywords, including “medicinal plants in Guam”, “traditional uses”, “bioactive compounds”, “pharmacological properties”, and “urinary tract infections”. This review highlights the traditional uses, bioactive compounds, and pharmacological properties of five medicinal plant species, namely Euphorbia hirta, Phyllanthus amarus, Premna serratifolia, Psidium guajava, and Urena lobata. Phenolics, alkaloids, terpenoids, essential oils, and polypeptides are the leading secondary metabolites reported in different plant extracts, which have been found to have significant antimicrobial, antioxidant, anti-inflammatory, antidiabetic, and anticancer properties. The therapeutic claims made about medicinal plants in Guam are well supported by the literature, having similar applications and pharmacological properties in other regions of the world. These medicinal plants have a lot of unexplored potential that might be utilized to develop more potent drugs for the treatment of infectious diseases, as well as food and herbal supplements. Full article

(This article belongs to the Topic Natural Products and Drug Discovery)

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14 pages, 2079 KiB

Open AccessArticle

Flavonol Glycosides from Eugenia uniflora Leaves and Their In Vitro Cytotoxicity, Antioxidant and Anti-Inflammatory Activities

by Ayodeji Oluwabunmi Oriola, Gugulethu Mathews Miya, Moganavelli Singh and Adebola Omowunmi Oyedeji

Sci. Pharm. 2023, 91(3), 42; https://doi.org/10.3390/scipharm91030042 - 24 Aug 2023

Viewed by 1938

Abstract

In view of the extensive use of Eugenia uniflora leaves for the management of tumours and other chronic inflammatory diseases in traditional medicine, an activity-guided fractionation of its leaf ethanolic extract led to the isolation of two flavonol glycosides. Cytotoxicity study was based [...] Read more.

In view of the extensive use of Eugenia uniflora leaves for the management of tumours and other chronic inflammatory diseases in traditional medicine, an activity-guided fractionation of its leaf ethanolic extract led to the isolation of two flavonol glycosides. Cytotoxicity study was based on the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) viability assay against the non-tumourigenic human embryonic kidney (HEK-293) cells, and the cancerous liver (Hep-G2) and cervical (HeLa) cell lines. Antioxidant tests were carried out using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and hydrogen peroxide (H₂O₂) radical scavenging assays, while an in vitro anti-inflammatory test was conducted using egg albumin denaturation (EAD) assay. Based on comprehensive spectroscopic and spectrometric evidence, the compounds were elucidated as myricitrin (1) and a newly described compound, 5,7-dihydroxy-3-(3,4,5-trihydroxy-6-methyltetrahydropyran-2-yloxy)-2-(2,4,5-trihydroxyphenyl)chromen-4-one, named “unifloratrin (2)”. The cytotoxicity of myricitrin (1) was comparable to 5-fluorouracil (standard drug), with a CC₅₀ of 8.5 ± 2.2 µg/100 µL against HeLa cells. It also demonstrated better antioxidant activity, with an IC₅₀ of 6.23 ± 1.09, 22.01 ± 2.59 and 30.46 ± 1.79 µM against DPPH, NO and H₂O₂ free radicals, respectively. At 20 µg/mL and an incubation time of 2 h, myricitrin was comparable to diclofenac (standard drug) in anti-inflammatory activity. This report may serve as a justification for the ethnomedicinal use of E. uniflora, while flavonol glycosides, such as myricitrin (1), could be further exploited as a candidate cytotoxic agent. Full article

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8 pages, 241 KiB

Open AccessCommunication

Preliminary Screening of South African Plants for Binding Affinity to the Serotonin Reuptake Transporter and Adenosine A₁/A_2A Receptors

by Andisiwe Mnqika, Adeyemi O. Aremu, H. D. Janse van Rensburg and Makhotso Lekhooa

Sci. Pharm. 2023, 91(3), 41; https://doi.org/10.3390/scipharm91030041 - 22 Aug 2023

Viewed by 1540

Abstract

In South African traditional medicine, Gomphocarpus fruticosus (L.) W.T. Aiton, Hypoxis hemerocallidea Fisch. & C.A. Mey., and Leonotis leonurus. (L.) R.Br. have been recorded among different ethnic groups to be a valuable herbal remedy for the management of depression-related conditions. The current study [...] Read more.

In South African traditional medicine, Gomphocarpus fruticosus (L.) W.T. Aiton, Hypoxis hemerocallidea Fisch. & C.A. Mey., and Leonotis leonurus. (L.) R.Br. have been recorded among different ethnic groups to be a valuable herbal remedy for the management of depression-related conditions. The current study investigated the affinity of these three plants toward the serotonin reuptake transporter (SERT) and adenosine A₁/A₂ receptors. Six solvents (water, methanol, acetone, dichloromethane, petroleum ether, and hexane) were used to extract the selected plants. We established that eight extracts exerted potential affinity based on the applied in vitro binding experiment. The methanol and acetone extracts of Hypoxis hemerocallidea had 60% specific binding of [³H]citalopram, an indication that almost 40% of the plant extracts were bound to the SERT. For the adenosine receptor binding assays, methanol and hexane extracts of Leonotis leonurus were the most active, with rA₁K_i values of 0.038 and 0.176 mg/mL, respectively. In addition, the dichloromethane extract of Gomphocarpus fruticosus had an rA₁K_i value of 6.46 mg/mL. Extracts from the more polar solvents methanol and dichloromethane had higher binding affinity. Additionally, these plant extracts acted as antagonists at the adenosine A₁ receptor. Overall, the current findings provide an indication of the potential antidepressant effects of some of the tested extracts based on their binding to the receptors evaluated. However, a combination of other in vitro assays is needed to establish possible mechanisms of action. In addition, computational analysis and profiling of plant extracts is crucial to identify the bioactive compounds with a higher affinity to the receptors. Ultimately, in vivo studies remain essential to allow for an in-depth elucidation of the mechanisms of action. Full article

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14 pages, 3969 KiB

Open AccessArticle

Hepatoprotective Activity, In Silico Analysis, and Molecular Docking Study of Verbascoside from Leucophyllum frutescens in Rats with Post-Necrotic Liver Damage

by Osmar Antonio Jaramillo-Morales, Erik Díaz-Cervantes, Lisa Dalla Via, Aida Nelly Garcia-Argaez, Josué Vidal Espinosa-Juárez, José Carlos Ovando-Zambrano, Victor Manuel Muñoz-Pérez, Carmen Valadez-Vega and Mirandeli Bautista

Sci. Pharm. 2023, 91(3), 40; https://doi.org/10.3390/scipharm91030040 - 16 Aug 2023

Cited by 1 | Viewed by 2343

Abstract

There is an urgent need for scientists to verify the pharmacological properties of medicinal plants. Leucophyllum frutescens (Lf) belongs to the family Scrophulariaceae, and it is used in the treatment of airway diseases such as cough, tuberculosis, and asthma. The methanolic extract [...] Read more.

There is an urgent need for scientists to verify the pharmacological properties of medicinal plants. Leucophyllum frutescens (Lf) belongs to the family Scrophulariaceae, and it is used in the treatment of airway diseases such as cough, tuberculosis, and asthma. The methanolic extract of the aerial parts of Lf allows for the isolation and identification of verbascoside (Vb). This study aimed to evaluate the hepatoprotective effect of Vb, a caffeoyl phenylethanoid glycoside (CPG), on post-necrotic liver damage induced by thioacetamide (TA) via in vivo and in silico studies, with the latter considering a cancerous process. The aerial parts of Lf were extracted by maceration using hexane methanol (5 L/500 g/8 days). Vb was isolated from methanol extract at approximately 30%. Wistar rats were intragastrically pretreated or not with a single dose of Vb (20 mg/kg) for four days. On the fourth day, a single dose of TA (6.6 mmol/kg) was intraperitoneally injected. Blood samples and parameters related to liver damage, like AST and ALT, were obtained. Vb significantly reduced the level of liver injury following thioacetamide-induced necrosis. This was corroborated by in silico assay and docking studies, demonstrating that Vb can interact with a HeLa target through hydrogen bonds and electrostatic interactions, achieving better performance than commercial chemotherapeutic Taxol^®, by 0.34 kcal/mol. AST and ALT were significantly lower in the rats pretreated with Vb. Furthermore, Vb did not induce cytotoxicity and had a median lethal dose (LD50) greater than 5000 mg/kg. These results suggest that Vb may be used as an alternative to reduce liver damage. Full article

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11 pages, 811 KiB

Open AccessCommunication

Compounded Hair Solutions and Foams Containing Minoxidil: Does the Color Change Impact Stability?

by Hudson C. Polonini and Carolina C. V. Silva

Sci. Pharm. 2023, 91(3), 39; https://doi.org/10.3390/scipharm91030039 - 15 Aug 2023

Viewed by 5717

Abstract

An increasing number of pharmacies around the world are producing hair solutions and foams containing minoxidil for alopecia, commonly using ready-to-use vehicles such as TrichoSol^TM or TrichoFoam^TM. However, it is paramount to determine the chemical and microbiological compatibility of these [...] Read more.

An increasing number of pharmacies around the world are producing hair solutions and foams containing minoxidil for alopecia, commonly using ready-to-use vehicles such as TrichoSol^TM or TrichoFoam^TM. However, it is paramount to determine the chemical and microbiological compatibility of these formulations so they can be safely implemented as vehicles of choice. Also, these products usually suffer from a change of color over time, which leads to many patients prematurely discontinuing treatment. As long-term treatment is recommended, this study aimed to assess the physical–chemical and microbiological stability and investigate the color change of compounded minoxidil formulations. For that, HPLC analyses and antimicrobial effectiveness testing were conducted in a bracketed study covering concentrations from 1.0% to 7.0% of minoxidil. HPLC, pH, and metals in 5.0% minoxidil compounded products were determined using ICP-MS to evaluate the mechanisms involved in their color change. The stability of the products varied from 120 to 380 days. The color change was remarkably noticeable, but apart from this parameter, no other quality attribute was affected throughout this period, including minoxidil content, which presented only minor fluctuations. No precipitation was observed, and pH was relatively stable. It is not expected that this yellow color will impact effectiveness. Finally, we created an indicative color chart of the behavior of minoxidil in the studied vehicles. Full article

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

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11 pages, 1466 KiB

Open AccessArticle

PBPK Evaluation of Sofosbuvir Dose in Pediatrics Using Simcyp^®

by Rania Elkeeb, Anomeh Avartoomian, Amira S. Gouda, Ahmed M. Abdel-Megied, Ola Abdallah and Eman Atef

Sci. Pharm. 2023, 91(3), 38; https://doi.org/10.3390/scipharm91030038 - 10 Aug 2023

Viewed by 1868

Abstract

The aim of the study is to evaluate the effectiveness of the pediatric sofosbuvir weight-based dosing strategy in providing an equitable drug exposure compared to the marketed dose. The physiologically based pharmacokinetic (PBPK) modeling and simulation is a valuable tool in assessing drug [...] Read more.

The aim of the study is to evaluate the effectiveness of the pediatric sofosbuvir weight-based dosing strategy in providing an equitable drug exposure compared to the marketed dose. The physiologically based pharmacokinetic (PBPK) modeling and simulation is a valuable tool in assessing drug dosing and toxicity in populations with physiological, pathological, and genetic pharmacokinetic (PK) variability. The PBPK model of the sofosbuvir compound was developed using Simcyp^® V20. The model was developed and verified using the published sofosbuvir’s physicochemical properties and clinical data from multiple studies on healthy adult volunteers, hepatitis C virus (HCV)-infected adults, and HCV-infected pediatrics. The AUC and C_max fold ratio of (predicted/observed) fell within the acceptable range of 0.5–2 in all tested adults’ data, confirming the successful development of the sofosbuvir Simcyp^® compound model. Using this model, a weight-based dosing regimen of 6 mg/kg in pediatric patients was simulated and compared to the 150 mg and 200 mg approved dose for 3–6 and 6–12 y/o pediatric patients, respectively. No dose adjustment was recommended in patients ages 6–12 y/o. However, compared to the approved 150 mg for 3–6 y/o, the weight base dose provided an equitable drug exposure to adults. Further clinical studies are warranted to verify this finding. Full article

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14 pages, 3221 KiB

Open AccessArticle

Chitosan-Based Nanocarriers for Delivery of Remdesivir

by Viktoria Milkova, Kamelia Kamburova, Petar Martinov, Neli Vilhelmova-Ilieva and Viktor Rashev

Sci. Pharm. 2023, 91(3), 37; https://doi.org/10.3390/scipharm91030037 - 09 Aug 2023

Cited by 2 | Viewed by 1479

Abstract

Stable multicomponent capsules for the delivery of remdesivir (Veklury^®) are produced through subsequent electrostatic adsorption of oppositely charged components on oil emulsion droplets. For the first time, the encapsulation and release of the medicine Veklury^® from polymer capsules was reported. [...] Read more.

Stable multicomponent capsules for the delivery of remdesivir (Veklury^®) are produced through subsequent electrostatic adsorption of oppositely charged components on oil emulsion droplets. For the first time, the encapsulation and release of the medicine Veklury^® from polymer capsules was reported. In this study, the effect of the physicochemical properties of chitosan on the size and stability of the produced structures is investigated, on the loaded amount of drug and on the kinetics of drug release in conditions close to the physiological ones. Microbiological studies of the capsules and their constituents were performed via in vitro assays against HCT-8 cell lines and human coronavirus HCoV-OC43. A detailed analysis was performed on the influence of the properties of produced capsules on cytotoxicity against the chosen cell line, as well as their effect on the replication cycle of the virus, the virucidal activity of the samples against the viability of the extracellular virions, and their effect on viral adsorption on the cell membrane. Full article

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14 pages, 2320 KiB

Open AccessArticle

Computational Assessment of Cannflavin A as a TAK1 Inhibitor: Implication as a Potential Therapeutic Target for Anti-Inflammation

by Sarunya Chuanphongpanich, Satapat Racha, Banthita Saengsitthisak, Pichai Pirakitikulr and Kannika Racha

Sci. Pharm. 2023, 91(3), 36; https://doi.org/10.3390/scipharm91030036 - 17 Jul 2023

Viewed by 2299

Abstract

TAK1 (transforming growth factor-beta-activated kinase 1) is a crucial therapeutic target in inflammation-related diseases. This study investigated the inhibitory potential of cannflavin A, a flavonoid found in Cannabis sativa, against TAK1. Through in silico approaches, including drug-likeness analysis, ADMET assessment, molecular docking, [...] Read more.

TAK1 (transforming growth factor-beta-activated kinase 1) is a crucial therapeutic target in inflammation-related diseases. This study investigated the inhibitory potential of cannflavin A, a flavonoid found in Cannabis sativa, against TAK1. Through in silico approaches, including drug-likeness analysis, ADMET assessment, molecular docking, and molecular dynamics simulation, the binding affinity and stability of cannflavin A were evaluated. The results demonstrate that cannflavin A exhibits excellent ADMET properties and displays superior binding affinity and stability at the ATP binding site of TAK1 when compared to the known inhibitor takinib. Notably, the decomposition of binding free energy unveils critical amino acid residues involved in TAK1 binding, underscoring the inhibitory effect of cannflavin A through TAK1 inhibition. These findings highlight the potential of cannflavin A as a TAK1 inhibitor and its significant implications for the development of targeted therapies in inflammation-related diseases. Through modulating inflammatory signaling pathways, cannflavin A holds promise for more effective and tailored treatment strategies, particularly in rheumatoid arthritis. This study contributes to the current understanding of cannflavin A’s application and provides a foundation for further research and innovative approaches in targeted therapies for inflammatory conditions. Full article

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11 pages, 2315 KiB

Open AccessBrief Report

Adjuvant Oligonucleotide Vaccine Increases Survival and Improves Lung Tissue Condition of B6.Cg-Tg (K18-ACE2)2 Transgenic Mice

by Volodymyr V. Oberemok, Kateryna V. Laikova, Kseniya A. Yurchenko, Ilya A. Novikov, Tatyana P. Makalish, Anatolii V. Kubyshkin, Oksana A. Andreeva and Anastasiya I. Bilyk

Sci. Pharm. 2023, 91(3), 35; https://doi.org/10.3390/scipharm91030035 - 12 Jul 2023

Viewed by 1659

Abstract

The main problem in creating anti-coronavirus vaccines that target mainly proteins of the outer membrane of the virus is the rapid variability in the RNA genome of the pathogen that encodes these proteins. In addition, the introduction of technologies that can affordably and [...] Read more.

The main problem in creating anti-coronavirus vaccines that target mainly proteins of the outer membrane of the virus is the rapid variability in the RNA genome of the pathogen that encodes these proteins. In addition, the introduction of technologies that can affordably and quickly produce flexible vaccine formulas that easily adapt to the emergence of new subtypes of SARS-CoV-2 is required. Universal adjuvant oligonucleotide vaccines based on conserved regions of the SARS-CoV-2 genome can take into account the dynamics of rapid changes in the virus genome, as well as be easily synthesized on automatic DNA synthesizers in large quantities in a short time. In this brief report, the effectiveness of four phosphorothioate constructs of the La-S-so-type adjuvant oligonucleotide vaccine is evaluated on B6.Cg-Tg (K18-ACE2)2 transgenic mice for the first time. In our primary trials, the oligonucleotide vaccine increased the survival rate of animals infected with SARS-CoV-2 and also reduced the destructive effects of the virus on the lung tissue of mice, activating both their innate and adaptive immunity. The obtained results show that the development of adjuvant oligonucleotide vaccine constructs of the La-S-so type is an affordable and efficient platform for the prevention of coronavirus infections, including those caused by SARS-CoV-2. Full article

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11 pages, 4160 KiB

Open AccessArticle

In Vitro Cytotoxicity and Antioxidant Studies of Dovyallis caffra-Mediated Cassiterite (SnO₂) Nanoparticles

by Jerry O. Adeyemi

Sci. Pharm. 2023, 91(3), 34; https://doi.org/10.3390/scipharm91030034 - 07 Jul 2023

Cited by 1 | Viewed by 1747

Abstract

Many medicinal plants found in Africa, such as Dovyallis caffra, have been reported to contain various bioactive compounds, which have been found to reduce metal salts into their corresponding metal-based nanoparticles. In this paper, the evaluation of synthesis, characterization, and biological properties [...] Read more.

Many medicinal plants found in Africa, such as Dovyallis caffra, have been reported to contain various bioactive compounds, which have been found to reduce metal salts into their corresponding metal-based nanoparticles. In this paper, the evaluation of synthesis, characterization, and biological properties of Dovyallis caffra-mediated cassiterite (SnO₂) nanoparticles was carried out. The physicochemical properties of the synthesized material were investigated using X-ray diffraction (XRD), energy dispersive X-ray analysis (EDX), scanning electron microscopy (SEM), and transmission electron microscopy (TEM) techniques. The characterization studies revealed that the material possessed a single tetragonal cassiterite SnO₂ phase, having a cluster-like foam appearance and an irregular spherical morphology with diameters ranging from 6.57 to 34.03 nm. The biological screening revealed that the prepared cassiterite (SnO₂) nanoparticles exhibited cytotoxicity against the MCF-7 breast cancer cells, with an IC₅₀ value of 62.33 µg mL⁻¹, better than the standard drug 5-fluorouracil, with an IC₅₀ value of 71.21 µg mL⁻¹. The radical scavenging potential of the nanoparticles, using the DPPH assay, showed that it possessed a slightly better activity than ascorbic acid, a common antioxidant. These results suggest that the Dovyallis caffra-mediated cassiterite (SnO₂) nanoparticles possess the potential to simultaneously generate and scavenge excess ROS, which in turn results in the exhibition of good cytotoxicity and antioxidant properties. Full article

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20 pages, 861 KiB

Open AccessReview

Chromobacterium Violaceum: A Model for Evaluating the Anti-Quorum Sensing Activities of Plant Substances

by Petya D. Dimitrova, Tsvetozara Damyanova and Tsvetelina Paunova-Krasteva

Sci. Pharm. 2023, 91(3), 33; https://doi.org/10.3390/scipharm91030033 - 03 Jul 2023

Cited by 8 | Viewed by 3726

Abstract

In the new antibiotic era, the exponential increase in multiresistant bacterial strains has become the main global health problem. Many researchers have focused their efforts on exploring novel or combined strategies for combating bacterial resistance. Good knowledge of the molecular mechanisms of resistance [...] Read more.

In the new antibiotic era, the exponential increase in multiresistant bacterial strains has become the main global health problem. Many researchers have focused their efforts on exploring novel or combined strategies for combating bacterial resistance. Good knowledge of the molecular mechanisms of resistance and bacterial virulence factors as key targets provides us with a good basis for resolving the problem. One particularly attractive and promising strategy is to attack the main regulatory “network” of bacterial virulence determinants known as quorum sensing (QS). The inhibition of QS signals will be a novel means of screening more effective quorum-sensing inhibitors (QSIs) and will play a key role in the use of next-generation antimicrobials in the battle against resistance. This motivated the present review to provide a comprehensive clarification of the regulatory mechanisms of quorum-sensing signaling pathways in Chromobacterium violaceum and the discovery of potential plant quorum-sensing inhibitors. Full article

(This article belongs to the Topic Natural Products and Drug Discovery)

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26 pages, 6437 KiB

Open AccessReview

Structural Aspect of Hydroxyethyl-Starch–Anticancer-Drug-Conjugates as State-of-the-Art Drug Carriers

by Koushik Chandra, Sansa Dutta, Haradhan Kolya and Chun-Won Kang

Sci. Pharm. 2023, 91(3), 32; https://doi.org/10.3390/scipharm91030032 - 29 Jun 2023

Cited by 1 | Viewed by 2083

Abstract

Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, [...] Read more.

Cancer is a genetic disorder and its treatment usually requires a long time and expensive diagnosis. While chemotherapy is the most conventional approach in treating most cancers, patients often suffer from undesired side effects due to various pharmacokinetic aspects. To address this issue, target-oriented drug-delivery systems (DDS) or pulsatile drug-delivery systems (PDDS) have recently been developed as an alternative tool that takes care of the entire pharmacodynamic activities of drug action. Hydroxyethyl starch (HES) has emerged as an effective clinical tool for delivering anticancer agents into target cells. These systems have demonstrated significant potential as anticancer drug carrier conjugates through their innate pharmacokinetic properties with their safety profile. This review focuses primarily on the structural aspect during the use of HES or HES-based polymers as carriers for delivering well-known anticancer drugs. This review also indicates a perspective on the long-term research needed for the sake of improving modern drug-delivery systems based on HES polymers and in the form of nanocarriers. Full article

(This article belongs to the Topic Natural Products and Drug Discovery)

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16 pages, 2809 KiB

Open AccessArticle

Analytical Investigation of Forced Oxidized Anti-VEGF IgG Molecules: A Focus on the Alterations in Antigen and Receptor Binding Activities

by Ayhan Parlar, Busra Gurel, Mehmet Reşit Sönmez and Meral Yüce

Sci. Pharm. 2023, 91(3), 31; https://doi.org/10.3390/scipharm91030031 - 28 Jun 2023

Viewed by 3457

Abstract

Alterations in the biological activity of the molecules under stress conditions have not been documented as widely in the literature yet. This study was designed to reveal the functional impacts of various oxidation conditions on a model mAb, a commercial anti-VEGF IgG molecule. [...] Read more.

Alterations in the biological activity of the molecules under stress conditions have not been documented as widely in the literature yet. This study was designed to reveal the functional impacts of various oxidation conditions on a model mAb, a commercial anti-VEGF IgG molecule. The responses to antigen binding, cell proliferation, FcRn receptors, and C1q binding, which rarely appear in the current literature, were investigated. The authors report peptide mapping data, post-translational modification (PTM) analysis, cell proliferation performance, and antigen (VEGF), C1q, and FcRn binding activities of the mAb under various stress conditions. The oxidation-prone site of the mAb was determined as Met252 in the DTLMISR peptide. The VEGF binding activity and anti-cell proliferation activity of the mAbs did not alter, while C1q and FcRn binding capacity significantly decreased under oxidative stress conditions. The full report is vital for many scientific and industrial processes about mAbs. The authors recommend performing functional analyses in addition to the structural studies while investigating the impacts of stress factors on therapeutic mAbs. Full article

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

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15 pages, 2715 KiB

Open AccessArticle

Impact of Compressional Force, Croscarmellose Sodium, and Microcrystalline Cellulose on Black Pepper Extract Tablet Properties Based on Design of Experiments Approach

by Chaowalit Monton, Thaniya Wunnakup, Jirapornchai Suksaeree, Laksana Charoenchai and Natawat Chankana

Sci. Pharm. 2023, 91(3), 30; https://doi.org/10.3390/scipharm91030030 - 27 Jun 2023

Cited by 2 | Viewed by 1994

Abstract

This study aimed to prepare tablets of black pepper extract using the Design of Experiments (DOE) approach. The levels of three factors—compressional force, croscarmellose sodium (CCS), and microcrystalline cellulose (MCC)—were screened using the one-factor-at-a-time technique, followed by the DOE utilizing the Box–Behnken design. [...] Read more.

This study aimed to prepare tablets of black pepper extract using the Design of Experiments (DOE) approach. The levels of three factors—compressional force, croscarmellose sodium (CCS), and microcrystalline cellulose (MCC)—were screened using the one-factor-at-a-time technique, followed by the DOE utilizing the Box–Behnken design. The respective variations for each factor were as follows: compressional force (1500–2500 psi), CCS (1–3%), and MCC (32–42%). The results indicated that compressional force significantly decreased tablet thickness and friability, while increasing hardness and prolonging disintegration time. CCS significantly shortened disintegration time but did not affect tablet thickness, hardness, and friability. MCC, on the other hand, significantly increased tablet thickness and hardness, while significantly decreasing friability. Furthermore, the study observed interactions among factors and quadratic effects of each factor, which significantly influenced tablet properties. The optimal tablet formulation consisted of 2.2% CCS, 37% MCC, and a compressional force of 2000 psi. These tablets had a weight of 198.39 ± 0.49 mg, a diameter of 9.67 ± 0.01 mm, a thickness of 1.98 ± 0.02 mm, a hardness of 7.36 ± 0.24 kP, a friability of 0.11 ± 0.02%, and a disintegration time of 5.59 ± 0.39 min. The actual values obtained using the optimal conditions closely matched the predicted values, with a low percent error (less than 5%). In conclusion, the application of the DOE approach successfully developed tablets of black pepper extract, which can be utilized as food supplement products. Full article

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14 pages, 1635 KiB

Open AccessArticle

Escherichia coli (Lilly) and Saccharomyces cerevisiae (Novo) rDNA Glucagon: An Assessment of Their Actions When Supplied Selectively to Periportal Cells in the Bivascularly Perfused Rat Liver

by Lívia Bracht, Jorgete Constantin, Rosane Marina Peralta and Adelar Bracht

Sci. Pharm. 2023, 91(3), 29; https://doi.org/10.3390/scipharm91030029 - 24 Jun 2023

Viewed by 1559

Abstract

The actions of Eli Lilly-rDNA glucagon and Novo Nordisk-rDNA glucagon on glycogen catabolism and related parameters were investigated using the bivascularly perfused rat liver. The technique allows glucagon to be supplied to a selective portion of the hepatic periportal region (≈39%) when the [...] Read more.

The actions of Eli Lilly-rDNA glucagon and Novo Nordisk-rDNA glucagon on glycogen catabolism and related parameters were investigated using the bivascularly perfused rat liver. The technique allows glucagon to be supplied to a selective portion of the hepatic periportal region (≈39%) when the former is infused into the hepatic artery in retrograde perfusion. Both glucagon preparations were equally effective in influencing metabolism (glucose output, glycolysis and O₂ uptake) when supplied to all cells along the liver sinusoids. When only a selective periportal region of the liver was supplied with the hormone, however, the action of Novo Nordisk-rDNA glucagon was proportional to the accessible cell space, whereas the action of Eli Lilly-rDNA glucagon greatly exceeded the action that was expected for the accessible space. Chromatographically, both rDNA preparations were not pure, but their impurities were not the same. The impurities in Eli Lilly-rDNA glucagon resembled those found in the similarly acting pancreatic Eli Lilly glucagon. It was concluded that the space-extrapolating action of Eli Lilly-rDNA glucagon is caused by a yet-to-be-identified impurity. The hypothesis was raised that an impurity in certain glucagon preparations can enhance cell-to-cell propagation of the glucagon signal, possibly via gap junctional communication. Full article

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

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Sci. Pharm., Volume 91, Issue 3 (September 2023) – 16 articles

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