Scientia Pharmaceutica

18 pages, 1082 KB

Open AccessArticle

Native Tapioca Starch Agglomerated Using Its Gelatinized Dispersion for Tablet Production by Direct Compression

by Rapee Jarungsirawat, Chaipat Siriwachirachai and Thaned Pongjanyakul

Sci. Pharm. 2026, 94(3), 73; https://doi.org/10.3390/scipharm94030073 (registering DOI) - 31 Aug 2026

This study aimed to investigate the physical properties of native tapioca starch (TS) ag-glomerated using its gelatinized dispersion as an agglomerating agent and to evaluate the performance of the resulting agglomerate tablets. The results demonstrate that TS agglomerated with gelatinized tapioca starch (GTS) [...] Read more.

This study aimed to investigate the physical properties of native tapioca starch (TS) ag-glomerated using its gelatinized dispersion as an agglomerating agent and to evaluate the performance of the resulting agglomerate tablets. The results demonstrate that TS agglomerated with gelatinized tapioca starch (GTS) exhibited increased particle strength as GTS content increased. Moreover, particle flowability was enhanced compared with that of native TS. The compressibility of TS agglomerates increased with higher GTS content, thereby reducing resistance to volume reduction and enhancing the plasticity of particle deformation under pressure, resulting in the greater tensile strength of the tablets. GTS showed superior performance to polyvinylpyrrolidone and sodium alginate at the concentration of 2% w/w in terms of Carr’s index and tablet hardness. Propranolol HCl (PNL) tablets prepared from agglomerates with GTS exhibited higher hardness than those without GTS, with tablet hardness increasing proportionally to GTS content. Additionally, GTS facilitated faster tablet disintegration, thereby accelerating PNL dissolution. In drug-loading tests, agglomerate tablets containing 3% GTS maintained acceptable physical properties when the PNL content did not exceed 20% w/w. Higher PNL loading may be achievable by increasing compression pressure. These findings indicate that native TS agglomerated with GTS is a promising tablet diluent for direct compression. Full article

► Show Figures

Graphical abstract

27 pages, 2576 KB

Open AccessArticle

Development and Microstructural Analysis of Rapid-Release Acanthus montanus Effervescent Mouthwash Tablets for Oral Care

by Piyanut Thongphasuk, Nuntachai Hanpramukkun, Arthimond Vutthiphong, Ratana Charoenwattanasatien, Phakkhananan Pakawanit and Sucharat Limsitthichaikoon

Sci. Pharm. 2026, 94(3), 72; https://doi.org/10.3390/scipharm94030072 (registering DOI) - 29 Aug 2026

Abstract

The translation of underutilized botanical resources into advanced therapeutic dosage forms represents a critical frontier in pharmaceutical sciences. This study systematically characterizes the phytochemical and biological profiles of three Acanthus species (Acanthus ebracteatus, Acanthus ilicifolius, and Acanthus montanus) to [...] Read more.

The translation of underutilized botanical resources into advanced therapeutic dosage forms represents a critical frontier in pharmaceutical sciences. This study systematically characterizes the phytochemical and biological profiles of three Acanthus species (Acanthus ebracteatus, Acanthus ilicifolius, and Acanthus montanus) to develop a functional, rapid-release effervescent mouthwash tablet for oral mucosal repair. Phytochemical screening demonstrated that ethanolic extraction selectively concentrated bioactive phenolics and saponins compared to conventional aqueous methods. The ethanolic A. montanus extract emerged as the premier candidate, exhibiting the highest total phenolic content, excellent biocompatibility with human gingival fibroblasts, and significant promotion of in vitro cellular migration. Furthermore, it demonstrated robust, broad-spectrum antimicrobial efficacy against key cariogenic (Streptococcus mutans) and opportunistic (Candida albicans) oral pathogens. To transition this botanical discovery into a viable delivery system, the optimized extract was integrated into an effervescent base via wet granulation utilizing absolute ethanol, followed by blending with extragranular excipients and single-stroke compression. The resulting optimized matrix, incorporating 10% sodium starch glycolate, achieved an ideal mechanical-kinetic balance, yielding exceptional structural toughness (0.23% friability) and rapid disintegration (2.02 min). Advanced 3D synchrotron X-ray tomographic microscopy revealed that this specific super-disintegrant ratio generates a highly interconnected, porous internal architecture driving accelerated capillary-mediated breakdown. Ultimately, this study successfully translates a botanical extract into a mechanistically optimized, functionally validated dosage form for targeted oral therapies. Full article

► Show Figures

Figure 1

33 pages, 7725 KB

Open AccessArticle

Phytochemical Study and Cytotoxic Properties of Hydroalcoholic Extracts of Epilobium parviflorum Schreb.: In Silico and In Vitro Insights

by Christian Goldiș, Roxana Racoviceanu, Mihaela Jorgovan, Roxana Negrea-Ghiulai, Codruța Șoica, Alexandra Prodea, Oana Bătrîna, Gabriela Antal and Alexandra Mioc

Sci. Pharm. 2026, 94(3), 71; https://doi.org/10.3390/scipharm94030071 - 23 Aug 2026

Abstract

Epilobium parviflorum Schreb. is a medicinal plant used traditionally against inflammatory disorders whose cytotoxic potential is still incompletely revealed. The current study investigates the phytochemical composition and in vitro cytotoxic activity of four hydroalcoholic extracts prepared from the aerial parts of E. parviflorum [...] Read more.

Epilobium parviflorum Schreb. is a medicinal plant used traditionally against inflammatory disorders whose cytotoxic potential is still incompletely revealed. The current study investigates the phytochemical composition and in vitro cytotoxic activity of four hydroalcoholic extracts prepared from the aerial parts of E. parviflorum by using maceration and Soxhlet extraction. The extracts were characterized in terms of total phenolic, flavonoid and tannins composition and LC-MS was used to identify its individual polyphenols. Their biological effects were assessed against four cancer cell lines (A375 melanoma, HT-29 colorectal adenocarcinoma, PANC-1 pancreatic carcinoma and SK-OV-3 ovarian adenocarcinoma cells), while using HaCaT keratinocytes as healthy cells in order to assess selectivity. Cell viability, cytoskeletal and nuclear morphology, mitochondrial respiration and network pharmacology were further investigated. A complex phenolic profile was revealed, with hyperoside being identified as the main component in all extracts while the extraction parameters strongly influenced the recovery of various phenolic compounds. All extracts reduced cancer cell viability in a dose-dependent manner after 24 h exposure, with the most pronounced effects observed at 720 and 1000 μg/mL, while HaCaT cells were left relatively unaffected. The morphological assessment indicated nuclear condensation, fragmentation and cytoskeletal disruption following the application of extracts. Moreover, high-resolution respirometry showed reduced oxidative phosphorylation and electron transfer system capacity thus indicating that early mitochondrial dysfunction may contribute to the cytotoxic effects. Network pharmacology revealed that ERBB2, CTNNB1, HSP90AA1 and HDAC6 might act as molecular targets in melanoma. Thus, these findings support the hypothesis that E. parviflorum hydroalcoholic extracts, particularly the 40% ethanol Soxhlet extract, may serve as important sources of bioactive phytocompounds with antiproliferative and apoptotic properties. Full article

(This article belongs to the Special Issue Anticancer Potential of Natural Products)

► Show Figures

Figure 1

37 pages, 7245 KB

Open AccessReview

Quinoline Scaffold in Drug Discovery: Synthetic Strategies, Therapeutic Applications, and Emerging Drug Candidates

by Ayoub El-Mrabet, Amal Haoudi, Amine Ez-Zoubi, Rachid Bouzammit, Abdellatif Alami and Ahmed Mazzah

Sci. Pharm. 2026, 94(3), 70; https://doi.org/10.3390/scipharm94030070 - 20 Aug 2026

Abstract

Quinoline is a bicyclic aromatic heterocycle composed of a fused benzene and pyridine ring, and it has held an important place in medicinal chemistry for nearly two centuries. F. Runge first isolated it from coal tar in 1834, and it was later found [...] Read more.

Quinoline is a bicyclic aromatic heterocycle composed of a fused benzene and pyridine ring, and it has held an important place in medicinal chemistry for nearly two centuries. F. Runge first isolated it from coal tar in 1834, and it was later found to form the structural core of well-known natural products such as quinine, camptothecin, and γ-fagarine. Its asymmetric electron distribution, amphoteric character, and ability to undergo both electrophilic and nucleophilic substitution confer considerable pharmacophoric versatility on the quinoline scaffold. This review covers the chemistry and therapeutic relevance of quinoline derivatives, with an emphasis on their pharmacological significance rather than on their synthesis alone. It begins with a brief account of the scaffold’s structural features and main synthetic routes, then examines the biological activities reported for quinoline-based compounds, including antibacterial, anticancer, anti-inflammatory, antimalarial, antiparasitic, antitubercular, antioxidant, and antiviral activities, together with structure–activity relationships discussed at the level of specific ligand–target interactions where data allow. The last section covers more recent directions in quinoline-based drug discovery, including PROTAC degraders, kinase inhibitors, and multitarget-directed ligands, an area not extensively addressed in earlier reviews of this scaffold. The literature surveyed here shows that quinoline derivatives continue to serve as a versatile scaffold for generating new leads, linking established synthetic chemistry with current mechanistic and computational approaches. The continued diversification of quinoline-based chemotypes and their biological mechanisms reinforces the importance of this scaffold as a versatile platform for medicinal chemistry and drug discovery. Full article

► Show Figures

Graphical abstract

43 pages, 5749 KB

Open AccessReview

Cytokines, the Tumor Microenvironment, and Selected Plant-Derived Natural Products

by Yulin Ren and A. Douglas Kinghorn

Sci. Pharm. 2026, 94(3), 69; https://doi.org/10.3390/scipharm94030069 - 19 Aug 2026

Abstract

Cytokines are produced by immune and other cells and work as cellular messengers to regulate an immune response and other biological processes. As the main components of the tumor microenvironment (TME), cytokines are involved in the major events of cancer development, including cancer [...] Read more.

Cytokines are produced by immune and other cells and work as cellular messengers to regulate an immune response and other biological processes. As the main components of the tumor microenvironment (TME), cytokines are involved in the major events of cancer development, including cancer and cancer stem cell proliferation, angiogenesis, invasion, and metastasis. They also modulate immune functions and inhibit tumor progression and resistance to conventional therapies and thus have been regarded as promising targets for cancer treatment. Recently, tumor reversibility has attracted wide interest, for which the TME plays a critical role. Many plant-derived products exhibit potential tumor-inhibitory and cytokine-modulatory activities, including andrographolide, artemisinin, berberine, camptothecin, capsaicin, curcumin, digoxin, morphine, paclitaxel, and vinblastine, indicating their possible use in cancer reversal. Thus, in the present review, correlations among cytokines, the TME, tumor immunity, and tumor reversibility have been discussed, and the potential effects of selected plant-derived natural products on these issues have been addressed. Full article

(This article belongs to the Special Issue Anticancer Potential of Natural Products)

► Show Figures

Graphical abstract

11 pages, 1582 KB

Open AccessCommunication

Tea Beverage-Dependent Reduction in Risperidone Concentration Following Mixing with Risperidone Oral Solution

by Hiroyuki Suzuki, Yosuke Nishikawa, Shurito Odashima, Taisuke Konno, Ryusuke Ouchi, Daisuke Kikuchi, Kensuke Usui, Kouji Okada, Shigeki Kisara, Hitoshi Nakamura and Yuriko Murai

Sci. Pharm. 2026, 94(3), 68; https://doi.org/10.3390/scipharm94030068 - 18 Aug 2026

Abstract

Risperidone (RIS) oral solution has a bitter taste and is sometimes mixed with beverages to improve palatability and medication adherence. Although the package insert advises against mixing with tea beverages, the effects of beverage type and tea leaf variety on RIS concentration remain [...] Read more.

Risperidone (RIS) oral solution has a bitter taste and is sometimes mixed with beverages to improve palatability and medication adherence. Although the package insert advises against mixing with tea beverages, the effects of beverage type and tea leaf variety on RIS concentration remain unclear. RIS oral solution was mixed with commercially available black tea, green tea, and hojicha beverages, and black tea leaf extracts. RIS concentration in the supernatant was quantified by high-performance liquid chromatography, and its recovery from precipitates was evaluated in selected samples. RIS concentration decreased in all black tea and green tea beverages and black tea extracts, whereas some hojicha beverages showed no significant decrease. The extent of reduction differed among beverage types and black tea leaf varieties. RIS was substantially recovered from precipitates redissolved in methanol or dissolution test fluid 1 (pH 1.2), whereas recovery from dissolution test fluid 2 (pH 6.8) was lower. Chromatographic and UV spectral analyses supported the presence of RIS in redissolved precipitates. The reduction in RIS concentration is associated, at least in part, with transfer into precipitates and depends on beverage type and tea leaf variety. These findings support the recommendation to avoid diluting RIS oral solution with tea beverages. Full article

► Show Figures

Figure 1

16 pages, 6891 KB

Open AccessArticle

Development and Validation of a Capillary Zone Electrophoresis Method with Indirect UV Detection for the Simultaneous Determination of Azelaic Acid and Salicylic Acid in Pharmaceutical and Cosmetic Preparations

by Șoimița Emiliana Măgerușan, Gabriel Hancu and Eleonora Mircia

Sci. Pharm. 2026, 94(3), 67; https://doi.org/10.3390/scipharm94030067 - 8 Aug 2026

Abstract

Azelaic acid (AZA) and salicylic acid (SA) are widely used active ingredients in pharmaceutical and cosmetic formulations for the treatment of acne, rosacea, hyperpigmentation, and other dermatological conditions. Despite their frequent co-administration, analytical methods for their simultaneous determination remain limited. In the present [...] Read more.

Azelaic acid (AZA) and salicylic acid (SA) are widely used active ingredients in pharmaceutical and cosmetic formulations for the treatment of acne, rosacea, hyperpigmentation, and other dermatological conditions. Despite their frequent co-administration, analytical methods for their simultaneous determination remain limited. In the present study, a capillary electrophoresis (CE) method with indirect UV detection was developed and validated for the simultaneous determination of AZA and SA in pharmaceutical and cosmetic preparations. Preliminary experiments demonstrated that direct UV detection was unsuitable because of the weak UV absorbance of AZA; therefore, indirect UV detection based on a sodium benzoate background electrolyte (BGE) was used. Following an initial one-factor-at-a-time (OFAT) screening, method optimization was performed using a face-centered central composite design (CCD) to evaluate the effects of BGE concentration, BGE pH, and separation voltage on the separation. The optimum separation was achieved using a 30 mM sodium benzoate BGE at pH 6.5 containing 5% (v/v) methanol, a separation voltage of +18 kV, a capillary temperature of 20 °C, and indirect UV detection at 230 nm. Baseline separation of both analytes was achieved within 5 min. The method was validated according to the ICH Q2(R2) guideline and demonstrated satisfactory accuracy, linearity, precision, selectivity, sensitivity, and robustness. The developed procedure was successfully applied to the analysis of commercial cosmetic formulations containing AZA, SA, or both active ingredients, providing assay results consistent with the declared contents. The proposed CE method provides a simple, rapid, cost-effective, and environmentally friendly alternative for the routine quality control of pharmaceutical and cosmetic formulations containing AZA and SA. Full article

► Show Figures

Figure 1

15 pages, 5385 KB

Open AccessReview

Bioactive Properties and Pharmaceutical Potential of New World Mistletoes of the Genus Tristerix: A Review

by Erick Poulsen-Silva, María Carolina Otero, Diego Verdugo-Igor, Gloria González, Sofía Díaz-Cornejo, Camila Fuentes, Maite Rodríguez-Díaz, Cristian Atala and Felipe Gordillo-Fuenzalida

Sci. Pharm. 2026, 94(3), 66; https://doi.org/10.3390/scipharm94030066 - 7 Aug 2026

Abstract

Mistletoes of the genus Tristerix, native to South America, represent a unique group of mostly hemiparasitic plants with potential medicinal applications. This review synthesizes existing knowledge on their biological and phytochemical properties, focusing on three main species endemic to Chile: Tristerix aphyllus [...] Read more.

Mistletoes of the genus Tristerix, native to South America, represent a unique group of mostly hemiparasitic plants with potential medicinal applications. This review synthesizes existing knowledge on their biological and phytochemical properties, focusing on three main species endemic to Chile: Tristerix aphyllus, T. corymbosus, and T. verticillatus. These species exhibit diverse interactions with host plants, animal pollinators, and seed dispersers, where host identity can influence their chemical profile. Around 17 metabolites have been found in flowers, fruits, and leaves from Tristerix spp., including flavonoids (e.g., quercetin, apigenin, luteolin), phenolic acids (e.g., caffeic acid; gallic acid), and alkaloids (e.g., pronuciferine and glaucine). Those have demonstrated antioxidant, anti-inflammatory, antimicrobial, and anti-tumoral properties. Despite their traditional uses in Chilean medicine for ailments such as gastric ulcers and throat infections, experimental research on Tristerix spp. remains scarce. This review highlights their bioactive potential, emphasizing the need for further investigation into their pharmacological applications, including in vivo and clinical studies. Full article

(This article belongs to the Topic Natural Products and Drug Discovery—2nd Edition)

► Show Figures

Graphical abstract

24 pages, 4956 KB

Open AccessArticle

Orotic Acid–1,2,4-Triazole Hybrids as Potential MMP-2,9 Modulating Wound-Healing Agents: Synthesis, Molecular Docking and Biological Evaluation

by Yuriy Karpenko, Volodymyr Parchenko, Lyudmila Kucherenko, Tetiana Chetvertak, Oleksii Bihdan, Iryna Pukhalska, Olena Roik, Daria Safronova, Ihor Meladze and Inna Bushueva

Sci. Pharm. 2026, 94(3), 65; https://doi.org/10.3390/scipharm94030065 - 5 Aug 2026

Abstract

The matrix metalloproteinases MMP-2 and MMP-9 are involved in extracellular matrix remodeling, inflammatory response, and tissue remodeling, and overactivity of certain metalloproteinases may also contribute to chronic wound healing. The aim of this work was to synthesize novel hybrid derivatives of orotic acid [...] Read more.

The matrix metalloproteinases MMP-2 and MMP-9 are involved in extracellular matrix remodeling, inflammatory response, and tissue remodeling, and overactivity of certain metalloproteinases may also contribute to chronic wound healing. The aim of this work was to synthesize novel hybrid derivatives of orotic acid and 1,2,4-triazole and investigate them as potential modulators of MMP-2/MMP-9. The structure of the compounds was confirmed by ¹H, ¹³C NMR spectroscopy, LC–MS, and elemental analysis. Pharmacokinetic properties were calculated using SwissADME, and enzyme interactions were characterized using molecular docking strategies, protein–ligand contact analysis, and 100 ns molecular dynamics. The inhibitory effect was also assessed in vitro by fluorimetry at a concentration of 10 μM. The compounds had an acceptable drug-like profile, without violations of Lipinski’s rule and PAINS warnings. The highest affinity for MMP-9 was also found for the three target proteins 17, 19 and 13, which showed values of −9.65, −9.47 and −9.17 kcal/mol, respectively, compared to −8.37 kcal/mol for NNGH. Dynamic molecular analysis confirmed the stability of the 13–MMP-9 complex. Compounds 17 and 13 inhibited MMP-9 by 94.2 ± 4.8% and 85.2 ± 3.8%, respectively, with little effect on MMP-2, whereas compound 19 showed balanced inhibition of MMP-2 and MMP-9 by 74.2 ± 4.4% and 79.2 ± 2.8%, respectively. The results identified 13 and 17 as potential compounds with preferential effects on MMP-9, and 19 as a possible dual inhibitor for wound healing activity studies. Full article

(This article belongs to the Special Issue Heterocyclic Chemistry in Drug Design 3.0)

► Show Figures

Figure 1

19 pages, 2127 KB

Open AccessArticle

Identifying and Evaluating Flavonoids as Potential Inhibitors of SARS-CoV-2 Main Protease (Mpro/3CL) Through Docking and Molecular Dynamics

by Getulio Flores-Tlalpa, Lenin Domínguez-Ramírez, Luis Márquez-Domínguez, Julio Reyes-Leyva, Paulina Cortés-Hernández, Fabiola Domínguez, Jesús Hernández, Irma Herrera-Camacho and Gerardo Santos-López

Sci. Pharm. 2026, 94(3), 64; https://doi.org/10.3390/scipharm94030064 - 31 Jul 2026

Abstract

Although the acute phase of the SARS-CoV-2 pandemic has subsided, the continued emergence of viral variants underscores the need for structurally diverse antiviral inhibitors. In this study, molecular docking followed by molecular dynamics (300 ns) simulations and binding free energy calculations using the [...] Read more.

Although the acute phase of the SARS-CoV-2 pandemic has subsided, the continued emergence of viral variants underscores the need for structurally diverse antiviral inhibitors. In this study, molecular docking followed by molecular dynamics (300 ns) simulations and binding free energy calculations using the Molecular Mechanics Poisson–Boltzmann Surface Area (MM-PBSA) method were employed to evaluate substituted flavonoids derived from Taraxacum officinale and Urtica dioica as potential inhibitors of the SARS-CoV-2 main protease (Mpro/3CLpro). Docking analysis identified several derivatives with favorable binding scores; however, dynamic refinement revealed differential stability among the ligand–protein complexes. Among the evaluated compounds, the luteolin derivative LND-17 showed the most consistent performance, exhibiting binding free energy estimates approaching those obtained for the reference inhibitors nirmatrelvir and ensitrelvir, sustained catalytic pocket occupancy, and energetic contributions involving the catalytic dyad (His41 and Cys145). Additional derivatives, including LNG-04, QND-07, and QNG-20, showed moderate stabilization but lower overall consistency. These findings highlight glycosylated flavonoids as promising scaffolds for future structure-based optimization and provide structural insights to guide experimental validation. Full article

► Show Figures

Figure 1

16 pages, 2013 KB

Open AccessArticle

Synthesis and Analgesic Activity of Cridanimod–Monoterpene Conjugates

by Danil D. Anikev, Anastasia Yu. Filippova, Olga I. Yarovaya, Serafim A. Tishchenko, Alla V. Pavlova, Alina A. Sonina, Kseniya S. Kovaleva, Mikhail V. Khvostov, Tatyana G. Tolstikova, Andrey Yu. Petrov and Nariman F. Salakhutdinov

Sci. Pharm. 2026, 94(3), 63; https://doi.org/10.3390/scipharm94030063 - 31 Jul 2026

Abstract

Cridanimod (acridoneacetic acid), the active ingredient of the immunomodulatory drug Cycloferon^®, has a well-characterized antiviral profile, but an unexplored analgesic potential. Bornane monoterpenes, notably (+)-camphor and (−)-fenchone, are established scaffolds for analgesic drug design. We therefore synthesized thirteen cridanimod–monoterpene conjugates—seven amides, [...] Read more.

Cridanimod (acridoneacetic acid), the active ingredient of the immunomodulatory drug Cycloferon^®, has a well-characterized antiviral profile, but an unexplored analgesic potential. Bornane monoterpenes, notably (+)-camphor and (−)-fenchone, are established scaffolds for analgesic drug design. We therefore synthesized thirteen cridanimod–monoterpene conjugates—seven amides, three acylhydrazones, and three esters—by EDCI/DMAP-mediated coupling or CDI/DBU-promoted esterification, and evaluated them in mice at an oral dose of 10.0 mg/kg in the acetic acid writhing and hot plate tests, with diclofenac sodium (10.0 mg/kg) as the reference. Acridoneacetic acid and Cycloferon^® were themselves inactive in both assays. By contrast, six of the thirteen conjugates were significantly active (p < 0.05) in at least one test, with distinct leads in each: amide 19 matched diclofenac in the writhing test (−63.7% vs. −64.4%), whereas acylhydrazone 23 exceeded diclofenac in the hot plate test (+43.9% vs. +25.7%). The divergent profiles suggest that different structural subclasses engage peripheral and central antinociceptive mechanisms. Conjugation thus converts an analgesically inactive immunomodulator into a substance yielding analgesics that match or exceed a standard NSAID at the same oral dose, providing a promising starting point for the development of new pain-relieving agents. Full article

(This article belongs to the Special Issue Pharmaceutical Applications of Heterocyclic Compounds)

► Show Figures

Figure 1

31 pages, 3169 KB

Open AccessReview

Potential Interactions of Active Compounds of Morinda citrifolia (Noni) on Targets Involved in Human Diseases

by Diana Rodríguez-Vera, Eunice D. Farfán-García, Elizabeth Estevez-Fregoso, Aldo A. Reséndiz-Albor, Ivonne Maciel Arciniega-Martínez, Eduardo Madrigal-Santillán, Jose A. Morales-González and Marvin A. Soriano-Ursúa

Sci. Pharm. 2026, 94(3), 62; https://doi.org/10.3390/scipharm94030062 - 20 Jul 2026

Cited by 1

Abstract

Morinda citrifolia (Noni) is well known as a plant with therapeutic potential and is also attractive to the food and cosmetic industries. Traditional medicine supports its use, mainly for the treatment of metabolic disorders and chronic inflammation but also for certain types of [...] Read more.

Morinda citrifolia (Noni) is well known as a plant with therapeutic potential and is also attractive to the food and cosmetic industries. Traditional medicine supports its use, mainly for the treatment of metabolic disorders and chronic inflammation but also for certain types of cancer. Noni has been the subject of considerable interest within the scientific community due to its purported health benefits. However, despite its growing popularity and extensive traditional use, significant gaps remain in the empirical understanding of its properties, mechanisms, and potential applications. To understand its biological activity, particular attention has been given to several chemical compounds present in its leaves and fruits, as they have been identified as bioactive agents. Moreover, several studies support the idea that specific flavonoids and anthraquinones from noni act on enzymes and transporters associated with glucose and lipid metabolism in humans. Its involvement in cardiovascular, neurological, metabolic, and inflammatory regulation across several high-burden diseases expands the potential medical applications of noni. This narrative review presents the current state of knowledge, highlighting preclinical studies that suggest the mechanisms of action underlying the observed effects, including theoretical approaches proposing specific interactions between noni compounds and proteins associated with human diseases as potential therapeutic targets. It also identifies areas where information remains insufficient and proposes future research directions for pharmacological applications, including the need for additional clinical studies and more comprehensive pharmacokinetic and toxicological evaluations. Full article

(This article belongs to the Topic Natural Products and Drug Discovery—2nd Edition)

► Show Figures

Figure 1

43 pages, 15500 KB

Open AccessReview

Natural Products in Modern Drug Discovery: Advances, Challenges and Emerging Technologies

by Sousana K. Papadopoulou, Efthymios Poulios, Fotis Tsopelas, Anna Tsantili-Kakoulidou and Constantinos Giaginis

Sci. Pharm. 2026, 94(3), 61; https://doi.org/10.3390/scipharm94030061 - 16 Jul 2026

Cited by 1

Abstract

Drug discovery is a complex and resource-intensive process, with lead identification representing a major bottleneck due to high attrition rates. Natural products have long served as a valuable source of structurally diverse and biologically active compounds, offering advantages such as evolutionary optimization, target [...] Read more.

Drug discovery is a complex and resource-intensive process, with lead identification representing a major bottleneck due to high attrition rates. Natural products have long served as a valuable source of structurally diverse and biologically active compounds, offering advantages such as evolutionary optimization, target specificity, and unique chemical diversity. This review provides a comprehensive and mechanistic overview of natural products as lead compounds, emphasizing their chemical characteristics, biological relevance, sources, mechanisms of action, and integration into modern drug discovery pipelines. A narrative review was conducted using major scientific databases (PubMed, Scopus, Web of Science, and Google Scholar), covering literature from 2000 to 2026. Relevant studies were selected based on scientific rigor and contribution to key themes, including natural product diversity, discovery strategies, and technological advancements. Natural products exhibit superior structural complexity and occupy unique chemical space compared to synthetic compounds, enabling effective interaction with diverse biological targets and supporting polypharmacological activity. Key sources include plants, microorganisms, and marine organisms, which have yielded numerous clinically important drugs. Advances in analytical techniques, genome mining, metabolomics, synthetic biology, and artificial intelligence have significantly improved discovery and optimization processes. Despite challenges related to complexity and scalability, natural products remain indispensable in drug discovery, with emerging technologies enhancing their potential for addressing unmet medical needs. Full article

► Show Figures

Figure 1

23 pages, 2858 KB

Open AccessArticle

Assessment of Anti-Influenza Activity of Pyrimidin-4(3H)-one Derivatives Using Prediction Models

by Yakov V. Gorokhov, Alexey D. Egorov, Nadezhda M. Andriyashina, Alexander N. Lobov, Irina S. Balashova, Aleksandrina S. Volobueva, Stanislav A. Grabovsky and Sophia S. Borisevich

Sci. Pharm. 2026, 94(3), 60; https://doi.org/10.3390/scipharm94030060 - 14 Jul 2026

Abstract

In this study, we used our own prediction models to assess the antiviral potential of pyrimidin-4(3H)-one derivatives against the A/H1N1 influenza virus strain. This assessment allows us to identify promising structures. The models are based on machine learning algorithms and molecular [...] Read more.

In this study, we used our own prediction models to assess the antiviral potential of pyrimidin-4(3H)-one derivatives against the A/H1N1 influenza virus strain. This assessment allows us to identify promising structures. The models are based on machine learning algorithms and molecular modeling results. In general, the prediction results are consistent with experimental data. The most promising compound, namely 12 (6-amino-2-(dimethylamino)pyrimidin-4(3H)-one), inhibits the reproduction of the A/Puerto Rico/8/34 (H1N1) influenza virus strain in vitro, likely by affecting the function of the endonuclease domain of the viral polymerase complex. Compound 12 can be used to create new PAN inhibitors by modifying its structure. Full article

(This article belongs to the Special Issue Computer-Aided Drug Design and Molecular Synthesis)

► Show Figures

Figure 1

27 pages, 987 KB

Open AccessReview

Analytical Strategies for the Determination of Dapagliflozin in Pharmaceutical and Biological Matrices: A Comprehensive Review

by Ecaterina Gliga, Denisa Gabriela Stroia, Gabriel Hancu and Eleonora Mircia

Sci. Pharm. 2026, 94(3), 59; https://doi.org/10.3390/scipharm94030059 - 14 Jul 2026

Abstract

Dapagliflozin (DAPA), a selective sodium–glucose cotransporter 2 inhibitor, is widely used in the management of type 2 diabetes mellitus, with additional indications in heart failure and chronic kidney disease. The growing analytical demand for DAPA determination in pharmaceutical formulations, fixed-dose combinations, and biological [...] Read more.

Dapagliflozin (DAPA), a selective sodium–glucose cotransporter 2 inhibitor, is widely used in the management of type 2 diabetes mellitus, with additional indications in heart failure and chronic kidney disease. The growing analytical demand for DAPA determination in pharmaceutical formulations, fixed-dose combinations, and biological matrices has stimulated the development of diverse analytical methods. This review provides a comprehensive evaluation of reported techniques for DAPA quantification in different matrices. Approaches discussed include chromatographic methods (TLC, RP-HPLC, UHPLC, LC-MS/MS), electromigration techniques (CE), and spectroscopic methods (UV–Vis, spectrofluorimetry). Emphasis is placed on key performance characteristics such as selectivity, sensitivity, linearity, robustness, and applicability to stability studies and bioanalysis. Recent trends, including the application of Quality by Design, green analytical chemistry principles, and advanced hyphenated techniques, are also addressed. While RP-HPLC remains widely used for routine quality control due to its robustness and accessibility, LC-MS/MS is generally regarded as the method of choice for trace-level bioanalysis owing to its superior sensitivity and selectivity. CE and spectroscopic techniques offer cost-effective and environmentally friendly alternatives, though with certain limitations. This review highlights current methodological gaps and outlines future directions for developing more sensitive and sustainable analytical strategies. Full article

► Show Figures

Figure 1

37 pages, 5844 KB

Open AccessReview

A Brief Review of Synthetic Strategies of α-Pyrone-Based Phloroglucinol Derivatives from Helichrysum spp. and Structure–Activity Insights

by Yulian Voynikov, Konstantin Konstantinov, Iliyan Ivanov and Stanimir Manolov

Sci. Pharm. 2026, 94(3), 58; https://doi.org/10.3390/scipharm94030058 - 13 Jul 2026

Abstract

This review summarizes the synthesis and structural modification of α-pyrone-containing phloroglucinol derivatives from Helichrysum species. Synthetic routes to both natural products and synthetic analogues are covered, highlighting strategies ranging from β-keto ester cyclodehydration to multicomponent condensations. Key methods include aldehyde-mediated dimerization, [...] Read more.

This review summarizes the synthesis and structural modification of α-pyrone-containing phloroglucinol derivatives from Helichrysum species. Synthetic routes to both natural products and synthetic analogues are covered, highlighting strategies ranging from β-keto ester cyclodehydration to multicomponent condensations. Key methods include aldehyde-mediated dimerization, fluoride-catalyzed heterodimerization, and acid-catalyzed cyclization to benzopyran frameworks. The reported approaches enabled access to diverse monopyrone, dipyrone, arzanol-type, and cyclized analogues. Additionally, retrosynthetic analyses toward phloroglucinol–pyrone heterodimers are discussed, highlighting convergent synthetic strategies for future access to benzofurane-, chromene-, and chromane-based analogues. This review integrates published experimental data with newly generated in silico predictions. Full article

► Show Figures

Figure 1

27 pages, 19520 KB

Open AccessArticle

Targeting PD-1/PD-L1-MAPK1 Signaling by a Novel Synergistic Combination of Rivastigmine and Epigallocatechin in Alzheimer’s Disease: An Integrated In Silico Approach

by Bhaswati Das and Marakanam Srinivasan Umashankar

Sci. Pharm. 2026, 94(3), 57; https://doi.org/10.3390/scipharm94030057 - 10 Jul 2026

Abstract

This study investigates the synergistic therapeutic potential of Rivastigmine (RVG) and Epigallocatechin (EGC) in Alzheimer’s disease (AD), a multifactorial neurodegenerative disorder characterized by neuroinflammation, oxidative stress, and dysregulated signaling pathways. Conventional therapies primarily provide symptomatic relief and target limited pathways, highlighting the need [...] Read more.

This study investigates the synergistic therapeutic potential of Rivastigmine (RVG) and Epigallocatechin (EGC) in Alzheimer’s disease (AD), a multifactorial neurodegenerative disorder characterized by neuroinflammation, oxidative stress, and dysregulated signaling pathways. Conventional therapies primarily provide symptomatic relief and target limited pathways, highlighting the need for multi-target strategies with improved efficacy and safety. An integrated in silico approach combining pharmacokinetic evaluation, network pharmacology, molecular docking, and molecular dynamics simulations is used to determine the synergistic potential of RVG and EGC. Pharmacokinetic analysis indicates favorable drug-likeness and acceptable ADME/Tox profiles for both compounds. Network pharmacology identified 146 overlapping targets associated with AD, highlighting key hub genes including NFKB1, MAPK1, STAT1, PRKACA, GRB2, LYN, and PTPN11, which are involved in neuroinflammation, synaptic signaling, and neuronal survival. Functional enrichment analysis indicated significant involvement of MAPK/ERK signaling and immune-regulatory pathways. Importantly, the PD-1/PD-L1 signaling pathway is identified as a novel mechanism connecting neuroimmune modulation with intracellular kinase-driven neurodegeneration. Molecular docking studies showed strong binding affinities of RVG and EGC toward key AD-related targets, particularly MAPK1, supported by stable hydrogen bonding and interaction profiles. Molecular dynamics simulations confirmed stable protein-ligand interactions, with EGC contributing structural stability and RVG exhibiting adaptive flexibility within the binding pocket. These results suggest that the RVG-EGC combination exhibits synergistic potential by simultaneously modulating neuroinflammatory, oxidative stress, and kinase-mediated signaling pathways. The integration of PD-1/PD-L1 and MAPK/ERK signaling provides a novel mechanistic pathway for multi-target therapeutic intervention in AD. Full article

(This article belongs to the Special Issue Computer-Aided Drug Design and Molecular Synthesis)

► Show Figures

Figure 1

18 pages, 2013 KB

Open AccessArticle

Pharmaceutical Development and Characteristics of Orally Disintegrating Tablets with Dihydroquercetin Formulation Modifications

by Roman P. Terekhov, Maria D. Korochkina, Elizaveta V. Krivozubova, Grigory Yu. Evzikov, Artem A. Svotin, Maria N. Anurova and Irina A. Selivanova

Sci. Pharm. 2026, 94(3), 56; https://doi.org/10.3390/scipharm94030056 - 9 Jul 2026

Abstract

Oral diseases cause a wide range of difficulties for patients. The natural bioactive compound dihydroquercetin (DHQ), which demonstrates regenerative, anti-inflammatory, antioxidative, and antibacterial effects, is of interest for their treatment. The combination of DHQ and l-lysine DHQ is “very easily soluble”. The [...] Read more.

Oral diseases cause a wide range of difficulties for patients. The natural bioactive compound dihydroquercetin (DHQ), which demonstrates regenerative, anti-inflammatory, antioxidative, and antibacterial effects, is of interest for their treatment. The combination of DHQ and l-lysine DHQ is “very easily soluble”. The aim of this study is to compare orally disintegrating tablets based on raw DHQ and on the DHQ-l-lysine composition. Following the guidelines outlined in the ICH Q8 (R2) standard, a fundamental quality target product profile and critical quality attributes were established. The Sediment Delivery Model (SeDeM) method was used to evaluate the substance suitability for direct compression. Quantitative analysis of the DHQ release was carried out by high-performance liquid chromatography, and infrared (IR) spectroscopy was performed using the attenuated total reflection technique without any prior sample preparation. The DHQ-l-lysine composition shows improved dimensions (4.12) and flowability (4.96). The release rate constants (K_release) were 8.14 and 3.61%/min, while the half-release periods (t_50%) were 6.14 and 13.85 min for tablets with DHQ (TF1) and DHQ-l-lysine compositions (TF2), respectively. The difference factor (f₁) and similarity factor (f₂) were 23.43% and 43.37%, respectively. The tablet manufacture had a critical impact on the characteristics of the IR spectra (the r values −0.8785 and 0.5474 for TF1 and TF2). The conducted study demonstrates the promise of using DHQ-l-lysine composition for developing effective dosage forms with improved technological characteristics and controlled release of the active substance. Full article

► Show Figures

Figure 1

30 pages, 11501 KB

Open AccessReview

Current Challenges and Approaches to the Development of Novel Drug Products for Otic Administration: A Narrative Review

by Elena O. Bakhrushina, Natalia N. Mikhailova, Anastasia N. Golub, Ksenia V. Eremeeva, Anna-Daniela Koynova, Anna A. Popova, Andrey B. Goryachev, Olga I. Stepanova, Ivan I. Krasnyuk, Jr. and Ivan I. Krasnyuk

Sci. Pharm. 2026, 94(3), 55; https://doi.org/10.3390/scipharm94030055 - 5 Jul 2026

Abstract

Acute otitis media is an inflammatory disease affecting all compartments of the middle ear, characterized by localized pain, fever, hearing impairment, and, occasionally, purulent exudate. It represents a significant clinical concern in both pediatric and adult populations, with approximately 709 million cases reported [...] Read more.

Acute otitis media is an inflammatory disease affecting all compartments of the middle ear, characterized by localized pain, fever, hearing impairment, and, occasionally, purulent exudate. It represents a significant clinical concern in both pediatric and adult populations, with approximately 709 million cases reported annually worldwide, 51% of which occur in children. However, currently available topical otic formulations are limited by their inability to achieve predictable therapeutic concentrations at the site of inflammation, resulting in reduced efficacy. In addition, the selection of appropriate active pharmaceutical ingredients (APIs) for drug products remains challenging; as a result, existing therapies do not comprehensively address all stages of pathogenesis. This study aimed to analyze existing locally acting formulations for middle ear drug delivery, evaluate their advantages and limitations, and assess modern approaches to the development of novel drug delivery systems and API combinations. A critical review of 69 publications (2010–2026) was conducted, supplemented by a strengths and limitations analysis of dosage forms and an evaluation of APIs based on clinical data. The findings highlight a lack of targeted drug delivery systems, limited efficacy of existing API combinations against bacterial biofilms, and their risk of ototoxicity. Emerging innovative drug delivery approaches, including microemulsions, vesicular systems, stimuli-responsive systems, and hydrogels, have demonstrated promising results in preclinical studies; however, their efficacy and safety remain to be confirmed in clinical settings before their full therapeutic potential in otitis media treatment can be realized. Full article

► Show Figures

Figure 1

Journal Description

Scientia Pharmaceutica

Latest Articles

Journal Menu

Journal Browser

Highly Accessed Articles

Latest Books

E-Mail Alert

News

Topics

Conferences

Special Issues

Further Information

Guidelines

MDPI Initiatives

Follow MDPI