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Pharmaceutics
Special Issues
Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems
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Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 15 December 2025 | Viewed by 1854

Special Issue Editors

Dr. Valeria Patricia Sülsen

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Guest Editor
1. Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina
2. Institute of Chemistry and Metabolism of Drugs (IQUIMEFA), University of Buenos Aires – National Scientific and Technical Research Council, Buenos Aires, Argentina
Interests: neglected diseases; antimicrobial activity; natural compounds; plant extracts; terpenoids; flavonoids; Asteraceae
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Maria Do Céu Costa

E-Mail Website
Guest Editor
1. CBIOS-Centro de Biociências/The Biosciences Research Center, ECTS-School of Health Sciences and Technologies, Lusófona University, Campo Grande, 376, 1749-024 Lisboa, Portugal
2. IPLUSO/NICiTeS-ERISA-Escola Superior de Saúde Ribeiro Sanches, Rua do Telhal aos Olivais, 8-8ª, 1900-693 Lisboa, Portugal
Interests: natural products chemistry; structure-activity relationships
Special Issues, Collections and Topics in MDPI journals
Dr. Jerónimo Ulloa

E-Mail Website
Guest Editor
1. Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Buenos Aires, Argentina
2. Institute of Chemistry and Metabolism of Drugs (IQUIMEFA), University of Buenos Aires—National Scientific and Technical Research Council, Buenos Aires, Argentina
Interests: neglected diseases; terpenoids; flavonoids; Asteraceae, medicinal plants, bioactive compounds
Dr. Juliana Marioni

E-Mail Website
Guest Editor
1. Department of Pharmaceutical Sciences, Faculty of Chemical Sciences, National University of Cordoba, Córdoba, Argentina
2. Pharmaceutical Technology Research and Development Unit (UNITEFA), National University of Cordoba—National Scientific and Technical Research Council, Córdoba, Argentina
Interests: natural products; antimicrobial activity; photodinamic therapy; nanocomposites

Special Issue Information

Dear Colleagues,

We are pleased to invite you to submit your work to this Special Issue of Pharmaceutics titled "Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems". This Special Issue will focus on the potential of natural products as antimicrobial agents and the development of innovative strategies for their delivery.

Natural products have long been a key source of compounds with antibacterial, antifungal, antiviral, and antiparasitic activity, offering promising therapeutic alternatives for infectious diseases. However, their clinical application is often limited by issues related to stability, bioavailability, and specificity, highlighting the need for advancements in drug delivery systems.

This Special Issue aims at gathering high-quality research and review articles on topics including, but not limited to, the following:

  • New sources of natural products with antimicrobial activity and their characterization with potential therapeutic applications in infectious diseases.
  • Development of advanced delivery systems, such as nanoformulations, lipid-based carriers, smart polymers, and other innovative approaches to enhance efficacy and safety.

Please note that studies solely focused on crude plant extracts, without identification of bioactive compounds, will not be considered for publication.

We look forward to your valuable contributions!

Dr. Valeria Patricia Sülsen
Prof. Dr. Maria Do Céu Costa
Dr. Jerónimo Ulloa
Dr. Juliana Marioni
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceutics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • antibacterial
  • antiparasitic
  • antifungal
  • antiviral
  • natural compounds
  • drug delivery

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (3 papers)

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Research

21 pages, 3291 KB  
Article
Modified Hevein-like Peptide from Amaranthus caudatus as a Promising Agent Against Pathogenic Candida Species
by Ekaterina I. Finkina, Anastasia A. Gerasimova, Olga V. Shevchenko, Ivan V. Bogdanov, Andrey A. Tagaev, Alexander D. Voropaev and Tatiana V. Ovchinnikova
Pharmaceutics 2025, 17(11), 1406; https://doi.org/10.3390/pharmaceutics17111406 - 30 Oct 2025
Viewed by 282
Abstract
Background/Objectives: Currently, infections caused by fungi of the Candida genus remain a significant global health concern. The rising incidence of mycoses, coupled with the rapid emergence of fungal resistance, highlights the urgent need to search for new antifungal agents. Here, we obtained the [...] Read more.
Background/Objectives: Currently, infections caused by fungi of the Candida genus remain a significant global health concern. The rising incidence of mycoses, coupled with the rapid emergence of fungal resistance, highlights the urgent need to search for new antifungal agents. Here, we obtained the recombinant hevein-like peptide from Amaranthus caudatus with two amino acid substitutions (F18W in the chitin-binding motif and M13A preventing the peptide from cleavage with cyanogen bromide during its biotechnological production). Methods: Antifungal potential of the modified hevein-like peptide, designated as mAc-AMP2, against susceptible and resistant strains of Candida albicans and non-albicans Candida species was studied. Results: We showed that mAc-AMP2 possessed anticandidal activities against all strains tested at nanomolar peptide concentrations. The presence of salts or serum affected the action of the peptide but its antifungal activity remained quite high. mAc-AMP2 exhibited anti-adherent properties and inhibited the formation of fungal biofilms. Using RP-HPLC, we demonstrated that degradation of the peptide in the presence of serum occurred rather slowly. mAc-AMP2 did not exhibit hemolytic and cytotoxic activities against the Caco-2 cell monolayer and peripheral blood mononuclear cells. Using flow cytometry, we demonstrated that the peptide at its high concentrations increased fungal membrane permeability. In resistance induction experiments, sensitivity of C. albicans toward mAc-AMP2 decreased over time, but restored after the peptide elimination. Conclusions: Taking into account all the data obtained, we suggest that the modified hevein-like peptide is a promising candidate for development of novel therapeutic agents to combat fungal infections caused by C. albicans and other Candida species. Full article
(This article belongs to the Special Issue Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems)
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13 pages, 2925 KB  
Article
Volatile Compounds as Upcoming Antigiardial Agents: In Vitro Action of Carvacrol, Thymol and p-Cymene on Giardia lamblia Trophozoites
by Marisa Machado, Ana Silva, Rui Linhares, Carlos Cavaleiro and Maria C. Sousa
Pharmaceutics 2025, 17(11), 1380; https://doi.org/10.3390/pharmaceutics17111380 - 24 Oct 2025
Viewed by 420
Abstract
Background/Objectives: Carvacrol and thymol are monoterpenes present in phenolic-rich essential oils extracted from aromatic plants that exhibit antimicrobial activity. This study evaluates the antiprotozoal effect of carvacrol, thymol and their precursor, p-Cymene, against Giardia lamblia and investigates their mechanism of action and cytotoxicity [...] Read more.
Background/Objectives: Carvacrol and thymol are monoterpenes present in phenolic-rich essential oils extracted from aromatic plants that exhibit antimicrobial activity. This study evaluates the antiprotozoal effect of carvacrol, thymol and their precursor, p-Cymene, against Giardia lamblia and investigates their mechanism of action and cytotoxicity profile. Methods: G. lamblia susceptibility, cell viability, swelling and adhesion abilities following application of carvacrol, thymol and p-Cymene were assessed. Ultrastructural changes were evaluated using electron microscopy. Cytotoxicity was determined in mammalian cell lines (murine macrophages RAW 264.7 and bovine aortic endothelial cells) exposed to the same IC50 concentrations effective against G. lamblia. Results: Carvacrol and thymol led to significant inhibition of G. lamblia trophozoite proliferation (IC50 ≅ 50 µg/mL). After 7 h of incubation, total cell number decreased by 30% (p < 0.01) with carvacrol and by 50% (p < 0.001) with thymol, accompanied by reduced motility and adhesion (<20% attached cells). At IC50 concentrations, G. lamblia trophozoites exposed to carvacrol and thymol underwent considerable ultrastructural alterations (e.g., aberrant-shaped cells, mitochondrial swelling and autophagosomal structures). Reduced trophozoite motility and adhesion capacity were also observed. In mammalian cells, thymol showed no significant cytotoxicity, whereas carvacrol significantly reduced viability in both cell lines. In contrast, p-Cymene showed no antigiardial activity. Conclusions: Our data suggests that carvacrol and thymol disrupt G. lamblia trophozoite integrity, possibly through alterations in membrane permeability and osmoregulatory processes. In conclusion, these compounds reveal in vitro antigiardial activity, supporting their potential as antigiardial drugs. Full article
(This article belongs to the Special Issue Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems)
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18 pages, 3383 KB  
Article
Selective Inhibition of Yersinia enterocolitica Type III Secretion by Lindera obtusiloba Extract and Cinnamtannin B1
by Jin-Hee Yoo and Tae-Jong Kim
Pharmaceutics 2025, 17(9), 1217; https://doi.org/10.3390/pharmaceutics17091217 - 18 Sep 2025
Viewed by 406
Abstract
Background/Objectives: Selective inhibition of bacterial virulence factors is a promising strategy to convert pathogenic bacteria into non-pathogenic commensals, circumventing the challenge of antibiotic resistance. This approach enables the host immune system to eliminate virulence-attenuated pathogens. Methods: In this study, we evaluated [...] Read more.
Background/Objectives: Selective inhibition of bacterial virulence factors is a promising strategy to convert pathogenic bacteria into non-pathogenic commensals, circumventing the challenge of antibiotic resistance. This approach enables the host immune system to eliminate virulence-attenuated pathogens. Methods: In this study, we evaluated the effects of Lindera obtusiloba Blume extract and cinnamtannin B1, the active component of the ethyl acetate fraction, on the type III secretion system (T3SS) of Yersinia enterocolitica. Results: The ethyl acetate fraction, at 100 mg/L, effectively suppressed all three T3SS components—the flagellar, Ysa, and Ysc T3SSs. Cinnamtannin B1, isolated from the ethyl acetate fraction through separation and identified through nuclear magnetic resonance spectrometer analysis, significantly inhibited flagellar and Ysa T3SS secretion, while selectively inhibiting expression of key effector proteins YopH and YopO in the Ysc T3SS. Additionally, cinnamtannin B1 reduced Y. enterocolitica-induced RAW 264.7 macrophage mortality and prevented poly (ADP-ribose) polymerase degradation, a marker of apoptosis. Conclusions: These findings suggest cinnamtannin B1 from L. obtusiloba as a selective T3SS-targeting compound with mechanistic potential for anti-virulence intervention. Further in vivo validation will be necessary to evaluate its therapeutic applicability. Full article
(This article belongs to the Special Issue Natural Products with Antimicrobial Activity and Their Pharmaceutical Delivery Systems)
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