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Pharmaceutics
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Natural Products for Antimicrobial and Drug Delivery: A Look into...
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Natural Products for Antimicrobial and Drug Delivery: A Look into the Future

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

Deadline for manuscript submissions: closed (10 April 2025) | Viewed by 8136

Special Issue Editor

Dr. Hélcio Silva Dos Santos

E-Mail Website
Guest Editor
Center for Exact Sciences and Technology—Chemistry Course, Vale do Acaraú University, Sobral, CE, Brazil
Interests: chalcones; natural products; antimicrobial activity; zebrafish; anxiolytic activity; spectroscopy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Resistance is a natural process of microorganisms; however, it has been intensified in recent years due to the excessive and incorrect use of antibiotics and antifungals. This, in turn, has caused the development of resistance factors, such as changes in places where antibiotics and antifungals act, membrane permeability, active pumping of antibiotics and antifungals out of the microorganisms and the production of enzymes that degrade antibiotics and antifungals.

Throughout our evolution, natural products have been of utmost significance in  producing antimicrobial agents. Additionally, emerging biodegradable and non-degradable polymer systems provide a novel avenue for the incorporation and release of active natural products. A controlled drug release system helps to keep the profile of drug concentration constant within the therapeutic range and avoids adverse side effects.

This Special Issue aims to collate papers that address the importance of natural products and drug delivery systems in combating microbial infections. Potential topics include, but is not limited to, the following: natural compounds; antimicrobial agents; drug delivery systems; essential oils; and mechanisms of action. We welcome submissions of both original research articles and review.

We look forward to receiving your contributions.

Dr. Hélcio Silva Dos Santos
Guest Editor

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

  • natural products
  • microbial infections
  • drug delivery systems
  • essential oils
  • mechanism of action

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Published Papers (5 papers)

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Research

29 pages, 11382 KiB  
Article
The Incorporation of CBD into Biodegradable DL-Lactide/Glycolide Copolymers Creates a Persistent Antibacterial Environment: An In Vitro Study on Streptococcus mutans and Staphylococcus aureus
by Ronit Vogt Sionov, Ahmad Siag, Emma Theresa Mersini, Natalya M. Kogan, Tatiana Alkhazov, Igor Koman, Praveen Rowlo, Vitaly Gutkin, Menachem Gross and Doron Steinberg
Pharmaceutics 2025, 17(4), 463; https://doi.org/10.3390/pharmaceutics17040463 - 2 Apr 2025
Viewed by 386
Abstract
Background: Cannabidiol (CBD) is a natural compound from the Cannabis sativa L. plant, which has anti-inflammatory, anti-nociceptive, neuroprotective, and antibacterial activities. Objective: The aim of this study was to develop a sustained-release device of CBD that can provide an antibacterial effect [...] Read more.
Background: Cannabidiol (CBD) is a natural compound from the Cannabis sativa L. plant, which has anti-inflammatory, anti-nociceptive, neuroprotective, and antibacterial activities. Objective: The aim of this study was to develop a sustained-release device of CBD that can provide an antibacterial effect against the Gram-positive bacteria Streptococcus mutans and Staphylococcus aureus for extended periods of time. Methods: CBD was incorporated into the biodegradable PURASORB 5010 or PURASORB 7510 DL-lactide/glycolide polymers using either dimethylsulfoxide (DMSO) or acetone as the solvent, and the dried polymer scaffolds were exposed daily to a fresh culture of bacteria. The bacterial growth was determined daily by optical density, and the metabolic activity of biofilms was determined using the MTT assay. Biofilm formation on the polymer scaffolds was visualized by HR-SEM. Its anti-inflammatory effect was determined by measuring the IL-6 release from LPS-stimulated RAW 264.7 macrophages by ELISA. Cell cytotoxicity on normal Vero epithelial cells was determined by the MTT assay. The daily release of CBD was determined by gas chromatography–mass spectrometry (GC-MS). Results: PURASORB 5010/CBD scaffolds had antibacterial activity against S. mutans UA159, S. aureus ATCC25923, and a clinical isolate of a multidrug-resistant S. aureus (MDRSA CI-M) strain for the tested period of up to 17 days. PURASORB 7510/CBD scaffolds also had antibacterial activity, but overall, it was less effective than PURASORB 5010/CBD over time. The addition of PEG400 to the copolymers significantly increased the antibacterial activity of PURASORB 7510/CBD but not of PURASORB 5010/CBD. The daily release of CBD from the polymer scaffolds was sufficient to reduce the LPS-induced IL-6 secretion from RAW 264.7 macrophages, and importantly, it was not cytotoxic to either RAW 264.7 macrophages or Vero epithelial cells. The daily release of CBD was found to be between 1.12 and 9.43 µg/mL, which is far below the cytotoxic dose of 25 µg/mL. Conclusions: The incorporation of CBD into the biodegradable PURASORB 5010 can be used to prepare sustained-release devices for medical purposes where combined antibacterial and anti-inflammatory activities are desirable. Full article
(This article belongs to the Special Issue Natural Products for Antimicrobial and Drug Delivery: A Look into the Future)
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17 pages, 5675 KiB  
Article
Antibacterial and Inhibitory Activity of Nora and Mepa Efflux Pumps of Estragole Complexed to β-Cyclodextrin (ES/β-CD) In Vitro Against Staphylococcus aureus Bacteria, Molecular Docking and MPO-Based Pharmacokinetics Prediction
by Roger Henrique Sousa da Costa, Renata Torres Pessoa, Eduardo dos Santos Silva, Isaac Moura Araujo, Sheila Alves Gonçalves, Janaína Esmeraldo Rocha, Francisco Nascimento Pereira Junior, Naiara Cipriano Oliveira, Victor Moreira de Oliveira, Matheus Nunes da Rocha, Emmanuel Silva Marinho, Natália Kelly Gomes de Carvalho, José Galberto Martins da Costa, Hélcio Silva dos Santos and Irwin Rose Alencar de Menezes
Pharmaceutics 2024, 16(11), 1469; https://doi.org/10.3390/pharmaceutics16111469 - 18 Nov 2024
Cited by 1 | Viewed by 1249
Abstract
Background/Objectives: The work investigates the effect of the estragole complex encapsulated in beta-cyclodextrin (ES/β-CD) in modulating bacterial resistance, specifically in Staphylococcus aureus strains expressing NorA and MepA efflux pumps. Efflux pumps are mechanisms that bacteria use to resist antibiotics by expelling them from [...] Read more.
Background/Objectives: The work investigates the effect of the estragole complex encapsulated in beta-cyclodextrin (ES/β-CD) in modulating bacterial resistance, specifically in Staphylococcus aureus strains expressing NorA and MepA efflux pumps. Efflux pumps are mechanisms that bacteria use to resist antibiotics by expelling them from the cell. Methodology: Several compounds and antibiotics, such as ciprofloxacin and norfloxacin, were used to evaluate the antimicrobial activity and the ability of the ES/β-CD complex to reverse resistance. Methods: The study included scanning electron microscopy assays, minimum inhibitory concentration (MIC) determination, and efflux pump inhibition tests. Results: The ES/β-CD complex did not show significant direct antibacterial activity. However, it modulated the action of norfloxacin, decreasing the MIC when combined with this antibiotic in the 1199B (NorA) strain. These results suggest a potential for synergy but not a direct inhibition of efflux pumps. Conclusion: ES/β-CD can potentiate the efficacy of some antibiotics but does not directly act as an efflux pump inhibitor; it is more of an antibiotic potentiator than a direct solution to bacterial resistance. The molecular docking simulation data suggest its high affinity for forming the ES/β-CD complex. The pharmacokinetic predictions based on MPO suggest that the compound has moderate lipophilicity, highly effective cellular permeability, and low incidence of organic toxicity, pointing to a promising pharmacological principle with controlled daily oral dosing. Conclusions: These results indicate this complex’s possible and relevant association as an adjuvant in antibiotic therapy to reduce multidrug-resistant bacteria; however, new in vivo assays are necessary to confirm this effect. Full article
(This article belongs to the Special Issue Natural Products for Antimicrobial and Drug Delivery: A Look into the Future)
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18 pages, 335 KiB  
Article
Antimicrobial Activities of Essential Oils of Different Pinus Species from Bosnia and Herzegovina
by Snježana Mirković, Vanja Tadić, Marina T. Milenković, Dušan Ušjak, Gordana Racić, Dragica Bojović and Ana Žugić
Pharmaceutics 2024, 16(10), 1331; https://doi.org/10.3390/pharmaceutics16101331 - 15 Oct 2024
Cited by 2 | Viewed by 1998
Abstract
Background/Objectives: The emergence of antimicrobial resistance has urged researchers to explore new antimicrobial agents, such as essential oils (EOs). The aim of this study was to examine chemical composition and antimicrobial activity of the EOs from the needles and green cones of four [...] Read more.
Background/Objectives: The emergence of antimicrobial resistance has urged researchers to explore new antimicrobial agents, such as essential oils (EOs). The aim of this study was to examine chemical composition and antimicrobial activity of the EOs from the needles and green cones of four Pinus species (Pinus mugo Turra., P. nigra J.F., P. syilvestris L., and P. halepensis Miller) from Bosnia and Herzegovina. Methods: Chemical profiles of EOs were assessed by gas chromatography, while microdilution method was used to test their antimicrobial activity. A synergistic action of EOs and gentamicin was investigated by the checkerboard assay. Results: The chemical composition of the tested EOs showed a high percentage of α-pinene, (E)-caryophyllene, limonene, germacrene D, myrcene, and δ-3-carene. EO from green cones of P. sylvestris showed high efficiency against S. aureus and E. faecalis. The MIC of P. nigra cones’ EO was 100 μg/mL against E. coli. The EO of P. halepensis green cones demonstrated the strongest activity against E. faecalis. EOs of P. halepensis needles and green cones exhibited the highest activity against C. albicans. Further, synergistic interaction was detected in combination of the selected EOs/gentamicin toward S. aureus and K. pneumoniae. Conclusions: Among the tested EOs, oils of P. sylvestris cones and P. halepensis cones and needles showed the greatest antimicrobial activity. The same EOs and EO from P. nigra cones displayed synergistic potential in combination with gentamicin, supporting their utilization as antimicrobial agents alone or in combination with antibiotics, which is in line with their ethnopharmacological usage and circular bioeconomy principles. Full article
(This article belongs to the Special Issue Natural Products for Antimicrobial and Drug Delivery: A Look into the Future)
26 pages, 4477 KiB  
Article
Encapsulation of Phloroglucinol from Rosenvingea intricata Macroalgae with Zinc Oxide Nanoparticles against A549 Lung Cancer Cells
by Sakthivel Muthu, Mythileeswari Lakshmikanthan, Edwin Edward-Sam, Mutheeswaran Subramanian, Lakshmanan Govindan, Afrina Begum Mithen Patcha, Kathiravan Krishnan, Nallusamy Duraisamy, Selvakumari Jeyaperumal and Al Thabiani Aziz
Pharmaceutics 2024, 16(10), 1300; https://doi.org/10.3390/pharmaceutics16101300 - 5 Oct 2024
Cited by 1 | Viewed by 1751
Abstract
Background/Objectives: Phloroglucinol (PHL), a phenolic compound extracted from the brown alga Rosenvingea intricata, exhibits potent antioxidant and anticancer properties. This study aims to extract, purify, and characterize PHL, and further develop functionalized zinc oxide nanoparticles (ZnO NPs) loaded with PHL to enhance its [...] Read more.
Background/Objectives: Phloroglucinol (PHL), a phenolic compound extracted from the brown alga Rosenvingea intricata, exhibits potent antioxidant and anticancer properties. This study aims to extract, purify, and characterize PHL, and further develop functionalized zinc oxide nanoparticles (ZnO NPs) loaded with PHL to enhance its therapeutic potential. Methods: PHL was extracted using acetone and purified through Sephadex LH-20 column chromatography, yielding a highly enriched fraction (F-3). The purified compound was characterized by FTIR, HPLC, NMR, and LC-MS. ZnO NPs were synthesized, PEGylated, and conjugated with PHL, forming ZnO-PEG-PHL NPs. Their characterization included DLS, zeta potential, XRD, SEM-EDAX, and encapsulation efficiency studies. Antioxidant assays (DPPH, FRAP, ABTS, RPA) were performed and in vitro cytotoxicity on A549 lung cancer cells were determined to evaluate the therapeutic efficacy of PHL. Results: The purified PHL fraction showed a high phenolic content (45.65 PHL mg/g), which was was confirmed by spectral analysis. The ZnO-PEG-PHL NPs increased in size from 32.36 nm to 46.68 nm, with their zeta potential shifting from −37.87 mV to −26.82 mV. The antioxidant activity was superior for the ZnO-PEG-PHL NPs in all assays, while the in vitro cytotoxicity tests showed an IC50 of 40 µg/mL compared to 60 µg/mL for the ZnO NPs and 70 µg/mL for PHL. Apoptotic studies revealed significant cell cycle arrest and apoptosis induction. Conclusions: The synthesized ZnO-PEG-PHL NPs demonstrated enhanced antioxidant and anticancer properties, making them promising candidates for cancer therapy and antioxidant applications. Full article
(This article belongs to the Special Issue Natural Products for Antimicrobial and Drug Delivery: A Look into the Future)
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26 pages, 5947 KiB  
Article
Lentisk (Pistacia lentiscus) Oil Nanoemulsions Loaded with Levofloxacin: Phytochemical Profiles and Antibiofilm Activity against Staphylococcus spp.
by Linda Maurizi, Alba Lasalvia, Maria Gioia Fabiano, Eleonora D’Intino, Francesca Del Cioppo, Caterina Fraschetti, Antonello Filippi, Maria Grazia Ammendolia, Antonietta Lucia Conte, Jacopo Forte, Davide Corinti, Maria Elisa Crestoni, Maria Carafa, Carlotta Marianecci, Federica Rinaldi and Catia Longhi
Pharmaceutics 2024, 16(7), 927; https://doi.org/10.3390/pharmaceutics16070927 - 11 Jul 2024
Cited by 5 | Viewed by 1759
Abstract
Most clinical isolates of both Staphylococcus aureus and Staphylococcus epidermidis show the capacity to adhere to abiotic surfaces and to develop biofilms resulting in a contribution to chronic human skin infections. Antibiotic resistance and poor biofilm penetration are the main causes of ineffective therapeutic treatment [...] Read more.
Most clinical isolates of both Staphylococcus aureus and Staphylococcus epidermidis show the capacity to adhere to abiotic surfaces and to develop biofilms resulting in a contribution to chronic human skin infections. Antibiotic resistance and poor biofilm penetration are the main causes of ineffective therapeutic treatment in killing bacteria within biofilms. A possible strategy could be represented by drug delivery systems, such as nanoemulsions (composed of bioactive oil, surfactant and water phase), which are useful for enhancing the drug permeation of a loaded drug inside the biofilm and its activity. Phytochemical characterization of Pistacia lentiscus oil (LO) by direct infusion Fourier-transform ion cyclotron resonance mass spectrometry (FT-ICR MS) allowed the identification of bioactive compounds with antimicrobial properties, including fatty acids and phenolic compounds. Several monoterpenes and sesquiterpenes have been also detected and confirmed by gas chromatography–mass spectrometric (GC-MS) analysis, together providing a complete metabolomic profiling of LO. In the present study, a nanoemulsion composed of LO has been employed for improving Levofloxacin water solubility. A deep physical–chemical characterization of the nanoemulsion including hydrodynamic diameter, ζ-potential, morphology, entrapment efficiency, stability release and permeation studies was performed. Additionally, the antimicrobial/antibiofilm activity of these preparations was evaluated against reference and clinical Staphylococcus spp. strains. In comparison to the free-form antibiotic, the loaded NE nanocarriers exhibited enhanced antimicrobial activity against the sessile forms of Staphylococcus spp. strains. Full article
(This article belongs to the Special Issue Natural Products for Antimicrobial and Drug Delivery: A Look into the Future)
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