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Pharmaceutics
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Recent Advances in Drug Discovery and Drug Delivery Systems for...
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Recent Advances in Drug Discovery and Drug Delivery Systems for Antimicrobial Therapy

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

Deadline for manuscript submissions: closed (31 July 2024) | Viewed by 8992

Special Issue Editors

Dr. João Augusto Oshiro Júnior

E-Mail Website
Guest Editor
Pharmaceutical Sciences Postgraduate Center for Biological and Health Sciences, State University of Paraíba, Av. Juvêncio Arruda, S/N, Campina Grande 58429-600, Paraíba, Brazil
Interests: drug delivery systems; hybrid materials; pharmaceutical technology; photodynamic therapy; drug discovery; antibacterial therapy
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Francisco Jaime Bezerra Mendonça Júnior

E-Mail Website
Guest Editor
Laboratory of Synthesis and Drug Delivery, State University of Paraíba, João Pessoa 58020-540, PB, Brazil
Interests: drug design; neglected diseases; antimicrobial; anti-cancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Given the growing issue of microbial resistance to conventional drugs, antimicrobial therapy has long been a crucial area of study. With the introduction of new antimicrobials, antimicrobial adjuvants, and better delivery methods in recent years, considerable breakthroughs have been made in antimicrobial therapy with regard to drug discovery and drug-delivery systems.

In this Special Issue, authors are invited to submit original research articles, reviews, and comments related to recent research in drug design and discovery, synthesis, and the pharmacological properties (in vitro and in vivo) of natural products and/or synthetic compounds that have the potential to become drug candidates for antimicrobial therapy. The issue will also present the development of inventive medication, delivery systems capable of improving the action and/or the pharmacokinetic and pharmacodynamic properties of drugs, drug candidates, and/or antibiotic adjuvants, with the aim of providing researchers with the most up-to-date information in this field.

Interest-related subjects include, but are not limited to:

  • Novel antibiotics, bacteriophages, and other antimicrobial compounds that have been discovered (i.e., by bioprospecting natural products) or developed (drug design and discovery, computational methods (ADMET, CADD, LBDD, SBDD, QSAR, and VS)) and are included in the category of novel antibacterial and adjuvant agents;
  • Drug-delivery systems: This category includes advancements in drug-delivery technology that can enhance the control over the spatial and temporal delivery of drugs at various scales, ranging from nano- and micro- to macro-sized scales, which improve the efficacy and specificity of antimicrobial;
  • Clinical trials including research on the safety and efficacy (in vitro and/or in vivo) of antimicrobial and adjuvant agents or drugs incorporated into delivery systems.

Dr. João Augusto Oshiro Júnior
Prof. Dr. Francisco Jaime Bezerra Mendonça Júnior
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 agents
  • antibiotics
  • antimicrobial
  • antibiotic adjuvants
  • drug discovery
  • drug delivery system
  • bioactive compunds
  • computer-aided drug design

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Published Papers (4 papers)

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Research

18 pages, 7065 KiB  
Article
The Efficacy of Hybrid Vaginal Ovules for Co-Delivery of Curcumin and Miconazole against Candida albicans
by Brenda Maria Silva Bezerra, Sara Efigênia Dantas de Mendonça y Araújo, José de Oliveira Alves-Júnior, Bolívar Ponciano Goulart de Lima Damasceno and João Augusto Oshiro-Junior
Pharmaceutics 2024, 16(3), 312; https://doi.org/10.3390/pharmaceutics16030312 - 23 Feb 2024
Cited by 3 | Viewed by 1990
Abstract
Curcumin (CUR) is a natural compound that can be combined with miconazole (MCZ) to improve vulvovaginal candidiasis (VVC) caused by Candida albicans treatment’s efficacy. This study aimed to develop ureasil–polyether (U-PEO) vaginal ovules loaded with CUR and MCZ for the treatment of VVC. [...] Read more.
Curcumin (CUR) is a natural compound that can be combined with miconazole (MCZ) to improve vulvovaginal candidiasis (VVC) caused by Candida albicans treatment’s efficacy. This study aimed to develop ureasil–polyether (U-PEO) vaginal ovules loaded with CUR and MCZ for the treatment of VVC. Physicochemical characterization was performed by thermogravimetry (TGA), differential thermal analysis (DTA), Fourier transform infrared spectroscopy (FTIR), and in vitro release. Antifungal assays were used to determine minimum inhibitory concentrations (MICs) and synergism between CUR and MCZ, and the activity of U-PEO ovules were performed by microdilution and agar diffusion. TGA results showed high thermal stability of the hybrid ovules. In DTA, the amorphous character of U-PEO and a possible interaction between CUR and MCZ were observed. FTIR showed no chemical incompatibility between the drugs. In vitro release resulted in 80% of CUR and 95% of MCZ released within 144 h. The MICs of CUR and MCZ were 256 and 2.5 µg/mL, respectively. After combining the drugs, the MIC of MCZ decreased four-fold to 0.625 µg/mL, while that of CUR decreased eight-fold to 32 µg/mL. Synergism was confirmed by the fractional inhibitory concentration index (FICI) equal to 0.375. U-PEO alone showed no antifungal activity. U-PEO/MCZ and U-PEO/CUR/MCZ ovules showed the greatest zones of inhibition (≥18 mm). The results highlight the potential of the ovules to be administered at a lower frequency and at reduced doses compared to available formulations. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery and Drug Delivery Systems for Antimicrobial Therapy)
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34 pages, 8740 KiB  
Article
Formulation and Comprehensive Evaluation of Biohybrid Hydrogel Membranes Containing Doxycycline or Silver Nanoparticles
by Diana Stan, Lavinia Liliana Ruta, Lorena-Andreea Bocancia-Mateescu, Andreea-Cristina Mirica, Dana Stan, Marin Micutz, Oana Brincoveanu, Ana-Maria Enciu, Elena Codrici, Ionela Daniela Popescu, Maria Linda Popa, Flaviana Rotaru and Cristiana Tanase
Pharmaceutics 2023, 15(12), 2696; https://doi.org/10.3390/pharmaceutics15122696 - 28 Nov 2023
Cited by 1 | Viewed by 2213
Abstract
Complicated wounds often require specialized medical treatments, and hydrogels have emerged as a popular choice for wound dressings in such cases due to their unique properties and the ability to incorporate and release therapeutic agents. Our focus was to develop and characterize a [...] Read more.
Complicated wounds often require specialized medical treatments, and hydrogels have emerged as a popular choice for wound dressings in such cases due to their unique properties and the ability to incorporate and release therapeutic agents. Our focus was to develop and characterize a new optimized formula for biohybrid hydrogel membranes, which combine natural and synthetic polymers, bioactive natural compounds, like collagen and hyaluronic acid, and pharmacologically active substances (doxycycline or npAg). Dynamic (oscillatory) rheometry confirmed the strong gel-like properties of the obtained hydrogel membranes. Samples containing low-dose DOXY showed a swelling index of 285.68 ± 6.99%, a degradation rate of 71.6 ± 0.91% at 20 h, and achieved a cumulative drug release of approximately 90% at pH 7.4 and 80% at pH 8.3 within 12 h. The addition of npAg influenced the physical properties of the hydrogel membranes. Furthermore, the samples containing DOXY demonstrated exceptional antimicrobial efficacy against seven selected bacterial strains commonly associated with wound infections and complications. Biocompatibility assessments revealed that the samples exhibited over 80% cell viability. However, the addition of smaller-sized nanoparticles led to decreased cellular viability. The obtained biohybrid hydrogel membranes show favorable properties that render them suitable for application as wound dressings. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery and Drug Delivery Systems for Antimicrobial Therapy)
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14 pages, 3698 KiB  
Article
Immobilization of Papain in Chitosan Membranes as a Potential Alternative for Skin Wounds
by Anne Emmanuelle Câmara da Silva Melo, Felipe Sanderson Ribeiro de Sousa, Alaine M. dos Santos-Silva, Ednaldo Gomes do Nascimento, Matheus F. Fernandes-Pedrosa, Caroline Addison Carvalho Xavier de Medeiros and Arnóbio Antônio da Silva-Junior
Pharmaceutics 2023, 15(12), 2649; https://doi.org/10.3390/pharmaceutics15122649 - 21 Nov 2023
Cited by 4 | Viewed by 1783
Abstract
Papain (an enzyme from the latex of Carica papaya) is an interesting natural bioactive macromolecule used as therapeutic alternative for wound healing due to debridement action in devitalized or necrotic tissues. However, its use in high doses can induce potential skin irritation [...] Read more.
Papain (an enzyme from the latex of Carica papaya) is an interesting natural bioactive macromolecule used as therapeutic alternative for wound healing due to debridement action in devitalized or necrotic tissues. However, its use in high doses can induce potential skin irritation and side effects. In this study, experiments explored the ability of chitosan membrane to immobilize papain, consequently improving enzymatic activity and controlling enzyme release. Papain-loading capacity was tested via experiments of force microscopy (AFM), scanning electron microscopy (SEM-FEG), and X-ray diffraction analyses. Fourier transform infrared spectroscopy and thermal analyses assessed the enzyme interactions with the copolymer. The investigation of the feasibility of membranes included pH on the surface, elasticity, and breaking strength measurements. The surface wettability and swelling capacity of different formulations revealed the best formulation for in vitro papain release experiments. The membranes had a transparent, rough, crystalline characteristic, which was homogeneous with the membrane within the neutrality. The immobilization of papain in the chitosan membrane resulted in a decrease in the vibration band characteristic of pure papain, suggesting a displacement in the vibration bands in the FTIR spectrum. The presence of papain decreased hydrophobicity on the surface of the membrane and disturbed the membrane’s ability to swell. Chitosan membranes containing papain 2.5% (0.04 g) and 5.0% (0.08 g) preserved feasible properties and improved the enzymatic activity compared (0.87 ± 0.12 AU/mg and 1.59 ± 0.10 AU/mg) with a free papain sample (0.0042 ± 0.001 AU/mg). Concentrations of over 10% (0.16 g) led to phase separation into membranes. Chitosan membranes exhibited a slow papain release behavior adjusted via the Higushi model. The experimental achievements suggest a novel and promising method for the enhancement of papain. The results indicate the potential for prolonged bioactivity for use on wounds. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery and Drug Delivery Systems for Antimicrobial Therapy)
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17 pages, 12889 KiB  
Article
Triose Phosphate Isomerase Structure-Based Virtual Screening and In Vitro Biological Activity of Natural Products as Leishmania mexicana Inhibitors
by Luis D. González-Morales, Adriana Moreno-Rodríguez, Lenci K. Vázquez-Jiménez, Timoteo Delgado-Maldonado, Alfredo Juárez-Saldivar, Eyra Ortiz-Pérez, Alma D. Paz-Gonzalez, Edgar E. Lara-Ramírez, Lilian Yépez-Mulia, Patricia Meza and Gildardo Rivera
Pharmaceutics 2023, 15(8), 2046; https://doi.org/10.3390/pharmaceutics15082046 - 29 Jul 2023
Cited by 4 | Viewed by 1973
Abstract
Cutaneous leishmaniasis (CL) is a public health problem affecting more than 98 countries worldwide. No vaccine is available to prevent the disease, and available medical treatments cause serious side effects. Additionally, treatment failure and parasite resistance have made the development of new drugs [...] Read more.
Cutaneous leishmaniasis (CL) is a public health problem affecting more than 98 countries worldwide. No vaccine is available to prevent the disease, and available medical treatments cause serious side effects. Additionally, treatment failure and parasite resistance have made the development of new drugs against CL necessary. In this work, a virtual screening of natural products from the BIOFACQUIM and Selleckchem databases was performed using the method of molecular docking at the triosephosphate isomerase (TIM) enzyme interface of Leishmania mexicana (L. mexicana). Finally, the in vitro leishmanicidal activity of selected compounds against two strains of L. mexicana, their cytotoxicity, and selectivity index were determined. The top ten compounds were obtained based on the docking results. Four were selected for further in silico analysis. The ADME-Tox analysis of the selected compounds predicted favorable physicochemical and toxicological properties. Among these four compounds, S-8 (IC50 = 55 µM) demonstrated a two-fold higher activity against the promastigote of both L. mexicana strains than the reference drug glucantime (IC50 = 133 µM). This finding encourages the screening of natural products as new anti-leishmania agents. Full article
(This article belongs to the Special Issue Recent Advances in Drug Discovery and Drug Delivery Systems for Antimicrobial Therapy)
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