Pharmaceutical Formulations with Antimicrobial Properties, 2nd Edition

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: 10 September 2024 | Viewed by 9039

Special Issue Editors


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Guest Editor
Department of Biomaterials, Faculty of Medical Dentistry, "Apollonia" University of Iasi, Pacurari Street, No. 11, 700511 Iasi, Romania
Interests: drug delivery; biomaterials; polymer nanoparticles; liposomes; hydrogels
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Guest Editor
“Cristofor Simionescu” Faculty of Chemical Engineering and Environment Protection, “Gheorghe Asachi” Technical University, Iasi, Romania
Interests: polysaccharide modification; bioactive polymers; biomaterials; hydrogels; interpenetrated networks; micro- and nanoparticles (spheres and capsules); hybrid and functionalized nanoparticles for drug targeting; drug delivery; polymer–drug conjugates
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Numerous studies on the systemic administration of antimicrobial drugs can be found in the literature. However, there are many challenges related to site-specific drug delivery, unwanted side effects and even potential toxicity. In order to address these, it is necessary to explore new approaches to the administration of active principles with antimicrobial properties. Therefore, in this Special Issue, we will focus on new delivery systems for antimicrobial applications, with a major emphasis on topical and targeted delivery. Examples of antimicrobial applications include wound healing; the prevention and treatment of periodontal diseases and tooth decay; and treatment of ear, skin, urinary tract, vaginal or respiratory infections. The systems used to release antimicrobial principles could take the form of gels, hydrogels, emulsions, micro- and nanoparticles (spheres, capsules, liposomes) or nanofibers.

Dr. Anca Niculina Cadinoiu
Prof. Dr. Marcel Popa
Guest Editors

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Keywords

  • drug delivery systems
  • antimicrobial properties
  • topical delivery
  • targeted delivery
  • hydrogels
  • nanoparticles
  • liposomes
  • emulsions
  • nanofibers

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Published Papers (5 papers)

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Research

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11 pages, 1020 KiB  
Article
Freeze-Drying of Encapsulated Bacteriophage T4 to Obtain Shelf-Stable Dry Preparations for Oral Application
by Paulina Śliwka, Grzegorz Skaradziński, Izabela Dusza, Aleksandra Grzywacz and Aneta Skaradzińska
Pharmaceutics 2023, 15(12), 2792; https://doi.org/10.3390/pharmaceutics15122792 - 17 Dec 2023
Cited by 1 | Viewed by 1011
Abstract
Therapeutic application of bacterial viruses (phage therapy) has in recent years been rediscovered by many scientists, as a method which may potentially replace conventional antibacterial strategies. However, one of the main problems related to phage application is the stability of bacterial viruses. Though [...] Read more.
Therapeutic application of bacterial viruses (phage therapy) has in recent years been rediscovered by many scientists, as a method which may potentially replace conventional antibacterial strategies. However, one of the main problems related to phage application is the stability of bacterial viruses. Though many techniques have been used to sustain phage activity, novel tools are needed to allow long-term phage storage and application in versatile forms. In this study, we combined two well-known methods for bacteriophage immobilization. First, encapsulated phages were obtained by means of extrusion–ionic gelation, and then alginate microspheres were dried using the lyophilization process (freeze-drying). To overcome the risk of phage instability upon dehydration, the microspheres were prepared with the addition of 0.3 M mannitol. Bacteriophage-loaded microspheres were stored at room temperature for 30 days and subsequently exposed to simulated gastric fluid (SGF). The survival of encapsulated phages after drying was significantly higher in the presence of mannitol. The highest number of viable bacteriophages exceeding 4.8 log10 pfu/mL in SGF were recovered from encapsulated and freeze-dried microspheres, while phages in lyophilized lysate were completely inactivated. Although the method requires optimization, it may be a promising approach for the immobilization of bacteriophages in terms of practical application. Full article
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17 pages, 6478 KiB  
Article
Enhancing the Functional Properties of Tea Tree Oil: In Vitro Antimicrobial Activity and Microencapsulation Strategy
by Franco Antonio Manzanelli, Soledad Ravetti, Sofia Gisella Brignone, Ariel Gustavo Garro, Sol Romina Martínez, Mariana Guadalupe Vallejo and Santiago Daniel Palma
Pharmaceutics 2023, 15(10), 2489; https://doi.org/10.3390/pharmaceutics15102489 - 19 Oct 2023
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Abstract
In the context of addressing antimicrobial drug resistance in periocular infections, Tea Tree Oil (TTO) has emerged as a promising therapeutic option. This study aimed to assess the efficacy of TTO against bacterial strains isolated from ocular infections, with a particular focus on [...] Read more.
In the context of addressing antimicrobial drug resistance in periocular infections, Tea Tree Oil (TTO) has emerged as a promising therapeutic option. This study aimed to assess the efficacy of TTO against bacterial strains isolated from ocular infections, with a particular focus on its ability to inhibit biofilm formation. Additionally, we designed and analyzed microcapsules containing TTO to overcome certain unfavorable physicochemical properties and enhance its inherent biological attributes. The quality of TTO was confirmed through rigorous analysis using GC-MS and UV-Vis techniques. Our agar diffusion assay demonstrated the effectiveness of Tea Tree Oil (TTO) against ocular bacterial strains, including Corynebacterium spp., coagulase-negative Staphylococcus spp., and Staphylococcus aureus, as well as a reference strain of Staphylococcus aureus (ATCC 25923). Notably, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) for all tested microorganisms were found to be 0.2% and 0.4%, respectively, with the exception of Corynebacterium spp., which exhibited resistance to TTO. Furthermore, TTO exhibited a substantial reduction in biofilm biomass, ranging from 30% to 70%, as determined by the MTT method. Through the spray-drying technique, we successfully prepared two TTO-containing formulations with high encapsulation yields (80–85%), microencapsulation efficiency (90–95%), and embedding rates (approximately 40%). These formulations yielded microcapsules with diameters of 6–12 μm, as determined by laser scattering particle size distribution analysis, and exhibited regular, spherical morphologies under scanning electron microscopy. Importantly, UV-Vis analysis post-encapsulation confirmed the presence of TTO within the capsules, with preserved antioxidant and antimicrobial activities. In summary, our findings underscore the substantial therapeutic potential of TTO and its microcapsules for treating ocular infections. Full article
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21 pages, 10286 KiB  
Article
Hybrid Materials with Antimicrobial Properties Based on Hyperbranched Polyaminopropylalkoxysiloxanes Embedded with Ag Nanoparticles
by Alexander Vasil’kov, Dmitry Migulin, Alexander Naumkin, Ilya Volkov, Ivan Butenko, Alexandre Golub, Vera Sadykova and Aziz Muzafarov
Pharmaceutics 2023, 15(3), 809; https://doi.org/10.3390/pharmaceutics15030809 - 02 Mar 2023
Cited by 3 | Viewed by 1405
Abstract
New hybrid materials based on Ag nanoparticles stabilized by a polyaminopropylalkoxysiloxane hyperbranched polymer matrix were prepared. The Ag nanoparticles were synthesized in 2-propanol by metal vapor synthesis (MVS) and incorporated into the polymer matrix using metal-containing organosol. MVS is based on the interaction [...] Read more.
New hybrid materials based on Ag nanoparticles stabilized by a polyaminopropylalkoxysiloxane hyperbranched polymer matrix were prepared. The Ag nanoparticles were synthesized in 2-propanol by metal vapor synthesis (MVS) and incorporated into the polymer matrix using metal-containing organosol. MVS is based on the interaction of extremely reactive atomic metals formed by evaporation in high vacuum (10−4–10−5 Torr) with organic substances during their co-condensation on the cooled walls of a reaction vessel. Polyaminopropylsiloxanes with hyperbranched molecular architectures were obtained in the process of heterofunctional polycondensation of the corresponding AB2-type monosodiumoxoorganodialkoxysilanes derived from the commercially available aminopropyltrialkoxysilanes. The nanocomposites were characterized using transmission (TEM) and scanning (SEM) electron microscopy, X-ray photoelectron spectroscopy (XPS), powder X-ray diffraction (PXRD) and Fourier-transform infrared spectroscopy (FTIR). TEM images show that Ag nanoparticles stabilized in the polymer matrix have an average size of 5.3 nm. In the Ag-containing composite, the metal nanoparticles have a “core-shell” structure, in which the “core” and “shell” represent the M0 and Mδ+ states, respectively. Nanocomposites based on silver nanoparticles stabilized with amine-containing polyorganosiloxane polymers showed antimicrobial activity against Bacillus subtilis and Escherichia coli. Full article
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19 pages, 3359 KiB  
Article
In Vitro and In Vivo Characterisation of a Mucoadhesive Buccal Film Loaded with Doxycycline Hyclate for Topical Application in Periodontitis
by Elena Dinte, Dana Maria Muntean, Vlad Andrei, Bianca Adina Boșca, Cristian Mircea Dudescu, Lucian Barbu-Tudoran, Gheorghe Borodi, Sanda Andrei, Adrian Florin Gal, Vasile Rus, Luciana-Mădălina Gherman, Oana Cadar, Reka Barabas, Mihaela Niculae and Aranka Ilea
Pharmaceutics 2023, 15(2), 580; https://doi.org/10.3390/pharmaceutics15020580 - 08 Feb 2023
Cited by 3 | Viewed by 2019
Abstract
Mucoadhesive films loaded with doxycycline hyclate (Doxy Hyc), consisting of mixtures of hydroxypropylmethyl cellulose (HPMC) E3, K4 and polyacrylic acid (Carbopol 940), were prepared by casting method, aiming to design a formulation intended for application in the oral cavity. The obtained film formulations [...] Read more.
Mucoadhesive films loaded with doxycycline hyclate (Doxy Hyc), consisting of mixtures of hydroxypropylmethyl cellulose (HPMC) E3, K4 and polyacrylic acid (Carbopol 940), were prepared by casting method, aiming to design a formulation intended for application in the oral cavity. The obtained film formulations exhibited a Doxy Hyc content between 7.52 ± 0.42 and 7.83 ± 0.41%, which had adequate mechanical properties for application in the oral cavity and pH values in the tolerance range. The x-ray diffraction studies highlighted the amorphisation of Doxy Hyc in the preparation process and the antibiotic particles present on the surface of the films, identified in the TEM images, which ensured a burst release effect in the first 15 min of the in vitro dissolution studies, after which Doxy Hyc was released by diffusion, the data presenting a good correlation with the Peppas model, n < 0.5. The formulation F1, consisting of HPMC K4 combined with C940 in a ratio of 5:3, the most performing in vitro, was tested in vivo in experimentally-induced periodontitis and demonstrated its effectiveness in improving the clinical parameters and reducing the salivary levels of matrix metalloproteinase-8 (MMP-8). The prepared Doxy Hyc loaded mucoadhesive buccal film could be used as an adjuvant for the local treatment of periodontitis, ensuring prolonged release of the antibiotic after topical application. Full article
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Review

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50 pages, 8523 KiB  
Review
Recent Progress and Trends in the Development of Electrospun and 3D Printed Polymeric-Based Materials to Overcome Antimicrobial Resistance (AMR)
by Pablo C. Caracciolo, Gustavo A. Abraham, Ernesto S. Battaglia and Silvestre Bongiovanni Abel
Pharmaceutics 2023, 15(7), 1964; https://doi.org/10.3390/pharmaceutics15071964 - 16 Jul 2023
Cited by 5 | Viewed by 2536
Abstract
Antimicrobial resistance (AMR) developed by microorganisms is considered one of the most critical public health issues worldwide. This problem is affecting the lives of millions of people and needs to be addressed promptly. Mainly, antibiotics are the substances that contribute to AMR in [...] Read more.
Antimicrobial resistance (AMR) developed by microorganisms is considered one of the most critical public health issues worldwide. This problem is affecting the lives of millions of people and needs to be addressed promptly. Mainly, antibiotics are the substances that contribute to AMR in various strains of bacteria and other microorganisms, leading to infectious diseases that cannot be effectively treated. To avoid the use of antibiotics and similar drugs, several approaches have gained attention in the fields of materials science and engineering as well as pharmaceutics over the past five years. Our focus lies on the design and manufacture of polymeric-based materials capable of incorporating antimicrobial agents excluding the aforementioned substances. In this sense, two of the emerging techniques for materials fabrication, namely, electrospinning and 3D printing, have gained significant attraction. In this article, we provide a summary of the most important findings that contribute to the development of antimicrobial systems using these technologies to incorporate various types of nanomaterials, organic molecules, or natural compounds with the required property. Furthermore, we discuss and consider the challenges that lie ahead in this research field for the coming years. Full article
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