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Pharmaceutics
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Pharmaceutical Formulations with Antimicrobial Properties
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Pharmaceutical Formulations with Antimicrobial Properties

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

Deadline for manuscript submissions: closed (10 December 2021) | Viewed by 49347

Special Issue Editors

Prof. Dr. Marcel Popa

E-Mail Website
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
Dr. Anca Niculina Cadinoiu

E-Mail Website
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
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 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.

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

Manuscript Submission Information

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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 (14 papers)

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Editorial

Jump to: Research, Review

4 pages, 200 KiB  
Editorial
Editorial on Special Issue “Pharmaceutical Formulations with Antimicrobial Properties”
by Anca N. Cadinoiu and Marcel Popa
Pharmaceutics 2023, 15(1), 137; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics15010137 - 30 Dec 2022
Viewed by 804
Abstract
Even though numerous studies on the systemic administration of antimicrobial drugs can be found in the literature, they still have many shortcomings related to the site-specific drug delivery, unwanted side effects and even potential toxicity [...] Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)

Research

Jump to: Editorial, Review

19 pages, 7498 KiB  
Article
Implant Surfaces Containing Bioglasses and Ciprofloxacin as Platforms for Bone Repair and Improved Resistance to Microbial Colonization
by Irina Negut, Carmen Ristoscu, Tatiana Tozar, Mihaela Dinu, Anca Constantina Parau, Valentina Grumezescu, Claudiu Hapenciuc, Marcela Popa, Miruna Silvia Stan, Luminita Marutescu, Ion N. Mihailescu and Mariana Carmen Chifiriuc
Pharmaceutics 2022, 14(6), 1175; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14061175 - 30 May 2022
Cited by 6 | Viewed by 2027
Abstract
Coatings are an attractive and challenging selection for improving the bioperformance of metallic devices. Composite materials based on bioglass/antibiotic/polymer are herein proposed as multifunctional thin films for hard tissue implants. We deposited a thin layer of the polymeric material by matrix-assisted pulsed laser [...] Read more.
Coatings are an attractive and challenging selection for improving the bioperformance of metallic devices. Composite materials based on bioglass/antibiotic/polymer are herein proposed as multifunctional thin films for hard tissue implants. We deposited a thin layer of the polymeric material by matrix-assisted pulsed laser evaporation—MAPLE onto Ti substrates. A second layer consisting of bioglass + antibiotic was applied by MAPLE onto the initial thin film. The antimicrobial activity of MAPLE-deposited thin films was evaluated on Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, and Pseudomonas aeruginosa standard strains. The biocompatibility of obtained thin films was assessed on mouse osteoblast-like cells. The results of our study revealed that the laser-deposited coatings are biocompatible and resistant to microbial colonization and biofilm formation. Accordingly, they can be considered viable candidates for biomedical devices and contact surfaces that would otherwise be amenable to contact transmission. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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18 pages, 7377 KiB  
Article
Preparation of Ligand Brush Nanocapsules for Robust Self-Controlled Antimicrobial Activity with Low Cytotoxicity at Target pH and Humidity
by Eunjoo Koh and Yong Taek Lee
Pharmaceutics 2022, 14(2), 280; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14020280 - 25 Jan 2022
Cited by 2 | Viewed by 1859
Abstract
This study prepared nanocapsules (NCs) with excellent self-controlled antimicrobial activity at pH 6–7 and humidity 45–100%, conditions in which most bacterial and fungal strains thrive. The nanocapsule substrate (NC@SiO2) was 676 nm in diameter, and the ligand-grafted capsule (NC@SiO2-g-MAA) [...] Read more.
This study prepared nanocapsules (NCs) with excellent self-controlled antimicrobial activity at pH 6–7 and humidity 45–100%, conditions in which most bacterial and fungal strains thrive. The nanocapsule substrate (NC@SiO2) was 676 nm in diameter, and the ligand-grafted capsule (NC@SiO2-g-MAA) was 888 nm. The large surface area and outer ligand brush of the NCs induced a rapid, self-controlled antibacterial response in the pH and humidity conditions needed for industrial and medical applications. Ligand-brush NCs containing an anionic antimicrobial drug had a rapid release effect because of the repellent electrostatic force and swelling properties of the ligand brushes. Controlled release of the drug was achieved at pH 6 and humidity of 45% and 100%. As many carboxylic acid groups are deprotonated into carboxylic acids at pH 5, the NC@SiO2-g-MAA had a high negative charge density. Carboxylic acid groups are anionized (–COO−) at pH 6 and above and push each other out of the capsule, expanding the outer shell as in a polymer brush to create the release behavior. The surface potential of the NC intermediate (NC@SiO2-MPS) was −23.45 [mV], and the potential of the capsule surface decreased to −36.4 [mV] when the MAA ligand brushes were grafted onto the surface of the capsule intermediate. In an antimicrobial experiment using Escherichia coli, a clear zone of 13–20 mm formed at pH 6, and the E. coli was eradicated completely at pH 6 and pH 7 when the humidity was 100%. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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Graphical abstract

13 pages, 1660 KiB  
Article
PLGA/PEG Nanoparticles Loaded with Cyclodextrin-Peganum harmala Alkaloid Complex and Ascorbic Acid with Promising Antimicrobial Activities
by Sherif Ashraf Fahmy, Noha Khalil Mahdy, Hadeer Al Mulla, Aliaa Nabil ElMeshad, Marwa Y. Issa and Hassan Mohamed El-Said Azzazy
Pharmaceutics 2022, 14(1), 142; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14010142 - 07 Jan 2022
Cited by 25 | Viewed by 3639
Abstract
Antimicrobial drugs face numerous challenges, including drug resistance, systemic toxic effects, and poor bioavailability. To date, treatment choices are limited, which warrants the search for novel potent antivirals, including those extracted from natural products. The seeds of Peganum harmala L. (Zygophyllaceae family) [...] Read more.
Antimicrobial drugs face numerous challenges, including drug resistance, systemic toxic effects, and poor bioavailability. To date, treatment choices are limited, which warrants the search for novel potent antivirals, including those extracted from natural products. The seeds of Peganum harmala L. (Zygophyllaceae family) have been reported to have antimicrobial, antifungal, and anticancer activities. In the present study, a 2-hydroxy propyl-β-cyclodextrin (HPβCD)/harmala alkaloid-rich fraction (HARF) host–guest complex was prepared using a thin-film hydration method to improve the water solubility and bioavailability of HARF. The designed complex was then co-encapsulated with ascorbic acid into PLGA nanoparticles coated with polyethylene glycol (HARF–HPßCD/AA@PLGA-PEG NPs) using the W/O/W multiple emulsion-solvent evaporation method. The average particle size, PDI, and zeta potential were 207.90 ± 2.60 nm, 0.17 ± 0.01, and 31.6 ± 0.20 mV, respectively. The entrapment efficiency for HARF was 81.60 ± 1.20% and for ascorbic acid was 88 ± 2.20%. HARF–HPßCD/AA@PLGA-PEG NPs had the highest antibacterial activity against Staphylococcus aureus and Escherichia coli (MIC of 0.025 mg/mL). They also exhibited high selective antiviral activity against the H1N1 influenza virus (IC50 2.7 μg/mL) without affecting the host (MDCK cells). In conclusion, the co-encapsulation of HPCD–HARF complex and ascorbic acid into PLGA-PEG nanoparticles significantly increased the selective H1N1 killing activity with minimum host toxic effects. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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16 pages, 2913 KiB  
Article
Liposomal Encapsulation Increases the Efficacy of Azithromycin against Chlamydia trachomatis
by Anita Bogdanov, László Janovák, Jasmina Vraneš, Tomislav Meštrović, Sunčanica Ljubin-Sternak, Zsuzsanna Cseh, Valéria Endrész, Katalin Burián, Željka Vanić and Dezső P. Virok
Pharmaceutics 2022, 14(1), 36; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics14010036 - 24 Dec 2021
Cited by 5 | Viewed by 2442
Abstract
Chlamydia trachomatis (C. trachomatis) is an obligate intracellular bacterium linked to ocular and urogenital infections with potentially serious sequelae, including blindness and infertility. First-line antibiotics, such as azithromycin (AZT) and doxycycline, are effective, but treatment failures have also been reported. Encapsulation [...] Read more.
Chlamydia trachomatis (C. trachomatis) is an obligate intracellular bacterium linked to ocular and urogenital infections with potentially serious sequelae, including blindness and infertility. First-line antibiotics, such as azithromycin (AZT) and doxycycline, are effective, but treatment failures have also been reported. Encapsulation of antibiotics in liposomes is considered an effective approach for improving their local effects, bioavailability, biocompatibility and antimicrobial activity. To test whether liposomes could enhance the antichlamydial action of AZT, we encapsulated AZT in different surface-charged elastic liposomes (neutral, cationic and anionic elastic liposomes) and assessed their antibacterial potential against the C. trachomatis serovar D laboratory strain as well as the clinical isolate C. trachomatis serovar F. A direct quantitative polymerase chain reaction (qPCR) method was used to measure chlamydial genome content 48 h post infection and to determine the recoverable chlamydial growth. All the liposomes efficiently delivered AZT to HeLa 229 cells infected with the laboratory Chlamydia strain, exhibiting the minimal inhibitory concentrations (MIC) and the minimal bactericidal concentrations (MBC) of AZT even 4–8-fold lower than those achieved with the free AZT. The tested AZT-liposomes were also effective against the clinical Chlamydia strain by decreasing MIC values by 2-fold relative to the free AZT. Interestingly, the neutral AZT-liposomes had no effect on the MBC against the clinical strain, while cationic and anionic AZT-liposomes decreased the MBC 2-fold, hence proving the potential of the surface-charged elastic liposomes to improve the effectiveness of AZT against C. trachomatis. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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16 pages, 4461 KiB  
Article
Biocomposite Hydrogels for the Treatment of Bacterial Infections: Physicochemical Characterization and In Vitro Assessment
by Delia Mihaela Rata, Anca Niculina Cadinoiu, Marcel Popa, Leonard Ionut Atanase, Oana Maria Daraba, Irina Popescu, Laura Ecaterina Romila and Daniela Luminita Ichim
Pharmaceutics 2021, 13(12), 2079; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13122079 - 04 Dec 2021
Cited by 12 | Viewed by 1985
Abstract
Hydrogels based on natural and synthetic polymers and inorganic nanoparticles proved to be a viable strategy in the fight against some Gram-positive and Gram-negative bacteria. Additionally, numerous studies have demonstrated the advantages of using ZnO nanoparticles in medicine due to their high antibacterial [...] Read more.
Hydrogels based on natural and synthetic polymers and inorganic nanoparticles proved to be a viable strategy in the fight against some Gram-positive and Gram-negative bacteria. Additionally, numerous studies have demonstrated the advantages of using ZnO nanoparticles in medicine due to their high antibacterial efficacy and relatively low cost. Consequently, the purpose of our study was to incorporate ZnO nanoparticles into chitosan/poly (vinyl alcohol)-based hydrogels in order to obtain a biocomposite with antimicrobial properties. These biocomposite hydrogels, prepared by a double crosslinking (covalent and ionic) were characterized from a structural, morphological, swelling degree, and mechanical point of view. FTIR spectroscopy demonstrated both the apparition of new imine and acetal bonds due to covalent crosslinking and the presence of the sulfate group following ionic crosslinking. The morphology, swelling degree, and mechanical properties of the obtained hydrogels were influenced by both the degree of covalent crosslinking and the amount of ZnO nanoparticles incorporated. In vitro cytotoxicity assessment showed that hydrogels without ZnONPs are non-cytotoxic while the biocomposite hydrogels are weak (with 3% ZnONPs) or moderately (with 4 and 5% ZnONPs) cytotoxic. Compared to nanoparticle-free hydrogels, the biocomposite hydrogels show significant antimicrobial activity against S. aureus, E. coli, and K. pneumonia. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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Graphical abstract

18 pages, 3734 KiB  
Article
Dual Cross-Linked Chitosan/PVA Hydrogels Containing Silver Nanoparticles with Antimicrobial Properties
by Dana M. Suflet, Irina Popescu, Irina M. Pelin, Daniela L. Ichim, Oana M. Daraba, Marieta Constantin and Gheorghe Fundueanu
Pharmaceutics 2021, 13(9), 1461; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13091461 - 13 Sep 2021
Cited by 43 | Viewed by 4252
Abstract
Stable chitosan/PVA-based hydrogels were obtained by combining covalent and physical cross-linking methods. As covalent cross-linkers, epoxy agents with different chain lengths were used, while freeze–thaw cycles were applied for additional physical cross-linking. The chemical structure of the hydrogel was examined by FTIR spectroscopy [...] Read more.
Stable chitosan/PVA-based hydrogels were obtained by combining covalent and physical cross-linking methods. As covalent cross-linkers, epoxy agents with different chain lengths were used, while freeze–thaw cycles were applied for additional physical cross-linking. The chemical structure of the hydrogel was examined by FTIR spectroscopy whereas the morphology was analyzed by SEM, showing well-defined pores with dimensions of around 50 μm in diameter. It was proved that gel fraction and the network morphology were deeply influenced by the synthesis conditions. Chitosan/PVA hydrogel showed a relative high swelling rate, reaching equilibrium in the first hour. The values obtained for the elastic modulus were relatively low (3–30 kPa); as a result, these hydrogels are soft and very flexible, and are ideal candidates for medical applications as wound or oral dressings. In addition, the natural antimicrobial activity of chitosan was enhanced by in situ generation of silver nanoparticles (AgNPs) under UV irradiation. The total amount of Ag from hydrogel was determined by elemental analyses and its crystalline state was confirmed by XRD. The CS/PVA hydrogels entrapped with AgNPs exhibited high inhibitory activity against S. aureus and K. pneumonia. The vitality tests confirmed the lack of cytotoxicity of CS/PVA hydrogels without and with AgNPs. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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17 pages, 4996 KiB  
Article
Formulation and Optimization of Butenafine-Loaded Topical Nano Lipid Carrier-Based Gel: Characterization, Irritation Study, and Anti-Fungal Activity
by Wael A. Mahdi, Sarah I. Bukhari, Syed Sarim Imam, Sultan Alshehri, Ameeduzzafar Zafar and Mohd Yasir
Pharmaceutics 2021, 13(7), 1087; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13071087 - 16 Jul 2021
Cited by 20 | Viewed by 2749
Abstract
The present study aims to prepare and optimize butenafine hydrochloride NLCs formulation using solid and liquid lipid. The optimized selected BF-NLCopt was further converted into Carbopol-based gel for topical application for the treatment of fungal infection. Box Behnken design was employed to optimize [...] Read more.
The present study aims to prepare and optimize butenafine hydrochloride NLCs formulation using solid and liquid lipid. The optimized selected BF-NLCopt was further converted into Carbopol-based gel for topical application for the treatment of fungal infection. Box Behnken design was employed to optimize the nanostructure lipids carriers (NLCs) using the lipid content (A), Tween 80 (B), and homogenization cycle (C) as formulation factors at three levels. Their effects were observed on the particle size (Y1) and entrapment efficiency (Y2). The selected formulation was converted into gel and further assessed for gel characterization, drug release, anti-fungal study, irritation study, and stability study. The solid lipid (Compritol 888 ATO), liquid lipid (Labrasol), and surfactant (tween 80) were selected based on maximum solubility. The optimization result showed a particle size of 111 nm with high entrapment efficiency of 86.35% for BF-NLCopt. The optimized BF-NLCopt converted to gel (1% w/v, Carbopol 934) and showed ideal gel evaluation results (drug content 99.45 ± 2.11, pH 6.5 ± 0.2, viscosity 519 ± 1.43 CPs). The drug release study result depicted a prolonged drug release (65.09 ± 4.37%) with high drug permeation 641.37 ± 46.59 µg (32.07 ± 2.32%) than BF conventional gel. The low value of irritation score (0.17) exhibited negligible irritation on the skin after application. The anti-fungal result showed greater efficacy than the BF gel at both time points. The overall conclusion of the results revealed NLCs-based gel of BF as an ideal delivery system to treat the fungal infection. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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15 pages, 965 KiB  
Article
The Biological Effects of Novel Nutraceuticals with Curcuminoids and Other Plant-Derived Immunomodulators and Pre-Probiotics
by Adina Elena Răducanu, Bianca-Maria Tihăuan, Ioana Cristina Marinaș, Oana Teodora Ciupercă, Carmen Elena Țebrencu, Elena Ionescu and Tatiana Onisei
Pharmaceutics 2021, 13(5), 666; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050666 - 06 May 2021
Cited by 7 | Viewed by 2790
Abstract
An effective and well-balanced immune system is pivotal for maintaining health. Diet and nutrition can affect the functioning of numerous immune parameters, with direct repercussions on homeostasis. Since our immune functions are indispensable in defending the body against pathogens and thus play a [...] Read more.
An effective and well-balanced immune system is pivotal for maintaining health. Diet and nutrition can affect the functioning of numerous immune parameters, with direct repercussions on homeostasis. Since our immune functions are indispensable in defending the body against pathogens and thus play a vital role in maintaining health, modulating immune response may well serve as the basis for the development of plant-based functional foods and novel nutraceuticals. This concept is currently utilized in attempts to prevent or mitigate inflammatory reactions via the development of targeted food products or active ingredients since an extended number of phytoconstituents (such as curcuminoids) are associated with beneficial effects on immunity. Immunomodulatory plant-based dietary supplements are considered effective in improving immune functions and reducing the incidence of immunological disorders or imbalances. Therefore, the main focus of this study was to evidence the beneficial biological effects such as antioxidant and antimicrobial, as well as nutritional status, biocompatibility and cell proliferation capacity and immunomodulation of two novel nutraceuticals. The first nutraceutic was based on curcuminoids and other actives from Trigonella foenum- graecum (seeds), Chelidonium majus L. (aerial parts), Taraxacum officinale L. (roots), vitamins (C, D3, A, E) and minerals (zinc) whereas the second one was made of probiotics such as Lactobacillus acidophilus and Bifidobacterium animalis subsp. Lactis combined with actives from Helianthus tuberosus (tubers) and Psyllium/Plantago ovata (husk) as herbal prebiotics. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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16 pages, 7671 KiB  
Article
Preparation of Topical Itraconazole with Enhanced Skin/Nail Permeability and In Vivo Antifungal Efficacy against Superficial Mycosis
by Laxman Subedi, Seung-Yub Song, Saurav Kumar Jha, Sung-Ho Lee, Rudra Pangeni, Kyo-Tan Koo, Beum Joon Kim, Seung-Sik Cho and Jin Woo Park
Pharmaceutics 2021, 13(5), 622; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050622 - 27 Apr 2021
Cited by 9 | Viewed by 2694
Abstract
In this study, a stable and highly skin-permeable topical delivery system for itraconazole (ITZ) was designed to provide effective treatment against superficial mycosis. Herein, ITZ was incorporated into a solution composed of ethanol, benzyl alcohol, hydrochloric acid, Transcutol P, and cyclomethicone as a [...] Read more.
In this study, a stable and highly skin-permeable topical delivery system for itraconazole (ITZ) was designed to provide effective treatment against superficial mycosis. Herein, ITZ was incorporated into a solution composed of ethanol, benzyl alcohol, hydrochloric acid, Transcutol P, and cyclomethicone as a delivery vehicle, solubilizer, protonating agent, permeation enhancer, and spreading agent, respectively. At 72 h, the optimal topical ITZ formulation (ITZ–TF#11) exhibited 135% enhanced skin permeability, which led to increases in drug deposition in the stratum corneum, epidermis, and dermis of 479%, 739%, and 2024%, respectively, compared with the deposition of 1% ITZ in ethanol (control). Moreover, on day 7, ITZ–TF#11 demonstrated 2.09- and 2.30-fold enhanced nail flux and drug deposition, compared with the control. At a dose of 40 mg/kg/day, ITZ–TF#11 showed 323% greater lesion recovery, a 165% lower mean erythema severity score, and a 37% lower mean logarithm of viable fungal cells in skin in the treated area, compared with mice that received oral ITZ at the same dose. Overall, the findings imply that ITZ–TF#11 is a superior alternative to oral ITZ for treatment of superficial mycosis. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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18 pages, 10386 KiB  
Article
Kinetic Release Studies of Antibiotic Patches for Local Transdermal Delivery
by Esra Altun, Esra Yuca, Nazmi Ekren, Deepak M. Kalaskar, Denisa Ficai, Georgiana Dolete, Anton Ficai and Oguzhan Gunduz
Pharmaceutics 2021, 13(5), 613; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13050613 - 23 Apr 2021
Cited by 32 | Viewed by 4536
Abstract
This study investigates the usage of electrohydrodynamic (EHD)-3D printing for the fabrication of bacterial cellulose (BC)/polycaprolactone (PCL) patches loaded with different antibiotics (amoxicillin (AMX), ampicillin (AMP), and kanamycin (KAN)) for transdermal delivery. The composite patches demonstrated facilitated drug loading and encapsulation efficiency of [...] Read more.
This study investigates the usage of electrohydrodynamic (EHD)-3D printing for the fabrication of bacterial cellulose (BC)/polycaprolactone (PCL) patches loaded with different antibiotics (amoxicillin (AMX), ampicillin (AMP), and kanamycin (KAN)) for transdermal delivery. The composite patches demonstrated facilitated drug loading and encapsulation efficiency of drugs along with extended drug release profiles. Release curves were also subjected to model fitting, and it was found that drug release was optimally adapted to the Higuchi square root model for each drug. They performed a time-dependent and diffusion-controlled release from the patches and followed Fick’s diffusion law by the Korsmeyer–Peppas energy law equation. Moreover, produced patches demonstrated excellent antimicrobial activity against Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) strains, so they could be helpful in the treatment of chronic infectious lesions during wound closures. As different tests have confirmed, various types of antibiotics could be loaded and successfully released regardless of their types from produced BC/PCL patches. This study could breathe life into the production of antibiotic patches for local transdermal applications in wound dressing studies and improve the quality of life of patients. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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18 pages, 2941 KiB  
Article
In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers
by Luca Éva Uhljar, Sheng Yuan Kan, Norbert Radacsi, Vasileios Koutsos, Piroska Szabó-Révész and Rita Ambrus
Pharmaceutics 2021, 13(4), 556; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13040556 - 15 Apr 2021
Cited by 53 | Viewed by 8590
Abstract
Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion [...] Read more.
Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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8 pages, 608 KiB  
Article
Stability Evaluation of Extemporaneously Compounded Vancomycin Ophthalmic Drops: Effect of Solvents and Storage Conditions
by Christopher Ross, Basir Syed, Joanna Pak, Vishal Jhanji, Jason Yamaki and Ajay Sharma
Pharmaceutics 2021, 13(2), 289; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13020289 - 23 Feb 2021
Cited by 2 | Viewed by 4040
Abstract
Vancomycin is the drug of choice for methicillin-resistant Staphylococcus aureus keratitis and other ocular infections. Vancomycin ophthalmic drops are not commercially available and require compounding. The present study was designed to investigate the stability of vancomycin ophthalmic drops in normal saline, phosphate-buffered saline [...] Read more.
Vancomycin is the drug of choice for methicillin-resistant Staphylococcus aureus keratitis and other ocular infections. Vancomycin ophthalmic drops are not commercially available and require compounding. The present study was designed to investigate the stability of vancomycin ophthalmic drops in normal saline, phosphate-buffered saline (PBS), and balanced salt solution (BSS) while stored at room temperature or under refrigeration. Vancomycin ophthalmic drops (50 mg/mL) were aseptically prepared from commercially available intravenous powder using PBS, BSS, and saline. Solutions were stored at room temperature and in a refrigerator for 28 days. The vancomycin stability was tested by a microbiology assay and high-performance liquid chromatography HPLC analysis immediately after formulation and at days 7, 14, and 28 after storage at room temperature or under refrigeration. The pH, turbidity was also tested. Vancomycin formulations in PBS, BSS and normal saline had initial pH of 5; 5.5; 3 respectively. The formulation in PBS developed turbidity and a slight decrease in pH upon storage. Microbiological assay did not show any change in zone of inhibition with any of the formulation upon storage either at room temperature or under refrigeration. HPLC analysis did not detect any decrease in vancomycin concentration or the accumulation of degraded products in any of the formulations upon storage either at room temperature or under refrigeration. Vancomycin ophthalmic drops prepared using PBS, BSS, and normal saline were stable up to the tested time point of 28 days, irrespective of their storage temperature. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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Review

Jump to: Editorial, Research

22 pages, 785 KiB  
Review
Can Plant Materials Be Valuable in the Treatment of Periodontal Diseases? Practical Review
by Anna Gościniak, Magdalena Paczkowska-Walendowska, Agnieszka Skotnicka, Marek A. Ruchała and Judyta Cielecka-Piontek
Pharmaceutics 2021, 13(12), 2185; https://0-doi-org.brum.beds.ac.uk/10.3390/pharmaceutics13122185 - 17 Dec 2021
Cited by 16 | Viewed by 4623
Abstract
Periodontal diseases are one of the most significant challenges in dental health. It is estimated that only a few percent of the worldwide population have entirely healthy teeth, and according to WHO, oral diseases may affect up to 3.5 billion people worldwide. One [...] Read more.
Periodontal diseases are one of the most significant challenges in dental health. It is estimated that only a few percent of the worldwide population have entirely healthy teeth, and according to WHO, oral diseases may affect up to 3.5 billion people worldwide. One of the most serious oral diseases is periodontitis, an inflammatory disease affecting periodontal tissues, caused by pathogenic bacteria and environmental factors such as the ageing population, abuse of tobacco products, and lack of adequate oral hygiene due low public awareness. Plant materials are widely and successfully used in the management of many conditions, including periodontitis. Plant materials for periodontitis exhibit antibacterial, anti-inflammatory, antioxidant activities and affect the periodontium structure. Numerous studies demonstrate the advantages of phytotherapy for periodontitis relief and indicate the usefulness of Baikal skullcap root, Pomegranate fruit peel and root cortex, Tea leaves, Chamomile flowers, Magnolia bark, Blackberry leaves and fruits, Cranberry fruits and Lippia sidoides essential oil. This review aims to analyze the use and applicability of selected plant materials in periodontitis management since it is of paramount importance to evaluate the evidence of the traditionally used plant materials in light of continuously growing interest in phytotherapy and its adjuvant role in the treatment of periodontitis. Full article
(This article belongs to the Special Issue Pharmaceutical Formulations with Antimicrobial Properties)
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