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Advanced Materials in Drug Release and Drug Delivery Systems (Second Volume)

A special issue of Materials (ISSN 1996-1944). This special issue belongs to the section "Biomaterials".

Deadline for manuscript submissions: closed (10 December 2022) | Viewed by 16703

Special Issue Editor


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Guest Editor
Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Bialystok, Kilinskiego 1, 15-089 Bialystok, Poland
Interests: multifunctional polymers; drug release; drug delivery systems; modified release formulations; multicompartment dosage forms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Investigations concerning the use of advanced materials when designing drug delivery systems represent a rapidly growing research field in materials/polymer science, chemical engineering and pharmaceutical technology. Nowadays, it is impossible to create modern drug delivery systems without multifunctional excipients that affect drug release, improve drug stability or enhance drug permeation and bioavailability.

In recent years, the search for novel materials or the modification and combination of existing materials have represented a trend in pharmaceutical technology. The chemical or physical modification of either naturally derived or synthetic materials/polymers can improve their characteristics and favourably affect the quality of the designed formulations. Therefore, a great deal of emphasis is placed on the design and testing of new materials with application potential in pharmaceutical technology.

This Special Issue will be a collection of full papers, short communications and review papers focusing on recent progress in functional materials/polymers with promising potential in drug delivery. Discussion of manufacturing, physical and chemical modification, characterization, as well as the combination of different materials and their application in the biomedical field is also welcome.

Prof. Katarzyna Winnicka
Guest Editor

Manuscript Submission Information

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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. Materials is an international peer-reviewed open access semimonthly 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 2600 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

  • multifunctional materials
  • chemical or physical modification of polymers
  • drug release
  • drug delivery systems
  • naturally derived or synthetic materials/polymers
  • materials engineering

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Published Papers (7 papers)

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Research

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22 pages, 5956 KiB  
Article
The Spray-Dried Alginate/Gelatin Microparticles with Luliconazole as Mucoadhesive Drug Delivery System
by Marta Szekalska, Magdalena Wróblewska, Anna Czajkowska-Kośnik, Katarzyna Sosnowska, Paweł Misiak, Agnieszka Zofia Wilczewska and Katarzyna Winnicka
Materials 2023, 16(1), 403; https://doi.org/10.3390/ma16010403 - 01 Jan 2023
Cited by 12 | Viewed by 2066
Abstract
Candida species are opportunistic fungi, which are primary causative agents of vulvovaginal candidiasis. The cure of candidiasis is difficult, lengthy, and associated with the fungi resistivity. Therefore, the research for novel active substances and unconventional drug delivery systems providing effective and safe treatment [...] Read more.
Candida species are opportunistic fungi, which are primary causative agents of vulvovaginal candidiasis. The cure of candidiasis is difficult, lengthy, and associated with the fungi resistivity. Therefore, the research for novel active substances and unconventional drug delivery systems providing effective and safe treatment is still an active subject. Microparticles, as multicompartment dosage forms due to larger areas, provide short passage of drug diffusion, which might improve drug therapeutic efficiency. Sodium alginate is a natural polymer from a polysaccharide group, possessing swelling, mucoadhesive, and gelling properties. Gelatin A is a natural high-molecular-weight polypeptide obtained from porcine collagen. The purpose of this study was to prepare microparticles by the spray-drying of alginate/gelatin polyelectrolyte complex mixture, with a novel antifungal drug—luliconazole. In the next stage of research, the effect of gelatin presence on pharmaceutical properties of designed formulations was assessed. Interrelations among polymers were evaluated with thermal analysis and Fourier transform infrared spectroscopy. A valid aspect of this research was the in vitro antifungal activity estimation of designed microparticles using Candida species: C. albicans, C. krusei, and C. parapsilosis. It was shown that the gelatin addition affected the particles size, improved encapsulation efficiency and mucoadhesiveness, and prolonged the drug release. Moreover, gelatin addition to the formulations improved the antifungal effect against Candida species. Full article
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13 pages, 8250 KiB  
Article
Controlled Drug Release Using Chitosan-Alginate-Gentamicin Multi-Component Beads
by Kyung Hee Park, Yeon Woo Choi, Heejoo Ryu, Hyoung Jae Lee, Jae-Hak Moon, Ho-Jun Song and Yeong-Joon Park
Materials 2022, 15(21), 7682; https://doi.org/10.3390/ma15217682 - 01 Nov 2022
Cited by 1 | Viewed by 1812
Abstract
This study aimed to develop improved multi-component beads with controlled, sustained delivery of antibiotics, such as gentamicin (GM). Antibiotic-loaded beads with rapid-release and the sustained-release system can be used for bone restoration. Single and multi-component beads were prepared by gelation using various combinations [...] Read more.
This study aimed to develop improved multi-component beads with controlled, sustained delivery of antibiotics, such as gentamicin (GM). Antibiotic-loaded beads with rapid-release and the sustained-release system can be used for bone restoration. Single and multi-component beads were prepared by gelation using various combinations of chitosan and calcium chloride as cationic components and alginate and citric acid as anions. GM release was also controlled by crosslinking using citric acid. The optimum beads were obtained using 5% or 2% sodium alginate, 3% chitosan, and 0.1 mol/L citric acid. The beads were characterized by FTIR, TG-DTG, swelling behavior, and SEM. All GM-loaded beads revealed good antimicrobial activity. The rate and kinetics of release in the phosphate buffer solution were controlled by changing the amount of chitosan in the calcium chloride solution and using citric acid as the crosslinking agent. Crosslinked beads were prepared for the release of about 80% of the loaded drug within 24 h. The study concluded that the chitosan-alginate beads provided faster GM release but crosslinking with citric acid was efficient for sustained-release beads containing gentamicin. Full article
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10 pages, 1304 KiB  
Article
Incorporation of Ethylcellulose Microparticles Containing a Model Drug with a Bitter Taste into Nanofibrous Mats by the Electrospinning Technique—Preliminary Studies
by Katarzyna Olechno, Nina Katarina Grilc, Špela Zupančič and Katarzyna Winnicka
Materials 2022, 15(15), 5286; https://doi.org/10.3390/ma15155286 - 31 Jul 2022
Cited by 2 | Viewed by 1225
Abstract
Electrospinning is considered a simple and comprehensive technique to formulate ultrafine fibres by using an electric field. Polymeric nanofibers constitute promising materials in biomedical applications as drug delivery systems. For their preparation, both natural and synthetic polymers are utilised. Owing to the potential [...] Read more.
Electrospinning is considered a simple and comprehensive technique to formulate ultrafine fibres by using an electric field. Polymeric nanofibers constitute promising materials in biomedical applications as drug delivery systems. For their preparation, both natural and synthetic polymers are utilised. Owing to the potential use of electrospun nanofibers as an orodispersible drug dosage form, ethylcellulose microparticles containing the antihistamine drug rupatadine fumarate, prepared by the spray drying technique to conceal the drug’s bitter taste, were incorporated into nanofibers. The obtained nanofibrous mats were evaluated for morphology, mechanical strength, disintegration time, the drug solid state and acceptability in terms of taste masking efficiency. Preliminary studies showed that hypromellose used as a single polymer was not a suitable substance for the manufacturing of nanofibers. Therefore, in order to facilitate the obtention of homogeneous nonwovens, different grades of polyethylene oxide (2,000,000–2M-Da and 4,000,000–4M-Da) were added, which improved the quality of the prepared mats. Nanofibers of the most satisfactory quality were obtained from hypromellose (6.5% w/v) and PEO (2M, 0.5% w/v). SEM image analysis has shown that the nanofibers were homogeneous and smooth and possessed a fast disintegration time (below 30 s) and an adequate drug content with a simultaneous taste-masking effect (as indicated by the in vivo and in vitro methods). However, further studies are necessary to refine their mechanical characteristics. Full article
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19 pages, 2491 KiB  
Article
Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect
by Katarzyna Olechno, Bartosz Maciejewski, Klaudia Głowacz, Joanna Lenik, Patrycja Ciosek-Skibińska, Anna Basa and Katarzyna Winnicka
Materials 2022, 15(6), 2126; https://doi.org/10.3390/ma15062126 - 14 Mar 2022
Cited by 12 | Viewed by 2524
Abstract
Orally disintegrating (orodispersible) films provide a versatile tool for drug administration, especially in the pediatric and geriatric population, since they reduce the risk of choking and do not necessitate drinking water during application. By considering their direct contact with the taste buds, palatability [...] Read more.
Orally disintegrating (orodispersible) films provide a versatile tool for drug administration, especially in the pediatric and geriatric population, since they reduce the risk of choking and do not necessitate drinking water during application. By considering their direct contact with the taste buds, palatability is an influential aspect related to patient compliance. The microparticles based on taste-masking polymers containing drugs enclosed inside effectively mask the unpleasant taste of medicines. Ethylcellulose is a hydrophobic polymer widely used as a taste-masking material. Rupatadine fumarate, a second-generation antihistamine drug, is characterised by an intense bitter taste; therefore, it is crucial to achieve a tolerable taste whilst developing orodispersible formulations with its content. The objective of this study was to develop orally disintegrating films with rupatadine fumarate in the form of ethylcellulose-based microparticles obtained from aqueous dispersions of ethylcellulose—Surelease® or Aquacoat® ECD. It was a technological challenge to achieve homogenous drug content per dosage unit and sufficient mechanical properties for film operating due to the necessity to suspend the microparticles in the casting solution. Although the process of obtaining films consisted of several steps (mixing, pouring, drying), the particles were homogeneously dispersed, and each film of the desired size contained the proper dose of the drug. The taste-masking effect was also maintained. This parameter was confirmed by three independent methods: in vivo by healthy volunteers, an electronic tongue and a dissolution test. The applied taste-evaluation techniques showed that the films containing Aquacoat® ECD microparticles have the highest degree of bitter taste reduction, which confirms the results obtained in our previous studies. Full article
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29 pages, 5561 KiB  
Article
Thiolated Silicone Oils as New Components of Protective Creams in the Prevention of Skin Diseases
by Agnieszka Kulawik-Pióro, Anna K. Drabczyk, Joanna Kruk, Magdalena Wróblewska, Katarzyna Winnicka and Justyna Tchórzewska
Materials 2021, 14(16), 4723; https://doi.org/10.3390/ma14164723 - 21 Aug 2021
Cited by 8 | Viewed by 2737
Abstract
This work investigates the possibility of using thiolated silicone oils as new components in protective creams and their impact on the efficacy of these products. Thiolated silicone oils were synthesized by amide bond formation between primary amino groups of poly17dimethylsiloxane-co-(3-aminopropyl)-methylsiloxane] and carboxylic groups [...] Read more.
This work investigates the possibility of using thiolated silicone oils as new components in protective creams and their impact on the efficacy of these products. Thiolated silicone oils were synthesized by amide bond formation between primary amino groups of poly17dimethylsiloxane-co-(3-aminopropyl)-methylsiloxane] and carboxylic groups of thiol ligand (3-mercaptopropionic acid) with carbodiimide as a coupling agent. To evaluate and compare the properties of these kinds of thiomers, three different emulsion o/w types were obtained. Emulsion E1 contained methyl silicone oil, E2 poly[dimethylsiloxane-co-(3-aminopropyl)-methylsiloxane], and E3 thiolated silicone oil (silicone-MPA), respectively. Physicochemical properties, including pH, conductivity, droplet size distribution, viscosity, and stability, were assessed. The efficacy of barrier creams in the prevention of occupational skin diseases depends on their mechanical and rheological properties. Thus, the method which imitates the spreadability conditions on the skin and how structure reconstruction takes places was performed. We also investigated textural profile, bioadhesion, protection against water and detergents, and water vapor permeability. Emulsion E3 was characterized by beneficial occlusion, spreadability, and adhesion properties. These features with prolonged residence time on the skin can make designed barrier creams more preferable for consumers. Full article
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19 pages, 2820 KiB  
Article
The Impact of Gelatin on the Pharmaceutical Characteristics of Fucoidan Microspheres with Posaconazole
by Marta Szekalska, Aleksandra Citkowska, Magdalena Wróblewska and Katarzyna Winnicka
Materials 2021, 14(15), 4087; https://doi.org/10.3390/ma14154087 - 22 Jul 2021
Cited by 10 | Viewed by 1981
Abstract
Fungal infections and invasive mycoses, despite the continuous medicine progress, are an important globally therapeutic problem. Multicompartment dosage formulations (e.g., microparticles) ensure a short drug diffusion way and high surface area of drug release, which as a consequence can provide improvement of therapeutic [...] Read more.
Fungal infections and invasive mycoses, despite the continuous medicine progress, are an important globally therapeutic problem. Multicompartment dosage formulations (e.g., microparticles) ensure a short drug diffusion way and high surface area of drug release, which as a consequence can provide improvement of therapeutic efficiency compared to the traditional drug dosage forms. As fucoidan is promising component with wide biological activity per se, the aim of this study was to prepare fucospheres (fucoidan microparticles) and fucoidan/gelatin microparticles with posaconazole using the one-step spray-drying technique. Pharmaceutical properties of designed fucospheres and the impact of the gelatin addition on their characteristics were evaluated. An important stage of this research was in vitro evaluation of antifungal activity of developed microparticles using different Candida species. It was observed that gelatin presence in microparticles significantly improved swelling capacity and mucoadhesiveness, and provided a sustained POS release. Furthermore, it was shown that gelatin addition enhanced antifungal activity of microparticles against tested Candida spp. strains. Microparticles formulation GF6, prepared by the spray drying of 20% fucoidan, 5% gelatin and 10% Posaconazole, were characterized by optimal mucoadhesive properties, high drug loading and the most sustained drug release (after 8 h 65.34 ± 4.10% and 33.81 ± 5.58% of posaconazole was dissolved in simulated vaginal fluid pH 4.2 or 0.1 M HCl pH 1.2, respectively). Full article
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Review

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27 pages, 5619 KiB  
Review
“Success Depends on Your Backbone”—About the Use of Polymers as Essential Materials Forming Orodispersible Films
by Katarzyna Olechno, Anna Basa and Katarzyna Winnicka
Materials 2021, 14(17), 4872; https://doi.org/10.3390/ma14174872 - 27 Aug 2021
Cited by 17 | Viewed by 3471
Abstract
Polymers constitute a group of materials having a wide-ranging impact on modern pharmaceutical technology. Polymeric components provide the foundation for the advancement of novel drug delivery platforms, inter alia orodispersible films. Orodispersible films are thin, polymeric scraps intended to dissolve quickly when put [...] Read more.
Polymers constitute a group of materials having a wide-ranging impact on modern pharmaceutical technology. Polymeric components provide the foundation for the advancement of novel drug delivery platforms, inter alia orodispersible films. Orodispersible films are thin, polymeric scraps intended to dissolve quickly when put on the tongue, allowing them to be easily swallowed without the necessity of drinking water, thus eliminating the risk of choking, which is of great importance in the case of pediatric and geriatric patients. Polymers are essential excipients in designing orodispersible films, as they constitute the backbone of these drug dosage form. The type of polymer is of significant importance in obtaining the formulation of the desired quality. The polymers employed to produce orodispersible films must meet particular requirements due to their oral administration and have to provide adequate surface texture, film thickness, mechanical attributes, tensile and folding strength as well as relevant disintegration time and drug release to obtain the final product characterized by optimal pharmaceutical features. A variety of natural and synthetic polymers currently utilized in manufacturing of orodispersible films might be used alone or in a blend. The goal of the present manuscript was to present a review about polymers utilized in designing oral-dissolving films. Full article
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