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Advanced Materials in Drug Release and Drug Delivery Systems

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

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 50439

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Prof. Dr. Katarzyna Winnicka

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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
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Dear Colleagues,

Investigations concerning advanced materials in 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, searching for novel materials or modifying and combining existing materials has 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

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Keywords

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

Related Special Issue

Advanced Materials in Drug Release and Drug Delivery Systems (Second Volume) in Materials (7 articles)

Published Papers (12 papers)

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Editorial

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4 pages, 179 KiB

Open AccessEditorial

Special Issue: Advanced Materials in Drug Release and Drug Delivery Systems

by Katarzyna Winnicka

Materials 2021, 14(4), 1042; https://doi.org/10.3390/ma14041042 - 23 Feb 2021

Cited by 1 | Viewed by 1776

Abstract

Development of new drug molecules is costly and requires longitudinal, wide-ranging studies; therefore, designing advanced pharmaceutical formulations for existing and well-known drugs seems to be an attractive device for the pharmaceutical industry [...] Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

Research

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20 pages, 8681 KiB

Open AccessArticle

Multivariate Design of 3D Printed Immediate-Release Tablets with Liquid Crystal-Forming Drug—Itraconazole

by Witold Jamróz, Jolanta Pyteraf, Mateusz Kurek, Justyna Knapik-Kowalczuk, Joanna Szafraniec-Szczęsny, Karolina Jurkiewicz, Bartosz Leszczyński, Andrzej Wróbel, Marian Paluch and Renata Jachowicz

Materials 2020, 13(21), 4961; https://doi.org/10.3390/ma13214961 - 04 Nov 2020

Cited by 15 | Viewed by 2599

Abstract

The simplicity of object shape and composition modification make additive manufacturing a great option for customized dosage form production. To achieve this goal, the correlation between structural and functional attributes of the printed objects needs to be analyzed. So far, it has not been deeply investigated in 3D printing-related papers. The aim of our study was to modify the functionalities of printed tablets containing liquid crystal-forming drug itraconazole by introducing polyvinylpyrrolidone-based polymers into the filament-forming matrices composed predominantly of poly(vinyl alcohol). The effect of the molecular reorganization of the drug and improved tablets’ disintegration was analyzed in terms of itraconazole dissolution. Micro-computed tomography was applied to analyze how the design of a printed object (in this case, a degree of an infill) affects its reproducibility during printing. It was also used to analyze the structure of the printed dosage forms. The results indicated that the improved disintegration obtained due to the use of Kollidon^®CL-M was more beneficial for the dissolution of itraconazole than the molecular rearrangement and liquid crystal phase transitions. The lower infill density favored faster dissolution of the drug from printed tablets. However, it negatively affected the reproducibility of the 3D printed object. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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15 pages, 3415 KiB

Open AccessArticle

How Does the CO₂ in Supercritical State Affect the Properties of Drug-Polymer Systems, Dissolution Performance and Characteristics of Tablets Containing Bicalutamide?

by Agata Antosik-Rogóż, Joanna Szafraniec-Szczęsny, Krzysztof Chmiel, Justyna Knapik-Kowalczuk, Mateusz Kurek, Karolina Gawlak, Vittorio P. Danesi, Marian Paluch and Renata Jachowicz

Materials 2020, 13(12), 2848; https://doi.org/10.3390/ma13122848 - 25 Jun 2020

Cited by 2 | Viewed by 2328

Abstract

The increasing demand for novel drug formulations has caused the introduction of the supercritical fluid technology, CO₂ in particular, into pharmaceutical technology as a method enabling the reduction of particle size and the formation of inclusion complexes and solid dispersions. In this paper, we describe the application of scCO₂ in the preparation of binary systems containing poorly soluble antiandrogenic drug bicalutamide and polymeric excipients, either Macrogol 6000 or Poloxamer^®407. The changes in the particle size and morphology were followed using scanning electron microscopy and laser diffraction measurements. Differential scanning calorimetry was applied to assess thermal properties, while X-ray powder diffractometry was used to determine the changes in the crystal structure of the systems. The dissolution of bicalutamide was also considered. Binary solid dispersions were further compressed, and the attributes of tablets were assessed. Tablets were analyzed directly after manufacturing and storage in climate chambers. The obtained results indicate that the use of supercritical CO₂ led to the morphological changes of particles and the improvement of drug dissolution. The flowability of blends containing processed binary systems was poor; however, they were successfully compressed into tablets exhibiting enhanced drug release. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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21 pages, 3869 KiB

Open AccessArticle

Utilization of Ethylcellulose Microparticles with Rupatadine Fumarate in Designing Orodispersible Minitablets with Taste Masking Effect

by Katarzyna Wasilewska, Patrycja Ciosek-Skibińska, Joanna Lenik, Stanko Srčič, Anna Basa and Katarzyna Winnicka

Materials 2020, 13(12), 2715; https://doi.org/10.3390/ma13122715 - 15 Jun 2020

Cited by 17 | Viewed by 3314

Abstract

Minitablets in orodispersible form constitute a flexible drug delivery tool for paediatric and geriatric population as they eliminate the risk of chocking and do not require drinking water in the application. Due to their direct contact with taste buds, taste sensation is an important factor. Preparing microparticles with taste masking polymers utilizing spray drying is an efficient technique for reducing the bitterness of drugs. Ethylcellulose is a hydrophobic polymer widely used as a taste masking material. Rupatadine fumarate, one of the newest antihistamines, features an intensive bitter taste, hence in designing orodispersible formulations, achieving an acceptable taste is a crucial issue. The main objective of this work was to formulate orodispersible minitablets containing taste masked ethylcellulose-based microparticles with rupatadine fumarate and evaluation of their quality, especially in terms of taste masking efficacy. The accessed data indicated that all obtained minitablets were characterized by beneficial pharmaceutical properties. Three independent methods: in vivo with healthy volunteers, in vitro drug dissolution, and “electronic tongue” confirmed that all designed formulations provided satisfactory taste masking rate and that formulation F15 (prepared with Pearlitol^® Flash and Surelease^® microparticles with rupatadine fumarate) was characterized by the lowest bitterness score. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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13 pages, 2487 KiB

Open AccessArticle

Sirolimus-Eluting Electrospun-Produced Matrices as Coatings for Vascular Stents: Dependence of Drug Release on Matrix Structure and Composition of the External Environment

by Zhanna K. Nazarkina, Boris P. Chelobanov, Vera S. Chernonosova, Irina V. Romanova, Andrey A. Karpenko and Pavel P. Laktionov

Materials 2020, 13(12), 2692; https://doi.org/10.3390/ma13122692 - 12 Jun 2020

Cited by 8 | Viewed by 2296

Abstract

Although a number of drug-eluting coatings for vascular stents (VSs) have been developed and are in commercial use, more efficient stent coatings and drug delivery systems are needed. Sirolimus (SRL) is a clinically important drug with antiproliferative and immunosuppressive activities that is widely used for coating stents. Here, we characterized SRL-enriched matrices, intended for coating vascular stents, that were produced by electrospinning (ES) on a drum collector from a solution of polycaprolactone (PCL) and human serum albumin (HSA), 1,1,1,3,3,3-hexafluoroisopropanol (HFIP), dimethyl sulfoxide (DMSO), and SRL. The release of tritium-labeled SRL (³H-SRL) from matrices in phosphate-buffered saline (PBS) or human blood plasma (BP) was studied. The introduction of DMSO in the ES blend decreased SRL release. The use of BP significantly accelerated SRL release through binding with serum biomolecules. The exchange of PBS or BP after every time point also increased SRL release. The maximum SRL release in BP was observed at 3 days. The matrices produced from the ES solution with DMSO and HSA released no more than 80% SRL after 27 days in BP, even under medium exchange conditions. Therefore, PCL-based matrices containing HSA, SRL, and DMSO can be used for coating VSs with prolonged SRL delivery. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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16 pages, 5325 KiB

Open AccessArticle

Prototype Gastro-Resistant Soft Gelatin Films and Capsules—Imaging and Performance In Vitro

by Bartosz Maciejewski, Vishnu Arumughan, Anette Larsson and Małgorzata Sznitowska

Materials 2020, 13(7), 1771; https://doi.org/10.3390/ma13071771 - 09 Apr 2020

Cited by 3 | Viewed by 2764

Abstract

The following study is a continuation of the previous work on preparation of gastro-resistant films by incorporation of cellulose acetate phthalate (CAP) into the soft gelatin film. An extended investigation on the previously described binary Gelatin-CAP and ternary Gelatin-CAP-carrageenan polymer films was performed. The results suggest that the critical feature behind formation of the acid-resistant films is a spinodal decomposition in the film-forming mixture. In the obtained films, upon submersion in an acidic medium, gelatin swells and dissolves, exposing a CAP-based acid-insoluble skeleton, partially coated by a residue of other ingredients. The dissolution-hindering effect appears to be stronger when iota-carrageenan is added to the film-forming mixture. The drug release study performed in enhancer cells confirmed that diclofenac sodium is not released in the acidic medium, however, at pH 6.8 the drug release occurs. The capsules prepared with a simple lab-scale process appear to be resistant to disintegration of the shell structure in acid, although imperfections of the sealing have been noticed. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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9 pages, 2523 KiB

Open AccessCommunication

Loading Graphene Quantum Dots into Optical-Magneto Nanoparticles for Real-Time Tracking In Vivo

by Yu Wang, Nan Xu, Yongkai He, Jingyun Wang, Dan Wang, Qin Gao, Siyu Xie, Yage Li, Ranran Zhang and Qiang Cai

Materials 2019, 12(13), 2191; https://doi.org/10.3390/ma12132191 - 08 Jul 2019

Cited by 12 | Viewed by 3176

Abstract

Fluorescence imaging offers a new approach to visualize real-time details on a cellular level in vitro and in vivo without radioactive damage. Poor light stability of organic fluorescent dyes makes long-term imaging difficult. Due to their outstanding optical properties and unique structural features, graphene quantum dots (GQDs) are promising in the field of imaging for real-time tracking in vivo. At present, GQDs are mainly loaded on the surface of nanoparticles. In this study, we developed an efficient and convenient one-pot method to load GQDs into nanoparticles, leading to longer metabolic processes in blood and increased delivery of GQDs to tumors. Optical-magneto ferroferric oxide@polypyrrole (Fe₃O₄@PPy) core-shell nanoparticles were chosen for their potential use in cancer therapy. The in vivo results demonstrated that by loading GQDs, it was possible to monitor the distribution and metabolism of nanoparticles. This study provided new insights into the application of GQDs in long-term in vivo real-time tracking. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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15 pages, 3708 KiB

Open AccessArticle

Preparation and In Vitro Release of Total Alkaloids from Alstonia Scholaris Leaves Loaded mPEG-PLA Microspheres

by Xiangyu Zheng, Hongli Li, Yi He, Mingwei Yuan, Meili Shen, Renyu Yang, Nianfeng Jiang, Minglong Yuan and Cui Yang

Materials 2019, 12(9), 1457; https://doi.org/10.3390/ma12091457 - 06 May 2019

Cited by 7 | Viewed by 2590

Abstract

Total alkaloids of Alstonia scholaris leaves (ASAs) are extracted from the lamp leaves, which have positive anti-inflammatory activity and remarkable effects in treating bronchitis. Due to its short half-life, we used a degradable mPEG-PLA to physically encapsulate the total alkali of the lamp stage, and prepared a sustained-release microsphere by double-emulsion method. The ASAs-loaded mPEG₁₀₀₀₀-PLA microspheres were screened for better performance by testing the morphology, average particle size, embedding rate and drug loading of different molecular weight mPEG-PLA microspheres, which can stably and continuously release for 15 days at 37 °C. The results of cytotoxicity and blood compatibility indicated that the drug-loaded microspheres have beneficial biocompatibility. Animal experiments showed that the drug-loaded microspheres had a beneficial anti-inflammatory effect. These results all indicated that mPEG-PLA is a controlled release carrier material suitable for ASAs. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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11 pages, 3126 KiB

Open AccessArticle

Versatile Layer-By-Layer Highly Stable Multilayer Films: Study of the Loading and Release of FITC-Labeled Short Peptide in the Drug Delivery Field

by Kun Nie, Xiang Yu, Navnita Kumar and Yihe Zhang

Materials 2019, 12(8), 1206; https://doi.org/10.3390/ma12081206 - 12 Apr 2019

Cited by 5 | Viewed by 3278

Abstract

A viable short FITC-peptide immobilization is the most essential step in the fabrication of multilayer films based on FITC-peptide. These functional multilayer films have potential applications in drug delivery, medical therapy, and so forth. These FITC-peptides films needed to be handled with a lot of care and precision due to their sensitive nature. In this study, a general immobilization method is reported for the purpose of stabilizing various kinds of peptides at the interfacial regions. Utilizing Mesoporous silica nanoparticles can help in the preservation of these FITC-peptides by embedding themselves into these covalently cross-linked multilayers. This basic outlook of the multilayer films is potent enough and could be reused as a positive substrate. The spatio-temporal retention property of peptides can be modulated by varying the number of capping layers. The release speed of guest molecules such as tyrosine within FITC-peptide or/and adamantane (Ad)-in short peptides could also be fine-tuned by the specific arrangements of the multilayers of mesoporous silica nanoparticles (MSNs) and hyaluronic acid- cyclodextrin (HA-CD) multilayer films. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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Review

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32 pages, 4276 KiB

Open AccessReview

Hydrogels as Potential Nano-, Micro- and Macro-Scale Systems for Controlled Drug Delivery

by Adam Chyzy, Monika Tomczykowa and Marta E. Plonska-Brzezinska

Materials 2020, 13(1), 188; https://doi.org/10.3390/ma13010188 - 02 Jan 2020

Cited by 76 | Viewed by 10436

Abstract

This review is an extensive evaluation and essential analysis of the design and formation of hydrogels (HGs) for drug delivery. We review the fundamental principles of HGs (their chemical structures, physicochemical properties, synthesis routes, different types, etc.) that influence their biological properties and medical and pharmaceutical applications. Strategies for fabricating HGs with different diameters (macro, micro, and nano) are also presented. The size of biocompatible HG materials determines their potential uses in medicine as drug carriers. Additionally, novel drug delivery methods for enhancing treatment are discussed. A critical review is performed based on the latest literature reports. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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21 pages, 3541 KiB

Open AccessReview

Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

by Katarzyna Wasilewska and Katarzyna Winnicka

Materials 2019, 12(20), 3386; https://doi.org/10.3390/ma12203386 - 17 Oct 2019

Cited by 107 | Viewed by 8285

Abstract

Polymers constitute the most important group of excipients utilized in modern pharmaceutical technology, playing an essential role in the development of drug dosage forms. Synthetic, semisynthetic, and natural polymeric materials offer opportunities to overcome different formulative challenges and to design novel dosage forms for controlled release or for site-specific drug delivery. They are extensively used to design therapeutic systems, modify drug release, or mask unpleasant drug taste. Cellulose derivatives are characterized by different physicochemical properties, such as swellability, viscosity, biodegradability, pH dependency, or mucoadhesion, which determine their use in industry. One cellulose derivative with widespread application is ethylcellulose. Ethylcellulose is used in pharmaceutical technology as a coating agent, flavoring fixative, binder, filler, film-former, drug carrier, or stabilizer. The aim of this article is to provide a broad overview of ethylcellulose utilization for pharmaceutical purposes, with particular emphasis on its multidirectional role in the development of oral and topical drug dosage forms. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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41 pages, 11206 KiB

Open AccessReview

CO-Releasing Materials: An Emphasis on Therapeutic Implications, as Release and Subsequent Cytotoxicity Are the Part of Therapy

by Muhammad Faizan, Niaz Muhammad, Kifayat Ullah Khan Niazi, Yongxia Hu, Yanyan Wang, Ya Wu, Huaming Sun, Ruixia Liu, Wensheng Dong, Weiqiang Zhang and Ziwei Gao

Materials 2019, 12(10), 1643; https://doi.org/10.3390/ma12101643 - 20 May 2019

Cited by 46 | Viewed by 6464

Abstract

The CO-releasing materials (CORMats) are used as substances for producing CO molecules for therapeutic purposes. Carbon monoxide (CO) imparts toxic effects to biological organisms at higher concentration. If this characteristic is utilized in a controlled manner, it can act as a cell-signaling agent for important pathological and pharmacokinetic functions; hence offering many new applications and treatments. Recently, research on therapeutic applications using the CO treatment has gained much attention due to its nontoxic nature, and its injection into the human body using several conjugate systems. Mainly, there are two types of CO insertion techniques into the human body, i.e., direct and indirect CO insertion. Indirect CO insertion offers an advantage of avoiding toxicity as compared to direct CO insertion. For the indirect CO inhalation method, developers are facing certain problems, such as its inability to achieve the specific cellular targets and how to control the dosage of CO. To address these issues, researchers have adopted alternative strategies regarded as CO-releasing molecules (CORMs). CO is covalently attached with metal carbonyl complexes (MCCs), which generate various CORMs such as CORM-1, CORM-2, CORM-3, ALF492, CORM-A1 and ALF186. When these molecules are inserted into the human body, CO is released from these compounds at a controlled rate under certain conditions or/and triggers. Such reactions are helpful in achieving cellular level targets with a controlled release of the CO amount. However on the other hand, CORMs also produce a metal residue (termed as i-CORMs) upon degradation that can initiate harmful toxic activity inside the body. To improve the performance of the CO precursor with the restricted development of i-CORMs, several new CORMats have been developed such as micellization, peptide, vitamins, MOFs, polymerization, nanoparticles, protein, metallodendrimer, nanosheet and nanodiamond, etc. In this review article, we shall describe modern ways of CO administration; focusing primarily on exclusive features of CORM’s tissue accumulations and their toxicities. This report also elaborates on the kinetic profile of the CO gas. The comprehension of developmental phases of CORMats shall be useful for exploring the ideal CO therapeutic drugs in the future of medical sciences. Full article

(This article belongs to the Special Issue Advanced Materials in Drug Release and Drug Delivery Systems)

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