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Polymers
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Polymers and Their Role in Drug Delivery
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Polymers and Their Role in Drug Delivery

A special issue of Polymers (ISSN 2073-4360). This special issue belongs to the section "Polymer Applications".

Deadline for manuscript submissions: 30 June 2024 | Viewed by 10287

Special Issue Editors

Dr. Panagiotis Barmpalexis

E-Mail Website
Guest Editor
School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: drug delivery systems; polyesters; controlled drug release; polymeric solid dispersions
Special Issues, Collections and Topics in MDPI journals
Dr. Konstantinos N. Kontogiannopoulos

E-Mail Website
Guest Editor
Laboratory of Organic Chemistry, School of Chemical Engineering, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece
Interests: nanotechnology; natural products; drug delivery systems; pharmaceutical technology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Polymers have played a significant role in improving drug delivery technology, by enabling the administration of therapeutic agents in several ways, such as by improving their solubility, and consequently their bioavailability when administrated orally, releasing them in constant doses over long periods via several routes of administration and achieving adjustable release for both hydrophilic and hydrophobic drugs. In this context, the rational design of polymers made to exert specific biological functions and the urge for customized drug delivery systems is currently the foundation for contemporary advancements in the field.

The in-depth discussion of polymers and the mechanisms of their incorporation into drug-delivery systems is a timely topic in the field of pharmaceutics, and despite the many advances in polymers and drug-delivery systems made over the years, there is still a need for novel, distinctive materials as a result of advancements in medicines.

Therefore, this special issue aims to cover all the latest methods, improvements and advantages concerning the role of polymers in drug delivery systems.

Dr. Panagiotis Barmpalexis
Dr. Konstantinos N. Kontogiannopoulos
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. Polymers 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 2700 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

  • advanced polymeric materials
  • pharmaceutical applications
  • biomedical applications
  • drug delivery systems
  • medical devices
  • polymer theory and modelling

Published Papers (6 papers)

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Research

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21 pages, 7320 KiB  
Article
Evaluation of Suitable Polymeric Matrix/Carriers during Loading of Poorly Water Soluble Drugs onto Mesoporous Silica: Physical Stability and In Vitro Supersaturation
by Afroditi Kapourani, Konstantinos Katopodis, Vasiliki Valkanioti, Melina Chatzitheodoridou, Christos Cholevas and Panagiotis Barmpalexis
Polymers 2024, 16(6), 802; https://doi.org/10.3390/polym16060802 - 13 Mar 2024
Viewed by 667
Abstract
The application of mesoporous carriers in formulations of amorphous solid dispersions (ASDs) has been suggested to enhance the stability of amorphous drugs. However, mesoporous carriers do not demonstrate satisfactory inhibitory effects on the precipitation of active pharmaceutical ingredients (APIs), and the inclusion of [...] Read more.
The application of mesoporous carriers in formulations of amorphous solid dispersions (ASDs) has been suggested to enhance the stability of amorphous drugs. However, mesoporous carriers do not demonstrate satisfactory inhibitory effects on the precipitation of active pharmaceutical ingredients (APIs), and the inclusion of an appropriate polymer within ASDs becomes imperative to maintaining drug supersaturation. The aim of this study was to evaluate ternary olanzapine (OLN) ASDs with Syloid 244FP and to find an appropriate polymeric carrier. The polymer’s selection criteria were based on the physical stability of the ASDs and the release rate of the drug from the systems. The polymers investigated were hydroxypropylmethyl cellulose (HPMC) and copovidone (coPVP). The formation of ASDs was achievable in all investigated cases, as demonstrated by the complete lack of crystallinity confirmed through both powder X-ray diffraction (pXRD) analysis and differential scanning calorimetry (DSC) for all developed formulations. The solvent shift method was employed to evaluate the ability of the studied carriers to inhibit the precipitation of supersaturated OLN. coPVP emerged as a more suitable precipitation inhibitor compared with HPMC and Syloid 244 FP. Subsequently, in vitro dissolution studies under non-sink conditions revealed a higher degree of supersaturation in ternary systems where coPVP was used as a polymeric carrier, as these systems exhibited, under the examined conditions, up to a 2-fold increase in the released OLN compared with the pure crystalline drug. Moreover, stability studies conducted utilizing pXRD demonstrated that ternary formulations incorporating coPVP and Syloid 244 FP maintained stability for an extended period of 8 months. In contrast, binary systems exhibited a comparatively shorter stability duration, indicating the synergistic effect of coPVP and Syloid 244 FP on the physical stability of the amorphous API. Attenuated total reflectance–Fourier transform infrared (ATR-FTIR) studies showed that the development of stronger molecular interactions can be provided as an explanation for this synergistic effect, as the formation of robust H-bonds may be considered responsible for inhibiting the precipitation of the supersaturated API. Therefore, the incorporation of coPVP into OLN ASDs with Syloid 244 FP is considered a highly promising technique for increasing the degree of OLN supersaturation in in vitro dissolution studies and improving the stability of systems. Full article
(This article belongs to the Special Issue Polymers and Their Role in Drug Delivery)
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17 pages, 4107 KiB  
Article
Engineered Shellac Beads-on-the-String Fibers Using Triaxial Electrospinning for Improved Colon-Targeted Drug Delivery
by Yaoyao Yang, Wei Chen, Menglong Wang, Jiachen Shen, Zheng Tang, Yongming Qin and Deng-Guang Yu
Polymers 2023, 15(10), 2237; https://doi.org/10.3390/polym15102237 - 09 May 2023
Cited by 13 | Viewed by 2094
Abstract
Colon-targeted drug delivery is gradually attracting attention because it can effectively treat colon diseases. Furthermore, electrospun fibers have great potential application value in the field of drug delivery because of their unique external shape and internal structure. In this study, a core layer [...] Read more.
Colon-targeted drug delivery is gradually attracting attention because it can effectively treat colon diseases. Furthermore, electrospun fibers have great potential application value in the field of drug delivery because of their unique external shape and internal structure. In this study, a core layer of hydrophilic polyethylene oxide (PEO) and the anti-colon-cancer drug curcumin (CUR), a middle layer of ethanol, and a sheath layer of the natural pH-sensitive biomaterial shellac were used in a modified triaxial electrospinning process to prepare beads-on-the-string (BOTS) microfibers. A series of characterizations were carried out on the obtained fibers to verify the process–shape/structure–application relationship. The results of scanning electron microscopy and transmission electron microscopy indicated a BOTS shape and core–sheath structure. X-ray diffraction results indicated that the drug in the fibers was in an amorphous form. Infrared spectroscopy revealed the good compatibility of the components in the fibers. In vitro drug release revealed that the BOTS microfibers provide colon-targeted drug delivery and zero-order drug release. Compared to linear cylindrical microfibers, the obtained BOTS microfibers can prevent the leakage of drugs in simulated gastric fluid, and they provide zero-order release in simulated intestinal fluid because the beads in BOTS microfibers can act as drug reservoirs. Full article
(This article belongs to the Special Issue Polymers and Their Role in Drug Delivery)
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12 pages, 2966 KiB  
Article
Single-Micelle-Templated Synthesis of Hollow Barium Carbonate Nanoparticle for Drug Delivery
by Bishnu Prasad Bastakoti, Nischal Bhattarai, Moses D. Ashie, Felix Tettey, Shin-ichi Yusa and Kenichi Nakashima
Polymers 2023, 15(7), 1739; https://doi.org/10.3390/polym15071739 - 31 Mar 2023
Cited by 5 | Viewed by 1311
Abstract
A laboratory-synthesized triblock copolymer poly(ethylene oxide-b-acrylic acid-b-styrene) (PEG-PAA-PS) was used as a template to synthesize hollow BaCO3 nanoparticles (BC-NPs). The triblock copolymer was synthesized using reversible addition–fragmentation chain transfer radical polymerization. The triblock copolymer has a molecular weight [...] Read more.
A laboratory-synthesized triblock copolymer poly(ethylene oxide-b-acrylic acid-b-styrene) (PEG-PAA-PS) was used as a template to synthesize hollow BaCO3 nanoparticles (BC-NPs). The triblock copolymer was synthesized using reversible addition–fragmentation chain transfer radical polymerization. The triblock copolymer has a molecular weight of 1.88 × 104 g/mol. Transmission electron microscopy measurements confirm the formation of spherical micelles with a PEG corona, PAA shell, and PS core in an aqueous solution. Furthermore, the dynamic light scattering experiment revealed the electrostatic interaction of Ba2+ ions with an anionic poly(acrylic acid) block of the micelles. The controlled precipitation of BaCO3 around spherical polymeric micelles followed by calcination allows for the synthesis of hollow BC-NPs with cavity diameters of 15 nm and a shell thickness of 5 nm. The encapsulation and release of methotrexate from hollow BC-NPs at pH 7.4 was studied. The cell viability experiments indicate the possibility of BC-NPs maintaining biocompatibility for a prolonged time. Full article
(This article belongs to the Special Issue Polymers and Their Role in Drug Delivery)
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16 pages, 3654 KiB  
Article
A Micro-In-Macro Gastroretentive System for the Delivery of Narrow-Absorption Window Drugs
by Mershen Govender, Thankhoe A. Rants’o and Yahya E. Choonara
Polymers 2023, 15(6), 1385; https://doi.org/10.3390/polym15061385 - 10 Mar 2023
Cited by 1 | Viewed by 1629
Abstract
A micro-in-macro gastroretentive and gastrofloatable drug delivery system (MGDDS), loaded with the model-drug ciprofloxacin, was developed in this study to address the limitations commonly experienced in narrow-absorption window (NAW) drug delivery. The MGDDS, which consists of microparticles loaded in a gastrofloatable macroparticle (gastrosphere) [...] Read more.
A micro-in-macro gastroretentive and gastrofloatable drug delivery system (MGDDS), loaded with the model-drug ciprofloxacin, was developed in this study to address the limitations commonly experienced in narrow-absorption window (NAW) drug delivery. The MGDDS, which consists of microparticles loaded in a gastrofloatable macroparticle (gastrosphere) was designed to modify the release of ciprofloxacin, allowing for an increased drug absorption via the gastrointestinal tract. The prepared inner microparticles (1–4 µm) were formed by crosslinking chitosan (CHT) and Eudragit® RL 30D (EUD), with the outer gastrospheres prepared from alginate (ALG), pectin (PEC), poly(acrylic acid) (PAA) and poly(lactic-co-glycolic) acid (PLGA). An experimental design was utilized to optimize the prepared microparticles prior to Fourier Transition Infrared (FTIR) spectroscopy, Scanning Electron Microscopy (SEM) and in vitro drug release studies. Additionally, the in vivo analysis of the MGDDS, employing a Large White Pig model and molecular modeling of the ciprofloxacin-polymer interactions, were performed. The FTIR results determined that the crosslinking of the respective polymers in the microparticle and gastrosphere was achieved, with the SEM analysis detailing the size of the microparticles formed and the porous nature of the MGDDS, which is essential for drug release. The in vivo drug release analysis results further displayed a more controlled ciprofloxacin release profile over 24 h and a greater bioavailability for the MGDDS when compared to the marketed immediate-release ciprofloxacin product. Overall, the developed system successfully delivered ciprofloxacin in a control-release manner and enhanced its absorption, thereby displaying the potential of the system to be used in the delivery of other NAW drugs. Full article
(This article belongs to the Special Issue Polymers and Their Role in Drug Delivery)
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21 pages, 3211 KiB  
Article
Formulation and Characterization of Fe3O4@PEG Nanoparticles Loaded Sorafenib; Molecular Studies and Evaluation of Cytotoxicity in Liver Cancer Cell Lines
by Mona Ebadi, Ahmad Rifqi Md Zain, Tengku Hasnan Tengku Abdul Aziz, Hossein Mohammadi, Clarence Augustine TH Tee and Muhammad Rahimi Yusop
Polymers 2023, 15(4), 971; https://doi.org/10.3390/polym15040971 - 16 Feb 2023
Cited by 5 | Viewed by 2533
Abstract
Iron oxide nanoparticles are one of the nanocarriers that are suitable for novel drug delivery systems due to low toxicity, biocompatibility, loading capacity, and controlled drug delivery to cancer cells. The purpose of the present study is the synthesis of coated iron oxide [...] Read more.
Iron oxide nanoparticles are one of the nanocarriers that are suitable for novel drug delivery systems due to low toxicity, biocompatibility, loading capacity, and controlled drug delivery to cancer cells. The purpose of the present study is the synthesis of coated iron oxide nanoparticles for the delivery of sorafenib (SFB) and its effects on cancer cells. In this study, Fe3O4 nanoparticles were synthesized by the co-precipitation method, and then sorafenib was loaded onto PEG@Fe3O4 nanoparticles. FTIR was used to ensure polyethylene glycol (PEG) binding to nanoparticles and loading the drug onto the nanoshells. A comparison of the mean size and the crystalline structure of nanoparticles was performed by TEM, DLS, and X-ray diffraction patterns. Then, cell viability was obtained by the MTT assay for 3T3 and HepG2 cell lines. According to FT-IR results, the presence of O–H and C–H bands at 3427 cm–1 and 1420 cm–1 peak correlate with PEG binding to nanoparticles. XRD pattern showed the cubic spinel structure of trapped magnetite nanoparticles carrying medium. The magnetic properties of nanoparticles were examined by a vibrating-sample magnetometer (VSM). IC50 values at 72 h for treatment with carriers of Fe3O4@PEG nanoparticle for the HepG2 cell line was 15.78 μg/mL (p < 0.05). This study showed that Fe3O4 nanoparticles coated by polyethylene glycol and using them in the drug delivery process could be beneficial for increasing the effect of sorafenib on cancer cells. Full article
(This article belongs to the Special Issue Polymers and Their Role in Drug Delivery)
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Review

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22 pages, 700 KiB  
Review
Stabilization of Essential Oil: Polysaccharide-Based Drug Delivery System with Plant-like Structure Based on Biomimetic Concept
by Xue-Yee Lim, Jing Li, Hong-Mei Yin, Mu He, Ling Li and Tong Zhang
Polymers 2023, 15(16), 3338; https://doi.org/10.3390/polym15163338 - 08 Aug 2023
Cited by 2 | Viewed by 1421
Abstract
Essential oils (EOs) have stability problems, including volatility, oxidation, photosensitivity, heat sensitivity, humidity sensitivity, pH sensitivity, and ion sensitivity. A drug delivery system is an effective way to stabilize EOs, especially due to the protective effect of polymeric drug carriers. Polysaccharides are frequently [...] Read more.
Essential oils (EOs) have stability problems, including volatility, oxidation, photosensitivity, heat sensitivity, humidity sensitivity, pH sensitivity, and ion sensitivity. A drug delivery system is an effective way to stabilize EOs, especially due to the protective effect of polymeric drug carriers. Polysaccharides are frequently employed as drug carrier materials because they are highly safe, come in a variety of forms, and have plentiful sources. Interestingly, the EO drug delivery system is based on the biomimetic concept since it corresponds to the structure of plant tissue. In this paper, we associate the biomimetic plant-like structures of the EO drug delivery system with the natural forms of EO in plant tissues, and summarize the characteristics of polysaccharide-based drug carriers for EO protection. Thus, we highlight the research progress on polysaccharides and their modified materials, including gum arabic, starch, cellulose, chitosan, sodium alginate, pectin, and pullulan, and their use as biomimetic drug carriers for EO preparations due to their abilities and potential for EO protection. Full article
(This article belongs to the Special Issue Polymers and Their Role in Drug Delivery)
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