Polymers for Designing Drug Delivery Systems

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

Deadline for manuscript submissions: closed (1 August 2023) | Viewed by 12788

Special Issue Editors


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Guest Editor
1. Department of Science and Engineereing of Oxide Materials and Nanomaterials, Faculty of Applied Chemistry and Materials Science, Politehnica University of Bucharest, RO-011061 Bucharest, Romania
2. National Research Center for Micro and Nanomaterials, University Politehnica of Bucharest, 060042 Bucharest, Romania
3. Academy of Romanian Scientists, 3 Ilfov Street, Bucharest, Romania
Interests: synthesis and characterization of nano and biomaterials
Special Issues, Collections and Topics in MDPI journals

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Guest Editor Assistant
1. Department of Science and Engineereing of Oxide Materials and Nanomaterials, Faculty of Applied Chemistry and Materials Science, Politehnica University of Bucharest, RO-011061 Bucharest, Romania
2. National Research Center for Micro and Nanomaterials, University Politehnica of Bucharest, 060042 Bucharest, Romania
Interests: synthesis and characterization of nanobiomaterials; polymers; pharmaceutical nanotechnology
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Owing to their highly versatile nature, in terms of physico-chemical, mechanical and biological properties, polymers have been extensively used in a plethora of applications. Among these applications, the design and development of drug delivery systems represents an essential direction, due to their biocompatibility and biodegradability. Moreover, they allow for the encapsulation of a wide variety of drug molecules with different affinities for water and lipids, which further enables the modulation of drug biodistribution, absorption and release. Aside from being used as drug delivery vehicles, numerous synthetic and natural polymers have demonstrated bioactivities when applied in biological systems, such as antimicrobial, antioxidant, anticancer and regenerative behaviors. Therefore, this field is continuously expanding and evolving towards the improvement of the currently available drug formulations. 

Thus, this Special Issue on “Polymers for Designing Drug Delivery Systems” aims to create a broad collection of the most recent and advanced research articles and comprehensive reviews on the topic of polymers, regarding the controlled release of biologically active molecules, in order to further contribute to the progress in the biomedical field.

Prof. Dr. Ecaterina Andronescu
Guest Editor
Cristina Chircov
Guest Editor Assistant

Manuscript Submission Information

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Keywords

  • drug delivery systems
  • antimicrobial therapies and biofilm modulation
  • core–shell systems
  • tissue engineering and regeneration
  • biopolymeric blends
  • smart biopolymers
  • wound dressings

Published Papers (6 papers)

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Research

20 pages, 6294 KiB  
Article
Nanocarrier of α-Tocopheryl Succinate Based on a Copolymer Derivative of (4,7-dichloroquinolin-2-yl)methanol and Its Cytotoxicity against a Breast Cancer Cell Line
by Hernán Valle, Raquel Palao-Suay, María Rosa Aguilar, Tulio A. Lerma, Manuel Palencia, Ramalinga Viswanathan Mangalaraja, Leonardo Guzmán, Dairo Pérez Sotelo and José Becerra
Polymers 2023, 15(22), 4342; https://doi.org/10.3390/polym15224342 - 07 Nov 2023
Viewed by 989
Abstract
In order to improve the water solubility and, therefore, bioavailability and therapeutic activity of anticancer hydrophobic drug α-tocopherol succinate (α-TOS), in this work, copolymers were synthesized via free radicals from QMES (1-[4,7-dichloroquinolin-2-ylmethyl]-4-methacryloyloxyethyl succinate) and VP (N-vinyl-2-pirrolidone) using different molar ratios, and were used [...] Read more.
In order to improve the water solubility and, therefore, bioavailability and therapeutic activity of anticancer hydrophobic drug α-tocopherol succinate (α-TOS), in this work, copolymers were synthesized via free radicals from QMES (1-[4,7-dichloroquinolin-2-ylmethyl]-4-methacryloyloxyethyl succinate) and VP (N-vinyl-2-pirrolidone) using different molar ratios, and were used to nanoencapsulate and deliver α-TOS into cancer cells MCF-7. QMES monomer was chosen because the QMES pendant group in the polymer tends to hydrolyze to form free 4,7-dichloro-2-quinolinemethanol (QOH), which also, like α-TOS, exhibit anti-proliferative effects on cancerous cells. From the QMES-VP 30:70 (QMES-30) and 40:60 (QMES-40) copolymers obtained, it was possible to prepare aqueous suspensions of empty nanoparticles (NPs) loaded with α-TOS by nanoprecipitation. The diameter and encapsulation efficiency (%EE) of the QMES-30 NPs loaded with α-TOS were 128.6 nm and 52%; while for the QMES-40 NPs loaded with α-TOS, they were 148.8 nm and 65%. The results of the AlamarBlue assay at 72 h of treatment show that empty QMES-30 NPs (without α-TOS) produced a marked cytotoxic effect on MCF-7 breast cancer cells, corresponding to an IC50 value of 0.043 mg mL−1, and importantly, they did not exhibit cytotoxicity against healthy HUVEC cells. Furthermore, NP-QMES-40 loaded with α-TOS were cytotoxic with an IC50 value of 0.076 mg mL−1, demonstrating a progressive release of α-TOS; however, the latter nanoparticles were also cytotoxic to healthy cells in the range of the assayed concentrations. These results contribute to the search for a new polymeric nanocarrier of QOH, α-TOS or other hydrophobic drugs for the treatment of cancer or others diseases treatable with these drugs. Full article
(This article belongs to the Special Issue Polymers for Designing Drug Delivery Systems)
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17 pages, 4232 KiB  
Article
Development and Characterization of Drug Loaded PVA/PCL Fibres for Wound Dressing Applications
by Ali Afzal, Mohammed Jalalah, Abid Noor, Zubair Khaliq, Muhammad Bilal Qadir, Rashid Masood, Ahsan Nazir, Sheraz Ahmad, Faheem Ahmad, Muhammad Irfan, Munazza Afzal, Mohd Faisal, Saeed A. Alsareii and Farid A. Harraz
Polymers 2023, 15(6), 1355; https://doi.org/10.3390/polym15061355 - 08 Mar 2023
Cited by 9 | Viewed by 2048
Abstract
Nowadays, synthetic polymers are used in medical applications due to their special biodegradable, biocompatible, hydrophilic, and non-toxic properties. The materials, which can be used for wound dressing fabrication with controlled drug release profile, are the need of the time. The main aim of [...] Read more.
Nowadays, synthetic polymers are used in medical applications due to their special biodegradable, biocompatible, hydrophilic, and non-toxic properties. The materials, which can be used for wound dressing fabrication with controlled drug release profile, are the need of the time. The main aim of this study was to develop and characterize polyvinyl alcohol/polycaprolactone (PVA/PCL) fibres containing a model drug. A dope solution comprising PVA/PCL with the drug was extruded into a coagulation bath and became solidified. The developed PVA/PCL fibres were then rinsed and dried. These fibres were tested for Fourier transform infrared spectroscopy, linear density, topographic analysis, tensile properties, liquid absorption, swelling behaviour, degradation, antimicrobial activity, and drug release profile for improved and better healing of the wound. From the results, it was concluded that PVA/PCL fibres containing a model drug can be produced by using the wet spinning technique and have respectable tensile properties; adequate liquid absorption, swelling %, and degradation %; and good antimicrobial activity with the controlled drug release profile of the model drug for wound dressing applications. Full article
(This article belongs to the Special Issue Polymers for Designing Drug Delivery Systems)
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20 pages, 4929 KiB  
Article
Release of Tretinoin Solubilized in Microemulsion from Carbopol and Xanthan Gel: In Vitro versus Ex Vivo Permeation Study
by Miroslava Špaglová, Martina Papadakos, Mária Čuchorová and Desana Matušová
Polymers 2023, 15(2), 329; https://doi.org/10.3390/polym15020329 - 09 Jan 2023
Cited by 6 | Viewed by 2141
Abstract
Background: Tretinoin (TRE) is, for its anti-comedogenic and comedolytic activity, widely used in the topical treatment of acne vulgaris. The effect lies in the regulation of sebum production and collagen synthesis. The study is devoted to the formulation of dermal gels containing TRE [...] Read more.
Background: Tretinoin (TRE) is, for its anti-comedogenic and comedolytic activity, widely used in the topical treatment of acne vulgaris. The effect lies in the regulation of sebum production and collagen synthesis. The study is devoted to the formulation of dermal gels containing TRE using microemulsion as the drug solubilizer. Methods: The aim was to evaluate the effect of the reference microemulsion (ME) and lecithin-containing microemulsion (MEL) on the release of TRE through the synthetic membrane (in vitro) and the pig’s ear skin (ex vivo) through the Franz cell diffusion method. Subsequently, after an ex vivo study, the amount of the drug in the skin influenced by the applied formulation was determined. In addition, the impact of ME on the microscopic structure, texture, and rheological properties of gels was evaluated. Results: On the basis of the analysis of texture, rheological properties, and drug release studies, Carbopol formulations appear to be more appropriate and stable. Considering the synthetic membrane as a stratum corneum, the Carbopol gel penetrated about 2.5-higher amounts of TRE compared to the Xanthan gel. In turn, ex vivo studies suggest that MEL slows the drug transfer to the dissolution medium, simulating absorption into the blood, which is a desirable effect in local treatment. The drug retention study proved the highest amounts of TRE in the skin to which microemulsion-Carbopol formulations were applied. Conclusion: The results confirm the benefit of TRE solubilization in ME due to its bioavailability from the tested dermal formulations. Full article
(This article belongs to the Special Issue Polymers for Designing Drug Delivery Systems)
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15 pages, 8692 KiB  
Article
Assessing the In Vivo Biocompatibility of Molecularly Imprinted Polymer Nanoparticles
by Samr Kassem, Stanislav S. Piletsky, Hasan Yesilkaya, Ozcan Gazioglu, Medhanie Habtom, Francesco Canfarotta, Elena Piletska, Alan C. Spivey, Eric O. Aboagye and Sergey A. Piletsky
Polymers 2022, 14(21), 4582; https://doi.org/10.3390/polym14214582 - 28 Oct 2022
Cited by 4 | Viewed by 2078
Abstract
Molecularly imprinted polymer nanoparticles (nanoMIPs) are high affinity synthetic receptors which show promise as imaging and therapeutic agents. Comprehensive analysis of the in vivo behaviour of nanoMIPs must be performed before they can be considered for clinical applications. This work reports the solid-phase [...] Read more.
Molecularly imprinted polymer nanoparticles (nanoMIPs) are high affinity synthetic receptors which show promise as imaging and therapeutic agents. Comprehensive analysis of the in vivo behaviour of nanoMIPs must be performed before they can be considered for clinical applications. This work reports the solid-phase synthesis of nanoMIPs and an investigation of their biodistribution, clearance and cytotoxicity in a rat model following both intravenous and oral administration. These nanoMIPs were found in each harvested tissue type, including brain tissue, implying their ability to cross the blood–brain barrier. The nanoMIPs were cleared from the body via both faeces and urine. Furthermore, we describe an immunogenicity study in mice, demonstrating that nanoMIPs specific for a cell surface protein showed moderate adjuvant properties, whilst those imprinted for a scrambled peptide showed no such behaviour. Given their ability to access all tissue types and their relatively low cytotoxicity, these results pave the way for in vivo applications of nanoMIPs. Full article
(This article belongs to the Special Issue Polymers for Designing Drug Delivery Systems)
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12 pages, 7060 KiB  
Article
3D Multicellular Tumor Spheroids in a Microfluidic Droplet System for Investigation of Drug Resistance
by Sang Ik Lee, Yoon Young Choi, Seong Goo Kang, Tae Hyeon Kim, Ji Wook Choi, Young Jae Kim, Tae-Hyung Kim, Taewook Kang and Bong Geun Chung
Polymers 2022, 14(18), 3752; https://doi.org/10.3390/polym14183752 - 08 Sep 2022
Cited by 8 | Viewed by 2574
Abstract
A three-dimensional (3D) tumor spheroid model plays a critical role in mimicking tumor microenvironments in vivo. However, the conventional culture methods lack the ability to manipulate the 3D tumor spheroids in a homogeneous manner. To address this limitation, we developed a microfluidic-based droplet [...] Read more.
A three-dimensional (3D) tumor spheroid model plays a critical role in mimicking tumor microenvironments in vivo. However, the conventional culture methods lack the ability to manipulate the 3D tumor spheroids in a homogeneous manner. To address this limitation, we developed a microfluidic-based droplet system for drug screening applications. We used a tree-shaped gradient generator to control the cell density and encapsulate the cells within uniform-sized droplets to generate a 3D gradient-sized tumor spheroid. Using this microfluidic-based droplet system, we demonstrated the high-throughput generation of uniform 3D tumor spheroids containing various cellular ratios for the analysis of the anti-cancer drug cytotoxicity. Consequently, this microfluidic-based gradient droplet generator could be a potentially powerful tool for anti-cancer drug screening applications. Full article
(This article belongs to the Special Issue Polymers for Designing Drug Delivery Systems)
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22 pages, 5521 KiB  
Article
An Investigation for Skin Tissue Regeneration Enhancement/Augmentation by Curcumin-Loaded Self-Emulsifying Drug Delivery System (SEDDS)
by Saima Mahmood, Prapanna Bhattarai, Nauman Rahim Khan, Zakia Subhan, Ghulam Razaque, Hassan A. Albarqi, Abdulsalam A. Alqahtani, Ali Alasiri and Lin Zhu
Polymers 2022, 14(14), 2904; https://doi.org/10.3390/polym14142904 - 17 Jul 2022
Cited by 5 | Viewed by 1929
Abstract
Diabetes, one of the global metabolic disorders, is often associated with delayed wound healing due to the elevated level of free radicals at the wound site, which hampers skin regeneration. This study aimed at developing a curcumin-loaded self-emulsifying drug delivery system (SEDDS) for [...] Read more.
Diabetes, one of the global metabolic disorders, is often associated with delayed wound healing due to the elevated level of free radicals at the wound site, which hampers skin regeneration. This study aimed at developing a curcumin-loaded self-emulsifying drug delivery system (SEDDS) for diabetic wound healing and skin tissue regeneration. For this purpose, various curcumin-loaded SEDDS formulations were prepared and optimized. Then, the SEDDS formulations were characterized by the emulsion droplet size, surface charge, drug content/entrapment efficiency, drug release, and stability. In vitro, the formulations were assessed for the cellular uptake, cytotoxicity, cell migration, and inhibition of the intracellular ROS production in the NIH3T3 fibroblasts. In vivo, the formulations’ wound healing and skin regeneration potential were evaluated on the induced diabetic rats. The results indicated that, after being dispersed in the aqueous medium, the optimized SEDDS formulation was readily emulsified and formed a homogenous dispersion with a droplet size of 37.29 ± 3.47 nm, surface charge of −20.75 ± 0.07 mV, and PDI value of less than 0.3. The drug content in the optimized formulation was found to be 70.51% ± 2.31%, with an encapsulation efficiency of 87.36% ± 0.61%. The SEDDS showed a delayed drug release pattern compared to the pure drug solution, and the drug release rate followed the Fickian diffusion kinetically. In the cell culture, the formulations showed lower cytotoxicity, higher cellular uptake, and increased ROS production inhibition, and promoted the cell migration in the scratch assay compared to the pure drug. The in vivo data indicated that the curcumin-loaded SEDDS-treated diabetic rats had significantly faster-wound healing and re-epithelialization compared with the untreated and pure drug-treated groups. Our findings in this work suggest that the curcumin-loaded SEDDS might have great potential in facilitating diabetic wound healing and skin tissue regeneration. Full article
(This article belongs to the Special Issue Polymers for Designing Drug Delivery Systems)
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