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Pharmaceutics
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Stimuli-Responsive Nanomedicine for the Effective and Controlled Delivery of Drug...
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Stimuli-Responsive Nanomedicine for the Effective and Controlled Delivery of Drug Molecules to the Tumor Microenvironment

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Nanomedicine and Nanotechnology".

Deadline for manuscript submissions: closed (20 November 2023) | Viewed by 18987

Special Issue Editor

Prof. Dr. Jonghoon Choi

E-Mail Website
Guest Editor
Department of Biomedical Engineering, School of Integrative Engineering, College of ICT Engineering, Chung-Ang University, Seoul 06974, Republic of Korea
Interests: nanomedicine; biosensor; theragnostics; drug delivery; nanobiomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Novel technologies are emerging for the externally controlled release and engineering of nanomedicines. In particular, technologies to quickly activate nanobiomaterials and effectively control the release of drugs are critical. Therefore, high-throughput screening and analyses of drug delivery by nanocarriers as well as their control in the tumor microenvironment by the external use of electromagnetic, thermal, and optical stimuli have become increasingly relevant. At the same time, new tools and instruments exciting target biomolecules in body tissues are also being developed. The achievement of these goals requires a detailed study of nanobiomaterials and the development of external stimuli-responsive drug delivery and controlled-release systems, as well as of assays for determining the function, properties, fate of the targeted cells. This Special Issue will highlight the current state-of-the-art technologies for the development of external stimuli-responsive nanocarriers for drug delivery as well as the most up-to-date technologies for the controlled release of drugs in the tumor microenvironment. These methods would also suggest prospects for optimizing techniques to achieve precise control and engineering of nanocarriers. This Special Issue will collect a series of research articles and review papers on these topics.

Prof. Dr. Jonghoon Choi
Guest Editor

Manuscript Submission Information

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Keywords

  • drug delivery
  • nanocarriers
  • nanomedicine
  • external stimuli
  • tumor microenvironment

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Published Papers (4 papers)

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Research

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16 pages, 28938 KiB  
Article
Redox-Responsive Polymersomes as Smart Doxorubicin Delivery Systems
by Carmen Ferrero, Marta Casas and Isidoro Caraballo
Pharmaceutics 2022, 14(8), 1724; https://doi.org/10.3390/pharmaceutics14081724 - 18 Aug 2022
Cited by 10 | Viewed by 2432
Abstract
Stimuli-responsive polymersomes have emerged as smart drug delivery systems for programmed release of highly cytotoxic anticancer agents such as doxorubicin hydrochloride (Dox·HCl). Recently, a biodegradable redox-responsive triblock copolymer (mPEG–PDH–mPEG) was synthesized with a central hydrophobic block containing disulfide linkages and two hydrophilic segments [...] Read more.
Stimuli-responsive polymersomes have emerged as smart drug delivery systems for programmed release of highly cytotoxic anticancer agents such as doxorubicin hydrochloride (Dox·HCl). Recently, a biodegradable redox-responsive triblock copolymer (mPEG–PDH–mPEG) was synthesized with a central hydrophobic block containing disulfide linkages and two hydrophilic segments of poly(ethylene glycol) methyl ether. Taking advantage of the self-assembly of this amphiphilic copolymer in aqueous solution, in the present investigation we introduce a solvent-exchange method that simultaneously achieves polymersome formation and drug loading in phosphate buffer saline (10 mM, pH 7.4). Blank and drug-loaded polymersomes (5 and 10 wt.% feeding ratios) were prepared and characterized for morphology, particle size, surface charge, encapsulation efficiency and drug release behavior. Spherical vesicles of uniform size (120–190 nm) and negative zeta potentials were obtained. Dox·HCl was encapsulated into polymersomes with a remarkably high efficiency (up to 98 wt.%). In vitro drug release studies demonstrated a prolonged and diffusion-driven release at physiological conditions (~34% after 48 h). Cleavage of the disulfide bonds in the presence of 50 mM glutathione (GSH) enhanced drug release (~77%) due to the contribution of the erosion mechanism. Therefore, the designed polymersomes are promising candidates for selective drug release in the reductive environment of cancer cells. Full article
(This article belongs to the Special Issue Stimuli-Responsive Nanomedicine for the Effective and Controlled Delivery of Drug Molecules to the Tumor Microenvironment)
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18 pages, 3992 KiB  
Article
Combinatorial Inhibition of Cell Surface Receptors Using Dual Aptamer-Functionalized Nanoconstructs for Cancer Treatment
by Hyojin Lee, Tae Hee Kim, Daechan Park, Mihue Jang, Justin J. Chung, Soo Hyun Kim, Sang-Heon Kim, Kwan Hyi Lee, Youngmee Jung and Seung Ja Oh
Pharmaceutics 2020, 12(7), 689; https://doi.org/10.3390/pharmaceutics12070689 - 21 Jul 2020
Cited by 4 | Viewed by 3037
Abstract
Membrane receptors overexpressed in diseased states are considered novel therapeutic targets. However, the single targeting approach faces several fundamental issues, such as poor efficacy, resistance, and toxicity. Here, we report a dual-targeting strategy to enhance anti-cancer efficacy via synergistic proximity interactions between therapeutics [...] Read more.
Membrane receptors overexpressed in diseased states are considered novel therapeutic targets. However, the single targeting approach faces several fundamental issues, such as poor efficacy, resistance, and toxicity. Here, we report a dual-targeting strategy to enhance anti-cancer efficacy via synergistic proximity interactions between therapeutics and two receptor proteins. Importantly, we report the first finding of an interaction between c-Met and nucleolin and demonstrate the therapeutic value of targeting the interaction between them. Bispecific nanocarriers densely grafted with anti-c-Met and -nucleolin aptamer increased the local concentration of aptamers at the target sites, in addition to inducing target receptor clustering. It was also demonstrated that the simultaneous targeting of c-Met and nucleolin inhibited the cellular functions of the receptors and increased anti-cancer efficacy by altering the cell cycle. Our findings pave the way for the development of an effective combinatorial treatment based on nanoconstruct-mediated interaction between receptors. Full article
(This article belongs to the Special Issue Stimuli-Responsive Nanomedicine for the Effective and Controlled Delivery of Drug Molecules to the Tumor Microenvironment)
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18 pages, 4454 KiB  
Article
NIR Laser-Responsive PNIPAM and Gold Nanorod Composites for the Engineering of Thermally Reactive Drug Delivery Nanomedicine
by Yejin Kwon, Yonghyun Choi, Jaehee Jang, Semi Yoon and Jonghoon Choi
Pharmaceutics 2020, 12(3), 204; https://doi.org/10.3390/pharmaceutics12030204 - 27 Feb 2020
Cited by 19 | Viewed by 4759
Abstract
When ingesting a drug on its own or injecting it directly into tissue, its concentration increases immediately within the body, which often exacerbates the side effects and increases its toxicity. To solve this problem, we synthesized the thermally reactive polymer poly(N-isopropylacrylamide) [...] Read more.
When ingesting a drug on its own or injecting it directly into tissue, its concentration increases immediately within the body, which often exacerbates the side effects and increases its toxicity. To solve this problem, we synthesized the thermally reactive polymer poly(N-isopropylacrylamide) (PNIPAM) using reversible addition–fragmentation chain transfer (RAFT) polymerization and prepared nanocarriers by binding PNIPAM to gold nanorods (GRs), with the anticancer agent doxorubicin (DOX) used as a model drug. PNIPAM changes from hydrophilic to hydrophobic at temperatures above its lower critical solution temperature, which represents a coil-to-globule volume phase transition. Because GRs absorb near-infrared (NIR) laser light and emit energy, PNIPAM aggregation occurs when the synthesized PNIPAM/GR are subjected to an NIR laser, and the temperature of the GRs rises. Using this principle, DOX was combined with the PNIPAM/GR complex, and the resulting anticancer effects with and without laser treatment were observed in Hela and MDA-MB-231 cells. In our proposed complex, the GR binding rate of PNIPAM reached 20% and the DOX binding rate reached 15%. The release profile of the drug following laser irradiation was determined using a drug release test and confocal microscopy imaging. It was subsequently confirmed that the release of the drug is higher at higher temperatures, especially with laser treatment. The proposed combination of temperature-reactive polymers and gold nanostructures shows promise for future research into controlled drug release. Full article
(This article belongs to the Special Issue Stimuli-Responsive Nanomedicine for the Effective and Controlled Delivery of Drug Molecules to the Tumor Microenvironment)
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Review

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19 pages, 2926 KiB  
Review
Stimuli-Responsive Nanomaterials for Application in Antitumor Therapy and Drug Delivery
by Son H. Pham, Yonghyun Choi and Jonghoon Choi
Pharmaceutics 2020, 12(7), 630; https://doi.org/10.3390/pharmaceutics12070630 - 4 Jul 2020
Cited by 133 | Viewed by 7705
Abstract
The new era of nanotechnology has produced advanced nanomaterials applicable to various fields of medicine, including diagnostic bio-imaging, chemotherapy, targeted drug delivery, and biosensors. Various materials are formed into nanoparticles, such as gold nanomaterials, carbon quantum dots, and liposomes. The nanomaterials have been [...] Read more.
The new era of nanotechnology has produced advanced nanomaterials applicable to various fields of medicine, including diagnostic bio-imaging, chemotherapy, targeted drug delivery, and biosensors. Various materials are formed into nanoparticles, such as gold nanomaterials, carbon quantum dots, and liposomes. The nanomaterials have been functionalized and widely used because they are biocompatible and easy to design and prepare. This review mainly focuses on nanomaterials responsive to the external stimuli used in drug-delivery systems. To overcome the drawbacks of conventional therapeutics to a tumor, the dual- and multi-responsive behaviors of nanoparticles have been harnessed to improve efficiency from a drug delivery point of view. Issues and future research related to these nanomaterial-based stimuli sensitivities and the scope of stimuli-responsive systems for nanomedicine applications are discussed. Full article
(This article belongs to the Special Issue Stimuli-Responsive Nanomedicine for the Effective and Controlled Delivery of Drug Molecules to the Tumor Microenvironment)
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