Advances in Nanocarriers for Drug Delivery and Targeting

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

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 19014

Special Issue Editors


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Guest Editor
Institute of Biosciences and Applications, National Centre for Scientific Research “Demokritos”, 15310 Athens, Greece
Interests: nano-sized systems; drug encapsulation and delivery; drug targeting; surface functionalization; material characterization; controlled release; natural products; metal complexes; radiopharmaceuticals
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Guest Editor
Department of Materials Science and Technology, University of Crete and Institute of Electronic Structure and Laser (I.E.S.L.), Foundation for Research and Technology-Hellas (FO.R.T.H.), Vassilika Vouton, Heraklion, 70013 Crete, Greece
Interests: design and engineering of protein and peptide biomaterials; drug delivery; self-assembling proteins and peptides; physico-chemical stability of biomolecules; microneedle drug delivery; protein and gene carriers; adenovirus proteins; amyloid fibrils
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nanotechnology has emerged as an area of active investigation, especially regarding its applications in medicine. Among all these applications, nanocarrier-assisted drug delivery systems have gained increasing recognition in recent years for the development of pharmaceuticals that have the property of being directed toward specific targets of the body so as to improve the therapeutic outcome while reducing side effects.

Nanocarriers serve as viable and durable nanovehicles for the targeted delivery of bioactive compounds such as vaccines, genes, drugs, and other biomolecules, providing increased solubility and thus bioavailability, biocompatibility, physicochemical stability, protection from degradation, and controllable release profiles.

In addition, the modifiable surfaces of nanocarriers also expand their usability in different biomedical applications, especially in targeted therapy. Indeed, their modification can not only stabilize but also functionalize them to be responsive to different stimuli, improving the therapeutic efficacy.

In this Special Issue of Pharmaceutics, research, mini-review, and review articles advancing our knowledge on nanosized drug delivery systems are invited. Topics include, but are not limited to, theoretical and experimental research on the synthesis and development of functionalized nanocarriers or nanoformulations with targeting potential, their physicochemical and biological characterization, nanoparticle interactions with the immune system, in vitro and in vivo studies, preclinical and clinical studies, as well as safety issues regarding their production, handling, and disposal. We look forward to receiving your contributions.

Dr. Eleftherios Halevas
Dr. Chrysoula Kokotidou
Guest Editors

Manuscript Submission Information

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Keywords

  • nano-sized systems
  • drug encapsulation
  • drug targeting
  • surface functionalization
  • biodistribution
  • controlled release
  • triggered release
  • biological evaluation

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Published Papers (9 papers)

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Research

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14 pages, 2497 KiB  
Article
Chlorambucil-Loaded Graphene-Oxide-Based Nano-Vesicles for Cancer Therapy
by Surabhi Kumari, Anuj Nehra, Kshitij Gupta, Anu Puri, Vinay Kumar, Krishna Pal Singh, Mukesh Kumar and Ashutosh Sharma
Pharmaceutics 2023, 15(2), 649; https://doi.org/10.3390/pharmaceutics15020649 - 15 Feb 2023
Cited by 5 | Viewed by 1970
Abstract
In this study, the authors have designed biocompatible nano-vesicles using graphene oxide (GO) for the release of chlorambucil (CHL) drugs targeting cancerous cells. The GO sheets were first sulfonated and conjugated with folic acid (FA) molecules for controlled release and high loading efficiency [...] Read more.
In this study, the authors have designed biocompatible nano-vesicles using graphene oxide (GO) for the release of chlorambucil (CHL) drugs targeting cancerous cells. The GO sheets were first sulfonated and conjugated with folic acid (FA) molecules for controlled release and high loading efficiency of CHL. The chlorambucil (CHL) drug loading onto the functionalized GO surface was performed through π-π stacking and hydrophobic interactions with the aromatic planes of GO. The drug loading and “in vitro” release from the nano-vesicles at different pH were studied. The average particle size, absorption, and loading efficiency (%) of FA-conjugated GO sheets (CHL-GO) were observed to be 300 nm, 58%, and 77%, respectively. The drug release study at different pH (i.e., 7.4 and 5.5) showed a slight deceleration at pH 7.4 over pH 5.5. The amount of drug released was very small at pH 7.4 in the first hour which progressively increased to 24% after 8 h. The rate of drug release was faster at pH 5.5; initially, 16% to 27% in the first 3 h, and finally it reached 73% after 9 h. These observations indicate that the drug is released more rapidly at acidic pH with a larger amount of drug-loading ability. The rate of drug release from the CHL-loaded GO was 25% and 75% after 24 h. The biotoxicity study in terms of % cell viability of CHL-free and CHL-loaded GO against human cervical adenocarcinoma cell line was found to have lower cytotoxicity of CHL-loaded nano-vesicles (IC50 = 18 μM) as compared to CHL-free (IC50 = 8 μM). It is concluded that a high drug-loading efficiency and controlled release with excellent biotoxicity of CHL-GO offers an excellent application in the biomedical field. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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13 pages, 2429 KiB  
Communication
The Diphtheria Toxin Translocation Domain Impairs Receptor Selectivity in Cancer Cell-Targeted Protein Nanoparticles
by Eric Voltà-Durán, Julieta M. Sánchez, Eloi Parladé, Naroa Serna, Esther Vazquez, Ugutz Unzueta and Antonio Villaverde
Pharmaceutics 2022, 14(12), 2644; https://doi.org/10.3390/pharmaceutics14122644 - 29 Nov 2022
Cited by 5 | Viewed by 1681
Abstract
Protein-based materials intended as nanostructured drugs or drug carriers are progressively gaining interest in nanomedicine, since their structure, assembly and cellular interactivity can be tailored by recruiting functional domains. The main bottleneck in the development of deliverable protein materials is the lysosomal degradation [...] Read more.
Protein-based materials intended as nanostructured drugs or drug carriers are progressively gaining interest in nanomedicine, since their structure, assembly and cellular interactivity can be tailored by recruiting functional domains. The main bottleneck in the development of deliverable protein materials is the lysosomal degradation that follows endosome maturation. This is especially disappointing in the case of receptor-targeted protein constructs, which, while being highly promising and in demand in precision medicines, enter cells via endosomal/lysosomal routes. In the search for suitable protein agents that might promote endosome escape, we have explored the translocation domain (TD) of the diphtheria toxin as a functional domain in CXCR4-targeted oligomeric nanoparticles designed for cancer therapies. The pharmacological interest of such protein materials could be largely enhanced by improving their proteolytic stability. The incorporation of TD into the building blocks enhances the amount of the material detected inside of exposed CXCR4+ cells up to around 25-fold, in absence of cytotoxicity. This rise cannot be accounted for by endosomal escape, since the lysosomal degradation of the new construct decreases only moderately. On the other hand, a significant loss in the specificity of the CXCR4-dependent cellular penetration indicates the unexpected role of the toxin segment as a cell-penetrating peptide in a dose-dependent and receptor-independent fashion. These data reveal that the diphtheria toxin TD displayed on receptor-targeted oligomeric nanoparticles partially abolishes the exquisite receptor specificity of the parental material and it induces nonspecific internalization in mammalian cells. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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16 pages, 3190 KiB  
Article
Spanlastics as a Potential Platform for Enhancing the Brain Delivery of Flibanserin: In Vitro Response-Surface Optimization and In Vivo Pharmacokinetics Assessment
by Waleed S. Alharbi, Rawan H. Hareeri, Mohammed Bazuhair, Mohamed A. Alfaleh, Nabil A. Alhakamy, Usama A. Fahmy, Abdullah A. Alamoudi, Shaimaa M. Badr-Eldin, Osama A. Ahmed, Shareefa A. AlGhamdi and Marianne J. Naguib
Pharmaceutics 2022, 14(12), 2627; https://doi.org/10.3390/pharmaceutics14122627 - 28 Nov 2022
Cited by 9 | Viewed by 2003
Abstract
Flibanserin was licensed by the United States Food and Drug Administration (FDA) as an oral non-hormonal therapy for pre-menopausal women with inhibited sexual desire disorder. However, it suffers from susceptibility to first-pass metabolism in the liver, low aqueous solubility, and degradation in the [...] Read more.
Flibanserin was licensed by the United States Food and Drug Administration (FDA) as an oral non-hormonal therapy for pre-menopausal women with inhibited sexual desire disorder. However, it suffers from susceptibility to first-pass metabolism in the liver, low aqueous solubility, and degradation in the acidic stomach environment. Such hurdles result in a limited oral bioavailability of 33%. Thus, the aim of the study was to utilize the principles of nanotechnology and the benefits of an intranasal route of administration to develop a formulation that could bypass these drawbacks. A response-surface randomized D-optimal strategy was used for the formulation of flibanserin spanlastics (SPLs) with reduced size and increased absolute zeta potential. Two numerical factors were studied, namely the Span 60: edge activator ratio (w/w) and sonication time (min), in addition to one categorical factor that deals with the type of edge activator. Particle size (nm) and zeta potential (mV) were studied as responses. A mathematical optimization method was implemented for predicting the optimized levels of the variables. The optimized formulation was prepared using a Span: sodium deoxycholate ratio of 8:2 w/w; a sonication time of 5 min showed particle sizes of 129.70 nm and a zeta potential of −33.17 mV. Further in vivo assessment following intranasal administration in rats showed boosted plasma and brain levels, with 2.11- and 2.23-fold increases (respectively) compared to raw FLB. The aforementioned results imply that the proposed spanlastics could be regarded as efficient drug carriers for the trans-nasal delivery of drugs to the brain. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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20 pages, 5045 KiB  
Article
Piper aduncum Essential Oil Rich in Dillapiole: Development of Hydrogel-Thickened Nanoemulsion and Nanostructured Lipid Carrier Intended for Skin Delivery
by Simone Braga Carneiro, Tainá Kreutz, Renata Pereira Limberger, Helder Ferreira Teixeira, Valdir Florêncio da Veiga Júnior and Letícia Scherer Koester
Pharmaceutics 2022, 14(11), 2525; https://doi.org/10.3390/pharmaceutics14112525 - 19 Nov 2022
Cited by 4 | Viewed by 2196
Abstract
The essential oil extracted from the leaves of Piper aduncum, an aromatic plant from the Amazon region, is rich in dillapiole and presents anti-inflammatory activity. In this study, nanoemulsions (NE) and nanostructured lipid carriers (NLC), which are biocompatible nanostructured systems of a [...] Read more.
The essential oil extracted from the leaves of Piper aduncum, an aromatic plant from the Amazon region, is rich in dillapiole and presents anti-inflammatory activity. In this study, nanoemulsions (NE) and nanostructured lipid carriers (NLC), which are biocompatible nanostructured systems of a lipid nature, were prepared by high-pressure homogenization for the yet unexplored skin delivery of dillapiole. The addition of hydroxyethylcellulose produced hydrogel-thickened NE or NLC in view to improving the viscosity and skin adherence of the nanoformulations. Formulations were characterized with respect to dillapiole content, droplet size, polydispersity index, zeta potential, morphology, rheological behavior, bioadhesion, skin permeation profile, and in vitro irritancy (HET-CAM). The formulations developed presented spherical, homogeneous nanometric particle size (around 130 nm), narrow polydispersity index (<0.3), and negative zeta potential (around −40 mV). Dillapiole content was slightly lower in NLC compared to NE since the production process involves heating. The hydrogels containing nanocarriers showed pseudoplastic behavior with bioadhesive characteristics. The developed formulations exhibited a controlled release profile, dillapiole delivery up to the dermis, the layer of interest for anti-inflammatory potential, and low irritant potential in the chorioallantoic membrane (HET-CAM). Both hydrogels-thickened NE and NLC seemed to be promising formulations for skin delivery of Piper aduncum essential oil. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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Review

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20 pages, 1849 KiB  
Review
The Recent Applications of PLGA-Based Nanostructures for Ischemic Stroke
by Jun Yan, Lei Huang, Juan Feng and Xue Yang
Pharmaceutics 2023, 15(9), 2322; https://doi.org/10.3390/pharmaceutics15092322 - 14 Sep 2023
Cited by 4 | Viewed by 1258
Abstract
With the accelerated development of nanotechnology in recent years, nanomaterials have become increasingly prevalent in the medical field. The poly (lactic acid–glycolic acid) copolymer (PLGA) is one of the most commonly used biodegradable polymers. It is biocompatible and can be fabricated into various [...] Read more.
With the accelerated development of nanotechnology in recent years, nanomaterials have become increasingly prevalent in the medical field. The poly (lactic acid–glycolic acid) copolymer (PLGA) is one of the most commonly used biodegradable polymers. It is biocompatible and can be fabricated into various nanostructures, depending on requirements. Ischemic stroke is a common, disabling, and fatal illness that burdens society. There is a need for further improvement in the diagnosis and treatment of this disease. PLGA-based nanostructures can facilitate therapeutic compounds’ passage through the physicochemical barrier. They further provide both sustained and controlled release of therapeutic compounds when loaded with drugs for the treatment of ischemic stroke. The clinical significance and potential of PLGA-based nanostructures can also be seen in their applications in cell transplantation and imaging diagnostics of ischemic stroke. This paper summarizes the synthesis and properties of PLGA and reviews in detail the recent applications of PLGA-based nanostructures for drug delivery, disease therapy, cell transplantation, and the imaging diagnosis of ischemic stroke. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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26 pages, 5229 KiB  
Review
The Role of Cyclodextrin in the Construction of Nanoplatforms: From Structure, Function and Application Perspectives
by Chengyuan Xing, Xiaoming Zheng, Tian Deng, Ling Zeng, Xin Liu and Xinjin Chi
Pharmaceutics 2023, 15(5), 1536; https://doi.org/10.3390/pharmaceutics15051536 - 19 May 2023
Cited by 3 | Viewed by 1830
Abstract
Cyclodextrins (CyDs) in nano drug delivery systems have received much attention in pursuit of good compatibility, negligible toxicity, and improved pharmacokinetics of drugs. Their unique internal cavity has widened the application of CyDs in drug delivery based on its advantages. Besides this, the [...] Read more.
Cyclodextrins (CyDs) in nano drug delivery systems have received much attention in pursuit of good compatibility, negligible toxicity, and improved pharmacokinetics of drugs. Their unique internal cavity has widened the application of CyDs in drug delivery based on its advantages. Besides this, the polyhydroxy structure has further extended the functions of CyDs by inter- and intramolecular interactions and chemical modification. Furthermore, the versatile functions of the complex contribute to alteration of the physicochemical characteristics of the drugs, significant therapeutic promise, a stimulus-responsive switch, a self-assembly capability, and fiber formation. This review attempts to list recent interesting strategies regarding CyDs and discusses their roles in nanoplatforms, and may act as a guideline for developing novel nanoplatforms. Future perspectives on the construction of CyD-based nanoplatforms are also discussed at the end of this review, which may provide possible direction for the construction of more rational and cost-effective delivery vehicles. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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22 pages, 1172 KiB  
Review
Surfactant and Block Copolymer Nanostructures: From Design and Development to Nanomedicine Preclinical Studies
by Orestis Kontogiannis, Dimitrios Selianitis, Nefeli Lagopati, Natassa Pippa, Stergios Pispas and Maria Gazouli
Pharmaceutics 2023, 15(2), 501; https://doi.org/10.3390/pharmaceutics15020501 - 2 Feb 2023
Cited by 9 | Viewed by 2145
Abstract
The medical application of nanotechnology in the field of drug delivery has so far exhibited many efforts in treating simple to extremely complicated and life-threatening human conditions, with multiple products already existing in the market. A plethora of innovative drug delivery carriers, using [...] Read more.
The medical application of nanotechnology in the field of drug delivery has so far exhibited many efforts in treating simple to extremely complicated and life-threatening human conditions, with multiple products already existing in the market. A plethora of innovative drug delivery carriers, using polymers, surfactants and the combination of the above, have been developed and tested pre-clinically, offering great advantages in terms of targeted drug delivery, low toxicity and immune system activation, cellular biomimicry and enhanced pharmacokinetic properties. Furthermore, such artificial systems can be tailor-made with respect to each therapeutic protocol and disease type falling under the scope of personalized medicine. The simultaneous delivery of multiple therapeutic entities of different nature, such as genes and drugs, can be achieved, while novel technologies can offer systems with multiple modalities often combining therapy with diagnosis. In this review, we present prominent, innovative and state-of-the-art scientific efforts on the applications of surfactant-based, polymer-based, and mixed surfactant-polymer nanoparticle drug formulations intended for use in the medical field and in drug delivery. The materials used, formulation steps, nature, properties, physicochemical characteristics, characterization techniques and pharmacokinetic behavior of those systems, are presented extensively in the length of this work. The material presented is focused on research projects that are currently in the developmental, pre-clinical stage. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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19 pages, 3655 KiB  
Review
Films, Gels and Electrospun Fibers from Serum Albumin Globular Protein for Medical Device Coating, Biomolecule Delivery and Regenerative Engineering
by Elahe Mahdipour and Kibret Mequanint
Pharmaceutics 2022, 14(11), 2306; https://doi.org/10.3390/pharmaceutics14112306 - 27 Oct 2022
Cited by 4 | Viewed by 2083
Abstract
Albumin is a natural biomaterial that is abundantly available in blood and body fluids. It is clinically used as a plasma expander, thereby increasing the plasma thiol concentration due to its cysteine residues. Albumin is a regulator of intervascular oncotic pressure, serves as [...] Read more.
Albumin is a natural biomaterial that is abundantly available in blood and body fluids. It is clinically used as a plasma expander, thereby increasing the plasma thiol concentration due to its cysteine residues. Albumin is a regulator of intervascular oncotic pressure, serves as an anti-inflammatory modulator, and it has a buffering role due to its histidine imidazole residues. Because of its unique biological and physical properties, albumin has also emerged as a suitable biomaterial for coating implantable devices, for cell and drug delivery, and as a scaffold for tissue engineering and regenerative medicine. As a biomaterial, albumin can be used as surface-modifying film or processed either as cross-linked protein gels or as electrospun fibers. Herein we have discussed how albumin protein can be utilized in regenerative medicine as a hydrogel and as a fibrous mat for a diverse role in successfully delivering drugs, genes, and cells to targeted tissues and organs. The review of prior studies indicated that albumin is a tunable biomaterial from which different types of scaffolds with mechanical properties adjustable for various biomedical applications can be fabricated. Based on the progress made to date, we concluded that albumin-based device coatings, delivery of drugs, genes, and cells are promising strategies in regenerative and personalized medicine. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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21 pages, 1809 KiB  
Review
Nanocarriers: A Reliable Tool for the Delivery of Anticancer Drugs
by Hussein Sabit, Mohamed Abdel-Hakeem, Tahsin Shoala, Shaimaa Abdel-Ghany, Mokhtar Mamdouh Abdel-Latif, Jawaher Almulhim and Mohamed Mansy
Pharmaceutics 2022, 14(8), 1566; https://doi.org/10.3390/pharmaceutics14081566 - 28 Jul 2022
Cited by 26 | Viewed by 3030
Abstract
Nanomedicines have gained popularity due to their potential therapeutic applications, especially cancer treatment. Targeted nanoparticles can deliver drugs directly to cancer cells and enable prolonged drug release, reducing off-target toxicity and increasing therapeutic efficacy. However, translating nanomedicines from preclinical to clinical settings has [...] Read more.
Nanomedicines have gained popularity due to their potential therapeutic applications, especially cancer treatment. Targeted nanoparticles can deliver drugs directly to cancer cells and enable prolonged drug release, reducing off-target toxicity and increasing therapeutic efficacy. However, translating nanomedicines from preclinical to clinical settings has been difficult. Rapid advancements in nanotechnology promise to enhance cancer therapies. Nanomedicine offers advanced targeting and multifunctionality. Nanoparticles (NPs) have several uses nowadays. They have been studied as drug transporters, tumor gene delivery agents, and imaging contrast agents. Nanomaterials based on organic, inorganic, lipid, or glycan substances and synthetic polymers have been used to enhance cancer therapies. This review focuses on polymeric nanoparticle delivery strategies for anticancer nanomedicines. Full article
(This article belongs to the Special Issue Advances in Nanocarriers for Drug Delivery and Targeting)
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