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Pharmaceutics
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Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds
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Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Delivery and Controlled Release".

Deadline for manuscript submissions: 31 January 2026 | Viewed by 7836

Special Issue Editors

Prof. Dr. João Paulo Fabi

E-Mail Website
Guest Editor
Department of Food Science and Experimental Nutrition, School of Pharmaceutical Sciences, University of São Paulo, São Paulo 05508000, Brazil
Interests: anticancer; colon cancer; bioactive compounds; nanoparticles; nanotechnology; pectin; bioactive polysaccharides.
Special Issues, Collections and Topics in MDPI journals
Dr. Thiécla Katiane Osvaldt Rosales

E-Mail Website
Guest Editor
Department of Food Science and Experimental Nutrition, School of Pharmaceutical Sciences, University of São Paulo, São Paulo 05508000, Brazil
Interests: colon cancer; bioavaivalability; bioactive compounds; nanotechnology; polyphenolic compounds; polysaccharides; targeted delivery

Special Issue Information

Dear Colleagues,

This Special Issue aims to explore the innovative use of nanocarriers in drug delivery systems, emphasizing their potential to improve the bioavailability, stability, and controlled release of bioactive compounds. Nanocarriers, such as liposomes, nanoparticles, dendrimers, and micelles, are engineered to encapsulate therapeutic agents and deliver them specifically to targeted sites, minimizing off-target effects and enhancing therapeutic efficacy. This Special Issue focuses on designing, characterizing, and functionalizing nanocarriers to deliver various bioactive compounds, including natural compounds, such as carotenoids, polyphenolic compounds, terpenes, peptides, and proteins. The research included in this Special Issue should also investigate advances in targeting strategies, such as ligand–receptor interactions, surface modifications, stimuli-responsive delivery systems, biomaterials, and methodologies. Emphasis is placed on overcoming challenges related to oral administration, absorption, biodistribution, toxicity, and immune responses. The goal is to provide a comprehensive understanding of how nanocarriers can revolutionize treatment regimens in diseases like cancer, diabetes, cardiovascular diseases, neurological disorders, and infections, thus advancing pharmaceutical sciences and precision medicine.

Prof. Dr. João Paulo Fabi
Dr. Thiécla Katiane Osvaldt Rosales
Guest Editors

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Keywords

  • absorption
  • bioavailability
  • bioactive compounds
  • drug delivery systems
  • nanoencapsulation
  • nanomaterials
  • nanocarrier systems
  • natural compounds
  • oral administration
  • precision therapy
  • targeted delivery

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Published Papers (5 papers)

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Research

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25 pages, 3645 KB  
Article
DOPC Liposomal Formulation of Antimicrobial Peptide LL17-32 with Reduced Cytotoxicity: A Promising Carrier Against Porphyromonas gingivalis
by Jinyang Han, Josephine L. Meade and Francisco M. Goycoolea
Pharmaceutics 2025, 17(11), 1424; https://doi.org/10.3390/pharmaceutics17111424 - 4 Nov 2025
Viewed by 246
Abstract
Background/Objectives: The rapid emergence of antibiotic-resistant oral pathogens has rendered many conventional therapies increasingly ineffective. Antimicrobial peptides (AMPs) have emerged as a promising therapeutic alternative due to their unique mechanisms of action and low propensity for inducing resistance. The delivery of novel therapeutic [...] Read more.
Background/Objectives: The rapid emergence of antibiotic-resistant oral pathogens has rendered many conventional therapies increasingly ineffective. Antimicrobial peptides (AMPs) have emerged as a promising therapeutic alternative due to their unique mechanisms of action and low propensity for inducing resistance. The delivery of novel therapeutic AMPs against oral cavity bacterial infections requires effective pharmaceutical dosage formulations. This study investigated the potential of two liposomal formulations for the association and delivery of the antimicrobial peptide (AMP) LL17-32 against the dental bacterial pathogen Porphyromonas gingivalis. Methods: Liposomes composed of either negatively charged soya lecithin (SL) or neutrally charged dioleoyl-phosphatidylcholine (DOPC) phospholipids were formulated and characterized based on their hydrodynamic size distribution, ζ-potential, morphology, membrane fluidity, peptide association efficiency, stability and release of peptide in vitro under physiological conditions. The characterization of their biological activity included efficiency of bacterial killing, bacterial adherence, and mammalian cell cytotoxicity using human gingival keratinocyte (TIGK) cells. Results: Both liposomal formulations exhibited spherical morphology with hydrodynamic diameters smaller than ~170 nm and demonstrated good colloidal stability. LL17-32 showed high association efficiency with both liposomal membranes, with no detectable LL17-32 in vitro release. In biological assays, peptide-loaded DOPC liposomes exhibited dose-dependent bactericidal activity against P. gingivalis, whereas SL liposomes significantly attenuated the bactericidal effect of LL17-32. Both formulations displayed reduced cytotoxicity toward human gingival keratinocyte (TIGK) cells versus free peptide. Conclusions: These findings suggest that DOPC liposomes represent a promising delivery system for LL17-32 by adhering to P. gingivalis and exhibiting minimal cytotoxicity to mammalian cells. This study emphasises the critical role of lipid charge in designing AMP delivery systems for antibacterial applications, while it additionally demonstrates the utility of flow cytometry as a quantitative tool to assess liposome–bacteria association. Full article
(This article belongs to the Special Issue Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds)
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14 pages, 2579 KB  
Article
Targeted Delivery of VEGF-siRNA to Glioblastoma Using Orientation-Controlled Anti-PD-L1 Antibody-Modified Lipid Nanoparticles
by Ayaka Matsuo-Tani, Makoto Matsumoto, Takeshi Hiu, Mariko Kamiya, Longjian Geng, Riku Takayama, Yusuke Ushiroda, Naoya Kato, Hikaru Nakamura, Michiharu Yoshida, Hidefumi Mukai, Takayuki Matsuo and Shigeru Kawakami
Pharmaceutics 2025, 17(10), 1298; https://doi.org/10.3390/pharmaceutics17101298 - 4 Oct 2025
Viewed by 1003
Abstract
Background/Objectives: Glioblastoma (GBM) is an aggressive primary brain tumor with limited therapeutic options despite multimodal treatment. Small interfering RNA (siRNA)-based therapeutics can silence tumor-promoting genes, but achieving efficient and tumor-specific delivery remains challenging. Lipid nanoparticles (LNPs) are promising siRNA carriers; however, conventional [...] Read more.
Background/Objectives: Glioblastoma (GBM) is an aggressive primary brain tumor with limited therapeutic options despite multimodal treatment. Small interfering RNA (siRNA)-based therapeutics can silence tumor-promoting genes, but achieving efficient and tumor-specific delivery remains challenging. Lipid nanoparticles (LNPs) are promising siRNA carriers; however, conventional antibody conjugation can impair antigen recognition and complicate manufacturing. This study aimed to establish a modular Fc-binding peptide (FcBP)-mediated post-insertion strategy to enable PD-L1-targeted delivery of VEGF-siRNA via LNPs for GBM therapy. Methods: Preformed VEGF-siRNA-loaded LNPs were functionalized with FcBP–lipid conjugates, enabling non-covalent anchoring of anti-PD-L1 antibodies through Fc interactions. Particle characteristics were analyzed using dynamic light scattering and encapsulation efficiency assays. Targeted cellular uptake and VEGF gene silencing were evaluated in PD-L1-positive GL261 glioma cells. Anti-tumor efficacy was assessed in a subcutaneous GL261 tumor model following repeated intratumoral administration using tumor volume and bioluminescence imaging as endpoints. Results: FcBP post-insertion preserved LNP particle size (125.2 ± 1.3 nm), polydispersity, zeta potential, and siRNA encapsulation efficiency. Anti-PD-L1–FcBP-LNPs significantly enhanced cellular uptake (by ~50-fold) and VEGF silencing in PD-L1-expressing GL261 cells compared to controls. In vivo, targeted LNPs reduced tumor volume by 65% and markedly suppressed bioluminescence signals without inducing weight loss. Final tumor weight was reduced by 63% in the anti-PD-L1–FcBP–LNP group (656.9 ± 125.4 mg) compared to the VEGF-siRNA LNP group (1794.1 ± 103.7 mg). The FcBP-modified LNPs maintained antibody orientation and binding activity, enabling rapid functionalization with targeting antibodies. Conclusions: The FcBP-mediated post-insertion strategy enables site-specific, modular antibody functionalization of LNPs without compromising physicochemical integrity or antibody recognition. PD-L1-targeted VEGF-siRNA delivery demonstrated potent, selective anti-tumor effects in GBM murine models. This platform offers a versatile approach for targeted nucleic acid therapeutics and holds translational potential for treating GBM. Full article
(This article belongs to the Special Issue Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds)
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15 pages, 1908 KB  
Article
Surface Functionalized Polyhydroxyalkanoate Nanoparticles via SpyTag–SpyCatcher System for Targeted Breast Cancer Treatment
by Jin Young Heo, Min Kyung Sung, Seonhye Jang, Hansol Kim, Youngdo Jeong, Dong-Jin Jang, Sang-Jae Lee, Seong-Bo Kim and Sung Tae Kim
Pharmaceutics 2025, 17(6), 721; https://doi.org/10.3390/pharmaceutics17060721 - 29 May 2025
Viewed by 1066
Abstract
Background/Objectives: Biodegradable polymers have emerged as promising platforms for drug delivery. Produced by microbiomes, polyhydroxyalkanoates (PHAs) offer excellent biocompatibility, biodegradability, and environmental sustainability. In this study, we report the surface functionalization of PHA-based nanoparticles (NPs) using the SpyTag–SpyCatcher system to enhance cellular uptake. [...] Read more.
Background/Objectives: Biodegradable polymers have emerged as promising platforms for drug delivery. Produced by microbiomes, polyhydroxyalkanoates (PHAs) offer excellent biocompatibility, biodegradability, and environmental sustainability. In this study, we report the surface functionalization of PHA-based nanoparticles (NPs) using the SpyTag–SpyCatcher system to enhance cellular uptake. Methods: Initial conjugation with mEGFP-SpyTag enabled visualization, followed by decoration with HER2-specific Affibody-SpyCatcher and/or TAT-SpyCatcher peptides. The prepared NPs retained a diameter of <200 nm and a negatively charged surface. Results: Affibody-functionalized NPs significantly enhanced internalization and cytotoxicity in HER2-overexpressing SK-BR-3 cells, whereas TAT-functionalized NPs promoted uptake across various cell types, independently of HER2 expression. Dual-functionalized NPs exhibited synergistic or attenuated effects based on the HER2 expression levels, highlighting the critical role of ligand composition in targeted delivery. Conclusions: The results of this study demonstrate that the SpyTag–SpyCatcher-mediated surface engineering of PHA NPs offers a modular and robust strategy for active targeting in nanomedicine. Full article
(This article belongs to the Special Issue Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds)
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Review

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23 pages, 2028 KB  
Review
Nanoencapsulation of Biotics: Feasibility to Enhance Stability and Delivery for Improved Gut Health
by Pedro Brivaldo Viana da Silva, Thiécla Katiane Osvaldt Rosales and João Paulo Fabi
Pharmaceutics 2025, 17(9), 1180; https://doi.org/10.3390/pharmaceutics17091180 - 11 Sep 2025
Viewed by 821
Abstract
The human gastrointestinal tract contains a complex and diverse community of microorganisms, referred to as the gut microbiota. Due to their close proximity to human cells, these microorganisms play a crucial role in maintaining the host’s health, influencing various metabolic processes, and providing [...] Read more.
The human gastrointestinal tract contains a complex and diverse community of microorganisms, referred to as the gut microbiota. Due to their close proximity to human cells, these microorganisms play a crucial role in maintaining the host’s health, influencing various metabolic processes, and providing protection against potentially harmful agents and pathogens. The disruption in this microbial ecosystem, known as dysbiosis, is associated with inflammatory and metabolic diseases, as well as certain types of cancer. Strategies to modulate the microbiota toward a state of homeostasis through the use of “biotics” (probiotics, prebiotics, synbiotics, and postbiotics) have increased. However, challenges such as low stability, loss of microbial viability, and difficulties in delivery to the intestine significantly decrease the progress of their clinical and nutritional applications. Microencapsulation and nanoencapsulation technologies offer potential solutions to enhance the stability, bioavailability, and controlled release of microorganisms and/or bioactive compounds within the gastrointestinal tract. Considering these aspects, this review provides a comprehensive overview of recent advances in nanoencapsulation techniques for biotics, highlighting their mechanisms of action, potential health benefits, and applications in functional foods and targeted therapies. Furthermore, it addresses existing limitations, evaluates feasibility, and discusses the future potential of these technologies in promoting gut health and disease prevention. Further research, especially through clinical studies, is mandatory to verify the safety and effectiveness of nanoencapsulated biotics and to obtain regulatory approval. Full article
(This article belongs to the Special Issue Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds)
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30 pages, 3428 KB  
Review
Lipid-Polymer Hybrid Nanoparticles as a Smart Drug Delivery System for Peptide/Protein Delivery
by Alharith A. A. Hassan, Eslam Ramadan, Katalin Kristó, Géza Regdon, Jr. and Tamás Sovány
Pharmaceutics 2025, 17(6), 797; https://doi.org/10.3390/pharmaceutics17060797 - 19 Jun 2025
Cited by 5 | Viewed by 4123
Abstract
The efficient oral delivery of therapeutic proteins and peptides poses a tremendous challenge due to their inherent instability, large molecular size, and susceptibility to enzymatic degradation. Several nanocarrier systems, such as liposomes, solid lipid nanoparticles, and polymeric nanoparticles, have been explored to overcome [...] Read more.
The efficient oral delivery of therapeutic proteins and peptides poses a tremendous challenge due to their inherent instability, large molecular size, and susceptibility to enzymatic degradation. Several nanocarrier systems, such as liposomes, solid lipid nanoparticles, and polymeric nanoparticles, have been explored to overcome these problems. Liposomes and other lipid-based nanocarriers show excellent biocompatibility and the ability to encapsulate hydrophobic and hydrophilic drugs; however, they often suffer from poor structural stability, premature leakage of the loaded drugs, and poor encapsulation efficiency for macromolecular peptides and proteins. On the other hand, polymeric nanoparticles are more stable and allow better control over drug release; nevertheless, they usually lack the necessary biocompatibility and cellular uptake efficiency. Recently, lipid-polymer hybrid nanoparticles (LPHNs) have emerged as an advanced solution combining the structural stability of polymers and the biocompatibility and surface functionalities of lipids to enhance the controlled release, stability, and bioavailability of protein and peptide drugs. In this review, an attempt was made to set a clear definition of the LPHNs and extend the concept and area, so to our knowledge, this is the first review that highlights six categories of the LPHNs based on their anatomy. Moreover, this review offers a detailed analysis of LPHN preparation methods, including conventional and nonconventional one-step and two-step processes, nanoprecipitation, microfluidic mixing, and emulsification methods. Moreover, the material attributes and critical process parameters affecting the output of the preparation methods were illustrated with supporting examples to enable researchers to select the suitable preparation method, excipients, and parameters to be manipulated to get the LPHNs with the predetermined quality. The number of reviews focusing on the formulation of peptide/protein pharmaceutics usually focus on a specific drug like insulin. To our knowledge, this is the first review that generally discusses LPHN-based delivery of biopharmaceuticals. by discussing representative examples of previous reports comparing them to a variety of nanocarrier systems to show the potentiality of the LPHNs to deliver peptides and proteins. Moreover, some ideas and suggestions were proposed by the authors to tackle some of the shortcomings highlighted in these studies. By presenting this comprehensive overview of LPHN preparation strategies and critically analyzing literature studies on this topic and pointing out their strong and weak points, this review has shown the gaps and enlightened avenues for future research. Full article
(This article belongs to the Special Issue Biomedical Applications of Nanocarriers in Targeted Delivery of Bioactive Compounds)
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