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Pharmaceutics
Special Issues
Targeted Drug Delivery for Diagnostic and Therapeutic Applications
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Targeted Drug Delivery for Diagnostic and Therapeutic Applications

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

Deadline for manuscript submissions: closed (28 February 2025) | Viewed by 8503

Special Issue Editors

Dr. Nina Kostevšek

E-Mail Website
Guest Editor
Department for nanostructured materials, Jozef Stefan Institute, 1000 Ljubljana, Slovenia
Interests: cancer therapy; gene delivery; contrast agents; magnetic resonance imaging; photothermal treatment; cell-based drug-delivery systems
Dr. Georgy Mikhaylov

E-Mail Website
Guest Editor
Department of Biochemistry and Molecular and Structural Biology, Jozef Stefan Institute, 1000 Ljubljana, Slovenia
Interests: cancer biochemistry; targeted drug delivery; biolumenescence; proteasee biology

Special Issue Information

Dear Colleagues,

Cancer is the second leading cause of death after cardiovascular diseases in developed countries. Despite rapid medicinal and pharmaceutical chemistry developments, chemotherapy is still a significant challenge. In the last decade, the development of effective targeted drug delivery systems for treating cancer has been a top priority in biomedical technology.

Targeted drug delivery is a system for specifying the drug moiety directly into its targeted body area (organ, cellular, and subcellular level of specific tissue) to overcome the specific toxic effect of conventional drug delivery, thereby reducing the amount of drug required for therapeutic efficacy. This targeted strategy enriches the concentration of the therapeutic agent in cells/tissues; as a result, low doses can be used, particularly if there is a contradiction between the therapeutic activity and the toxic effects of the agent. Increasing the concentration of therapeutic agents in the target location also improves their therapeutic index by enhancing the efficacy and/or increasing the tolerability in biological systems. Thus, targeted drug delivery is a priority approach in modern pharmacology.

This Special Issue intends to provide a forum for original research articles and reviews on the development of targeted drug delivery approaches. We invite researchers to share their ideas and results related to the development of drug delivery platforms and their potential application in treatment and diagnostics.

Dr. Nina Kostevšek
Dr. Georgy Mikhaylov
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. Pharmaceutics is an international peer-reviewed open access monthly 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 2900 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

  • drug delivery
  • theranostics
  • nanocarriers
  • cancer treatment
  • therapeutic nanoparticles
  • targeting
  • liposomes
  • nanosomes

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Published Papers (3 papers)

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Research

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22 pages, 10335 KiB  
Article
Intranasal Mucoadhesive In Situ Gel of Glibenclamide-Loaded Bilosomes for Enhanced Therapeutic Drug Delivery to the Brain
by Meenakshi Tripathi, Laxmi Gharti, Amit Bansal, Hemlata Kaurav and Sandeep Sheth
Pharmaceutics 2025, 17(2), 193; https://doi.org/10.3390/pharmaceutics17020193 - 4 Feb 2025
Cited by 1 | Viewed by 1030
Abstract
Background: The neuroprotective efficacy of glibenclamide (GLIB) has been demonstrated in multiple rodent models of ischemia, hemorrhagic stroke, traumatic brain damage, spinal cord injury, and metastatic brain tumors. Due to its poor solubility, GLIB has low oral bioavailability, limiting its transportation to the [...] Read more.
Background: The neuroprotective efficacy of glibenclamide (GLIB) has been demonstrated in multiple rodent models of ischemia, hemorrhagic stroke, traumatic brain damage, spinal cord injury, and metastatic brain tumors. Due to its poor solubility, GLIB has low oral bioavailability, limiting its transportation to the brain via the oral route. Objectives: Here, we attempted to develop and optimize an intranasal mucoadhesive in situ gel of GLIB-loaded bilosomes using a 32 Box–Behnken design for brain drug delivery. Methods: To facilitate a longer residence time of the administered dose within the nasal cavity, the prepared bilosomes were loaded into a mucoadhesive in situ gel providing resistance to rapid mucociliary clearance. The amounts of sodium deoxycholate, the cholesterol/Span 40 mixture, and the molar ratio between the mixture’s components were chosen as independent variables, while the entrapment efficiency and in vitro drug release were selected as dependent variables. Results and conclusions: The optimal formulation was analyzed for particle size and entrapment efficiency, which were found to be 270.6 nm and 68.39%, respectively. In vitro drug release from optimal formulation after 12 h was 87.29 ± 1.98% as compared to 52.01 ± 2.04% of plain in situ gel of drug. An in vivo brain drug delivery study performed on Swiss albino mice showed that the brain concentration of drug through intranasal administration from mucoadhesive in situ gel of GLIB-bilosomes after 12 h was 2.12 ± 0.16 µg/mL as compared to 0.68 ± 0.04 µg/mL from plain in situ gel of drug. Conclusively, the developed bilosomal formulation offers a favorable intranasal substitute with enhanced therapeutic drug delivery to the brain. Full article
(This article belongs to the Special Issue Targeted Drug Delivery for Diagnostic and Therapeutic Applications)
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29 pages, 13658 KiB  
Article
HER-2 Receptor and αvβ3 Integrin Dual-Ligand Surface-Functionalized Liposome for Metastatic Breast Cancer Therapy
by Dilip Kumar Arya, Hemali Deshpande, Ashish Kumar, Kumarappan Chidambaram, Prashant Pandey, Shabnam Anjum, Payal Deepak, Vikas Kumar, Santosh Kumar, Giriraj Pandey, Saurabh Srivastava and Paruvathanahalli Siddalingam Rajinikanth
Pharmaceutics 2024, 16(9), 1128; https://doi.org/10.3390/pharmaceutics16091128 - 27 Aug 2024
Cited by 5 | Viewed by 1988
Abstract
Human epidermal growth factor receptor-2 (HER2)-positive breast cancer metastasis remains the primary cause of mortality among women globally. Targeted therapies have revolutionized treatment efficacy, with Trastuzumab (Trast), a monoclonal antibody, targeting HER2-positive advanced breast cancer. The tumor-homing peptide iRGD enhances the intratumoral accumulation [...] Read more.
Human epidermal growth factor receptor-2 (HER2)-positive breast cancer metastasis remains the primary cause of mortality among women globally. Targeted therapies have revolutionized treatment efficacy, with Trastuzumab (Trast), a monoclonal antibody, targeting HER2-positive advanced breast cancer. The tumor-homing peptide iRGD enhances the intratumoral accumulation and penetration of therapeutic agents. Liposomes serve as versatile nanocarriers for both hydrophilic and hydrophobic drugs. Gefitinib (GFB) is a potential anticancer drug against HER2-positive breast cancer, while Lycorine hydrochloride (LCH) is a natural compound with anticancer and anti-inflammatory properties. This study developed TPGS-COOH-coated liposomes co-loaded with GFB and LCH, prepared by the solvent injection method, and surface-functionalized with Trast and iRGD. The dual surface-decorated liposomes (DSDLs) were characterized for their particle size (PS), polydispersity index (PDI), zeta potential (ZP), surface chemistry, surface morphology, and their crystallinity during in-vitro drug release, drug encapsulation, and in-vitro cell line studies on SK-BR-3 and MDA-MB-231 breast cancer cells. The half-maximum inhibitory concentration (IC-50) values of single decorated liposomes (SDLs), iRGD-LP, and Trast-LP, as well as DSDLs (iRGD-Trast-LP) on SK-BR-3 cells, were 6.10 ± 0.42, 4.98 ± 0.36, and 4.34 ± 0.32 μg/mL, respectively. Moreover, the IC-50 values of SDLs and DSDLs on MDA-MB-231 cells were 15.12 ± 0.68, 13.09 ± 0.59, and 11.08 ± 0.48 μg/mL, respectively. Cellular uptake studies using confocal laser scanning microscopy (CLSM) showed that iRGD and Trast functionalization significantly enhanced cellular uptake in both cell lines. The wound-healing assay demonstrated a significant reduction in SDL and DSDL-treated MDA-MB-231 cell migration compared to the control. Additionally, the blood compatibility study showed minimal hemolysis (less than 5% RBC lysis), indicating good biocompatibility and biosafety. Overall, these findings suggest that TPGS-COOH-coated, GFB and LCH co-loaded, dual-ligand (iRGD and Trast) functionalized, multifunctional liposomes could be a promising therapeutic strategy for treating HER2-positive metastatic breast cancer. Full article
(This article belongs to the Special Issue Targeted Drug Delivery for Diagnostic and Therapeutic Applications)
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Review

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21 pages, 819 KiB  
Review
Anatomical Targeting of Anticancer Drugs to Solid Tumors Using Specific Administration Routes: Review
by Akira Saito, Joji Kitayama, Ryozo Nagai and Kenichi Aizawa
Pharmaceutics 2023, 15(6), 1664; https://doi.org/10.3390/pharmaceutics15061664 - 6 Jun 2023
Cited by 8 | Viewed by 4426
Abstract
Despite remarkable recent progress in developing anti-cancer agents, outcomes of patients with solid tumors remain unsatisfactory. In general, anti-cancer drugs are systemically administered through peripheral veins and delivered throughout the body. The major problem with systemic chemotherapy is insufficient uptake of intravenous (IV) [...] Read more.
Despite remarkable recent progress in developing anti-cancer agents, outcomes of patients with solid tumors remain unsatisfactory. In general, anti-cancer drugs are systemically administered through peripheral veins and delivered throughout the body. The major problem with systemic chemotherapy is insufficient uptake of intravenous (IV) drugs by targeted tumor tissue. Although dose escalation and treatment intensification have been attempted in order to increase regional concentrations of anti-tumor drugs, these approaches have produced only marginal benefits in terms of patient outcomes, while often damaging healthy organs. To overcome this problem, local administration of anti-cancer agents can yield markedly higher drug concentrations in tumor tissue with less systemic toxicity. This strategy is most commonly used for liver and brain tumors, as well as pleural or peritoneal malignancies. Although the concept is theoretically reasonable, survival benefits are still limited. This review summarizes clinical results and problems and discusses future directions of regional cancer therapy with local administration of chemotherapeutants. Full article
(This article belongs to the Special Issue Targeted Drug Delivery for Diagnostic and Therapeutic Applications)
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