Research

19 pages, 6671 KiB

Open AccessArticle

Naxitamab Activity in Neuroblastoma Cells Is Enhanced by Nanofenretinide and Nanospermidine

by Lucrezia Galassi, Martina Rossi, Pietro Lodeserto, Monia Lenzi, Francesca Borsetti, Manuela Voltattorni, Giovanna Farruggia, Paolo Blasi and Isabella Orienti

Pharmaceutics 2023, 15(2), 648; https://doi.org/10.3390/pharmaceutics15020648 - 15 Feb 2023

Cited by 1 | Viewed by 1756

Abstract

Neuroblastoma cells highly express the disialoganglioside GD2, a tumor-associated carbohydrate antigen, which is also expressed in neurons, skin melanocytes, and peripheral nerve fibers. Immunotherapy with monoclonal anti-GD2 antibodies has a proven efficacy in clinical trials and is included in the standard treatment for [...] Read more.

Neuroblastoma cells highly express the disialoganglioside GD2, a tumor-associated carbohydrate antigen, which is also expressed in neurons, skin melanocytes, and peripheral nerve fibers. Immunotherapy with monoclonal anti-GD2 antibodies has a proven efficacy in clinical trials and is included in the standard treatment for children with high-risk neuroblastoma. However, the strong neuro-toxicity associated with anti-GD2 antibodies administration has hindered, until now, the possibility for dose-escalation and protracted use, thus restraining their therapeutic potential. Strategies to increase the efficacy of anti-GD2 antibodies are actively sought, with the aim to enable chronic treatments that could eradicate minimal residual disease and subsequent relapses, often occurring after treatment. Here, we report that Nanofenretinide and Nanospermidine improved the expression of GD2 in neuroblastoma cells (CHP-134) and provided different effects in combination with the anti-GD2 antibody naxitamab. In particular, Nanofenretinide significantly increased the cytotoxic effect of naxitamab while Nanospermidine inhibited cell motility at extents proportional to naxitamab concentration. In neuroblastoma cells characterized by a low and heterogeneous basal expression of GD2, such as SH-SY5Y, which may represent the cell heterogeneity in tumors after chemotherapy, both Nanofenretinide and Nanospermidine increased GD2 expression in approximately 50% of cells, thus shifting the tumor population towards improved sensitivity to anti-GD2 antibodies. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

12 pages, 2763 KiB

Open AccessArticle

Dual Effect of Chemo-PDT with Tumor Targeting Nanoparticles Containing iRGD Peptide

by Gye Lim Kim, Byeongmin Park, Eun Hyang Jang, Jaeun Gu, Seo Ra Seo, Hyein Cheung, Hyo Jung Lee, Sangmin Lee and Jong-Ho Kim

Pharmaceutics 2023, 15(2), 614; https://doi.org/10.3390/pharmaceutics15020614 - 11 Feb 2023

Cited by 2 | Viewed by 1704

Abstract

Nanotechnology, including self-aggregated nanoparticles, has shown high effectiveness in the treatment of solid tumors. To overcome the limitations of conventional cancer therapies and promote therapeutic efficacy, a combination of PDT and chemotherapy can be considered an effective strategy for cancer treatment. This study [...] Read more.

Nanotechnology, including self-aggregated nanoparticles, has shown high effectiveness in the treatment of solid tumors. To overcome the limitations of conventional cancer therapies and promote therapeutic efficacy, a combination of PDT and chemotherapy can be considered an effective strategy for cancer treatment. This study presents the development of tumor-targeting polysialic acid (PSA) nanoparticles for chemo-PDT to increase the cellular uptake and cytotoxic effect in cancer cells. Chlorin e6 (Ce6), a photosensitizer, and the iRGD peptide (sequence; cCRGDKGPDC) were conjugated to the amine of N-deacetylated PSA. They generate reactive oxygen species (ROS), especially singlet oxygen (¹O₂), and target integrin αvβ3 on the cancer cell surface. To offer a chemotherapeutic effect, doxorubicin (Dox) was assembled into the core of hydrophobically modified PSA by connecting it with Ce6; this was followed by its sustained release from the nanoparticles. These nanoparticles are able to generate ROS under 633 nm visible-light irradiation, resulting in the strong cytotoxicity of Dox with anticancer effects in HCT116 cells. PSA nanoparticles with the dual effect of chemo-PDT improve conventional PDT, which has a poor ability to deliver photosensitizers to cancer cells. Using their combination with Dox chemotherapy, rapid removal of cancer cells can be expected. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

24 pages, 5445 KiB

Open AccessArticle

Cannabidiol-Loaded Extracellular Vesicles from Human Umbilical Cord Mesenchymal Stem Cells Alleviate Paclitaxel-Induced Peripheral Neuropathy

by Anil Kumar Kalvala, Arvind Bagde, Peggy Arthur, Tanmay Kulkarni, Santanu Bhattacharya, Sunil Surapaneni, Nil Kumar Patel, Ramesh Nimma, Aragaw Gebeyehu, Nagavendra Kommineni, Yan Li, David G. Meckes, Jr., Li Sun, Bipika Banjara, Keb Mosley-Kellum, Thanh Cong Dinh and Mandip Singh

Pharmaceutics 2023, 15(2), 554; https://doi.org/10.3390/pharmaceutics15020554 - 07 Feb 2023

Cited by 5 | Viewed by 3113 | Correction

Abstract

In cancer patients, chronic paclitaxel (PTX) treatment causes excruciating pain, limiting its use in cancer chemotherapy. The neuroprotective potential of synthetic cannabidiol (CBD) and CBD formulated in extracellular vesicles (CBD-EVs) isolated from human umbilical cord derived mesenchymal stem cells was investigated in C57BL/6J [...] Read more.

In cancer patients, chronic paclitaxel (PTX) treatment causes excruciating pain, limiting its use in cancer chemotherapy. The neuroprotective potential of synthetic cannabidiol (CBD) and CBD formulated in extracellular vesicles (CBD-EVs) isolated from human umbilical cord derived mesenchymal stem cells was investigated in C57BL/6J mice with PTX-induced neuropathic pain (PIPN). The particle size of EVs and CBD-EVs, surface roughness, nanomechanical properties, stability, and release studies were all investigated. To develop neuropathy in mice, PTX (8 mg/kg, i.p.) was administered every other day (four doses). In terms of decreasing mechanical and thermal hypersensitivity, CBD-EVs treatment was superior to EVs treatment or CBD treatment alone (p < 0.001). CBD and CBD-EVs significantly reduced mitochondrial dysfunction in dorsal root ganglions and spinal homogenates of PTX-treated animals by modulating the AMPK pathway (p < 0.001). Studies inhibiting the AMPK and 5HT1A receptors found that CBD did not influence the neurobehavioral or mitochondrial function of PIPN. Based on these results, we hypothesize that CBD and CBD-EVs mitigated PIPN by modulating AMPK and mitochondrial function. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Graphical abstract

28 pages, 9940 KiB

Open AccessArticle

Composite Nanoarchitectonics of Photoactivated Titania-Based Materials with Anticancer Properties

by Nefeli Papadopoulou-Fermeli, Nefeli Lagopati, Natassa Pippa, Elias Sakellis, Nikos Boukos, Vassilis G. Gorgoulis, Maria Gazouli and Evangelia A. Pavlatou

Pharmaceutics 2023, 15(1), 135; https://doi.org/10.3390/pharmaceutics15010135 - 30 Dec 2022

Cited by 8 | Viewed by 1911

Abstract

The synthesis of titania-based composite materials with anticancer potential under visible-light irradiation is the aim of this study. In specific, titanium dioxide (TiO₂) nanoparticles (NPs) chemically modified with silver were embedded in a stimuli-responsive microgel (a crosslinked interpenetrating network (IP) network [...] Read more.

The synthesis of titania-based composite materials with anticancer potential under visible-light irradiation is the aim of this study. In specific, titanium dioxide (TiO₂) nanoparticles (NPs) chemically modified with silver were embedded in a stimuli-responsive microgel (a crosslinked interpenetrating network (IP) network that was synthesized by poly (N-Isopropylacrylamide) and linear chains of polyacrylic acid sodium salt, forming composite particles. The ultimate goal of this research, and for our future plans, is to develop a drug-delivery system that uses optical fibers that could efficiently photoactivate NPs, targeting cancer cells. The produced Ag-TiO₂ NPs, the microgel and the composite materials were characterized through X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), micro-Raman spectroscopy, ultraviolet-visible spectroscopy (UV-Vis), dynamic light scattering (DLS) and transmission electron microscopy (TEM). Our results indicated that Ag-TiO₂ NPs were successfully embedded within the thermoresponsive microgel. Either Ag-TiO₂ NPs or the composite materials exhibited high photocatalytic degradation efficiency on the pollutant rhodamine B and significant anticancer potential under visible-light irradiation. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

20 pages, 2778 KiB

Open AccessArticle

Radiolabeling, Quality Control and In Vivo Imaging of Multimodal Targeted Nanomedicines

by Phuoc-Vinh Nguyen, Emilie Allard-Vannier, Nicolas Aubrey, Christine Labrugère-Sarroste, Igor Chourpa, Julien Sobilo, Alain Le Pape and Katel Hervé-Aubert

Pharmaceutics 2022, 14(12), 2679; https://doi.org/10.3390/pharmaceutics14122679 - 01 Dec 2022

Cited by 2 | Viewed by 1143

Abstract

Following our previous study on the development of EGFR-targeted nanomedicine (NM-scFv) for the active delivery of siRNA in EGFR-positive cancers, this study focuses on the development and the quality control of a radiolabeling method to track it in in vivo conditions with nuclear [...] Read more.

Following our previous study on the development of EGFR-targeted nanomedicine (NM-scFv) for the active delivery of siRNA in EGFR-positive cancers, this study focuses on the development and the quality control of a radiolabeling method to track it in in vivo conditions with nuclear imaging. Our NM-scFv is based on the electrostatic complexation of targeted nanovector (NV-scFv), siRNA and two cationic polymers. NV-scFv comprises an inorganic core, a fluorescent dye, a polymer layer and anti-EGFR ligands. To track NM-scFv in vivo with nuclear imaging, the DTPA chemistry was used to radiolabel NM-scFv with ¹¹¹In. DTPA was thiolated and introduced onto NV-scFv via the maleimide chemistry. To obtain suitable radiolabeling efficiency, different DTPA/NV-scFv ratios were tested, including 0.03, 0.3 and 0.6. At the optimized ratio (where the DTPA/NV-scFv ratio was 0.3), a high radiolabeling yield was achieved (98%) and neither DTPA-derivatization nor indium-radiolabeling showed any impact on NM-scFv’s physicochemical characteristics (D_H ~100 nm, PDi < 0.24). The selected NM-scFv-DTPA demonstrated good siRNA protection capacity and comparable in vitro transfection efficiency into EGFR-overexpressing cells in comparison to that of non-derivatized NM-scFv (around 67%). Eventually, it was able to track both qualitatively and quantitatively NM-scFv in in vivo environments with nuclear imaging. Both the radiolabeling and the NM-scFv showed a high in vivo stability level. Altogether, a radiolabeling method using DTPA chemistry was developed with success in this study to track our NM-scFv in in vivo conditions without any impact on its active targeting and physicochemical properties, highlighting the potential of our NM-scFv for future theranostic applications in EGFR-overexpressing cancers. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Graphical abstract

12 pages, 1883 KiB

Open AccessArticle

Folate-Functionalization Enhances Cytotoxicity of Multivalent DNA Nanocages on Triple-Negative Breast Cancer Cells

by Valeria Unida, Giulia Vindigni, Sofia Raniolo, Carmine Stolfi, Alessandro Desideri and Silvia Biocca

Pharmaceutics 2022, 14(12), 2610; https://doi.org/10.3390/pharmaceutics14122610 - 26 Nov 2022

Cited by 3 | Viewed by 1299

Abstract

DNA is an excellent programmable polymer for the generation of self-assembled multivalent nanostructures useful for biomedical applications. Herein, we developed (i) folate-functionalized nanocages (Fol-NC), very efficiently internalized by tumor cells overexpressing the α isoform of the folate receptor; (ii) AS1411-linked nanocages (Apt-NC), internalized [...] Read more.

DNA is an excellent programmable polymer for the generation of self-assembled multivalent nanostructures useful for biomedical applications. Herein, we developed (i) folate-functionalized nanocages (Fol-NC), very efficiently internalized by tumor cells overexpressing the α isoform of the folate receptor; (ii) AS1411-linked nanocages (Apt-NC), internalized through nucleolin, a protein overexpressed in the cell surface of many types of cancers; and (iii) nanostructures that harbor both folate and AS1411 aptamer functionalization (Fol-Apt-NC). We analyzed the specific miRNA silencing activity of all types of nanostructures harboring miRNA sequestering sequences complementary to miR-21 and the cytotoxic effect when loaded with doxorubicin in a drug-resistant triple-negative breast cancer cell line. We demonstrate that the presence of folate as a targeting ligand increases the efficiency in miR-21 silencing compared to nanocages functionalized with AS1411. Double-functionalized nanocages (Fol-Apt-NC), loaded with doxorubicin, resulted in an increase of over 51% of the cytotoxic effect on MDA-MB-231 cells compared to free doxorubicin, demonstrating, besides selectivity, the ability of nanocages to overcome Dox chemoresistance. The higher efficiency of the folate-functionalized nanocages is due to the way of entrance, which induces more than four times higher intracellular stability and indicates that the folate-mediated route of cell entry is more efficient than the nucleolin-mediated one when both folate and AS1411 modifications are present. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

19 pages, 6333 KiB

Open AccessArticle

Light- and Redox-Responsive Block Copolymers of mPEG-SS-ONBMA as a Smart Drug Delivery Carrier for Cancer Therapy

by Yu-Lun Lo, Yao-Hsing Fang, Yen-Ju Chiu, Chia-Yu Chang, Chih-Hsien Lee, Zi-Xian Liao and Li-Fang Wang

Pharmaceutics 2022, 14(12), 2594; https://doi.org/10.3390/pharmaceutics14122594 - 24 Nov 2022

Cited by 3 | Viewed by 1527

Abstract

The development of stimuli-responsive polymeric micelles for targeted drug delivery has attracted much research interest in improving therapeutic outcomes. This study designs copolymers responsive to ultraviolet (UV) light and glutathione (GSH). A disulfide linkage is positioned between a hydrophilic poly(ethylene glycol) monomethyl ether [...] Read more.

The development of stimuli-responsive polymeric micelles for targeted drug delivery has attracted much research interest in improving therapeutic outcomes. This study designs copolymers responsive to ultraviolet (UV) light and glutathione (GSH). A disulfide linkage is positioned between a hydrophilic poly(ethylene glycol) monomethyl ether (mPEG) and a hydrophobic o-nitrobenzyl methacrylate (ONBMA) to yield amphiphilic copolymers termed mPEG-SS-pONBMA. Three copolymers with different ONBMA lengths are synthesized and formulated into micelles. An increase in particle size and a decrease in critical micelle concentration go together with increasing ONBMA lengths. The ONB cleavage from mPEG-SS-pONBMA-formed micelles results in the transformation of hydrophobic cores into hydrophilic ones, accelerating drug release from the micelles. Obvious changes in morphology and molecular weight of micelles upon combinational treatments account for the dual-stimuli responsive property. Enhancement of a cell-killing effect is clearly observed in doxorubicin (DOX)-loaded micelles containing disulfide bonds compared with those containing dicarbon bonds upon UV light irradiation. Collectedly, the dual-stimuli-responsive mPEG-SS-pONBMA micelle is a better drug delivery carrier than the single-stimuli-responsive mPEG-CC-pONBMA micelle. After HT1080 cells were treated with the DOX-loaded micelles, the high expression levels of RIP-1 and MLKL indicate that the mechanism involved in cell death is mainly via the DOX-induced necroptosis pathway. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

17 pages, 2908 KiB

Open AccessArticle

pH-Sensitive Liposomes for Enhanced Cellular Uptake and Cytotoxicity of Daunorubicin in Melanoma (B16-BL6) Cell Lines

by Hamad Alrbyawi, Ishwor Poudel, Manjusha Annaji, Sai H. S. Boddu, Robert D. Arnold, Amit K. Tiwari and R. Jayachandra Babu

Pharmaceutics 2022, 14(6), 1128; https://doi.org/10.3390/pharmaceutics14061128 - 26 May 2022

Cited by 13 | Viewed by 2696

Abstract

Daunorubicin (DNR) was delivered using a pH-sensitive liposomal system in B16-BL6 melanoma cell lines for enhanced cytotoxic effects. DNR was encapsulated within liposomes and CL as a component of the lipid bilayer. PEGylated pH-sensitive liposomes, containing CL, were prepared in the molar ratio [...] Read more.

Daunorubicin (DNR) was delivered using a pH-sensitive liposomal system in B16-BL6 melanoma cell lines for enhanced cytotoxic effects. DNR was encapsulated within liposomes and CL as a component of the lipid bilayer. PEGylated pH-sensitive liposomes, containing CL, were prepared in the molar ratio of 40:30:5:17:8 for DOPE/cholesterol/DSPE-mPEG (2000)/CL/SA using the lipid film hydration method and loaded with DNR (drug: lipid ratio of 1:5). The CL liposomes exhibited high drug encapsulation efficiency (>90%), a small size (~94 nm), narrow size distribution (polydispersity index ~0.16), and a rapid release profile at acidic pH (within 1 h). Furthermore, the CL liposomes exhibited 12.5- and 2.5-fold higher cytotoxicity compared to DNR or liposomes similar to DaunoXome^®. This study provides a basis for developing DNR pH-sensitive liposomes for melanoma treatment. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Graphical abstract

Review

Jump to: Research, Other

21 pages, 1338 KiB

Open AccessReview

Immunotherapy Innovations in the Fight against Osteosarcoma: Emerging Strategies and Promising Progress

by Shigao Cheng, Huiyuan Wang, Xuejia Kang and Hui Zhang

Pharmaceutics 2024, 16(2), 251; https://doi.org/10.3390/pharmaceutics16020251 - 08 Feb 2024

Viewed by 1070

Abstract

Immunosuppressive elements within the tumor microenvironment are the primary drivers of tumorigenesis and malignant advancement. The presence, as well as the crosstalk between myeloid-derived suppressor cells (MDSCs), osteosarcoma-associated macrophages (OS-Ms), regulatory T cells (Tregs), and endothelial cells (ECs) with osteosarcoma cells cause the [...] Read more.

Immunosuppressive elements within the tumor microenvironment are the primary drivers of tumorigenesis and malignant advancement. The presence, as well as the crosstalk between myeloid-derived suppressor cells (MDSCs), osteosarcoma-associated macrophages (OS-Ms), regulatory T cells (Tregs), and endothelial cells (ECs) with osteosarcoma cells cause the poor prognosis of OS. In addition, the consequent immunosuppressive factors favor the loss of treatment potential. Nanoparticles offer a means to dynamically and locally manipulate immuno-nanoparticles, which present a promising strategy for transforming OS-TME. Additionally, chimeric antigen receptor (CAR) technology is effective in combating OS. This review summarizes the essential mechanisms of immunosuppressive cells in the OS-TME and the current immune-associated strategies. The last part highlights the limitations of existing therapies and offers insights into future research directions. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

26 pages, 4283 KiB

Open AccessReview

Advancing Cancer Therapy with Copper/Disulfiram Nanomedicines and Drug Delivery Systems

by Xuejia Kang, Sanika Jadhav, Manjusha Annaji, Chung-Hui Huang, Rajesh Amin, Jianzhong Shen, Charles R. Ashby, Jr., Amit K. Tiwari, R. Jayachandra Babu and Pengyu Chen

Pharmaceutics 2023, 15(6), 1567; https://doi.org/10.3390/pharmaceutics15061567 - 23 May 2023

Cited by 5 | Viewed by 2841

Abstract

Disulfiram (DSF) is a thiocarbamate based drug that has been approved for treating alcoholism for over 60 years. Preclinical studies have shown that DSF has anticancer efficacy, and its supplementation with copper (CuII) significantly potentiates the efficacy of DSF. However, the results of [...] Read more.

Disulfiram (DSF) is a thiocarbamate based drug that has been approved for treating alcoholism for over 60 years. Preclinical studies have shown that DSF has anticancer efficacy, and its supplementation with copper (CuII) significantly potentiates the efficacy of DSF. However, the results of clinical trials have not yielded promising results. The elucidation of the anticancer mechanisms of DSF/Cu (II) will be beneficial in repurposing DSF as a new treatment for certain types of cancer. DSF’s anticancer mechanism is primarily due to its generating reactive oxygen species, inhibiting aldehyde dehydrogenase (ALDH) activity inhibition, and decreasing the levels of transcriptional proteins. DSF also shows inhibitory effects in cancer cell proliferation, the self-renewal of cancer stem cells (CSCs), angiogenesis, drug resistance, and suppresses cancer cell metastasis. This review also discusses current drug delivery strategies for DSF alone diethyldithocarbamate (DDC), Cu (II) and DSF/Cu (II), and the efficacious component Diethyldithiocarbamate–copper complex (CuET). Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

23 pages, 7601 KiB

Open AccessReview

Tailored Functionalized Protein Nanocarriers for Cancer Therapy: Recent Developments and Prospects

by Mohamed A. A. Abdelhamid, Mi-Ran Ki, Amer Ali Abd El-Hafeez, Ryeo Gang Son and Seung Pil Pack

Pharmaceutics 2023, 15(1), 168; https://doi.org/10.3390/pharmaceutics15010168 - 03 Jan 2023

Cited by 5 | Viewed by 2578

Abstract

Recently, the potential use of nanoparticles for the targeted delivery of therapeutic and diagnostic agents has garnered increased interest. Several nanoparticle drug delivery systems have been developed for cancer treatment. Typically, protein-based nanocarriers offer several advantages, including biodegradability and biocompatibility. Using genetic engineering [...] Read more.

Recently, the potential use of nanoparticles for the targeted delivery of therapeutic and diagnostic agents has garnered increased interest. Several nanoparticle drug delivery systems have been developed for cancer treatment. Typically, protein-based nanocarriers offer several advantages, including biodegradability and biocompatibility. Using genetic engineering or chemical conjugation approaches, well-known naturally occurring protein nanoparticles can be further prepared, engineered, and functionalized in their self-assembly to meet the demands of clinical production efficiency. Accordingly, promising protein nanoparticles have been developed with outstanding tumor-targeting capabilities, ultimately overcoming multidrug resistance issues, in vivo delivery barriers, and mimicking the tumor microenvironment. Bioinspired by natural nanoparticles, advanced computational techniques have been harnessed for the programmable design of highly homogenous protein nanoparticles, which could open new routes for the rational design of vaccines and drug formulations. The current review aims to present several significant advancements made in protein nanoparticle technology, and their use in cancer therapy. Additionally, tailored construction methods and therapeutic applications of engineered protein-based nanoparticles are discussed. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

35 pages, 4348 KiB

Open AccessReview

siRNA Functionalized Lipid Nanoparticles (LNPs) in Management of Diseases

by Tutu Kalita, Saba Abbasi Dezfouli, Lalit M. Pandey and Hasan Uludag

Pharmaceutics 2022, 14(11), 2520; https://doi.org/10.3390/pharmaceutics14112520 - 19 Nov 2022

Cited by 16 | Viewed by 3678

Abstract

RNAi (RNA interference)-based technology is emerging as a versatile tool which has been widely utilized in the treatment of various diseases. siRNA can alter gene expression by binding to the target mRNA and thereby inhibiting its translation. This remarkable potential of siRNA makes [...] Read more.

RNAi (RNA interference)-based technology is emerging as a versatile tool which has been widely utilized in the treatment of various diseases. siRNA can alter gene expression by binding to the target mRNA and thereby inhibiting its translation. This remarkable potential of siRNA makes it a useful candidate, and it has been successively used in the treatment of diseases, including cancer. However, certain properties of siRNA such as its large size and susceptibility to degradation by RNases are major drawbacks of using this technology at the broader scale. To overcome these challenges, there is a requirement for versatile tools for safe and efficient delivery of siRNA to its target site. Lipid nanoparticles (LNPs) have been extensively explored to this end, and this paper reviews different types of LNPs, namely liposomes, solid lipid NPs, nanostructured lipid carriers, and nanoemulsions, to highlight this delivery mode. The materials and methods of preparation of the LNPs have been described here, and pertinent physicochemical properties such as particle size, surface charge, surface modifications, and PEGylation in enhancing the delivery performance (stability and specificity) have been summarized. We have discussed in detail various challenges facing LNPs and various strategies to overcome biological barriers to undertake the safe delivery of siRNA to a target site. We additionally highlighted representative therapeutic applications of LNP formulations with siRNA that may offer unique therapeutic benefits in such wide areas as acute myeloid leukaemia, breast cancer, liver disease, hepatitis B and COVID-19 as recent examples. Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

► Show Figures

Figure 1

Other

Jump to: Research, Review

1 pages, 163 KiB

Open AccessCorrection

Correction: Kalvala et al. Cannabidiol-Loaded Extracellular Vesicles from Human Umbilical Cord Mesenchymal Stem Cells Alleviate Paclitaxel-Induced Peripheral Neuropathy. Pharmaceutics 2023, 15, 554

by Anil Kumar Kalvala, Arvind Bagde, Peggy Arthur, Tanmay Kulkarni, Santanu Bhattacharya, Sunil Surapaneni, Nil Kumar Patel, Ramesh Nimma, Aragaw Gebeyehu, Nagavendra Kommineni, Yan Li, David G. Meckes, Jr., Li Sun, Bipika Banjara, Keb Mosley-Kellum, Thanh Cong Dinh and Mandip Singh

Pharmaceutics 2023, 15(9), 2200; https://doi.org/10.3390/pharmaceutics15092200 - 25 Aug 2023

Viewed by 494

Abstract

“Yan Li” was not included as an author in the original publication [...] Full article

(This article belongs to the Special Issue Functionalized Nanoparticles in Cancer Therapeutics)

Journal Menu

Journal Browser

Functionalized Nanoparticles in Cancer Therapeutics

Share This Special Issue

Special Issue Editors

Special Issue Information

Keywords

Published Papers (13 papers)

Research

Review

Other

Further Information

Guidelines

MDPI Initiatives

Follow MDPI