Synthetic-polymer-assisted antisense oligonucleotide delivery: targeted approaches for precision disease treatment

• Ana Cubillo Alvarez,
• Dylan Maguire and
• Ruairí P. Brannigan

Beilstein J. Nanotechnol. 2025, 16, 435–463, doi:10.3762/bjnano.16.34

• with high-molecular-weight PEI (Mw ≈ 25 kDa) [116]. Early studies by Kim et al. [117] and Xie et al. [118] investigated the targeted modulatory effects of siRNAs and ASOs delivered using branched and linear PEI carriers conjugated with folate and linoleic acid, respectively. In both reports, the

Radiosensitizing properties of dual-functionalized carbon nanostructures loaded with temozolomide

• Radmila Milenkovska,
• Nikola Geskovski,
• Dushko Shalabalija,
• Ljubica Mihailova,
• Petre Makreski,
• Dushko Lukarski,
• Igor Stojkovski,
• Maja Simonoska Crcarevska and
• Kristina Mladenovska

Beilstein J. Nanotechnol. 2025, 16, 229–251, doi:10.3762/bjnano.16.18

• accumulation in the brain tumor cells (through the active targeting of the formulations towards membrane folate receptors of GBM). Detailed physicochemical and biopharmaceutical characterizations of the prepared TMZ-loaded dual-functionalized CNs was performed, and the cytotoxicity/radiosensitizing properties

• effect of PEG on cell growth and its biocompatibility by inducing metabolism modulations and survival autophagy through creating an intracellular hypoxic environment. Although there is no consensus on whether the role of folate in cancer cells is protective or harmful, a cytotoxic effect was also

• inactivation of tumor suppressor genes in correlation with overexpression of folate receptors, on the other side. Including the differences in particle size of the CNs in the actual study (Table 1), that is, the slightly higher value for d50 of the dual-functionalized hybrid CN (374 vs 270 nm), similar values

Nanocarriers and macrophage interaction: from a potential hurdle to an alternative therapeutic strategy

• Naths Grazia Sukubo,
• Paolo Bigini and
• Annalisa Morelli

Beilstein J. Nanotechnol. 2025, 16, 97–118, doi:10.3762/bjnano.16.10

• ]. In RA, the predominance of M1 macrophages in inflamed joints drives synovitis and cartilage destruction. Yang and colleagues developed folic acid-modified silver nanoparticles (FA-AgNPs) to target M1 macrophages via folate receptor-mediated endocytosis. Once internalized, these NPs scavenged ROS

Dual-functionalized architecture enables stable and tumor cell-specific SiO₂NPs in complex biological fluids

• Iris Renata Sousa Ribeiro,
• Raquel Frenedoso da Silva,
• Romênia Ramos Domingues,
• Adriana Franco Paes Leme and
• Mateus Borba Cardoso

Beilstein J. Nanotechnol. 2024, 15, 1238–1252, doi:10.3762/bjnano.15.100

• -depth studies in complex environments to evaluate nanoparticle stability, protein corona formation, hemolytic activity, and targeting capabilities. To address this issue, fluorescent silica nanoparticles (SiO2NPs) are here functionalized with zwitterionic (kinetic stabilizer) and folate groups

• [1][2][3][4]. Consequently, the scientific community has focused on improving the targeting of nanoparticles (NPs) to tumor cells through surface functionalization with active groups (e.g., folate, monoclonal antibodies) [5][6][7]. However, according to the literature, only 0.7% of the injected dose

• play a key role in obtaining NPs with the desired stability and functionality in bodily fluids [12]. Here, we proposed developing SiO2NPs colloidally stable in biological media and targetable to tumor cells through selective binding with folate receptors, highly expressed in tumor cell lines

Realizing active targeting in cancer nanomedicine with ultrasmall nanoparticles

• André F. Lima,
• Giselle Z. Justo and
• Alioscka A. Sousa

Beilstein J. Nanotechnol. 2024, 15, 1208–1226, doi:10.3762/bjnano.15.98

• difference was attributed to easier tumor clearance (tumor intravasation back to blood vessels) of off-targeted 3 nm NPs compared to 30 nm ones. Common functional ligands employed in actively targeted usNPs encompass small molecules such as folate, aptamers, peptides, full antibodies, and antibody fragments

• ][156][157][158][159]; and Table 2 provides a quantitative assessment of tumor uptake for actively targeted usNPs compared to control groups, limited to studies including quantitative values of % ID/g. 5.1 Folic acid ligand/folate receptor Wu et al. developed core–shell silica NPs (Cornell dots, or C

• multifunctional C’ dots. (B) Competitive cell-binding assay of targeted usNPs (EC112002) revealed a 40-fold improvement in affinity for folate receptor binding compared to free folic acid. (C) Z-stacks of confocal microscopy images of a tumor spheroid treated with targeted usNPs (first and second rows) and

Unveiling the potential of alginate-based nanomaterials in sensing technology and smart delivery applications

• Shakhzodjon Uzokboev,
• Khojimukhammad Akhmadbekov,
• Ra’no Nuritdinova,
• Salah M. Tawfik and
• Yong-Ill Lee

Beilstein J. Nanotechnol. 2024, 15, 1077–1104, doi:10.3762/bjnano.15.88

• folate (FA) and polyethylene glycol (PEG) onto the alginic acid backbone. These compounds can be utilized in the encapsulation of doxorubicin (DOX) by coating with upconversion nanoparticles (UCNPs), as shown in Figure 3A. When DOX-loaded UCNP-Al-NH-PEG-NH-FA was used, an effective encapsulation

Therapeutic effect of F127-folate@PLGA/CHL/IR780 nanoparticles on folate receptor-expressing cancer cells

• Thi Ngoc Han Pham,
• Phuong-Thao Dang-Luong,
• Hong-Phuc Nguyen,
• Loc Le-Tuan,
• Xuan Thang Cao,
• Thanh-Danh Nguyen,
• Vy Tran Anh and
• Hieu Vu_Quang

Beilstein J. Nanotechnol. 2024, 15, 954–964, doi:10.3762/bjnano.15.78

• chemotherapeutic agent chlorambucil (CHL) and the imaging agent IR780. The approach in this study incorporates Pluronic F127-folate onto the PLGA nanoparticles, which enables targeted delivery to folate receptor-expressing cancer cells. The F127-folate@PLGA/CHL/IR780 nanoparticles were formulated using a

• nanoprecipitation technique, resulting in small size, high homogeneity, and negative surface charge. Importantly, the folate-targeted nanoparticles demonstrated enhanced uptake and cytotoxicity in folate receptor-positive cancer cell lines (MCF-7 and HepG-2) compared to folate receptor-negative cells (HEK 293

• ). Additionally, the F127-folate@PLGA/CHL/IR780 nanoparticles exhibited a lower IC50 value against cancer cells than non-targeted F127@PLGA/CHL/IR780 nanoparticles. These findings suggest that the developed F127-folate@PLGA/CHL/IR780 nanoparticles hold promise as a theragnostic system for targeted cancer therapy

Nanocarrier systems loaded with IR780, iron oxide nanoparticles and chlorambucil for cancer theragnostics

• Phuong-Thao Dang-Luong,
• Hong-Phuc Nguyen,
• Loc Le-Tuan,
• Xuan-Thang Cao,
• Vy Tran-Anh and
• Hieu Vu Quang

Beilstein J. Nanotechnol. 2024, 15, 180–189, doi:10.3762/bjnano.15.17

• alcohol)-based nanoparticles (NPs) using the single emulsion technique. Then the NPs were coated with F127 and F127-folate by simple incubation for five days. The nanoparticles have the hydrodynamic size of approx. 250 nm with negative charge. Similar to chlorambucil and IR780, iron oxide loadings were

• observed for all three kinds of NPs. The release of chlorambucil was quicker at pH 5.4 than at pH 7.4 at 37 °C. The F127@NPs and F127-folate@NPs demonstrated much greater cell uptake and toxicity up to 72 h after incubation. Our in vitro results of F127@NPs and F127-folate@NPs have demonstrated the ability

• of these systems to serve as medication and imaging agent carriers for cancer treatment and diagnostics, respectively. Keywords: cancer; chlorambucil; F127-folate; IR780; iron oxide nanoparticles; PLGA; theragnostics; Introduction Theragnostic nanoparticles (NPs) are a diagnostic and therapeutic

Antibody-conjugated nanoparticles for target-specific drug delivery of chemotherapeutics

• Mamta Kumari,
• Amitabha Acharya and
• Praveen Thaggikuppe Krishnamurthy

Beilstein J. Nanotechnol. 2023, 14, 912–926, doi:10.3762/bjnano.14.75

• receptor (ER), folate receptors (FRs), human epithelial receptor (HER-2) and transferrin receptors (TfRs) [30][31][32][33][34], has been explored extensively. The selective targeting of these molecular targets via antibody-conjugated NPs provides an efficient platform to accurately deliver the drug cargo

Nanotechnology – a robust tool for fighting the challenges of drug resistance in non-small cell lung cancer

• Filip Gorachinov,
• Fatima Mraiche,
• Diala Alhaj Moustafa,
• Ola Hishari,
• Yomna Ismail,
• Jensa Joseph,
• Maja Simonoska Crcarevska,
• Marija Glavas Dodov,
• Nikola Geskovski and
• Katerina Goracinova

Beilstein J. Nanotechnol. 2023, 14, 240–261, doi:10.3762/bjnano.14.23

• include ανβ3 integrin, aminopeptidase N (CD13), lymphocyte homing receptor (CD44), programmed death ligand-1 (CD274), folate receptor protein, nucleolin receptor, epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), human epidermal growth factor receptor 2 (HER2

Cyclodextrins as eminent constituents in nanoarchitectonics for drug delivery systems

• Makoto Komiyama

Beilstein J. Nanotechnol. 2023, 14, 218–232, doi:10.3762/bjnano.14.21

• an eminent solution to this problem. For example, polyamidoamine dendrimer (generation 3) conjugated with α-CyD (average number = 2.4) is very effective to deliver siRNA to cells [62][63]. By appending folate, the conjugates are successfully targeted to tumor cells on which folate receptors are

Recent advances in green carbon dots (2015–2022): synthesis, metal ion sensing, and biological applications

• Aisha Kanwal,
• Naheed Bibi,
• Sajjad Hyder,
• Arif Muhammad,
• Hao Ren,
• Jiangtao Liu and
• Zhongli Lei

Beilstein J. Nanotechnol. 2022, 13, 1068–1107, doi:10.3762/bjnano.13.93

• to target folate-receptor cancer cells [114]. Pork-based CDs without any surface-passivating agent were synthesized. Pork meat, itself, is composed of many organic molecules that can provide multiple heteroatoms in the CDs. The resulting CDs have excellent advantages such as a high QY of 17.3% and

Theranostic potential of self-luminescent branched polyethyleneimine-coated superparamagnetic iron oxide nanoparticles

• Rouhollah Khodadust,
• Ozlem Unal and
• Havva Yagci Acar

Beilstein J. Nanotechnol. 2022, 13, 82–95, doi:10.3762/bjnano.13.6

• modification may change the internalization pathway of the nanoparticles. As an example, in 2009, Gabrielson et al. demonstrated that folic acid modification of PEI polyplex enhances internalization via a caveolar pathway in cells expressing folate receptors [64]. Since caveolae-mediated internalization

Comprehensive review on ultrasound-responsive theranostic nanomaterials: mechanisms, structures and medical applications

• Sepand Tehrani Fateh,
• Lida Moradi,
• Elmira Kohan,
• Michael R. Hamblin and
• Amin Shiralizadeh Dezfuli

Beilstein J. Nanotechnol. 2021, 12, 808–862, doi:10.3762/bjnano.12.64

The impact of molecular tumor profiling on the design strategies for targeting myeloid leukemia and EGFR/CD44-positive solid tumors

• Nikola Geskovski,
• Nadica Matevska-Geshkovska,
• Simona Dimchevska Sazdovska,
• Marija Glavas Dodov,
• Kristina Mladenovska and
• Katerina Goracinova

Beilstein J. Nanotechnol. 2021, 12, 375–401, doi:10.3762/bjnano.12.31

• cells, which could be used as potential targets for a NDDS-based therapeutic approach (Table 1). The folate receptor is usually overexpressed in all cancer cells and the high frequency (ca. 70%) of folate receptor (FR) β expression in CML and AML relative to normal hematopoietic cells suggests the

• authors noticed that the cytotoxicity of folate-functionalized liposomes was greater in FR positive cell lines and that the effect could be blocked through the addition of 1 mM folic acid. Additionally, the authors revealed that the functionalized carriers increased the median survival of the mouse

Differences in surface chemistry of iron oxide nanoparticles result in different routes of internalization

• Barbora Svitkova,
• Vlasta Zavisova,
• Veronika Nemethova,
• Martina Koneracka,
• Miroslava Kretova,
• Filip Razga,
• Monika Ursinyova and
• Alena Gabelova

Beilstein J. Nanotechnol. 2021, 12, 270–281, doi:10.3762/bjnano.12.22

• ], just like in our study. In line with our results, Langston Suen and Chau [61] reported the uptake of folate-decorated NPs of 50 nm in size by CME into retinal pigment epithelium cells, while 250 nm particles were dominated by CavME. Surprisingly, the addition of CME inhibitors to the culture medium

Applications of superparamagnetic iron oxide nanoparticles in drug and therapeutic delivery, and biotechnological advancements

• Maria Suciu,
• Corina M. Ionescu,
• Alexandra Ciorita,
• Septimiu C. Tripon,
• Dragos Nica,
• Hani Al-Salami and
• Lucian Barbu-Tudoran

Beilstein J. Nanotechnol. 2020, 11, 1092–1109, doi:10.3762/bjnano.11.94

• for MRI and fluorescence imaging with good cytocompatibility. Park et al. [161] synthesized SPIONs coated with folate containing 64Cu for positronic emission tomography and MRI. Cai et al. [162] obtained 12 nm SPIONs coated with a near-infrared fluorescent dye for dual in vivo imagistics (MRI and

Luminescent gold nanoclusters for bioimaging applications

• Nonappa

Beilstein J. Nanotechnol. 2020, 11, 533–546, doi:10.3762/bjnano.11.42

• of streptavidin with biotin was exploited for imaging human hepatoma cells (HepG2, Figure 4C). HepG2 are cancerous cells that contain excess biotin. Retnakumari et al. studied the surface functionalization of Au-BSA NCs with folic acid (FA) for selective binding, internalization and imaging of folate

Multilayer capsules made of weak polyelectrolytes: a review on the preparation, functionalization and applications in drug delivery

• Varsha Sharma and
• Anandhakumar Sundaramurthy

Beilstein J. Nanotechnol. 2020, 11, 508–532, doi:10.3762/bjnano.11.41

• efficient carriers for controlled release. The later work on capsule/lipid systems incorporated with neoglycolipid or folate-linked lipid showed high affinity to lectin (concanavalin A) and breast cancer cells (MCF-7) [109]. The efficient delivery of the daunorubicin hydrochloride (DNR) anticancer drug to

• cancer cells was achieved through folate-targeted sodium alginate/chitosan capsules. The lipid coating on the PAH/PSS microcapsule surface significantly reduced the permeability of the capsule walls [110]. Alternatively, carbohydrate functionalization has been widely used in hepatic drug delivery systems

Interactions at the cell membrane and pathways of internalization of nano-sized materials for nanomedicine

• Valentina Francia,
• Daphne Montizaan and
• Anna Salvati

Beilstein J. Nanotechnol. 2020, 11, 338–353, doi:10.3762/bjnano.11.25

• active targeting [9][10][11][12]. These surface-functionalized nanomaterials should be internalized preferentially by cells that overexpress the targeted receptors. Examples of targeting moieties often exploited in nanomedicine are transferrin and folate, which target tumour cells overexpressing the

Rational design of block copolymer self-assemblies in photodynamic therapy

• Maxime Demazeau,
• Laure Gibot,
• Anne-Françoise Mingotaud,
• Patricia Vicendo,
• Clément Roux and
• Barbara Lonetti

Beilstein J. Nanotechnol. 2020, 11, 180–212, doi:10.3762/bjnano.11.15

• a hydrophilic shell for micelle stabilization, and the derivatized polylysin (Plys) acts as a hydrophobic core to load the photosensitizer (BODIPY), while PMAGP mainly serves to direct the target delivery to hepatoma cancer cells. Folate (FA) has been extensively studied as a targeting moiety [116

• ] due to the overexpression of folate receptors in a number of tumor types including ovarian [117] or breast cancers [118]. One of the most recent examples of FA use in PDT applications is by Li et al., where the authors have designed a FA-PEO-PLA construct to deliver hypocrellin B, a sensitizer

Molecular architectonics of DNA for functional nanoarchitectures

• Debasis Ghosh,
• Lakshmi P. Datta and
• Thimmaiah Govindaraju

Beilstein J. Nanotechnol. 2020, 11, 124–140, doi:10.3762/bjnano.11.11

• co-workers showed that self-assembled DNA tetrahedron nanoarchitectures with narrow size distribution could deliver siRNA into tumor cells [71]. The programmable DNA strands were functionalized with tumor-targeting folate ligands. The nanoarchitecture consisted of six DNA strands having a total of

Polydopamine-coated Au nanorods for targeted fluorescent cell imaging and photothermal therapy

• Boris N. Khlebtsov,
• Andrey M. Burov,
• Timofey E. Pylaev and
• Nikolai G. Khlebtsov

Beilstein J. Nanotechnol. 2019, 10, 794–803, doi:10.3762/bjnano.10.79

• with functional groups still remains challenging. Here, we coated AuNRs with a polydopamine (PDA) shell and functionalized AuNR-PDA particles with folic acid and rhodamine 123 (R123) to fabricate AuNR-PDA-R123-folate nanocomposites. To the best of our knowledge, such AuNR-PDA-based composites combining

• fluorescent imaging and plasmonic phothothermal abilities have not been reported previously. The multifunctional nanoparticles were stable in cell buffer, nontoxic and suitable for targeted fluorescent imaging and photothermal therapy of cancer cells. We demonstrate the enhanced accumulation of folate

• -functionalized nanoparticles in folate-positive HeLa cells in contrast to the folate-negative HEK 293 cells using fluorescent microscopy. The replacement of folic acid with polyethylene glycol (PEG) leads to a decrease in nanoparticle uptake by both folate-positive and folate-negative cells. We performed NIR

Multiwalled carbon nanotube hybrids as MRI contrast agents

• Nikodem Kuźnik and
• Mateusz M. Tomczyk

Beilstein J. Nanotechnol. 2016, 7, 1086–1103, doi:10.3762/bjnano.7.102

• exhibit high over-expression of the folate receptor, the targeting effect was remarkable and was found to reach 64% signal enhancement in reference to 45% for the non-functionalized hybrids. Lamanna and Vittorio were able to localize the marked cells by their darkened contrast and emphasized the unique

Chemiresistive/SERS dual sensor based on densely packed gold nanoparticles

• Sanda Boca,
• Cosmin Leordean,
• Simion Astilean and
• Cosmin Farcau

Beilstein J. Nanotechnol. 2015, 6, 2498–2503, doi:10.3762/bjnano.6.259

• folic acid molecules. Folic acid is a low molecular weight vitamin compound, which has been shown to be an effective targeting vector of various cancer cell lines which over-express folate receptors [7]. It also proved to be an effective capping ligand for linking onto various polymer backbones or