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

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

Biomimetic nanocarriers: integrating natural functions for advanced therapeutic applications

• Hugo Felix Perini,
• Beatriz Sodré Matos,
• Carlo José Freire de Oliveira and
• Marcos Vinicius da Silva

Beilstein J. Nanotechnol. 2024, 15, 1619–1626, doi:10.3762/bjnano.15.127

• or active targeting mechanisms. In the passive strategy, coated nanocarriers can traverse permeable vessels (as observed in tumors, for example) and exhibit tropism toward specific pathological targets based on the size, surface charge, and physicochemical properties of the nanostructure. The active

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

• induce colloidal destabilization and/or changes in their original biochemical identity, compromising their ability to selectively accumulate at target sites. In this way, these systems usually lack active targeting, offering limited therapeutic effectiveness. In the literature, there is a paucity of in

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

• demonstrate favorable tumor penetration and intratumoral diffusion. Active targeting strategies, incorporating ligands for specific tumor receptor binding, serve to further enhance usNP tumor selectivity and therapeutic performance. Numerous preclinical studies have already demonstrated the potential of

• . Keywords: active targeting; cancer; nanoclusters; renal clearance; ultrasmall nanoparticles; Review 1 Introduction Nanotechnology has opened new avenues for tackling unmet challenges in medicine [1][2][3]. In the field of oncology, a notable application involves the use of engineered nanoparticles (NPs

• primarily occurs via transendothelial transport pathways [6][7]. Regardless of the mode of NP extravasation, active targeting strategies have been widely explored to further enhance NP accumulation in tumors and NP internalization by cancer cells [8][9]. Active targeting involves the modification of NPs

Recent updates in applications of nanomedicine for the treatment of hepatic fibrosis

• Damai Ria Setyawati,
• Fransiska Christydira Sekaringtyas,
• Riyona Desvy Pratiwi,
• A’liyatur Rosyidah,
• Rohimmahtunnissa Azhar,
• Nunik Gustini,
• Gita Syahputra,
• Idah Rosidah,
• Etik Mardliyati,
• Tarwadi and
• Sjaikhurrizal El Muttaqien

Beilstein J. Nanotechnol. 2024, 15, 1105–1116, doi:10.3762/bjnano.15.89

• fibrosis. We first emphasize the challenges of conventional drugs for penetrating the biological barriers of the liver. After that, we highlight design principles of nanocarriers for achieving improved drug delivery of antifibrosis drugs through passive and active targeting strategies. Keywords: active

• ]. The EPR effect has been a cornerstone for cancer nanomedicine development, and various types of nanocarrier drug delivery systems have been developed to take advantage of this passively targeted strategy. Moreover, active targeting strategies have been developed to further improve the drug

• , liver-targeted nanocarriers are needed to increase the drug concentration in the liver with minimum off-target effects. For this purpose, both passive and active targeting strategies of nanomedicine-based drug deliveries have been studied. Liposomes, micelles, solid lipid NPs, and gold NPs are examples

Curcumin-loaded nanostructured systems for treatment of leishmaniasis: a review

• Douglas Dourado,
• Thayse Silva Medeiros,
• Éverton do Nascimento Alencar,
• Edijane Matos Sales and
• Fábio Rocha Formiga

Beilstein J. Nanotechnol. 2024, 15, 37–50, doi:10.3762/bjnano.15.4

• antileishmanial drugs to such sites. Overall, drug targeting results in increased treatment efficacy and reduced toxicity, mostly by reducing drug doses and preventing its interaction with unwanted receptors [30][65]. In this scenario, active targeting happens by the functionalization of nanocarriers, making drug

Elasticity, an often-overseen parameter in the development of nanoscale drug delivery systems

• Agnes-Valencia Weiss and
• Marc Schneider

Beilstein J. Nanotechnol. 2023, 14, 1149–1156, doi:10.3762/bjnano.14.95

• potentially cause undesired side effects [31]. Nevertheless, effective cellular uptake of the majority of soft nanoparticles can be improved either by tuning the material properties or by active targeting. The usage of nanoparticles with high deformability for enhanced passive tumor targeting seems to be a

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

• the theranostic applications of ACNPs for the treatment of cancer. Keywords: active targeting; chemical conjugation; chemotherapeutics; drug delivery; monoclonal antibody; Introduction Off-target side effects, such as myelosuppression, mucositis, alopecia, organ dysfunction, and thrombocytopenia

• active targeting via the functionalization of ligands, such as antibodies or proteins, that interact with receptors overexpressed at the target site [5][6]. However, the movement of NPs is hampered by biological barriers such as endothelial, cellular, skin, and mucosal barriers, which obstruct their

• NPs specifically bind to the cell surface proteins and deliver the drug cargo to tumor sites via passive or active targeting. As a result, the therapeutic ratio is improved. At the same time, the systemic toxicity is reduced and the therapeutic efficacy is increased [13]. Antibody-conjugated NPs

Overview of mechanism and consequences of endothelial leakiness caused by metal and polymeric nanoparticles

• Magdalena Lasak and
• Karol Ciepluch

Beilstein J. Nanotechnol. 2023, 14, 329–338, doi:10.3762/bjnano.14.28

• achievable utilizing NPs less than 100 nm in diameter. In contrast, active targeting strategies involve functionalizing the NP surface with appropriate ligands specific for receptors overexpressed by the cancer cells (e.g., folic acid and transferrin). The combination of the paracellular gap size resulting

• from the EPR effect and active targeting strategies may increase the efficacy of the therapy. Nevertheless, the accumulation in other, non-targeted organs indicates the existence of a method of NP transport through the endothelium other than EPR [26][28][29][32]. Sindhwani et al. identified an active

Recent progress in cancer cell membrane-based nanoparticles for biomedical applications

• Qixiong Lin,
• Yueyou Peng,
• Yanyan Wen,
• Xiaoqiong Li,
• Donglian Du,
• Weibin Dai,
• Wei Tian and
• Yanfeng Meng

Beilstein J. Nanotechnol. 2023, 14, 262–279, doi:10.3762/bjnano.14.24

• anticancer effects [76]. After QT was delivered to tumor tissue by the active targeting ability of the membrane, the sensitivity to radiotherapy was effectively improved, and a strong anticancer effect was exerted under X-ray irradiation [76]. Gong et al. designed a pH-responsive multifunctional biomimetic

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

• copolymer core–shell NPs, (ii) polymer–polypeptide hybrid core–shell NPs, and (iii) polymer–lipid hybrid core–shell NPs additionally decorated with ligands for overexpressed receptors on cancer cells [92]. Traditionally selected overexpressed cancer cell surface markers for the active targeting of NPs

• can be subsequently modified using thiolene chemistry to introduce positive charges [−NH2 (cysteamine, ENT)], negative charges [−COOH (3-mercaptopropionic acid, ECT)], and active targeting ligands [thiogalactose residues (EGT)] for fine-tuning the charges in the shell in different biological

Use of nanosystems to improve the anticancer effects of curcumin

• Andrea M. Araya-Sibaja,
• Norma J. Salazar-López,
• Krissia Wilhelm Romero,
• José R. Vega-Baudrit,
• J. Abraham Domínguez-Avila,
• Carlos A. Velázquez Contreras,
• Ramón E. Robles-Zepeda,
• Mirtha Navarro-Hoyos and
• Gustavo A. González-Aguilar

Beilstein J. Nanotechnol. 2021, 12, 1047–1062, doi:10.3762/bjnano.12.78

• coefficient. Another study reported a co-loaded CUR–lactoferrin NLC that was prepared as a potential delivery system to cancerous cells through both active and passive targeting [70]. For example, the lactoferrin vector was used for active targeting due to its ability to target tumor cells (mediated by

• shown to increase the antiproliferative effect (IC50 12.4 µM) of CUR, as compared to the free molecule (IC50 17.2 µM) within the assayed range (5–40 µM) [132]. Cui et al. [134] reported the use of CUR-loaded MNP to achieve active targeting in conjunction with transferrin receptor binding peptide T7

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

• transcription factors, but also as roadmaps for active targeting using novel nanoparticles (NPs). Furthermore, the use of nanotechnology for the delivery of cytotoxic drugs can also be valuable in facilitating cell-specific administration of drugs, improving their bioavailability, reducing side effects, and

• the BM within 6 h after administration [28]. The addition of larger quantities of surface-oriented DSPE-PEG resulted in a reduction of BM uptake, probably due to steric hindrance of the anionic amphiphile, which is considered as the active targeting moiety. In their further research, the authors

• a general strategy of active targeting. It could be essential in leukemia treatment, especially in the cases where a persistent clone dominates the leukemia cell population. Taking into account the molecular profile of the disease, there are a plethora of overexpressed molecules in leukemia cancer

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

• system, blood circulation time, biodistribution, and cellular recognition and internalization can be tailored [1][2][3][7][8]. Moreover, the surface of nanomedicines can be engineered by introducing functional groups to reduce clearance and increase biodistribution, as well as for active targeting

• purposes [1][2][9][10]. In fact, nanomedicines can be engineered to interact with specific cell receptors, opening up new strategies for targeting specific cell types and organs [9][10][11][12]. Despite this high engineering potential, active targeting remains one of the major challenges for nanomedicine

• description of the known endocytic pathways in cells. Review 1 Interactions of nano-sized materials at the cell surface and recognition by cell receptors 1.1 Active targeting The first steps in nanoparticle–cell interactions are those happening at the cell surface, including the adhesion of nanoparticles to

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

• hydrophilic block, effectively rendering the self-assemblies highly negatively charged at physiological pH values. Indeed, negatively charged nanoparticles are known to be capable of evading the mononuclear phagocyte system and enjoy prolonged blood circulation [58][110]. Active targeting through hydrophilic

• . When targeting cell surface receptors, two strategies can be distinguished using antibodies directed against a chosen receptor, or using the ligand of the receptor itself. The group of Torchilin pioneered the use of antibody-based active targeting by copolymer self-assemblies [119], and applied it to

Bombesin receptor-targeted liposomes for enhanced delivery to lung cancer cells

• Mohammad J. Akbar,
• Pâmela C. Lukasewicz Ferreira,
• Melania Giorgetti,
• Leanne Stokes and
• Christopher J. Morris

Beilstein J. Nanotechnol. 2019, 10, 2553–2562, doi:10.3762/bjnano.10.246

• solutions are used in combination [13]. In preclinical studies, improved therapeutic responses have been achieved by adopting an active targeting approach. Typically, this involves the incorporation of a surface-bound moiety that selectively binds to a cognate receptor/protein on the tumour cell surface

Targeting strategies for improving the efficacy of nanomedicine in oncology

• Gonzalo Villaverde and
• Alejandro Baeza

Beilstein J. Nanotechnol. 2019, 10, 168–181, doi:10.3762/bjnano.10.16

• ]. Active targeting: from cellular to organelle vectorization Once the nanoparticle reaches the tumoral area, it faces a complex scenario. Tumoral masses are not composed by an homogeneous tumoral cell distribution but they are formed by a myriad of different cell populations, from tumoral cells to immune

• solutions, a real alternative? Active targeting is already one of the most used strategies for bringing nanoformulations into tumoral cells. Although usually great results were achieved in vitro, the in vivo assays have shown smaller effects regarding cell internalization. There has been no real enhancement

• diagnosis in early stages of the disease. Thus, active targeting is still widely studied not only for nanomedicine but also for conjugate drugs [58][59]. As was mentioned above, there are three levels of active targeting: tissular targeting, cellular targeting and intracellular or organelle targeting. A

PLGA nanoparticles as a platform for vitamin D-based cancer therapy

• Maria J. Ramalho,
• Joana A. Loureiro,
• Bárbara Gomes,
• Manuela F. Frasco,
• Manuel A. N. Coelho and
• M. Carmo Pereira

Beilstein J. Nanotechnol. 2015, 6, 1306–1318, doi:10.3762/bjnano.6.135

• active targeting, using functionalized NPs [21]. Thus, the drug toxicity on healthy cells could be reduced, increasing NPs accumulation in the target tissues [19]. Although several studies on vitamin D3 encapsulation for food fortification have been conducted, very few works reported the use of