Development of a mucoadhesive drug delivery system and its interaction with gastric cells

• Ahmet Baki Sahin,
• Serdar Karakurt and
• Deniz Sezlev Bilecen

Beilstein J. Nanotechnol. 2025, 16, 371–384, doi:10.3762/bjnano.16.28

• rate. The mucoadhesive characteristic of the system was tested in situ and in vitro. In addition, the in vitro cytotoxicity and internalization of the nanoparticles by mucus-secreting gastric cells were also investigated. We believe that usage of the developed system may increase the retention time of

• concluded that EudAlg nanoparticles do not significantly affect the viability of AGS cell (Figure 4A). Internalization of nanoparticles When nanoparticles are designed for biomedical applications, two important properties to be considered are toxicity and cellular uptake. The cellular uptake of

• nanoparticles is a dynamic process where both endocytosis and exocytosis are involved. The uptake also depends on the concentration of nanoparticles and the duration of the process. Studies conducted with the AGS cell line revealed that nanoparticle internalization generally reaches a plateau within the first 2

Graphene oxide–chloroquine conjugate induces DNA damage in A549 lung cancer cells through autophagy modulation

• Braham Dutt Arya,
• Sandeep Mittal,
• Prachi Joshi,
• Alok Kumar Pandey,
• Jaime E. Ramirez-Vick,
• Govind Gupta and
• Surinder P. Singh

Beilstein J. Nanotechnol. 2025, 16, 316–332, doi:10.3762/bjnano.16.24

• in 115 mL of solution and the amount of unbound drug left in supernatant, respectively. where mo, msup, and mGO are total amount of drug used initially, unbound drug obtained in the supernatant, and weight of GO, respectively. Cellular internalization of the GO–Chl nanoconjugate and flow-cytometry

• -based propidium iodide uptake analysis The efficacy of nanomedicines mainly depends upon the effective cellular internalization and their transport to the appropriate intercellular effector site [52][53]. Studies have shown that based on its size and surface characteristics (i.e., hydrophilicity or

• of vacuoles were observed in the treated cells (Figure 4a, black arrows). Furthermore, TEM micrographs reveal the presence and effective cellular internalization of the GO–Chl nanoconjugate in A549 cells (Figure 4a; red arrows and Figure 4b), corroborating our previous findings [25]. To investigate

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

• through the BBTB and uptake into the tumor cells were obtained, as a precondition for higher extent and rate of their internalization and optimal risk/benefit ratio of the treatment with TMZ. This knowledge is based on a lot of publications in which nanoparticulated formulations of different materials

• cell membranes observed after uptake of GO. The mechanisms of MWCNTs-G internalization have not been specifically studied; however, the knowledge from studies of CNTs and graphene/GO can be extrapolated. Some of the previous publications show accumulation of CNTs in phagocytic cells without toxic

• mediate the internalization in addition to the impact of interaction with the biological fluids (i.e., surface adsorption of molecules). In this respect, in the study of Dabrowski et al. [81], the impact of particle size of graphene on the efficacy of internalization was evaluated in normal (LL-24) and

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

• affect NP internalization. They actively engulf NCs and accelerate their clearance, acting differentially in a time-dependent manner and altering the fate of nanomaterials [26]. In addition to immune-related barriers, the physicochemical properties of the nanomaterial itself can impair the NCs’ ability

• shapes like ellipsoids, discoids, and nanorods with higher aspect ratios are more effectively localized close to blood vessel walls, enhancing their internalization into endothelial cells and potentially improving their therapeutic delivery [1]. After systemic administration, NCs tend to accumulate in

• in KCs, is essential for clearing infections caused by the Gram-positive bacterium Listeria monocytogenes [30]. In nanomedicine, SRs are also responsible for clearing negatively charged NPs such as those composed of silica [31][32]. This interaction leads to the internalization of NCs via endocytosis

Mechanistic insights into endosomal escape by sodium oleate-modified liposomes

• Ebrahim Sadaqa,
• Satrialdi,
• Fransiska Kurniawan and
• Diky Mudhakir

Beilstein J. Nanotechnol. 2024, 15, 1667–1685, doi:10.3762/bjnano.15.131

• transforming drug delivery methodologies [1]. Despite their potential, liposomes encounter substantial challenges from the point of administration to achieving therapeutic efficacy. One of the primary obstacles is their propensity for endosomal entrapment. Following internalization via endocytosis, liposomes

• inhibitor of caveolae-mediated endocytosis, also significantly reduced uptake (p < 0.001), suggesting the involvement of caveolae in the internalization of Unmodified-Lipo. Amiloride, which blocks macropinocytosis, had no significant effect (p < 0.99), indicating a negligible role for macropinocytosis in

• findings that fatty acids often use macropinocytosis for internalization [17]. Filipin significantly inhibited uptake (p < 0.001), showing that caveolae-mediated endocytosis also plays an important role in SO-Lipo uptake. These results align with reports that anionic particles undergo caveolae-mediated

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

• -based nanocarriers is understanding the fundamental building blocks, size, shape, and biological properties to mimic real cells and enable their internalization [31][32]. One efficient strategy for producing biomimetic nanocarriers involves camouflage with biological membranes. The phospholipids

Polymer lipid hybrid nanoparticles for phytochemical delivery: challenges, progress, and future prospects

• Iqra Rahat,
• Pooja Yadav,
• Aditi Singhal,
• Mohammad Fareed,
• Jaganathan Raja Purushothaman,
• Mohammed Aslam,
• Raju Balaji,
• Sonali Patil-Shinde and
• Md. Rizwanullah

Beilstein J. Nanotechnol. 2024, 15, 1473–1497, doi:10.3762/bjnano.15.118

• . Cell cycle analysis and apoptotic studies by flow cytometry revealed much higher apoptotic activity and cellular internalization of CUR-PLHNPs in MCF-7 cells compared to free CUR. Further, the CUR-PLHNPs showed a significantly lower IC50 value (i.e., 7 µg/mL) than free CUR (10.72 µg/mL). Zhao et al

• . fabricated RGD ligand-directed PLHNPs for site-specific delivery of CUR to treat melanoma [83]. The CUR-RGD-PLHNPs showed small PS, low polydispersity index (PDI), high ZP, and high EE. The CUR-RGD-PLHNPs showed 4.3 times higher cellular internalization in HUVECs cells than the native counterpart. Apoptotic

• studies in AsPC-1 and BxPC-3 cells suggested that the fabricated UA-PLHNPs exhibited much higher cellular internalization and cytotoxicity. Further, the developed AU-PLHNPs revealed negligible erythrocyte hemolytic activity. Similarly, Wang et al. fabricated UA-encapsulated chitosan-coated liposomes for

Nanotechnological approaches for efficient N2B delivery: from small-molecule drugs to biopharmaceuticals

• Selin Akpinar Adscheid,
• Akif E. Türeli,
• Nazende Günday-Türeli and
• Marc Schneider

Beilstein J. Nanotechnol. 2024, 15, 1400–1414, doi:10.3762/bjnano.15.113

• ]. N2B drug transport includes intracellular, paracellular, and extracellular mechanisms [42]. While the intracellular pathway is based on the drug’s internalization by the neurons followed by axonal transport, the extracellular pathway is based on the drugs’ transport through the paracellular space [61

• [67][68]. Significant portions of the NPs studied for N2B delivery are approx. 200 nm, which is the average size of olfactory exons [44][60]. Rejman et al. demonstrated that the clathrin-mediated pathway of endocytosis has an upper limit for internalization of approximately 200 nm. Their study also

• revealed that an increase in particle size led to a shift towards caveolae-mediated internalization, the primary pathway for particles sized around 500 nm [69]. This shows the possibility of an even more extended particle size range to be considered for N2B delivery [69]. Regarding surface characteristics

Interaction of graphene oxide with tannic acid: computational modeling and toxicity mitigation in C. elegans

• Romana Petry,
• James M. de Almeida,
• Francine Côa,
• Felipe Crasto de Lima,
• Diego Stéfani T. Martinez and
• Adalberto Fazzio

Beilstein J. Nanotechnol. 2024, 15, 1297–1311, doi:10.3762/bjnano.15.105

• directly affects delivered dose, internalization, and biodistribution in organisms. In the EPA medium, GO exhibited aggregation and precipitation at concentrations of 5.0 and 10 mg·L−1, respectively, a phenomenon attributable to the screening effect of salt ions diminishing the repulsive forces between GO

• each depth was recorded in the profiles shown in Figure 7, which were normalized regarding the maximum intensity found in the region. The intensity profiles and the respective spectra, were used to draw conclusions about GO’s internalization in the organisms. According to Figure 7, GO was found along

• the entire nematode cuticle. Furthermore, GO was found internally in the head, intestine, and pharynx of nematodes, regardless of the presence of TA. Internalization of GO in the gonads was also observed and to some extend in eggs, although in the latter the occurrence of GO signal decreased after the

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

• from the tubes and transferred to a 96-well plate. The quantification of hemoglobin in the supernatant and the preparation of positive and negative controls were performed as described above. Folate receptor expression and internalization of SiO2NPs in healthy and tumor cells To verify the folate

• a chemiluminescent solution (Clarity™ Western ECL Substrate – 1705060, Bio-Rad) for 5 min. Antibody to β-actin (AC-15, Novus) was used as an endogenous control for all samples. To assess the internalization of NPs, HaCat and KB cells were cultured in a 96-well plate (1 × 104 cells/well) for 24 h

• (DAPI). After that, samples were analyzed on the Operetta High Content Screening System microscope (PerkinElmer Life Sciences). To obtain quantitative information on the internalization of functionalized and non-functionalized SiO2NPs, the flow cytometry technique was used. HaCat and KB cells were

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

• 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

Synthesis, characterization and anticancer effect of doxorubicin-loaded dual stimuli-responsive smart nanopolymers

• Ömür Acet,
• Pavel Kirsanov,
• Burcu Önal Acet,
• Inessa Halets-Bui,
• Dzmitry Shcharbin,
• Şeyda Ceylan Cömert and
• Mehmet Odabaşı

Beilstein J. Nanotechnol. 2024, 15, 1189–1196, doi:10.3762/bjnano.15.96

• . Physicochemical features such as size, shape, and surface charge play an extremely important role in the internalization of nanostructures. The uptake of nanoparticles into cells requires two steps. The first is the binding to the cell membrane, and the second is the uptake into the cell [34]. The zeta potential

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

• effects of TiO2 NPs, with diameters around 20 and 200 nm, and SiO2 NPs on proliferation, fibrosis, adhesion, and migration of LX-2 cells as a model of HSC activation were studied. The results show that the internalization of both TiO2 NPs and SiO2 NPs suppressed classical outcomes of cellular fibrosis

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

• of folic acid did not change the level of the cell signal. F127 also assists in the accumulation of the nanoparticles in the cell via clathrin-mediated endocytosis and caveolae-mediated endocytosis [9][44]. In our study, F127 enhanced the internalization of the nanoparticles in MCF7, HepG2, and HEK

• with the binding of F127 nanoparticles. Clathrin-mediated endocytosis and caveolin-mediated endocytosis occur in most of the cells; therefore, the internalization of the nanoparticles to the cell would be unselective [45]. Thus, there were fluorescent signals in the cells, most of which were incubated

• folate on the surface of nanoparticles promotes the internalization of nanoparticles by cancer cells. Within the cell, the CHL released from the nanoparticles would bind to DNA and halt the development of cancer cells. Without CHL, the nanoparticles had no cytotoxic impact on the cells (data not shown

A review on the structural characterization of nanomaterials for nano-QSAR models

• Salvador Moncho,
• Eva Serrano-Candelas,
• Jesús Vicente de Julián-Ortiz and
• Rafael Gozalbes

Beilstein J. Nanotechnol. 2024, 15, 854–866, doi:10.3762/bjnano.15.71

• ]. Additionally, focusing on the role of the NM as contrast agent in magnetic resonance imaging, the authors added the specific property of cellular internalization of iron, measured as the amount of iron inside the cells [25]. Zhang et al. [79] created a predictive model that uses regression trees to predict the

Cholesterol nanoarchaeosomes for alendronate targeted delivery as an anti-endothelial dysfunction agent

• Horacio Emanuel Jerez,
• Yamila Roxana Simioni,
• Kajal Ghosal,
• Maria Jose Morilla and
• Eder Lilia Romero

Beilstein J. Nanotechnol. 2024, 15, 517–534, doi:10.3762/bjnano.15.46

• also reported the increased internalization of nanoarchaeosomes compared to HSPC-Chol liposomes by HUVECs [36]. As discussed below, the massive internalization of nanoarchaeosomes is due to their high content of PGP-Me, a ligand of SRA-I/II. Effect of endocytosis on HUVECs and THP-1 macrophages The

• nanoarchaeosomes is PGP-Me, a polar double negatively charged archaeolipid, which is a ligand of SRAI/II (a trimeric transmembrane glycoprotein that mediates the extensive internalization of polyanionic ligands) [40]. SRAI/II is expressed by J774A.1 cells in intermediate amounts [41]. The expression of SRAI/II by

• /II. We observed here that nanoARC(ALN) was much less cytotoxic for THP-1 macrophages than for J774A1 cells, probably, because the expression of SRA1 in THP-1 macrophages (and subsequent internalization) is reported to be lower than in J774A1 macrophages [43]. Co-cultures Mild inflammation model The

Nanomedicines against Chagas disease: a critical review

• Maria Jose Morilla,
• Kajal Ghosal and
• Eder Lilia Romero

Beilstein J. Nanotechnol. 2024, 15, 333–349, doi:10.3762/bjnano.15.30

• in inflamed tissues and could be delivered to amastigotes after being endocytosed by infected cells. In addition, since endocytosis occurs with cellular energy expenditure, the internalization of BNZ would be independent of its permeability and dose. In this way, very small doses of BNZ could be site

Assessing phytotoxicity and tolerance levels of ZnO nanoparticles on Raphanus sativus: implications for widespread adoptions

• Pathirannahalage Sahan Samuditha,
• Nadeesh Madusanka Adassooriya and
• Nazeera Salim

Beilstein J. Nanotechnol. 2024, 15, 115–125, doi:10.3762/bjnano.15.11

• (p < 0.05) in soluble protein content by 23.1%, accompanied by a notable increase in IAA by 31.1%, indicating potential toxicity. The use of atomic absorption spectroscopy confirmed the internalization of zinc in seedlings, with a statistically significant increase (p < 0.05). In control plants

• . Zn contents in seedlings The successful Zn internalization was confirmed by atomic absorption spectroscopy (AAS) analysis (Figure 5a) indicating that R. sativus can accumulate Zn at high concentrations (0.36 mg Zn g−1 DW of seedlings at 0 mg/L and 1.76 mg Zn g−1 DW of seedlings at 10,000 mg/L, p

• < 0.05). Even though the Zn internalization was increased by 27.4% (0.46 mg Zn g−1 DW) in the R. sativus seedlings treated with 1000 mg/L of ZnO NPs, without showing any adverse effects on morphology (Figure 5b) compared to that of the control, this increment was not significant (p > 0.05). Discussion

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

• delivery specific to macrophage targets, such as ᴅ-mannose, phosphatidylserine, or lactoferrin. This may reduce the drug resistance of the parasite in the long term. Furthermore, the surface charge of nanostructures may influence internalization since positive charges favor electrostatic interactions of

• way, there is an internalization of the NPs containing this polymer and delivery of the drug for leishmanicidal activity. Additionally, the conjugation of the nanoparticles with sugars, such as mannose, makes drug delivery targeted and specific to the macrophage receptor, increasing the uptake by the

• IC50 values of 0.15 ± 0.08, 0.09 ± 0.07, and 0.07 ± 0.04 μM and selectivity index (SI) of 80, 255, and 314, respectively. In addition to the influence of the nanostructure, sugar promotes greater internalization of these nanoparticles due to the mannose receptors on the surface of macrophages [111

Curcumin-loaded albumin submicron particles with potential as a cancer therapy: an in vitro study

• Nittiya Suwannasom,
• Netsai Sriaksorn,
• Chutamas Thepmalee,
• Krissana Khoothiam,
• Ausanai Prapan,
• Hans Bäumler and
• Chonthida Thephinlap

Beilstein J. Nanotechnol. 2023, 14, 1127–1140, doi:10.3762/bjnano.14.93

• cellular uptake and internalization [52]. In earlier studies, particles up to 1000 nm were found in various cytoplasmic areas, mainly taken up by cells through endocytic mechanisms [53]. The peanut-shaped microparticles prepared in this study have an aspect ratio (length/width) as high as 1.6. Several

Recognition mechanisms of hemoglobin particles by monocytes – CD163 may just be one

• Jonathan-Gabriel Nimz,
• Pichayut Rerkshanandana,
• Chiraphat Kloypan,
• Ulrich Kalus,
• Saranya Chaiwaree,
• Axel Pruß,
• Radostina Georgieva,
• Yu Xiong and
• Hans Bäumler

Beilstein J. Nanotechnol. 2023, 14, 1028–1040, doi:10.3762/bjnano.14.85

• cell surface adhesion of the test particles. On the other hand, binding to the particles caused a conformational change within the structure of BSA. This denatured BSA promoted binding by scavenger receptor A (SR-A/CD204) and, thus, induced internalization of the protein–particle–receptor complex. In

Prediction of cytotoxicity of heavy metals adsorbed on nano-TiO₂ with periodic table descriptors using machine learning approaches

• Joyita Roy,
• Souvik Pore and
• Kunal Roy

Beilstein J. Nanotechnol. 2023, 14, 939–950, doi:10.3762/bjnano.14.77

• internalization and bioaccumulation in the HK-2 cells. The increase in the concentration of heavy metals and their adsorption to nano-TiO2 induces toxicity by increasing the generation of ROS in the HK-2 cells. Comparison with the previous work The present work describes the development of a model for heavy

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

• of the specific nature of the targeting antibody. ACNPs are expected to accumulate at the target site and to improve the tumor uptake. ACNPs receptor binding efficacies were determined using in vitro studies including cellular uptake and internalization studies [71]. Multivalent effect of antibody

• the receptor-mediated uptake and internalization of NPs in A549 cells. They clearly indicated a significant disparity between in vivo and in vitro outcomes of NP targeting efficacy in the presence of a protein corona [80]. Su et al. reported that protein corona formation alters the active and passive

• the effect of this protein corona. They observed a higher internalization of BLf-AgNPs than of bare AgNPs, which indicates that the protein corona improved the intracellular efficiency of the NPs. Moreover, the BLf corona also increased the bioavailability of the NPs in THP1 cells and resulted in

Green SPIONs as a novel highly selective treatment for leishmaniasis: an in vitro study against Leishmania amazonensis intracellular amastigotes

• Brunno R. F. Verçoza,
• Robson R. Bernardo,
• Luiz Augusto S. de Oliveira and
• Juliany C. F. Rodrigues

Beilstein J. Nanotechnol. 2023, 14, 893–903, doi:10.3762/bjnano.14.73

• internalization of the SPIONs. First, promastigotes were treated with 100 µg/mL of SPIONs for 24 h (Figure 3A–C). TEM images confirmed the presence of SPION aggregates randomly distributed throughout the cytoplasm of the promastigotes (Figure 3A–C, arrowheads). The images suggest that these aggregates have

The steep road to nonviral nanomedicines: Frequent challenges and culprits in designing nanoparticles for gene therapy

• Yao Yao,
• Yeongun Ko,
• Grant Grasman,
• Jeffery E. Raymond and
• Joerg Lahann

Beilstein J. Nanotechnol. 2023, 14, 351–361, doi:10.3762/bjnano.14.30

• Need for Multimodal Characterization of Nanoparticles The methods chosen to investigate NP uptake and transfection can be biased towards particular properties and may provide limited insights into the efficiency of NP internalization and efficacy. Typically, cellular uptake and transfection efficiency

• ) [16]. Unfortunately, confocal imaging is limited by relatively low throughput (even with automation) and can be ambiguous when determining internalization within 500 nm of the cell membrane [17]. However, widefield fluorescence microscopy is still widely used when it comes to observing the expression

• papers, Figure 1b). Despite the robust data it can provide, flow cytometry counts the total number of cells associated with NPs and cannot distinguish internalized cargo from surface-bound NPs [1][17]. To precisely quantify internalization, a secondary method is required that can differentiate between