PEGylated lipids in lipid nanoparticle delivery dynamics and therapeutic innovation

• Peiyang Gao

Beilstein J. Nanotechnol. 2025, 16, 1914–1930, doi:10.3762/bjnano.16.133

• Peiyang Gao Independent researcher, 140 First St, Cambridge, MA, 02140, USA 10.3762/bjnano.16.133 Abstract Lipid nanoparticles (LNPs) have become significant vehicles in the delivery of therapeutic substances, particularly for nucleic acid vaccines and gene therapies. A key component in the

• PEG; immunogenicity; lipid nanoparticles; PEG alternatives; PEG lipids; therapeutic delivery; Review Introduction Lipid nanoparticles (LNPs) have become a promising platform in modern nanomedicine, especially for delivering genetic payloads such as mRNA and siRNA. These nanoscale particles can

• cosmetics, hydrogels, and lubricants [62]. In lipid nanoparticles, PEG is normally incorporated in the form of PEG lipids, which reside in the surface bilayer to reduce particle aggregation and nonspecific binding. However, studies have shown that PEGylated LNPs can elicit immune responses and accelerated

Targeting the vector of arboviruses Aedes aegypti with nanoemulsions based on essential oils: a review with focus on larvicidal and repellent properties

• Laryssa Ferreira do Nascimento Silva,
• Douglas Dourado,
• Thayse Silva Medeiros,
• Mariana Alice Gonzaga Gabú,
• Maria Cecilia Queiroga dos Santos,
• Daiane Rodrigues dos Santos,
• Mylena Lemos dos Santos,
• Gabriel Bezerra Faierstein,
• Rosângela Maria Rodrigues Barbosa and
• Fabio Rocha Formiga

Beilstein J. Nanotechnol. 2025, 16, 1894–1913, doi:10.3762/bjnano.16.132

• , nanotechnological strategies have been used, such as polymeric nanocarriers [30], solid lipid nanoparticles [31], liposomes [32], and nanoemulsions [13][14][33]. Among these strategies, nanoemulsions, kinetically stable nanometric dispersions (20–500 nm) of two immiscible liquids, stabilized by surfactants, have

Exploring the potential of polymers: advancements in oral nanocarrier technology

• Rousilândia de Araujo Silva,
• Igor Eduardo Silva Arruda,
• Luise Lopes Chaves,
• Mônica Felts de La Roca Soares and
• Jose Lamartine Soares Sobrinho

Beilstein J. Nanotechnol. 2025, 16, 1751–1793, doi:10.3762/bjnano.16.122

Advances of aptamers in esophageal cancer diagnosis, treatment and drug delivery

• Yang Fei,
• Hui Xu,
• Chunwei Zhang,
• Jingjing Wang and
• Yong Jin

Beilstein J. Nanotechnol. 2025, 16, 1734–1750, doi:10.3762/bjnano.16.121

• help of aptamers. Common nanocarrier systems, including micelles, liposomes, metal nanoparticles, and solid lipid nanoparticles, demonstrate well-established fabrication protocols, yet often face challenges with in vivo stability. Emerging nanoplatforms, such as four-way junction RNA nanostructures

Enhancing the therapeutical potential of metalloantibiotics using nano-based delivery systems

• Alejandro Llamedo,
• Marina Cano,
• Raquel G. Soengas and
• Francisco J. García-Alonso

Beilstein J. Nanotechnol. 2025, 16, 1350–1366, doi:10.3762/bjnano.16.98

• , studies have demonstrated that mannose receptor-targeted rifampicin delivery through solid lipid nanoparticles (SLNs) can be effectively applied to the treatment of infections, highlighting the role of polymer-based systems in enhancing drug delivery to macrophages [53]. Both passive and active targeting

• by phagocytic cells, which is particularly beneficial for treating infections with biofilm-forming bacteria [67][68][69]. Solid lipid nanoparticles: SLNs are sub-micrometer colloidal carriers, typically ranging from 50 to 1000 nm, composed of lipids that remain solid at room and body temperatures

Ferroptosis induction by engineered liposomes for enhanced tumor therapy

• Alireza Ghasempour,
• Mohammad Amin Tokallou,
• Mohammad Reza Naderi Allaf,
• Mohsen Moradi,
• Hamideh Dehghan,
• Mahsa Sedighi,
• Mohammad-Ali Shahbazi and
• Fahimeh Lavi Arab

Beilstein J. Nanotechnol. 2025, 16, 1325–1349, doi:10.3762/bjnano.16.97

• traditional methods, such as thin film hydration, to produce liposomes and lipid nanoparticles [113][120]. Microfluidics offers exceptional control over particle size, lower variability, higher EE, and better scalability, making it the most advanced and practical approach for nanoparticle production [115][119

Better together: biomimetic nanomedicines for high performance tumor therapy

• Imran Shair Mohammad,
• Gizem Kursunluoglu,
• Anup Kumar Patel,
• Hafiz Muhammad Ishaq,
• Cansu Umran Tunc,
• Dilek Kanarya,
• Mubashar Rehman,
• Omer Aydin and
• Yin Lifang

Beilstein J. Nanotechnol. 2025, 16, 1246–1276, doi:10.3762/bjnano.16.92

• polarization, and cRGD modification further enhances tumor accumulation [32]. In another study, Hou et al. employed M1-type macrophages and loaded them with sorafenib (SF) to develop lipid nanoparticles (M1/SLNPs). The M1/SLNPs showed an increase in tumor accumulation and enhanced the SF tumor targeting

• -modified nanosystem showed increased drug accumulation and enhanced therapeutic activity both in subcutaneous and orthotopic tumor models [125][126]. Another study regarding targeted therapy and improved drug delivery to the brain used the dual modification of RBC-coated lipid nanoparticles with T7 peptide

Serum heat inactivation diminishes ApoE-mediated uptake of D-Lin-MC3-DMA lipid nanoparticles

• Demian van Straten,
• Luuk van de Schepop,
• Rowan Frunt,
• Pieter Vader and
• Raymond M. Schiffelers

Beilstein J. Nanotechnol. 2025, 16, 740–748, doi:10.3762/bjnano.16.57

• surface of nanoparticles after administration has garnered substantial attention due to the significant effects it has on their performance. Lipid nanoparticles (LNPs) depend on protein corona formation to mediate their targeting. Such protein–nanoparticle interactions are often initially studied using in

• a crucial part during pre-clinical nanoparticle development. The influence of the protein corona is particularly evident for the efficacy of lipid nanoparticles used for RNA delivery. Lipid nanoparticles (LNPs) protect the encapsulated RNA from premature clearance and simultaneously facilitate the

Aprepitant-loaded solid lipid nanoparticles: a novel approach to enhance oral bioavailability

• Mazhar Hussain,
• Muhammad Farooq,
• Muhammad Asad Saeed,
• Muhammad Ijaz,
• Sherjeel Adnan,
• Zeeshan Masood,
• Muhammad Waqas,
• Wafa Ishaq and
• Nabeela Ameer

Beilstein J. Nanotechnol. 2025, 16, 652–663, doi:10.3762/bjnano.16.50

• , Robert Stevenson Road, Edinburgh, EH9 3FB, United Kingdom 10.3762/bjnano.16.50 Abstract Objectives of the present study are the development of aprepitant (APT)-loaded solid lipid nanoparticles (SLNs) using the polymers poloxamer 407 and β-cyclodextrin for enhanced solubility and their pharmacokinetic

• . Therefore, the optimal SLN formulation APT-CD-NP4 is a promising tool for oral administration with sustained release to improve the bioavailability of the BCS class-IV drug APT. Keywords: aprepitant; β-cyclodextrin; pharmacokinetic study; poloxamer; solid lipid nanoparticles; Introduction Cancer is a

• class-IV drug [10]. Low solubility and poor dissolution of BCS class-IV drugs can be improved by using techniques such as incorporating the drug or prodrug into lipid or polymeric formulations, using solid lipid nanoparticles (SLNs), applying surfactants, adjusting the pH value, reducing particle size

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

• antitumour activity in xenograft mouse models. Later experiments investigated the effect resulting from the incorporation of targeting agents into the surface of lipid–polycation vectors. For example, Yuan et al. prepared transferrin-conjugated PEI1200–lipid nanoparticles (LPNs), for the targeted delivery of

• exhibited greater splice correction effectiveness on mRNA and protein levels, measured by the increase in luciferase activity on engineered HeLa cells containing an altered luciferase gene. In later reports, Yang et al. demonstrated that bPEI–lipid nanoparticles functionalised with small cell-penetrating

Recent advances in photothermal nanomaterials for ophthalmic applications

• Jiayuan Zhuang,
• Linhui Jia,
• Chenghao Li,
• Rui Yang,
• Jiapeng Wang,
• Wen-an Wang,
• Heng Zhou and
• Xiangxia Luo

Beilstein J. Nanotechnol. 2025, 16, 195–215, doi:10.3762/bjnano.16.16

• bovine ILM and the unusually thick human ILM. In addition, this photoporation strategy allowed model nanoparticles to break through the ILM barrier for highly successful delivery to the retina and was also able to increase the efficacy of mRNA-loaded lipid nanoparticles in the bovine retina fivefold. In

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

• high buffering capacities in the acidic pH range of endosomes (pH 5–6). Lipid nanoparticles (LNPs), which include cationic and ionizable materials, exhibit such intracellularly triggered delivery mechanisms and are often used to carry nucleic acids into cells. In this case, the endosomal escape is

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

• ; intranasal delivery; liposomes; nanomedicine; nanostructured lipid carriers (NLCs); polymer nanoparticles; RNA delivery; solid lipid nanoparticles (SLNs); Introduction The central nervous system (CNS) consists of the brain and the spinal cord and is considered the body’s processing and control center. While

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

• fact that there are over 50 nanotechnology-based medical products approved by regulatory bodies worldwide for various medical purposes, including AmBisome® (liposomal amphotericin B) for fungal infections, Visudyn® (liposomal vertepor) for macular degeneration, and Onpattro® (lipid nanoparticles with

Classification and application of metal-based nanoantioxidants in medicine and healthcare

• Nguyen Nhat Nam,
• Nguyen Khoi Song Tran,
• Tan Tai Nguyen,
• Nguyen Ngoc Trai,
• Nguyen Phuong Thuy,
• Hoang Dang Khoa Do,
• Nhu Hoa Thi Tran and
• Kieu The Loan Trinh

Beilstein J. Nanotechnol. 2024, 15, 396–415, doi:10.3762/bjnano.15.36

• : (1) nanoliposomes, which are a nanoscale bilayer lipid vesicle [132]; (2) nanocapsules, which consist of an inner aqueous core surrounded by a nontoxic polymeric membrane [133]; (3) solid lipid nanoparticles, which consist of a solid lipid core stabilized by a surfactant [134]; and (4) nanocrystals

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

• countries’ institutions (Brazil and Argentina), and private pharmaceutical companies. The project started proposing a sublingual formulation of BNZ within liposomes or lipid nanoparticles, assuming the intact formulations could reach the blood, avoid the hepatic first-pass metabolism, and reduce the

• toxicity of BNZ. The project, however, failed in its attempt to incorporate BNZ into liposomes, while lipid nanoparticles could not be formulated into sublingual tablets. The project changed to formulate BNZ/hydroxypropyl-β-cyclodextrin complexes. These complexes were prepared on a scale seven times larger

• nanoparticles orally and intravenously administered has also been tested (Table 3). For example, oral solid lipid nanoparticles loaded with a poorly bioavailable lipophilic cyclic compound derived from dithiocarbazate, effectively reduced parasitemia, diminished inflammation and lesions of the liver and heart

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

• , lipid nanoparticles, nano- and microemulsions, liposomes, or metallic nanoparticles [68]. Costa-Lima and colleagues incorporated bisnaphthalimidopropyldiaaminooctane (BNIPDaoct) into PLGA polymeric nanoparticles and obtained particles with sizes around 150 nm, with encapsulation efficiency around 90

• following the Ambisome® path. Nanostructured lipid carriers Nanostructured lipid carriers (NLCs) are lipid-based formulations with a solid matrix at room temperature that differ from solid lipid nanoparticles when it comes to their matrix organizational level. Nanostructured lipid carriers offer advantages

• such as enhanced stability, low toxicity, increased shelf life, improved drug loading capacity, and biocompatibility over other conventional lipid-based nanocarriers, such as nanoemulsions and solid lipid nanoparticles [91]. Due to their properties, the use of NLCs has been a successful strategy for

Nanotechnological approaches in the treatment of schistosomiasis: an overview

• Lucas Carvalho,
• Michelle Sarcinelli and
• Beatriz Patrício

Beilstein J. Nanotechnol. 2024, 15, 13–25, doi:10.3762/bjnano.15.2

• lipid nanoparticles (SLN) are solid lipid matrices at room and body temperature [35]. Their advantages are similar to classic nanocarriers, such as protection of labile drugs from biodegradation process, excellent excipient tolerability, and prolonged release. In addition, some disadvantages of the

• liposomes (500 mg/kg) could be more efficient than free PZQ treatment. Similar results have been shown in other works that also used liposome with PZQ in different concentrations [50][51][52][53]. In addition, Xie et al. [54] studied the pharmacokinetics of solid lipid nanoparticles composed of castor oil

• encapsulating PZQ. They observed that the drug took more than one week in vitro to be released. A pharmacokinetic study in vivo also showed that the PZQ concentration in the plasma was sustained for longer times when the nanoformulation was studied in mice. Thus, the results show that solid lipid nanoparticles

Nanostructured lipid carriers containing benznidazole: physicochemical, biopharmaceutical and cellular in vitro studies

• Giuliana Muraca,
• María Esperanza Ruiz,
• Rocío C. Gambaro,
• Sebastián Scioli-Montoto,
• María Laura Sbaraglini,
• Gisel Padula,
• José Sebastián Cisneros,
• Cecilia Yamil Chain,
• Vera A. Álvarez,
• Cristián Huck-Iriart,
• Guillermo R. Castro,
• María Belén Piñero,
• Matias Ildebrando Marchetto,
• Catalina Alba Soto,
• Germán A. Islan and
• Alan Talevi

Beilstein J. Nanotechnol. 2023, 14, 804–818, doi:10.3762/bjnano.14.66

• efficiently. Many developments have been made in the past years resulting in lipid formulations such as liposomes, solid lipid nanoparticles (SLNs), and nanoemulsions, which increased the apparent solubility of BNZ and its efficacy against parasites [17]. Remarkably, oil-in-water nanoemulsions improved the

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

• polymeric (e.g., core–shell micelles), oligomeric (e.g., lipid nanoparticles), or biomacromolecular (e.g., protein nanoparticles) components complicates matters only further by generating a higher-than-normal background through non-specific interactions with the assay media. In addition, a significant bias

Polymer nanoparticles from low-energy nanoemulsions for biomedical applications

• Santiago Grijalvo and
• Carlos Rodriguez-Abreu

Beilstein J. Nanotechnol. 2023, 14, 339–350, doi:10.3762/bjnano.14.29

• escape from endosomes. Notably, lipid nanoparticles enabled the remarkably fast development of mRNA vaccines against COVID-19. Still, there is much to be done to reach the final goal of developing formulations that can deliver drugs at preset rates and periods of time to specific targets [1]. To this end

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

• the nanosystems [136][137]. Lipid nanoparticles (LNPs) in clinical trials are mainly composed of ionizable cationic lipids, amphipathic phospholipids, cholesterol, diffusible PEG lipids (for transient protection), and a targeting ligand [138]. After IV administration, lung capillaries receive the

• payload into the cytoplasm and efficacious transfection [142][143][144][145][146][147][148]. Besides the efforts for liver and liver hepatocyte targeting, different research groups are working on the challenge of developing lipid nanoparticles for specific organ targeting after IV administration

• , including lipid nanoparticles for lung targeting or targeting relevant cell types, that is, epithelial cells, endothelial cells, immune cells of the lungs, B cells, and T cells. Data regarding the biodistribution of polymers, polymer lipids, and lipid nanoparticles indicate that the internal and external

Facile preparation of Au- and BODIPY-grafted lipid nanoparticles for synergized photothermal therapy

• Yuran Wang,
• Xudong Li,
• Haijun Chen and
• Yu Gao

Beilstein J. Nanotechnol. 2022, 13, 1432–1444, doi:10.3762/bjnano.13.118

• nanoparticles limit their therapeutic applications. Previously, gold nanoclusters carrying lipid nanoparticles (Au-LNPs) have been reported after simply mixing Au3+ with preformed diethylenetriaminepentaacetic acid lipid nanoparticles to solve this contradiction. Au-LNPs demonstrated enhanced photothermal

• synergistic PTT in the treatment of cancer and other diseases. Keywords: BODIPY; gold nanoparticles; lipid nanoparticles; photothermal therapy; synergism; Introduction Photothermal therapy (PTT) relies on photothermal agents (PTAs) to convert light into heat energy to burn cancer cells. Due to its spatial

• reported for PTT use. In a previous reported work, we synthesized tiny gold nanoclusters by simply mixing Au3+ with preformed lipid nanoparticles (LNPs) containing diethylenetriaminepentaacetic acid (DTPA) [8]. The Au-grafted LNPs (Au-LNPs) showed significantly enhanced photothermal effects in comparison

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

• treatments, which was accompanied by a dose-dependent increase in cytochrome C expression and a dose-dependent decrease in CDK1 expression. Solid lipid nanoparticles (SLN). SLN were first developed ca. 1990 (with patents and papers published a few years after) [60] and are the first generation of lipid

• -loaded polymeric (PNP with PLGA) and lipid nanoparticles (SLN with hydrogenated coco-glycerides and poloxamer 188). They reported greater stability at 135 days (>90% retention), lower average particle size (127.10 ± 11.30 nm), and higher EE% (90.49 ± 1.20%) in CUR-SL, as compared to CUR-PNP (338.20

• nanoparticles (50–1000 nm) [61]. They contain crystallized lipid droplets that are solid at room and body temperatures [62][63], with the drug or the molecule of interest loaded into the solid lipid phase [64]. The advantages of SLN include high drug loading capacity, great stability, good biocompatibility, and

Photothermally active nanoparticles as a promising tool for eliminating bacteria and biofilms

• Mykola Borzenkov,
• Piersandro Pallavicini,
• Angelo Taglietti,
• Laura D’Alfonso,
• Maddalena Collini and
• Giuseppe Chirico

Beilstein J. Nanotechnol. 2020, 11, 1134–1146, doi:10.3762/bjnano.11.98

• studied. The state-of-the art in antimicrobial polymeric nanoparticles, with an emphasis on the relationship between their structure and activity, is well presented in a recent review [29]. The antibacterial properties of solid lipid nanoparticles are also a subject of specific research interest as they