methotrexate-loaded nanoparticles / Clinical Hospital Sao Paulo, Hospital Santa Marcelina, Prevent Senior - LARVOL DELTA

Study of caspase-6 activity in aggressive HCT116 cells using methotrexate-encapsulated lactoferrin-conjugated solid lipid nanoparticles via in silico and in vitro approaches. (PubMed, Sci Rep) - "Methotrexate-encapsulated solid lipid nanoparticles (MTX-SLNs) and lactoferrin-decorated MTX-loaded nanoparticles (MTX-Lf-SLNs) present a promising strategy for treating colorectal cancer. Migration assays further validated their capacity to obstruct cancer cell invasiveness, suggesting a potential to impede metastasis. Utilizing the bioactivity of lactoferrin for precise delivery, MTX-Lf-SLNs offer an attractive approach to enhance anti colon cancer efficacy while reducing unwanted side effects."

Journal • Preclinical • Colon Cancer • Colorectal Cancer • Oncology • Solid Tumor • CASP6 • IL1B • IL6 • TNFA

Biomimetic ROS-responsive hyaluronic acid nanoparticles loaded with methotrexate for targeted anti-atherosclerosis. (PubMed, Regen Biomater) - "Specifically, a safe ROS-responsive carrier based on hyaluronic acid (HSP) was prepared to load methotrexate (MTX), a drug known for its ability to enhance lipid excretion, resulting in the formation of MTX-loaded nanoparticles (MTXNPs). In vivo experiments showed that MM/MTXNPs exhibited superior accumulation at AS plaque sites, facilitated by the surface membrane layer containing integrin α4β1 and CD47, resulting in an enhanced therapeutic effect in inhibiting plaque development compared to free MTX and MTXNPs. Therefore, HSP represents a promising nanocarrier to load hydrophobic MTX, enabling effective and biocompatible enhancement of AS treatment."

Journal • Atherosclerosis • Cardiovascular • Dyslipidemia • Inflammation • ITGA4

Magnetic and pH-responsive magnetite/chitosan (core/shell) nanoparticles for dual-targeted methotrexate delivery in cancer therapy. (PubMed, Drug Deliv Transl Res) - "In the biocompatibility assessment, the magnetite/chitosan particles showed excellent hemocompatibility ex vivo and no cytotoxic effects on normal MCF-10 A and cancer MCF-7 cells. Furthermore, the Methotrexate-loaded nanoparticles significantly enhanced the antitumor activity reducing the half-maximal inhibitory concentration by ≈ 2.7-fold less compared to the free chemotherapeutic."

Journal • Oncology

Design, optimization, and evaluation of methotrexate loaded and albumin coated polymeric nanoparticles. (PubMed, J Biomater Sci Polym Ed) - "Methotrexate-loaded nanoparticles were produced by evaporating the emulsification fluid. Our primary findings demonstrate that the albumin nanoparticles containing methotrexate are designed to deliver the drug gradually. With minimal cytotoxicity, the intended preparation might give the brain an appropriate dosage of methotrexate."

Journal • Oncology

Microneedle-assisted percutaneous delivery of methotrexate-loaded nanoparticles enabling sustained anti-inflammatory effects in psoriasis therapy. (PubMed, J Mater Chem B) - "Compared to psoriasiform mice treated with 15.8 μg MTX-loaded MNs every day, 47.4 μg MTX@HMSN/CS-loaded MNs reduce the frequency of treatment to once every 3 days and achieve comparable amelioration. Therefore, MTX@HMSN/CS loaded MNs are a promising treatment strategy for psoriasis due to their durability, efficacy, convenience, and safety in relieving psoriasis-like skin inflammation."

Journal • Dermatitis • Dermatology • Immunology • Inflammation • Psoriasis

Glucosamine-Modified Mesoporous Silica-Coated Magnetic Nanoparticles: A "Raisin-Cake"-like Structure as an Efficient Theranostic Platform for Targeted Methotrexate Delivery. (PubMed, Pharmaceutics) - "The MTT assay showed comparable toxicity between MTX-loaded nanoparticles and free MTX. An in vivo breast cancer model was established in BALB/C mice, and the distribution of MTX-conjugated MNP@MSN particles was visualized using MRI. The MTX-conjugated particles showed significant anti-tumor potential together with MRI contrast enhancement."

Journal • Breast Cancer • Oncology • Solid Tumor

Topical Methotrexate Loaded Nanoparticles for The Treatment of Vitiligo: a clinical trial. (EADV 2023) - "Topical MTX nano gel is a new effective treatment option of active Vitiligo"

Clinical • Dermatology • Vitiligo

An Oral 3D Printed PLGA-Tocopherol PEG Succinate Nanocomposite Hydrogel for High-Dose Methotrexate Delivery in Maintenance Chemotherapy. (PubMed, Biomedicines) - "Therefore, to achieve improved bioavailability for MTX, this study aimed to design and develop a novel drug delivery system employing TPGS and a biodegradable polymer, i.e., PLGA, to construct methotrexate-loaded nanoparticles fixated in alginate-gelatine 3D printable hydrogel ink to form a solid 3D printed tablet for oral delivery...The in vitro release profile displayed a controlled and prolonged release of methotrexate over 24 h. The in silico modeling study displayed P-gp ATPase inhibition, suggesting enhanced MTX absorption from the gastrointestinal site. The 3D-printed hydrogel-based tablet has the potential to overcome the chemotherapeutic challenges that are experienced with conventional therapies."

Journal • Gastrointestinal Disorder • Infectious Disease • Oncology

Antiproliferative and apoptotic potential of methotrexate lipid nanoparticle in murine breast cancer model. (PubMed, Nanomedicine (Lond)) - "Aim: To evaluate the efficacy of novel methotrexate-loaded nanoparticles (MTX-NPs) in vitro and in vivo in the treatment of breast cancer. The solid lipid NPs (SLNPs) showed strong cellular uptake, increased apoptosis, controlled cytotoxicity at lower IC of methotrexate and a sizable reduction in tumor burden. MTX-NP oral formulation can be a promising candidate in breast cancer treatment with improved cellular uptake and in vivo efficacy."

Journal • Preclinical • Breast Cancer • Oncology • Solid Tumor

Methotrexate-loaded nanoparticles ameliorate experimental model of autoimmune arthritis by regulating the balance of interleukin-17-producing T cells and regulatory T cells. (PubMed, J Transl Med) - "The results suggest that MTX-loaded NPs have therapeutic potential for RA."

Journal • Immunology • Inflammatory Arthritis • Oncology • Rheumatoid Arthritis • Rheumatology • CD19 • CD4 • FOXP3 • IL17A • IL2RA • TNFA

Pharmacokinetic Comparison between Methotrexate-Loaded Nanoparticles and Nanoemulsions as Hard- and Soft-Type Nanoformulations: A Population Pharmacokinetic Modeling Approach. (PubMed, Pharmaceutics) - "The clearance and bioavailability of methotrexate-loaded nanoemulsions tended to decrease by 99% and increase by 19%, respectively, compared to those of the nanoparticles. The exploration of significant pharmacokinetic differences between drug formulations and their correlations presented in this study provide new perspectives on the development of nanoformulations."

Clinical • Journal • PK/PD data

Polymeric Nanoscale Drug Carriers Mediate the Delivery of Methotrexate for Developing Therapeutic Interventions Against Cancer and Rheumatoid Arthritis. (PubMed, Front Oncol) - "This review is focused on understanding the design and development of MTX-loaded nanoparticles alongside the inclusion of recent findings for the treatment of cancers. In this paper, we have made a coordinated effort to show the potential of novel drug delivery systems by achieving effective and target-specific delivery of methotrexate."

Journal • Review • Immunology • Inflammatory Arthritis • Lip Cancer • Oncology • Rheumatoid Arthritis • Rheumatology • DHFR

Poly-allylamine hydrochloride and fucoidan-based self-assembled polyelectrolyte complex nanoparticles for cancer therapeutics. (PubMed, J Biomed Mater Res A) - "Furthermore, the designed polyelectrolyte complex nanoparticles as well as the methotrexate (MTX) disodium salt-loaded composites were systematically characterized using various techniques...Finally, we investigated the anticancer efficacy of MTX-loaded nanoparticles on MCF-7 cells and HeLa cells and the satisfactory results were obtained.."

Journal • Oncology

Mucoadhesive and pH responsive fucoidan-chitosan nanoparticles for the oral delivery of methotrexate. (PubMed, Int J Biol Macromol) - "MTX-loaded nanoparticles were 7-fold more effective in inhibiting lung cancer cells proliferation than the free drug, showing the potential of fucoidan-chitosan nanoparticles to improve the cytotoxicity of free methotrexate on A549 lung cancer cells. These results also demonstrate that fucoidan/chitosan nanoparticles may provide a suitable platform for poor-water soluble compounds' oral delivery."

Journal