Nanoparticles are being developed to enhance drug delivery to cancer tumors, leveraging advantages such as the enhanced permeability and retention (EPR) effect. However, traditional nanoparticles often face challenges with low specificity for cancer cells, leading to inefficient delivery and unwanted side effects. Esterase-responsive nanoparticles offer a maximum targeted approach to tumor cells because they release their therapeutic payload at the tumor site under the influence of esterase activity. This review explores the role of esterase-responsive nanoparticles in drug and gene delivery, examines esterase prodrug therapy, and discusses prostate-specific membrane antigen (PSMA) targets esterase-responsive nanoparticles in prostate cancer treatment. Additionally, we reviewed the current research progress and future potential of esterase-responsive nanoparticles in enhancing drug and gene delivery.
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http://dx.doi.org/10.1016/j.bmc.2024.118001 | DOI Listing |
Bioorg Med Chem
December 2024
Department of Education, Central University of Kerala, Tejaswini Hills, Periye, Kasaragod 671320, Kerala, India. Electronic address:
Nanoparticles are being developed to enhance drug delivery to cancer tumors, leveraging advantages such as the enhanced permeability and retention (EPR) effect. However, traditional nanoparticles often face challenges with low specificity for cancer cells, leading to inefficient delivery and unwanted side effects. Esterase-responsive nanoparticles offer a maximum targeted approach to tumor cells because they release their therapeutic payload at the tumor site under the influence of esterase activity.
View Article and Find Full Text PDFPharm Pat Anal
September 2024
Department of Regulatory Affairs, National Institute of Pharmaceutical Education & Research-Hyderabad, Balanagar, Hyderabad, Telangana, 500037, India.
The release of active agents in tumors rather than normal tissues, limits systemic exposure and toxicities. Targeting over-expressed esterase enzyme in the tumor microenvironment can selectively release immune-active agents like Programmed Death-1 (PD-1) and PD-1 ligand inhibitors from ester-sensitive lipid nanocarriers, offering a novel approach compared with conventional therapies. PD-1 and PD-L1 association cause T-cell inactivation, whereas blocking their association improves their cytotoxic mechanism.
View Article and Find Full Text PDFACS Appl Bio Mater
September 2024
School of Chemistry, Indian Institute of Science Education and Research Thiruvananthapuram, Thiruvananthapuram 695551, Kerala India.
Floxuridine is a potential clinical anticancer drug for the treatment of various cancers. However, floxuridine typically causes unfavorable side effects due to its very poor tumor selectivity, and, hence, there is a high demand for the development of novel approaches that permit the targeted delivery of floxuridine into cancerous cells. Herein, the design and synthesis of an esterase-responsive multifunctional nanoformulation for the targeted delivery of floxuridine in esterase-overexpressed cancer cells is reported.
View Article and Find Full Text PDFInt J Pharm
August 2024
Department of Orthopaedics, Affiliated Hospital of Guilin Medical University, Guilin, Guangxi 541000, China. Electronic address:
Rhein, a natural anthraquinone compound derived from traditional Chinese medicine, exhibits potent anti-inflammatory properties via modulating the level of Reactive oxygen or nitrogen species (RONS). Nevertheless, its limited solubility in water, brief duration of plasma presence, as well as its significant systemic toxicity, pose obstacles to its in vivo usage, necessitating the creation of a reliable drug delivery platform to circumvent these difficulties. In this study, an esterase-responsive and mitochondria-targeted nano-prodrug was synthesized by conjugating Rhein with the polyethylene glycol (PEG)-modified triphenyl phosphonium (TPP) molecule, forming TPP-PEG-RH, which could spontaneously self-assemble into RPT NPs when dispersed in aqueous media.
View Article and Find Full Text PDFInt J Biol Macromol
August 2024
Beijing Key Laboratory of Environmental & Viral Oncology, College of Chemistry and Life Science, Beijing University of Technology, Beijing 100124, China.
As a clinical anti-glioma agent, the therapeutic effect of carmustine (BCNU) was largely decreased because of the drug resistance mediated by O-alkylguanine-DNA alkyltransferase (AGT) and the blood-brain barrier (BBB). To overcome these obstacles, we synthesized a BCNU-loaded hypoxia/esterase dual stimulus-activated nanomicelle, abbreviated as T80-HACB/BCNU NPs. In this nano-system, Tween 80 acts as the functional coating on the surface of the micelle to facilitate transport across the BBB.
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