ArticleBioconjugate chemistry
Polypeptide point modifications with fatty acid and amphiphilic block copolymers for enhanced brain delivery.
Article in Bioconjugate chemistry. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 32 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
32 citing papers in PubMed, 80 citations in OpenAlex.
- Investigating the Cytosolic Delivery of Proteins by Lipid Nanoparticles Using the Chloroalkane Penetration Assay.Biochemistry · 2024Article
- A Historical Review of Brain Drug Delivery.Pharmaceutics · 2022Review
- Co-delivery of paclitaxel and curcumin to foliate positive cancer cells using Pluronic-coated iron oxide nanoparticles.Progress in biomaterials · 2019Article
- Iron Oxide Nanoparticle Delivery of Peptides to the Brain: Reversal of Anxiety during Drug Withdrawal.Frontiers in neuroscience · 2017Article
- Exosomes as drug delivery vehicles for Parkinson's disease therapy.Journal of controlled release : official journal of the Controlled Release Society · 2015Article
- Agile delivery of protein therapeutics to CNS.Journal of controlled release : official journal of the Controlled Release Society · 2014Review
- Macrophages offer a paradigm switch for CNS delivery of therapeutic proteins.Nanomedicine (London, England) · 2014Article
- Can formulation and drug delivery reduce attrition during drug discovery and development-review of feasibility, benefits and challenges.Acta pharmaceutica Sinica. B · 2014Review
- Brain delivery of proteins via their fatty acid and block copolymer modifications.Journal of drug targeting · 2013Review
- Preclinical evaluation of radiosensitizing activity of Pluronic block copolymers.International journal of radiation biology · 2013Article
- Antioxidant-based therapies for angiotensin II-associated cardiovascular diseases.American journal of physiology. Regulatory, integrative and comparative physiology · 2013Review
- Conjugates of superoxide dismutase 1 with amphiphilic poly(2-oxazoline) block copolymers for enhanced brain delivery: synthesis, characterization and evaluation in vitro and in vivo.Molecular pharmaceutics · 2013Article
- Specific transfection of inflamed brain by macrophages: a new therapeutic strategy for neurodegenerative diseases.PloS one · 2013Article
- Blood-borne macrophage-neural cell interactions hitchhike on endosome networks for cell-based nanozyme brain delivery.Nanomedicine (London, England) · 2012Article
- Principles of strategic drug delivery to the brain (SDDB): development of anorectic and orexigenic analogs of leptin.Physiology & behavior · 2011Review
- Active Targeted Macrophage-mediated Delivery of Catalase to Affected Brain Regions in Models of Parkinson's Disease.Journal of nanomedicine & nanotechnology · 2011Article
- Cell-mediated transfer of catalase nanoparticles from macrophages to brain endothelial, glial and neuronal cells.Nanomedicine (London, England) · 2011Article
- Pluronic-based cationic block copolymer for forming pDNA polyplexes with enhanced cellular uptake and improved transfection efficiency.Biomaterials · 2011Article
- Polyelectrolyte complex optimization for macrophage delivery of redox enzyme nanoparticles.Nanomedicine (London, England) · 2011Article
- Nanoparticle-mediated brain-specific drug delivery, imaging, and diagnosis.Pharmaceutical research · 2010Review
Corrections and comments
- Erratum issued
Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
There is a tremendous need to enhance delivery of therapeutic polypeptides to the brain to treat disorders of the central nervous system (CNS). The brain delivery of many polypeptides is severely restricted by the blood-brain barrier (BBB). The present study demonstrates that point modifications of a BBB-impermeable polypeptide, horseradish peroxidase (HRP), with lipophilic (stearoyl) or amphiphilic (Pluronic block copolymer) moieties considerably enhance the transport of this polypeptide across the BBB and accumulation of the polypeptide in the brain in vitro and in vivo. The enzymatic activity of the HRP was preserved after the transport. The modifications of the HRP with amphiphilic block copolymer moieties through degradable disulfide links resulted in the most effective transport of the HRP across in vitro brain microvessel endothelial cell monolayers and efficient delivery of HRP to the brain. Stearoyl modification of HRP improved its penetration by about 60% but also increased the clearance from blood. Pluronic modification using increased penetration of the BBB and had no significant effect on clearance so that uptake by brain was almost doubled. These results show that point modification can improve delivery of even highly impermeable polypeptides to the brain.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.