ArticlePharmaceutical research2011
Brain mitochondrial drug delivery: influence of drug physicochemical properties.
Article in Pharmaceutical research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
What it found
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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.
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Who cites it
10 citing papers in PubMed, 35 citations in OpenAlex.
- Interspecies scaling of suprachoroidal drug delivery using ocular geometry and drug physicochemical properties.Scientific reports · 2026Article
- Advancements in mitochondrial-targeted nanotherapeutics: overcoming biological obstacles and optimizing drug delivery.Frontiers in immunology · 2024Review
- Predictors and nomogram of in-hospital mortality in sepsis-induced myocardial injury: a retrospective cohort study.BMC anesthesiology · 2023Article
- Investigating the Effect of Esterification on Retinal Pigment Epithelial Uptake Using Rhodamine B Derivatives.Translational vision science & technology · 2020Article
- Article
- Intracellular drug bioavailability: a new predictor of system dependent drug disposition.Scientific reports · 2017Article
- Rapid Method To Determine Intracellular Drug Concentrations in Cellular Uptake Assays: Application to Metformin in Organic Cation Transporter 1-Transfected Human Embryonic Kidney 293 Cells.Drug metabolism and disposition: the biological fate of chemicals · 2016Article
- Pilot study of the effect of lipophilic vs. hydrophilic beta-adrenergic blockers being taken at time of intracardiac defibrillator discharge on subsequent PTSD symptoms.Neurobiology of learning and memory · 2014Article
- Computational approaches to analyse and predict small molecule transport and distribution at cellular and subcellular levels.Biopharmaceutics & drug disposition · 2014Review
- Functionalized nanosystems for targeted mitochondrial delivery.Mitochondrion · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
purposeTo determine the influence of drug physicochemical properties on brain mitochondrial delivery of 20 drugs at physiological pH.
methodsThe delivery of 8 cationic drugs (beta-blockers), 6 neutral drugs (corticosteroids), and 6 anionic drugs (non-steroidal anti-inflammatory drugs, NSAIDs) to isolated rat brain mitochondria was determined with and without membrane depolarization. Multiple linear regression was used to determine whether lipophilicity (Log D), charge, polarizability, polar surface area (PSA), and molecular weight influence mitochondrial delivery.
resultsThe Log D for beta-blockers, corticosteroids, and NSAIDs was in the range of -1.41 to 1.37, 0.72 to 2.97, and -0.98 to 2, respectively. The % mitochondrial uptake increased exponentially with an increase in Log D for each class of drugs, with the uptake at a given lipophilicity obeying the rank order cationic>anionic>neutral. Valinomycin reduced membrane potential and the delivery of positively charged propranolol and betaxolol. The best equation for the combined data set was Log % Uptake = 0.333 Log D + 0.157 Charge - 0.887 Log PSA + 2.032 (R(2) = 0.738).
conclusionsDrug lipopohilicity, charge, and polar surface area and membrane potential influence mitochondrial drug delivery, with the uptake of positively charged, lipophilic molecules being the most efficient.
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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.