1979
DOI: 10.1126/science.432641
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Liposomes and Local Hyperthermia: Selective Delivery of Methotrexate to Heated Tumors

Abstract: Liposomes with phase transitions a few degrees above physiological temperature delivered more than four times as much methotrexate to murine tumors heated to 42 degrees C as to unheated control tumors. Most of the accumulated drug appeared to be intracellular and bound to dihydrofolate reductase, the enzyme blocked by methotrexate in its role as an antineoplastic agent.

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Cited by 329 publications
(130 citation statements)
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“…Most nanoparticles currently being used are successful by reducing side‐effects or as a means to solubilize hydrophobic drugs to induce fewer side effects 24. However, there has been significant preclinical work focused on developing new strategies for improving the delivery and efficacy of drugs using nanoparticles that are responsive to external stimuli such as heat,25, 26, 27, 28 light,29, 30, 31, 32, 33 ultrasound34 or tumor environment factors such as lower pH35, 36, 37, 38 or expression of certain enzymes 39, 40…”
Section: Introductionmentioning
confidence: 99%
“…Most nanoparticles currently being used are successful by reducing side‐effects or as a means to solubilize hydrophobic drugs to induce fewer side effects 24. However, there has been significant preclinical work focused on developing new strategies for improving the delivery and efficacy of drugs using nanoparticles that are responsive to external stimuli such as heat,25, 26, 27, 28 light,29, 30, 31, 32, 33 ultrasound34 or tumor environment factors such as lower pH35, 36, 37, 38 or expression of certain enzymes 39, 40…”
Section: Introductionmentioning
confidence: 99%
“…Regarding improvement of tumor specificity of drug delivery, efficient strategies are the use of nano-sized particles with a long circulation property with stimuli-sensitive properties as drug carriers. The former can improve accumulation of the carriers in tumor tissues through the enhanced permeation and retention (EPR) effect [4,5] and the latter can increase therapeutic effect by releasing drug specifically at the diseased tissues upon application of stimuli to the target sites [6][7][8]. In addition, another important function for the improvement of accuracy of drug delivery might be imaging function of carriers [9][10][11][12][13][14].…”
Section: Introductionmentioning
confidence: 99%
“…The potential of using temperature-sensitive liposomes in combination with local hyperthermia for targeted control of local drug release has been shown (68,69). Liposomes remain relatively stable in the circulation at temperatures well below the phase transition temperature (T c ) of the liposome membrane.…”
Section: Ultrasound-facilitated Drug Deliverymentioning
confidence: 99%