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Immuno or Targeted Liposomes

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Enhanced Permeation and Retention (EPR) Effect. Enhanced ... DaunoXome: Daunorubicin citrate liposome injection. DSPC (10) 704 mg. Cholesterol (5) 168 mg ... – PowerPoint PPT presentation

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Title: Immuno or Targeted Liposomes


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Immuno or Targeted Liposomes
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Immuno or Targeted Liposomes
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Immuno or Targeted Liposomes
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Doxil Liposomal Doxrubicin for IV Infusion
  • Doxrubicin 20 mg
  • MPEG-DSPE 31.9 mg
  • Fully Hydrogenated Soy PC 95.8 mg
  • Cholesterol 31.9 mg
  • Histidine as buffer
  • Sucrose
  • D. W. for injection q.s. to 10 mL

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Stealth Liposomes
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(No Transcript)
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Enhanced Permeation and Retention (EPR) Effect
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Enhanced Permeation and Retention (EPR) Effect
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Doxil Liposomal Doxrubicin for IV Infusion
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Lipoplatin Liposomal Cisplatin
  • Cisplatin
  • MPEG2000-DSPE
  • Fully Hydrogenated Soy PC
  • Cholesterol
  • DPPG
  • Mean Diameter 110 nm

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Lipoplatin
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Lipoplatin
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Lipoplatin
  • The cytotoxicity of Lipoplatin is substantially
    reduced compared to Cisplatin, which means that
    higher concentrations can be administered
  • Lipoplatin stays in circulation for extended
    periods of time and the Cisplatin is slowly
    released
  • Lioplatin can selectively target tissues with
    altered vascularization, therefore targeting
    primary tumors and metastasis this reduces the
    overall toxic effects on normal tissues

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DaunoXome Daunorubicin citrate liposome injection
  • DSPC (10) 704 mg
  • Cholesterol (5) 168 mg
  • Daunorubicin (1) 50 mg
  • Sucrose 2.125mg
  • Glycine 94 mg
  • Calcium Chloride Dihydrate 7 mg
  • Mean Diameter 45 nm
  • Vd 6.4 (1006)
  • T1/2 4.41 (0.77)

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Amphotericin B (AmB)
      
  • AmB a natural fermentation product from
    Streptomyces nodous
  • Consist of a large, amphipathic macrolide lactone
    ring that presents seven conjugated double bonds
    on one side and seven polar hydroxyl groups on
    the other side

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Amphotericin B
  • Insoluble in water, slightly soluble in methanol
    (around 0.5 mg/ml) , soluble in DMSO (30-40
    mg/ml).
  • Broad-spectrum antifungal activity
  • Antifungal of choice for the treatment of
    life-threatening infections, despite sever acute
    and chronic toxicity, including dose-limiting
    nephrotoxicity
  • LD50 in mice, i.v. 4 mg/kg, i.p. 88 mg/kg

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Amphotericin B
  • AmB acts by binding to the sterol component of a
    cell membrane, forms pores or channels in
    sterol-containing membranes, which changes
    permeability of cell membrane and causes leakage
    of protones, monovalent cations and other cell
    constituents leading to cell death.
  • The affinity of AmB for ergosterol (the primary
    sterol of fungal membrane) is almost 10-fold
    higher than cholesterol (the primary sterol of
    mammalian membrane)
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