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Carboplatin liposomes coated with O -palmitoylpullulan: In vitro characterization

International Journal of Pharmaceutics, ISSN: 0378-5173, Vol: 147, Issue: 2, Page: 153-164
1997
  • 17
    Citations
  • 0
    Usage
  • 12
    Captures
  • 0
    Mentions
  • 0
    Social Media
Metric Options:   Counts1 Year3 Year

Metrics Details

  • Citations
    17
    • Citation Indexes
      17
  • Captures
    12

Article Description

Encapsulation and stability of carboplafin in large unilamellar liposomes (LUV) of l -α egg phosphatidylcholine (PC), uncoated and coated with O -palmitoylpullulan (OPP), were studied. Synthesized OPP was characterized by infrared (IR) spectroscopy, revealing the existence of a covalent bond between the pullulan and palmitoyl groups, and by proton nuclear magnetic resonance ( 1 H-NMR) spectroscopy, allowing the calculation of the substitution degree of palmitcyl groups in pullulan (0.4%). Moreover, encapsulated carboplatin does not change the fluorescence polarization of either 1,6-diphenyl-1,3,5-hexatriene (DPH) or 3-fp-(6-phenyl-1,3,5-hexatrienyl)phenylpropionic acid (DPHPA), suggesting that this drug does not modify the membrane lipid organization either in the bilayer core or in the outer domains, as monitored by DPH and by DPH-PA, respectively. Carboplatin encapsulation in LUV and their stability seem to be simultaneously improved by hydration in a medium without chloride ions and with an ionic strength equivalent to 0.6% NaCI. Additionally, it is shown that stability of carboplatin liposomes, as measured by the platinum remaining associated with liposomes (platinum latency), is improved by coating with OPP, for an OPP/PC weight ratio of 3. Higher OPP/PC weight ratio values (e.g. 7.5) induce an opposite effect.

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