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Related Experiment Videos

Photodynamic ultradeformable liposomes: Design and characterization.

J Montanari1, A P Perez, F Di Salvo

  • 1Laboratorio de Diseño de Estrategias de Targeting de Drogas (LDTD), Departamento de Ciencia y Tecnología, Universidad Nacional de Quilmes, Roque Saenz Peña 180, Bernal B1876BXD, Buenos Aires, Argentina.

International Journal of Pharmaceutics
|December 13, 2006
PubMed
Summary
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Ultradeformable liposomes (UDL) successfully encapsulated hydrophobic and hydrophilic zinc phthalocyanines (ZnPc and ZnPcMet), enhancing their stability and photodynamic properties for potential therapeutic applications against intracellular pathogens.

Area of Science:

  • Materials Science
  • Nanotechnology
  • Photochemistry

Background:

  • Phthalocyanines (Pc) are promising photosensitizers but often suffer from poor solubility and aggregation.
  • Ultradeformable liposomes (UDL) offer a potential strategy to improve drug delivery and stability.
  • Encapsulating Pcs in UDL could enhance their photodynamic therapy (PDT) efficacy.

Purpose of the Study:

  • To synthesize and characterize hydrophobic (ZnPc) and hydrophilic (ZnPcMet) phthalocyanines.
  • To load these phthalocyanines into ultradeformable liposomes (UDL).
  • To evaluate the physicochemical properties, stability, and photodynamic activity of the UDL-encapsulated phthalocyanines.

Main Methods:

  • Synthesis of hydrophobic ZnPc and hydrophilic ZnPcMet.

Related Experiment Videos

  • Encapsulation of ZnPc and ZnPcMet into UDL composed of soybean phosphatidylcholine and sodium cholate.
  • Characterization of vesicle size, Zeta potential, encapsulation efficiency, and phase transition enthalpy.
  • Assessment of matrix elasticity and content leakage through nanoporous barriers.
  • Measurement of singlet oxygen quantum yield (Phi(Delta)) in aqueous media.
  • Cytotoxicity assays (MTT) on Vero and J-774 cells under dark and irradiated conditions.
  • Evaluation of endo-lysosomal confinement using HPTS dye.

    • Main Results:

    • UDL vesicles (100 nm, negative Zeta potential) were formed with high encapsulation efficiencies (85% for ZnPc, 53% for ZnPcMet).
    • UDL-phthalocyanines exhibited significantly enhanced matrix elasticity and reduced content leakage compared to non-UDL.
    • UDL-ZnPc improved aqueous solubility and maintained monomeric state, retaining high singlet oxygen yield (0.61).
    • UDL-ZnPcMet showed a four-fold increase in singlet oxygen yield (0.21) compared to free ZnPcMet.
    • Free phthalocyanines were non-toxic; only liposomal ZnPc at 10 microM showed toxicity to J-774 cells under irradiation.
    • Endo-lysosomal confinement was maintained, suggesting potential for targeting intracellular pathogens.

    Conclusions:

    • UDL effectively encapsulate both hydrophobic and hydrophilic phthalocyanines, improving their stability and photophysical properties.
    • The enhanced elasticity and reduced leakage of UDL-phthalocyanines are crucial for effective delivery.
    • UDL-encapsulation significantly boosts the singlet oxygen generation of phthalocyanines, enhancing their potential as photodynamic agents.
    • This formulation strategy holds promise for developing improved photodynamic therapies targeting intracellular pathogens within the endo-lysosomal system.