Photochemical Internalisation: A Novel Drug Delivery System

  title={Photochemical Internalisation: A Novel Drug Delivery System},
  author={P{\aa}l Kristian Selbo and Anders H{\o}gset and Lina Prasmickaite and Kristian Berg},
  journal={Tumor Biology},
  pages={103 - 112}
The present report reviews a number of recently published papers on a novel technology for the cytosolic delivery of macromolecules named photochemical internalisation (PCI). PCI is based upon the light activation of a drug (a photosensitiser) specifically located in the membrane of endocytic vesicles. Light which is absorbed by the photosensitiser induces the formation of reactive oxygen species, of which singlet oxygen (1O2) is the predominant form. Singlet oxygen oxidises biomolecules in the… 

Figures and Tables from this paper

Photochemical internalization (PCI): a new modality for light activation of endocytosed therapeuticals.

  • A. DietzeP. Selbo K. Berg
  • Biology, Chemistry
    Journal of environmental pathology, toxicology and oncology : official organ of the International Society for Environmental Toxicology and Cancer
  • 2006
PCI is based on the light activation of photosensitizers specifically located in the membrane of endocytic vesicles inducing the rupture of this membrane upon illumination, which has been shown to enhance the biological activity of a large variety of macromolecules and other molecules that do not readily penetrate the plasma membrane.

Photochemical internalization provides time- and space-controlled endolysosomal escape of therapeutic molecules.

  • P. SelboA. Weyergang K. Berg
  • Biology, Chemistry
    Journal of controlled release : official journal of the Controlled Release Society
  • 2010

Enhancing the efficacy of cytotoxic agents for cancer therapy using photochemical internalisation

The applications of PCI are summarized, with the main emphasis placed on cancer chemotherapy, which enables the drugs to reach their intended subcellular target more efficiently and improves their efficacy.

The Potential of Photochemical Internalization (PCI) for the Cytosolic Delivery of Nanomedicines

Macromolecules with therapeutic potential include proteins such as ribosome-inactivating protein toxins for treatment of cancer and other indications, antibodies and growth factors for cell surface targeting, peptides and mRNA for vaccination, DNA utilizing nonviral and viral vectors for gene therapy, and oligonucleotides and nanoparticles for drug delivery.

Light-directed delivery of nucleic acids.

A protocol for light-directed delivery of nucleic acids through the use of photochemical internalization (PCI) technology, based on a photosensitizing compound that localizes to endocytic membranes, which offers the possibility for site-specific delivery ofucleic acids to a place of interest.

Polyacrylamide nanoparticles as a delivery system in photodynamic therapy.

The results suggest that, in order to induce photodynamic damage, the nanoparticles need only to be associated with the tumor cell closely enough to deliver singlet oxygen: their internalization within target cells may not be necessary.

Self-assembly of Amphiphilic Porphyrins to Construct Nanoparticles for Highly Efficient Photodynamic Therapy.

An efficient synthesis strategy is proposed that converts small molecules into nanoparticles in 100% aqueous solution via the molecular assemble without addition of any foreign species to improve amphiphilicity in tumour photodynamic therapy.

Enhanced photodynamic destruction of a transplantable fibrosarcoma using photochemical internalisation of gelonin

It is concluded that PCI with gelonin can markedly enhance the effect of PDT on this type of tumour and may have a role clinically as an adjunct to surgery to control localised disease.

Photochemical Internalization Enhances the Cytotoxic Effect of the Protein Toxin Gelonin and Transgene Expression in Sarcoma Cells¶

It is shown that PCI induced the endocytic escape of therapeutic substances in cells derived from human soft-tissue sarcomas and became up to four-fold more sensitive to light when combining photochemical treatment with gelonin incubation.



Photochemical internalization: a novel technology for delivery of macromolecules into cytosol.

Results presented here show that PCI can induce efficient light-directed delivery of macromolecules into the cytosol, indicating that PCI may have a variety of useful applications for site-specific drug delivery, e.g., in gene therapy, vaccination, and cancer treatment.

Photochemical internalisation increases the cytotoxic effect of the immunotoxin MOC31‐gelonin

The results indicate that PCI is a promising tool for increasing the cytotoxic effect of the immunotoxin MOC31‐gelonin conjugate in a light‐dependent manner and is important for further improvement of the PCI concept towards possible use in cancer therapy.

Evaluation of Different Photosensitizers for Use in Photochemical Gene Transfection¶

Neither AlPcS2a nor Photofrin affects the uptake of the transfecting DNA over the plasma membrane, therefore photochemical permeabilization of endocytic vesicles seems to be the most likely mechanism responsible for the positive PCI effect on gene transfection.

Photochemical transfection: a new technology for light-induced, site-directed gene delivery.

It is shown that illumination of photosensitizer-treated cells induces a substantial increase in the efficiency of transfection by DNA-poly-L-lysine complexes, and in a human melanoma cell line the light treatment can increase the transfectation efficiency more than 20-fold, reaching transfections levels of about 50% of the surviving cells.

Photochemical Transfection: A Technology for Efficient Light-Directed Gene Delivery

PCI constitutes an efficient light-inducible gene transfer method in vivo, which potentially can be developed into a site-specific method for gene delivery in in vivo gene therapy.

In vivo documentation of photochemical internalization, a novel approach to site specific cancer therapy

It was found that in vitro gelonin treatment of WiDr cells isolated from photosensitizer‐treated mice potentiated a light‐induced decrease of clonal survival, and the synergistic effect of combining photoactivation of photosenitizer located in endocytic vesicles and gel onin is indeed a result of PCI of gelon in vivo.

5-Aminolevulinic Acid–based Photochemical Internalization of the Immunotoxin MOC31-gelonin Generates Synergistic Cytotoxic Effects In Vitro¶

It is demonstrated that PCI, by combining 5-ALA, MOC31-gelonin and light, induces a synergistic cytotoxic effect against the WiDr cells.

Lysosomes and Microtubules as Targets for Photochemotherapy of Cancer

The identity of the intracellular targets responsible for photochemically induced cell death depends on the parameters mentioned above and the special cases of lysosomes and microtubules as targets for photochemical treatment of cells in culture will be discussed.

Liposome-bound Zn (II)-phthalocyanine. Mechanisms for cellular uptake and photosensitization.