Development and biodistribution of a theranostic aluminum phthalocyanine nanophotosensitizer
2016 (English)In: Photodiagnosis and Photodynamic Therapy, ISSN 1572-1000, E-ISSN 1873-1597, Vol. 13, 48-57 p.Article in journal (Refereed) PublishedText
Background: Aluminum phthalocyanine (AlPc) is an efficient second generation photosensitizer (PS) with high fluorescence ability. Its use in photodynamic therapy (PDT) is hampered by hydrophobicity and poor biodistribution. Methods: AlPc was converted to a biocompatible nanostructure by incorporation into amphiphilic polyethylene glycol-polycaprolactone (PECL) copolymer nanoparticles, allowing efficient entrapment of the PS in the hydrophobic core, water dispersibility and biodistribution enhancement by PEG-induced surface characteristics. A series of synthesized PECL copolymers were used to prepare nanophotosensitizers with an average diameter of 66.5-99.1 nm and encapsulation efficiency (EE%) of 66.4-78.0%. One formulation with favorable colloidal properties and relatively slow release over 7 days was selected for in vitro photophysical assessment and in vivo biodistribution studies in mice. Results: The photophysical properties of AlPc were improved by encapsulating AlPc into PECL-NPs, which showed intense fluorescence emission at 687 nm and no AlPc aggregation has been induced after entrapment into the nanoparticles. Biodistribution of AlPc loaded NPs (AlPc-NPs) and free AlPc drug in mice was monitored by in vivo whole body fluorescence imaging and ex vivo organ imaging, with in vivo imaging system (IVIS). Compared to a AlPc solution in aqueous TWEEN 80 (2 w/v%), the developed nanophotosensitizer showed targeted drug delivery to lungs, liver and spleen as monitored by the intrinsic fluorescence of AlPc at different time points (1 h, 24 h and 48 h) post iv. administration. Conclusions: The AlPc-based copolymer nanoparticles developed offer potential as a single agent multifunctional theranostic nanophotosensitizer for PDT coupled with imaging-guided drug delivery and biodistribution, and possibly also fluorescence diagnostics.
Place, publisher, year, edition, pages
2016. Vol. 13, 48-57 p.
Aluminum phthalocyanine, Copolymer, Nanoparticles, Nanophotosensitizer, Biodistribution, Imaging
Cancer and Oncology
IdentifiersURN: urn:nbn:se:kth:diva-185380DOI: 10.1016/j.pdpdt.2015.12.005ISI: 000372376500009PubMedID: 26708297ScopusID: 2-s2.0-84960932016OAI: oai:DiVA.org:kth-185380DiVA: diva2:920544
FunderSwedish Cancer SocietySwedish Childhood Cancer Foundation
QC 201604182016-04-182016-04-182016-05-16Bibliographically approved