Delivery of the photosensitizer Pc 4 in PEG-PCL micelles for in vitro PDT studies.

Abstract:

:The silicon phthalocyanine Pc 4 is a second-generation photosensitizer that has several properties superior to other photosensitizers currently approved by the FDA, and it has shown significant promise for photodynamic therapy (PDT) in several cancer cells in vitro and model tumor systems in vivo. However, because of the high hydrophobicity of Pc 4, its formulation for in vivo delivery and favorable biodistribution become challenging. To this end, we are studying encapsulation and delivery of Pc 4 in block copolymer micelles. Here, we report the development of biocompatible PEG-PCL micelle nanoparticles, encapsulation of Pc 4 within the micelle core by hydrophobic association with the PCL block, and in vitro PDT studies of the micelle-formulated Pc 4 in MCF-7c3 human breast cancer cells. Our studies demonstrate efficient encapsulation of Pc 4 in the micelles, intracellular uptake of the micelle-formulated Pc 4 in cells, and significant cytotoxic effect of the formulation upon photoirradiation. Quantitative estimation of the extent of Pc 4 loading in the micelles and the photocytotoxicity of the micelle-incorporated Pc 4 demonstrate the promise of our approach to develop a biocompatible nanomedicine platform for tumor-targeted delivery of Pc 4 for site-selective PDT.

journal_name

J Pharm Sci

authors

Master AM,Rodriguez ME,Kenney ME,Oleinick NL,Gupta AS

doi

10.1002/jps.22007

subject

Has Abstract

pub_date

2010-05-01 00:00:00

pages

2386-98

issue

5

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)32652-6

journal_volume

99

pub_type

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