Abstract
Phthalocyanine (Pc) is a type of promising sensitizer molecules for photodynamic therapy (PDT), but its hydrophobicity substantially prevents its applications. In this study, we efficiently encapsulate Pc into poly(N-isopropylacrylamide) (pNIPAM) microgel particles, without or with lipid decoration (i.e., Pc@pNIPAM or Pc@pNIPAM/lipid), to improve its water solubility and prevent aggregation in aqueous medium. The incorporation of lipid molecules significantly enhances the Pc loading efficiency of pNIPAM. These Pc@pNIPAM and Pc@pNIPAM/lipid composite microspheres show thermo-triggered release of Pc and/or lipid due to the phase transition of pNIPAM. Furthermore, in the in vitro experiments, these composite particles work as drug carriers for the hydrophobic Pc to be internalized into HeLa cells. After internalization, the particles show efficient fluorescent imaging and PDT effect. Our work demonstrates promising candidates in promoting the use of hydrophobic drugs including photosensitizers in tumor therapies.
Highlights
Phthalocyanines (Pc) and their derivatives have significant potential as theranostic agents for fluorescence imaging-guided drug delivery and photodynamic therapy (PDT) applications [1,2,3]
In one of our previous work we have reported that pNIPAM microgel particles with decorated lipids can be utilized as carriers of hydrophilic drugs, for controlled drug loading and release due to their biocompatibility and stimuli-responsive phase transition [20]
The Pc and lipid loaded particles became visualized under fluorescence observation, which endowed the particles with fluorescence imaging ability
Summary
Phthalocyanines (Pc) and their derivatives have significant potential as theranostic agents for fluorescence imaging-guided drug delivery and photodynamic therapy (PDT) applications [1,2,3]. Various strategies have been explored to enhance the water solubility and overcome aggregation of Pc molecules, including chemical conjugation of them with hydrophilic polymers [9,10], and encapsulation of them into nano- or microcarriers, including micelles [11], liposomes [4], dendrimers [5,12], nanoparticles [13,14], etc Among these formulas, noncovalent encapsulation of the hydrophobic Pc into carriers, such as macromoleculars and micro-/nanoparticles, is most well received due to the facile manipulation for drug encapsulation, enhanced drug loading efficiency, and preserved intrinsic properties of the carrier [5,7]. The as-prepared Pc@pNIPAM and Pc@pNIPAM/lipid composite microspheres show thermo-responsive drug release behavior and PDT effect in HeLa cells
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