Folate-conjugated polymeric micelle HB-loaded on targeting effect by intraperitoneal to ovarian cancer in vitro and in vivo.

Folate-conjugated polymeric micelle HB-loaded on targeting effect by intraperitoneal to ovarian cancer in vitro and in vivo.

Cancer Sci. 2018 Apr 04;:

Authors: Li J, Yao S, Wang K, Lu Z, Su X, Li L, Yuan C, Feng J, Yan S, Kong B, Song K

Abstract
Photodynamic therapy (PDT) is considered as an innovative and attractive modality to treat ovarian cancer. In this study, a biodegradable polymer poly (ethylene glycol)-poly (lactic acid)(PLA)-folate (FA-PEG-PLA) was prepared in order to synthesize an active targeting, water soluble and pharmacomodulated photosensitizer nano-carriers. The drug loading content, encapsulation efficiency, in vitro and in vivo release were characterized, in which HB/FA-PEG-PLA micelles had a high encapsulation efficiency and much slower control release for drugs compared to free drugs (p<0.05). To evaluate the targeting ability of the HB/FA-PEG-PLA micelles, the cellular uptake study in vitro were tested, which owned significantly enhanced uptake of HB/FA-PEG-PLA micelles in SKOV3 (FR+) compared to A2780 cancer cells (FR-). The enhanced uptake of HB/FA-PEG-PLA micelles to cancer cells resulted in a more effective post-PDT killing of SKOV3 cells compared to plain micelles and free drugs. Binding and uptake of HB/FA-PEG-PLA micelles by SKOV3 cells were also observed in vivo after intraperitoneal injection of folate targeted micelles in tumor-bearing ascitic ovarian cancer animals. The drug levels in ascitic tumor tissues were increased by 20-fold (p<0.001), which underscored the effect of a regional therapy approach with folate targeting. Furthermore, the HB-loaded micelles were mainly distributed in kidney and liver (the main clearance organs) in biodistribution. These results demonstrated that our new developed PDT photosensitizer HB/FA-PEG-PLA micelles has a high drug-loading capacity, good biocompatibility, control drug release, and enhanced targeting and antitumor effect, which is a potential approach to future targeting ovarian cancer therapy. This article is protected by copyright. All rights reserved.

PMID: 29617063 [PubMed - as supplied by publisher]

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