PMID- 32262006
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20200408
IS  - 2050-7518 (Electronic)
IS  - 2050-750X (Linking)
VI  - 2
IP  - 47
DP  - 2014 Dec 21
TI  - Folate-modified bexarotene-loaded bovine serum albumin nanoparticles as a 
      promising tumor-targeting delivery system.
PG  - 8361-8371
LID - 10.1039/c4tb01102c [doi]
AB  - Bexarotene (BEX), a high-affinity agonist for retinoid X receptors (RXRs), shows 
      apparent biological activities and distinct inhibitive efficacy in both cancer 
      therapy and prevention. This study exploited a folate-decorated delivery of 
      bexarotene-loaded bovine serum albumin nanoparticles, which could solubilize the 
      poorly water-soluble drug and overcome the nonspecific targeting disadvantage. 
      Bexarotene-loaded bovine serum albumin nanoparticles (BEX-BSANPs) were optimized 
      by a desolvation technique, subsequently conjugated with folate by carbodiimide 
      reaction. The resultant folate-modified bexarotene-loaded bovine serum albumin 
      nanoparticles (FA-BEX-BSANPs) showed a spherical shape, with a diameter of 195.3 
      +/- 5.6 nm, a zeta potential of -33.64 +/- 1.97 mV, and 71.28 +/- 1.93 mug folate was 
      coupled per mg BSA. Differential scanning calorimetry and X-ray diffraction 
      analysis confirmed the amorphous state of bexarotene in the folate-conjugates. 
      The in vitro drug release of bexarotene presented a controlled and sustained 
      release pattern. The in vitro cytotoxicity, cell apoptosis and cellular uptake 
      experiments of the nanoparticles were performed by MTT assay, propidium iodide 
      staining, fluorescence microscopy and flow cytometric analysis on A549 and MCF-7 
      cancer cells. Both the BEX-BSANPs and FA-BEX-BSANPs induced an enhanced cancer 
      cell apoptotic effect in contrast to BEX solution. The cells showed an excellent 
      binding for folate-modified nanoparticles. Especially, the interference effect on 
      the cellular internalization process by an excess folic acid was relatively 
      dramatic for the FR-positive MCF-7 cells in comparison to the modest change seen 
      in the FR-negative A549 cell lines, indicating that the uptake was mediated by 
      the folate receptors. Together these data suggested that the folate-modified 
      bexarotene-loaded delivery system, which demonstrated better biocompatibility and 
      potential superiority, could be an appropriate cancer therapy in targeting tumors 
      in the future.
FAU - Qi, Lisi
AU  - Qi L
AD  - School of Pharmaceutical Science, Center for Pharmaceutical Research & Drug 
      Delivery Systems, Shandong University, Jinan, Shandong Province 250012, P. R. 
      China. yuxialuan@sdu.edu.cn.
FAU - Guo, Yuanyuan
AU  - Guo Y
FAU - Luan, Jingjing
AU  - Luan J
FAU - Zhang, Dianrui
AU  - Zhang D
FAU - Zhao, Zhongxi
AU  - Zhao Z
FAU - Luan, Yuxia
AU  - Luan Y
LA  - eng
PT  - Journal Article
DEP - 20141027
PL  - England
TA  - J Mater Chem B
JT  - Journal of materials chemistry. B
JID - 101598493
SB  - IM
EDAT- 2014/12/21 00:00
MHDA- 2014/12/21 00:01
CRDT- 2020/04/09 06:00
PHST- 2020/04/09 06:00 [entrez]
PHST- 2014/12/21 00:00 [pubmed]
PHST- 2014/12/21 00:01 [medline]
AID - 10.1039/c4tb01102c [doi]
PST - ppublish
SO  - J Mater Chem B. 2014 Dec 21;2(47):8361-8371. doi: 10.1039/c4tb01102c. Epub 2014 
      Oct 27.