Novel folate-targeted docetaxel-loaded nanoparticles for tumour targeting: in vitro and in vivo evaluation. Issue 69 (6th July 2016)

• Record Type: Journal Article
• Authors: Han, M. H.; Li, Z. T.; Bi, D. D.; Guo, Y. F.; Kuang, H. X.; Wang, X. T.
• Is Part Of: RSC advances. Volume 6:Issue 69(2016)
• Page Start: 64306
• Page End: 64314
• Publication Date: 2016-07-06
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c6ra04466b
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Cholesterol-PEG1000 -FA (folic acid) was synthesized as a stabilizer to encapsulate DTX, for the construction of a promising targeted delivery system for breast cancer therapy. Abstract : Cholesterol-PEG1000 (Chol-PEG) has shown great potential in drug delivery. In our work, the synthesis ofChol-PEG1000 -FA (folic acid) was firstly achieved via an amide reaction of NH2 on the surface ofChol-PEG1000 -NH2, and then docetaxel-loadedChol-PEG1000 -FA nanoparticles were prepared by the precipitation–ultrasonication combined high-pressure homogenization (HPH) technique, and were characterized by particle size, zeta potential and morphology; meanwhile the average drug loading of the resulting DTX/Chol-PEG1000 -FA nanoparticles reached up to 68%. The anti-tumor efficiency and targeting ability of docetaxel-loadedChol-PEG1000 -FA nanoparticles (DTX-FA-Nps) were demonstrated by their in vitro and in vivo anti-tumor activity against 4T1 cells. The docetaxel-loaded Chol-PEG1000 nanoparticles with and without FA conjugation proved to be of satisfactory size and distribution, with favorable drug release and high drug encapsulation efficiency. In vitro results showed the higher anti-tumor efficiency of the DTX-FA-Nps and DTX-Nps (docetaxel-loaded Chol-PEG1000 nanoparticles) than docetaxel solutions (DTX-Sol). The tumor-targeting effects of the FA conjugated Chol-PEG1000 are also studied. The IC50 values of DTX-Sol, DTX-Nps and DTX-FA-Nps are 1.6260, 0.3772 and 0.0171 μg mL −1, respectively, for 4T1 cancer cells after 48 h of treatment. The inhibition rate for the DTX-FA-Nps at 10 mg kg −1 was 74.83% ( P < 0.01). Based on these results, the DTX-loadedChol-PEG1000 -FA nanoparticles may be a promising targeted delivery system for breast cancer therapy.