The cellular uptake and anti-tumor activity of conjugated linoleic acid-paclitaxel-loaded iRGD-modified lysolipid-containing thermosensitive liposomes

doi:10.5246/jcps.2019.02.012

Abstract

Abstract:

In the present study, we prepared the iRGD-modified lysolipid-containing thermosensitive liposomes (LTSL) containing conjugated linoleic acid-paclitaxel (CLA-PTX), also known as iRGD-LTSL-CLA-PTX. The in vitro cellular uptake and invitro cytotoxicity of iRGD-LTSL-CLA-PTX were evaluated in B16-F10 melanoma cells. The in vivo anti-tumor effect of iRGD-LTSL-CLA-PTX was investigated using B16-F10 tumor-bearing C57BL/6 mice. The results of the cellular uptake experimentindicated that the increased cellular uptake of CLA-PTX in the iRGD-LTSL-CLA-PTX-treated groups was 2.05-, 3.31- or 4.83-foldcompared with that in the SSL-CLA-PTX group after a 2-, 4- or 6-h incubation at 42°C, respectively. The in vivo antitumor results showed that iRGD-LTSL-CLA-PTX/heat significantly inhibited the growth of B16-F10 tumors compared with the CLA-PTX solution (LTSL-CLA-PTX, LTSL-CLA-PTX/heat and iRGD-LTSL-CLA-PTX) (P<0.01). In conclusion, the antitumor effect of iRGD-LTSL-CLA-PTX was confirmed on B16-F10 melanoma in vitro and in vivo, which was induced by both the effect of iRGD and LTSL.

Key words: iRGD, Lysolipid-containing thermosensitive liposomes, CLA-PTX, Antitumor effect, In vitro, In vivo

CLC Number:

R943

Supporting:

Yanli Hao, Ting Zhong, Ruo Du, Hua Zhang, Bilin Liu, Xuan Zhang. The cellular uptake and anti-tumor activity of conjugated linoleic acid-paclitaxel-loaded iRGD-modified lysolipid-containing thermosensitive liposomes[J]. Journal of Chinese Pharmaceutical Sciences, 2019, 28(2): 121-133.

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