Co-administration of tariquidar using functionalized nanostructured lipid carriers overcomes resistance to docetaxel in multidrug resistant MCF7/ADR cells
- Authors
- Kim, Chang Hyun; Lee, Tae Hwa; Kim, Byuong Deok; Kim, Hyeon Kyun; Lyu, Min Jeong; Jung, Hyun Min; Goo, Yoon Tae; Kang, Myung Joo; Lee, Sangkil; Choi, Young Wook
- Issue Date
- May-2022
- Publisher
- Editions de Sante
- Keywords
- Co-administration; Docetaxel; Multidrug resistance; Nanostructured lipid carriers; P-gp inhibitor; Tariquidar
- Citation
- Journal of Drug Delivery Science and Technology, v.71
- Journal Title
- Journal of Drug Delivery Science and Technology
- Volume
- 71
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/57121
- DOI
- 10.1016/j.jddst.2022.103323
- ISSN
- 1773-2247
2588-8943
- Abstract
- To overcome multidrug resistance (MDR) and to enhance the efficacy of docetaxel (DTX), tariquidar (TRQ) was co-administered with DTX using nanostructured lipid carriers (NLC) functionalized with polyethylene glycol (PEG) and RIPL peptide (P/R). DTX- and TRQ-loaded plain NLC and P/R-NLC (P/R–N) were prepared using the solvent emulsification evaporation technique. All NLC samples showed a homogeneous spherical morphology and nano-sized dispersion (<210 nm) (zeta potential, −19 to −6 mV). DTX or TRQ was successfully encapsulated in NLC formulations (encapsulation efficiency >95%; drug loading 73–90 μg/mg). All NLC formulations were stable for 4 weeks when stored at 4 °C. Drug release was diffusion-controlled. DTX/TRQ combination at a 1:1 w/w ratio showed the highest synergism with a combination index value of 0.285 and was selected as the optimum combination. TRQ-P/R–N significantly enhanced the intracellular accumulation of Rhodamine 123 in MCF7/ADR cells. The co-administration of drug-loaded P/R-Ns led to potent and dose-dependent cytotoxicity and high MDR reversal efficiency. Co-treatment with DTX-P/R–N and TRQ-P/R–N increased apoptosis and enhanced G2/M cell cycle phase distribution in MCF7/ADR cells. These results indicate that the co-administration of DTX and TRQ using P/R-Ns may be a promising strategy to overcome MDR by P-gp inhibition in tumor treatments. © 2022
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