Recurrence and metastasis are the shortcomings of the clinical treatment of colon cancer. Finding an efficacy strategy for the treatment of colon cancer is important. In recent years, PLGA has been shown to have potential as a broad therapeutic drug delivery system. this study aimed to design a dual-loaded nanoparticles drug delivery system to overcome the limitations of chemotherapeutic drugs in colon cancer therapy. We developed epidermal growth factor (EGF) functionalized poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) co-loaded with 5-fluorouracil (5Fu) and perfluorocarbon (PFC) ([email protected]/PFC) for target therapy of colon cancer. [email protected] /PFC NPs were estimated to have an average size of 200 nm with a 5Fu-loading efficiency of 7.29%. In vitro release profile exhibited a pH-responsive release. CCK-8, Hoechst33342 staining and flow cytometry assays were performed to investigate the functions of [email protected]/PFC NPs in SW620 cells. Targeted [email protected]/PFC NPs also exhibited higher cellular uptake than non-targeted NPs in colon cancer cells. [email protected]/PFC NPs were found to have the best efficiency on cell viability suppression and apoptosis induction in SW620 cells. In xenograft mice, [email protected]/PFC NPs had the best suppressive effects on tumor growth compared with 5Fu, [email protected] and [email protected]/PFC NPs. The results of histopathological analysis further indicated that EGF-targeted NPs were the most efficient on tumor growth inhibition. Mechanically, the data demonstrated the improved therapeutic outcomes were owing to the fact that PFC could relieve tumor hypoxia via transporting oxygen to the tumor. We creatively constructed a biocompatible nanodrug delivery system and functionalized nanoparticles may provide new potential for selective delivery of chemotherapy drugs to cancers.

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This is a list of supplementary files associated with this preprint. Click to download.
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On 27 Mar, 2020
On 26 Mar, 2020
On 25 Mar, 2020
On 25 Mar, 2020
On 23 Mar, 2020
Received 18 Mar, 2020
Received 14 Mar, 2020
On 03 Mar, 2020
On 26 Feb, 2020
Invitations sent on 26 Feb, 2020
On 26 Feb, 2020
On 25 Feb, 2020
On 25 Feb, 2020
On 11 Jan, 2020
Received 31 Dec, 2019
On 20 Dec, 2019
Received 20 Dec, 2019
Invitations sent on 16 Dec, 2019
On 16 Dec, 2019
On 13 Dec, 2019
On 12 Dec, 2019
On 12 Dec, 2019
Posted 20 Nov, 2019
On 09 Dec, 2019
Received 06 Dec, 2019
Received 30 Nov, 2019
Received 25 Nov, 2019
On 23 Nov, 2019
On 22 Nov, 2019
Received 22 Nov, 2019
On 22 Nov, 2019
On 19 Nov, 2019
On 15 Nov, 2019
On 11 Nov, 2019
On 11 Nov, 2019
On 11 Nov, 2019
Invitations sent on 11 Nov, 2019
On 27 Mar, 2020
On 26 Mar, 2020
On 25 Mar, 2020
On 25 Mar, 2020
On 23 Mar, 2020
Received 18 Mar, 2020
Received 14 Mar, 2020
On 03 Mar, 2020
On 26 Feb, 2020
Invitations sent on 26 Feb, 2020
On 26 Feb, 2020
On 25 Feb, 2020
On 25 Feb, 2020
On 11 Jan, 2020
Received 31 Dec, 2019
On 20 Dec, 2019
Received 20 Dec, 2019
Invitations sent on 16 Dec, 2019
On 16 Dec, 2019
On 13 Dec, 2019
On 12 Dec, 2019
On 12 Dec, 2019
Posted 20 Nov, 2019
On 09 Dec, 2019
Received 06 Dec, 2019
Received 30 Nov, 2019
Received 25 Nov, 2019
On 23 Nov, 2019
On 22 Nov, 2019
Received 22 Nov, 2019
On 22 Nov, 2019
On 19 Nov, 2019
On 15 Nov, 2019
On 11 Nov, 2019
On 11 Nov, 2019
On 11 Nov, 2019
Invitations sent on 11 Nov, 2019
Recurrence and metastasis are the shortcomings of the clinical treatment of colon cancer. Finding an efficacy strategy for the treatment of colon cancer is important. In recent years, PLGA has been shown to have potential as a broad therapeutic drug delivery system. this study aimed to design a dual-loaded nanoparticles drug delivery system to overcome the limitations of chemotherapeutic drugs in colon cancer therapy. We developed epidermal growth factor (EGF) functionalized poly (lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) co-loaded with 5-fluorouracil (5Fu) and perfluorocarbon (PFC) ([email protected]/PFC) for target therapy of colon cancer. [email protected] /PFC NPs were estimated to have an average size of 200 nm with a 5Fu-loading efficiency of 7.29%. In vitro release profile exhibited a pH-responsive release. CCK-8, Hoechst33342 staining and flow cytometry assays were performed to investigate the functions of [email protected]/PFC NPs in SW620 cells. Targeted [email protected]/PFC NPs also exhibited higher cellular uptake than non-targeted NPs in colon cancer cells. [email protected]/PFC NPs were found to have the best efficiency on cell viability suppression and apoptosis induction in SW620 cells. In xenograft mice, [email protected]/PFC NPs had the best suppressive effects on tumor growth compared with 5Fu, [email protected] and [email protected]/PFC NPs. The results of histopathological analysis further indicated that EGF-targeted NPs were the most efficient on tumor growth inhibition. Mechanically, the data demonstrated the improved therapeutic outcomes were owing to the fact that PFC could relieve tumor hypoxia via transporting oxygen to the tumor. We creatively constructed a biocompatible nanodrug delivery system and functionalized nanoparticles may provide new potential for selective delivery of chemotherapy drugs to cancers.

Figure 1

Figure 2

Figure 3

Figure 4

Figure 5

Figure 6
This is a list of supplementary files associated with this preprint. Click to download.
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