CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro
Objective To prepare CREKA peptide-modified docetaxel (DTX) loaded liposomes (CREKA-lipo-DTX) and to evaluate their targeted binding ability and anti-proliferative activity in vitro. Methods Firstly, Michael addition reaction was used to synthesize the targeted part DSPE-PEG2000-CREKA, and then CREK...
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| Format: | Article |
| Language: | zho |
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Editorial Office of Journal of Third Military Medical University
2020-11-01
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| Series: | Di-san junyi daxue xuebao |
| Subjects: | |
| Online Access: | http://aammt.tmmu.edu.cn/Upload/rhtml/202005276.htm |
| _version_ | 1818918500169678848 |
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| author | YANG Wenbo HAO Lan WANG Zhigang2 ZHANG Ronggui |
| author_facet | YANG Wenbo HAO Lan WANG Zhigang2 ZHANG Ronggui |
| author_sort | YANG Wenbo |
| collection | DOAJ |
| description | Objective To prepare CREKA peptide-modified docetaxel (DTX) loaded liposomes (CREKA-lipo-DTX) and to evaluate their targeted binding ability and anti-proliferative activity in vitro. Methods Firstly, Michael addition reaction was used to synthesize the targeted part DSPE-PEG2000-CREKA, and then CREKA-lipo-DTX was prepared by thin film hydration-ultrasound method, and its basic characterization was evaluated. Both PC-3 cells and RWPE-1 cells were divided into 3 groups respectively (n=3): blank control group, PEG-lipo-DiI group and CREKA-lipo-DiI group. After co-incubation with the cells, the cellular uptake of liposomes was analyzed qualitatively and quantitatively by laser confocal microscopy and flow cytometry respectively, so as to evaluate the targeting effect of CREKA modified vector on PC-3 cells. The cellular uptake of liposomes was analyzed qualitatively and quantitatively by laser confocal microscopy and flow cytometry respectively. The anti-proliferative activity of CREKA-lipo-DTX was evaluated by CCK-8 assay and Annexin V-PI apoptosis detection kit on blank control group, free DTX group, PEG-lipo-DiI group and CREKA-PEG-DiI group of PC-3 cells. Results CREKA-lipo-DTX was successfully prepared, with an average particle size of 130.37±1.44 nm, and encapsulation rate of (91.93±4.64)%. The obtained drug carrier had good stability and showed good slow-release behavior in vitro. The results of laser confocal microscopy and flow cytometry analysis indicated that the uptake of CREKA-modified liposomes by PC-3 cells was significantly increased (P < 0.05) when compared with the unmodified liposome group (PEG-lipo-DiI), while no such difference was seen in RWPE-1 cells (P>0.05). In vitro anti-tumor experimental results suggested that enhanced killing effect of DTX on PC-3 cells and significantly increased numbers of early and late apoptotic PC-3 cells were observed in the CREKA-lipo-DTX group when compared with the free DTX and PEG-lipo -DTX groups (P < 0.05). Conclusion A high-efficiency and low-toxicity lipoid drug delivery system with long cycle and tumor specific targeting characteristics has been successfully prepared, which can specifically target PC-3 cells in vitro, and thus can improve the anti-tumor effect of the carrier in vitro. |
| first_indexed | 2024-12-20T00:50:57Z |
| format | Article |
| id | doaj.art-8688701b4e454566a6a4a1f062732602 |
| institution | Directory Open Access Journal |
| issn | 1000-5404 |
| language | zho |
| last_indexed | 2024-12-20T00:50:57Z |
| publishDate | 2020-11-01 |
| publisher | Editorial Office of Journal of Third Military Medical University |
| record_format | Article |
| series | Di-san junyi daxue xuebao |
| spelling | doaj.art-8688701b4e454566a6a4a1f0627326022022-12-21T19:59:16ZzhoEditorial Office of Journal of Third Military Medical UniversityDi-san junyi daxue xuebao1000-54042020-11-0142212017211510.16016/j.1000-5404.202005276CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitroYANG Wenbo0HAO Lan1WANG Zhigang22ZHANG Ronggui3 Department of Urology, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, 400010, ChinaChongqing Key Laboratory of Ultrasound Molecular Imaging, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, 400010, China Chongqing Key Laboratory of Ultrasound Molecular Imaging, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, 400010, China Department of Urology, the Second Affiliated Hospital of Chongqing Medical University, Chongqing, 400010, ChinaObjective To prepare CREKA peptide-modified docetaxel (DTX) loaded liposomes (CREKA-lipo-DTX) and to evaluate their targeted binding ability and anti-proliferative activity in vitro. Methods Firstly, Michael addition reaction was used to synthesize the targeted part DSPE-PEG2000-CREKA, and then CREKA-lipo-DTX was prepared by thin film hydration-ultrasound method, and its basic characterization was evaluated. Both PC-3 cells and RWPE-1 cells were divided into 3 groups respectively (n=3): blank control group, PEG-lipo-DiI group and CREKA-lipo-DiI group. After co-incubation with the cells, the cellular uptake of liposomes was analyzed qualitatively and quantitatively by laser confocal microscopy and flow cytometry respectively, so as to evaluate the targeting effect of CREKA modified vector on PC-3 cells. The cellular uptake of liposomes was analyzed qualitatively and quantitatively by laser confocal microscopy and flow cytometry respectively. The anti-proliferative activity of CREKA-lipo-DTX was evaluated by CCK-8 assay and Annexin V-PI apoptosis detection kit on blank control group, free DTX group, PEG-lipo-DiI group and CREKA-PEG-DiI group of PC-3 cells. Results CREKA-lipo-DTX was successfully prepared, with an average particle size of 130.37±1.44 nm, and encapsulation rate of (91.93±4.64)%. The obtained drug carrier had good stability and showed good slow-release behavior in vitro. The results of laser confocal microscopy and flow cytometry analysis indicated that the uptake of CREKA-modified liposomes by PC-3 cells was significantly increased (P < 0.05) when compared with the unmodified liposome group (PEG-lipo-DiI), while no such difference was seen in RWPE-1 cells (P>0.05). In vitro anti-tumor experimental results suggested that enhanced killing effect of DTX on PC-3 cells and significantly increased numbers of early and late apoptotic PC-3 cells were observed in the CREKA-lipo-DTX group when compared with the free DTX and PEG-lipo -DTX groups (P < 0.05). Conclusion A high-efficiency and low-toxicity lipoid drug delivery system with long cycle and tumor specific targeting characteristics has been successfully prepared, which can specifically target PC-3 cells in vitro, and thus can improve the anti-tumor effect of the carrier in vitro.http://aammt.tmmu.edu.cn/Upload/rhtml/202005276.htmcreka peptideprostate cancerliposometargeted therapy |
| spellingShingle | YANG Wenbo HAO Lan WANG Zhigang2 ZHANG Ronggui CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro Di-san junyi daxue xuebao creka peptide prostate cancer liposome targeted therapy |
| title | CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro |
| title_full | CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro |
| title_fullStr | CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro |
| title_full_unstemmed | CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro |
| title_short | CREKA peptide-modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro |
| title_sort | creka peptide modified docetaxel loaded liposomes for targeted treatment of prostate cancer in vitro |
| topic | creka peptide prostate cancer liposome targeted therapy |
| url | http://aammt.tmmu.edu.cn/Upload/rhtml/202005276.htm |
| work_keys_str_mv | AT yangwenbo crekapeptidemodifieddocetaxelloadedliposomesfortargetedtreatmentofprostatecancerinvitro AT haolan crekapeptidemodifieddocetaxelloadedliposomesfortargetedtreatmentofprostatecancerinvitro AT wangzhigang2 crekapeptidemodifieddocetaxelloadedliposomesfortargetedtreatmentofprostatecancerinvitro AT zhangronggui crekapeptidemodifieddocetaxelloadedliposomesfortargetedtreatmentofprostatecancerinvitro |