In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles
Cancer remains a disease with one of the highest mortality rates worldwide. The poor water solubility and tissue selectivity of commonly used chemotherapeutic agents contribute to their poor efficacy and serious adverse effects. This study proposes an alternative to the traditional physicochemically...
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MDPI AG
2023-11-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/11/2644 |
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| author | Dan Yun Dengyuan Liu Jinlin Liu Yanyi Feng Hongyu Chen Simiao Chen Qingchun Xie |
| author_facet | Dan Yun Dengyuan Liu Jinlin Liu Yanyi Feng Hongyu Chen Simiao Chen Qingchun Xie |
| author_sort | Dan Yun |
| collection | DOAJ |
| description | Cancer remains a disease with one of the highest mortality rates worldwide. The poor water solubility and tissue selectivity of commonly used chemotherapeutic agents contribute to their poor efficacy and serious adverse effects. This study proposes an alternative to the traditional physicochemically combined modifications used to develop targeted drug delivery systems, involving a simpler surface modification strategy. cRGDyK peptide (RGD)-modified PLGA nanoparticles (NPs) loaded with paclitaxel were constructed by coating the NP surfaces with polydopamine (PD). The average particle size of the produced NPs was 137.6 ± 2.9 nm, with an encapsulation rate of over 80%. In vitro release tests showed that the NPs had pH-responsive drug release properties. Cellular uptake experiments showed that the uptake of modified NPs by tumor cells was significantly better than that of unmodified NPs. A tumor cytotoxicity assay demonstrated that the modified NPs had a lower IC<sub>50</sub> and greater cytotoxicity than those of unmodified NPs and commercially available paclitaxel formulations. An in vitro cytotoxicity study indicated good biosafety. A tumor model in female BALB/c rats was established using murine-derived breast cancer 4T1 cells. RGD-modified NPs had the highest tumor-weight suppression rate, which was higher than that of the commercially available formulation. PTX-PD-RGD-NPs can overcome the limitations of antitumor drugs, reduce drug toxicity, and increase efficacy, showing promising potential in cancer therapy. |
| first_indexed | 2024-03-09T16:31:24Z |
| format | Article |
| id | doaj.art-6679f517e0e14cf3857e2e955cac8237 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T16:31:24Z |
| publishDate | 2023-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-6679f517e0e14cf3857e2e955cac82372023-11-24T15:01:14ZengMDPI AGPharmaceutics1999-49232023-11-011511264410.3390/pharmaceutics15112644In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded NanoparticlesDan Yun0Dengyuan Liu1Jinlin Liu2Yanyi Feng3Hongyu Chen4Simiao Chen5Qingchun Xie6Center for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for New Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCancer remains a disease with one of the highest mortality rates worldwide. The poor water solubility and tissue selectivity of commonly used chemotherapeutic agents contribute to their poor efficacy and serious adverse effects. This study proposes an alternative to the traditional physicochemically combined modifications used to develop targeted drug delivery systems, involving a simpler surface modification strategy. cRGDyK peptide (RGD)-modified PLGA nanoparticles (NPs) loaded with paclitaxel were constructed by coating the NP surfaces with polydopamine (PD). The average particle size of the produced NPs was 137.6 ± 2.9 nm, with an encapsulation rate of over 80%. In vitro release tests showed that the NPs had pH-responsive drug release properties. Cellular uptake experiments showed that the uptake of modified NPs by tumor cells was significantly better than that of unmodified NPs. A tumor cytotoxicity assay demonstrated that the modified NPs had a lower IC<sub>50</sub> and greater cytotoxicity than those of unmodified NPs and commercially available paclitaxel formulations. An in vitro cytotoxicity study indicated good biosafety. A tumor model in female BALB/c rats was established using murine-derived breast cancer 4T1 cells. RGD-modified NPs had the highest tumor-weight suppression rate, which was higher than that of the commercially available formulation. PTX-PD-RGD-NPs can overcome the limitations of antitumor drugs, reduce drug toxicity, and increase efficacy, showing promising potential in cancer therapy.https://www.mdpi.com/1999-4923/15/11/2644nanoparticlesRGDPLGAsurface modificationantitumor effect |
| spellingShingle | Dan Yun Dengyuan Liu Jinlin Liu Yanyi Feng Hongyu Chen Simiao Chen Qingchun Xie In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles Pharmaceutics nanoparticles RGD PLGA surface modification antitumor effect |
| title | In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles |
| title_full | In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles |
| title_fullStr | In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles |
| title_full_unstemmed | In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles |
| title_short | In Vitro/In Vivo Preparation and Evaluation of cRGDyK Peptide-Modified Polydopamine-Bridged Paclitaxel-Loaded Nanoparticles |
| title_sort | in vitro in vivo preparation and evaluation of crgdyk peptide modified polydopamine bridged paclitaxel loaded nanoparticles |
| topic | nanoparticles RGD PLGA surface modification antitumor effect |
| url | https://www.mdpi.com/1999-4923/15/11/2644 |
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