Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation
The accumulation and penetration of antitumor drugs in tumor tissues are directly related to their antitumor effects. The particle size of the nanodrug delivery system is one of the most important factors for the accumulation and penetration of antitumor drugs within tumor tissues. Generally, nanode...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2020-01-01
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| Series: | Drug Delivery |
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| Online Access: | http://dx.doi.org/10.1080/10717544.2020.1827086 |
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| author | Yunyan Chen Mengfei Guo Ding Qu Yuping Liu Jian Guo Yan Chen |
| author_facet | Yunyan Chen Mengfei Guo Ding Qu Yuping Liu Jian Guo Yan Chen |
| author_sort | Yunyan Chen |
| collection | DOAJ |
| description | The accumulation and penetration of antitumor drugs in tumor tissues are directly related to their antitumor effects. The particle size of the nanodrug delivery system is one of the most important factors for the accumulation and penetration of antitumor drugs within tumor tissues. Generally, nanodelivery systems of intermediate size (100–120 nm) are capable of efficient accumulation owing to prolonged circulation and enhanced permeability and retention (EPR) effect; however, smaller ones (20–40 nm) are effective for deep penetration within tumor tissue. Currently a conventional drug delivery system cannot possess two types of optimal sizes, simultaneously. To solve this and to enhance cervical cancer treatment, a furin-responsive triterpenine-based liposomal complex (PEGcleavable Tf-CTM/L), with Tf-CTM (transferrin-modified tripterine-loaded coix seed oil microemulsion) in core, coated with a thermo-sensitive lipid and a kind of PEG shell modified with a furin-cleavable peptide was developed to improve tumor-specific accumulation and penetration. Herein, PEGcleavable Tf-CTM/L was capable of efficient accumulation because of EPR effect. The PEG shells could timely detach under stimulation of overexpressed furin protein to solve the problem of the steric hindrance dilemma. The small-sized Tf-CTM released under stimulation of tumor microthermal environment in cervical cancer, which was efficient with regards to deep penetration at tumor sites. Notably, compared to the use of triterpenine alone, PEGcleavable Tf-CTM/L promoted anticervical efficacy and displayed diminished systemic toxicity by efficient accumulation and deep penetration of antitumor drugs within tumor tissues. Our study provides a new strategy, and holds promising potential for anticervical cancer treatment. |
| first_indexed | 2024-12-17T07:39:53Z |
| format | Article |
| id | doaj.art-c99b0b3ed2864bca8b139bdbac3e1e27 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-17T07:39:53Z |
| publishDate | 2020-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-c99b0b3ed2864bca8b139bdbac3e1e272022-12-21T21:58:11ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642020-01-012711608162410.1080/10717544.2020.18270861827086Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulationYunyan Chen0Mengfei Guo1Ding Qu2Yuping Liu3Jian Guo4Yan Chen5Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese MedicineAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese MedicineAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese MedicineAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese MedicineAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese MedicineAffiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese MedicineThe accumulation and penetration of antitumor drugs in tumor tissues are directly related to their antitumor effects. The particle size of the nanodrug delivery system is one of the most important factors for the accumulation and penetration of antitumor drugs within tumor tissues. Generally, nanodelivery systems of intermediate size (100–120 nm) are capable of efficient accumulation owing to prolonged circulation and enhanced permeability and retention (EPR) effect; however, smaller ones (20–40 nm) are effective for deep penetration within tumor tissue. Currently a conventional drug delivery system cannot possess two types of optimal sizes, simultaneously. To solve this and to enhance cervical cancer treatment, a furin-responsive triterpenine-based liposomal complex (PEGcleavable Tf-CTM/L), with Tf-CTM (transferrin-modified tripterine-loaded coix seed oil microemulsion) in core, coated with a thermo-sensitive lipid and a kind of PEG shell modified with a furin-cleavable peptide was developed to improve tumor-specific accumulation and penetration. Herein, PEGcleavable Tf-CTM/L was capable of efficient accumulation because of EPR effect. The PEG shells could timely detach under stimulation of overexpressed furin protein to solve the problem of the steric hindrance dilemma. The small-sized Tf-CTM released under stimulation of tumor microthermal environment in cervical cancer, which was efficient with regards to deep penetration at tumor sites. Notably, compared to the use of triterpenine alone, PEGcleavable Tf-CTM/L promoted anticervical efficacy and displayed diminished systemic toxicity by efficient accumulation and deep penetration of antitumor drugs within tumor tissues. Our study provides a new strategy, and holds promising potential for anticervical cancer treatment.http://dx.doi.org/10.1080/10717544.2020.1827086tripterinemicroemulsionliposomepenetrationaccumulationanticervical cancer |
| spellingShingle | Yunyan Chen Mengfei Guo Ding Qu Yuping Liu Jian Guo Yan Chen Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation Drug Delivery tripterine microemulsion liposome penetration accumulation anticervical cancer |
| title | Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation |
| title_full | Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation |
| title_fullStr | Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation |
| title_full_unstemmed | Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation |
| title_short | Furin-responsive triterpenine-based liposomal complex enhances anticervical cancer therapy through size modulation |
| title_sort | furin responsive triterpenine based liposomal complex enhances anticervical cancer therapy through size modulation |
| topic | tripterine microemulsion liposome penetration accumulation anticervical cancer |
| url | http://dx.doi.org/10.1080/10717544.2020.1827086 |
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