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Targeting self-assembled F127-peptide polymer with pH sensitivity for release of anticancer drugs.

ABSTRACT: The treatment of breast cancer mainly relies on chemotherapy drugs, which present significant side effects. The most typical example is the cardiotoxicity and bone marrow suppression associated with doxorubicin (DOX). Therefore, this drug is not the first choice in clinical treatment. We designed ATN-FFPFF-ATN, a new targeted antitumor drug carrier, polymerized from phenylalanine dipeptide (FF), ATN-161 peptide, and Pluronic® F-127. The peptide and Pluronic® F-127 are linked with acetal and are, therefore, acid-sensitive. As cancer can reduce pH through complex mechanisms and subsequently maintain acid ambience, our vehicle can smartly unravel at a peculiar position, through which the drug can specifically accumulate inside the tumor. ATN-161 is a protein ligand of integrin α₅β₁, which is highly expressed on the surface of some breast cancer cells. This targeting peptide sequence can play a role in the selective delivery of DOX to tumor cells. The DOX-carrying vector was able to significantly inhibit cell proliferation and promote cell apoptosis in MDA-MB-231 cells. Based on these results, ATN-FFPFF-ATN with pH response is a promising vehicle for DOX delivery.

SUBMITTER: Han W

PROVIDER: S-EPMC8693612 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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Targeting self-assembled F127-peptide polymer with pH sensitivity for release of anticancer drugs.

Han Wenzhao W Meng Fanwei F Gan Hao H Guo Feng F Ke Junfeng J Wang Liping L

RSC advances 20210105 3

The treatment of breast cancer mainly relies on chemotherapy drugs, which present significant side effects. The most typical example is the cardiotoxicity and bone marrow suppression associated with doxorubicin (DOX). Therefore, this drug is not the first choice in clinical treatment. We designed ATN-FFPFF-ATN, a new targeted antitumor drug carrier, polymerized from phenylalanine dipeptide (FF), ATN-161 peptide, and Pluronic® F-127. The peptide and Pluronic® F-127 are linked with acetal and are, ...[more]

PMID: 35424141

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Project description:The use of an appropriate delivery system capable of protecting, translocating, and selectively releasing therapeutic moieties to desired sites can promote the efficacy of an active compound. In this work, we have developed a nanoformulation which preserves its magnetization to load a model anticancerous drug and to explore the controlled release of the drug in a cancerous environment. For the preparation of the nanoformulation, self-assembled magnetic nanospheres (MNS) made of superparamagnetic iron oxide nanoparticles were grafted with a monolayer of (3-aminopropyl)triethoxysilane (APTES). A direct functionalization strategy was used to avoid the loss of the MNS magnetization. The successful preparation of the nanoformulation was validated by structural, microstructural, and magnetic investigations. X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared spectroscopy (FTIR) were used to establish the presence of APTES on the MNS surface. The amine content quantified by a ninhydrin assay revealed the monolayer coverage of APTES over MNS. The monolayer coverage of APTES reduced only negligibly the saturation magnetization from 77 emu/g (for MNS) to 74 emu/g (for MNS-APTES). Detailed investigations of the thermoremanent magnetization were carried out to assess the superparamagnetism in the MNS. To make the nanoformulation pH-responsive, the anticancerous drug Nintedanib (NTD) was conjugated with MNS-APTES through the acid liable imine bond. At pH 5.5, which mimics a cancerous environment, a controlled release of 85% in 48 h was observed. On the other hand, prolonged release of NTD was found at physiological conditions (i.e., pH 7.4). In vitro cytotoxicity study showed dose-dependent activity of MNS-APTES-NTD for human lung cancer cells L-132. About 75% reduction in cellular viability for a 100 μg/mL concentration of nanoformulation was observed. The nanoformulation designed using MNS and monolayer coverage of APTES has potential in cancer therapy as well as in other nanobiological applications.

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Targeting self-assembled F127-peptide polymer with pH sensitivity for release of anticancer drugs.

Publications

Targeting self-assembled F127-peptide polymer with pH sensitivity for release of anticancer drugs.

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