Co-Delivery of Letrozole and Cyclophosphamide via Folic Acid-Decorated Nanoniosomes for Breast Cancer Therapy: Synergic Effect, Augmentation of Cytotoxicity, and Apoptosis Gene Expression

Breast cancer is one of the most prevalent causes of cancer mortality in women. In order to increase patient prognosis and survival rates, new technologies are urgently required to deliver therapeutics in a more effective and efficient manner. Niosome nanoparticles have been recently employed as therapeutic platforms capable of loading and carrying drugs within their core for both mono and combination therapy. Here, niosome-based nanoscale carriers were investigated as a targeted delivery system for breast cancer therapy. The platform developed consists of niosomes loaded with letrozole and cyclophosphamide (NLC) and surface-functionalized with a folic-acid-targeting moiety (NLCPFA). Drug release from the formulated particles exhibited pH-sensitive properties in which the niosome showed low and high release in physiological and cancerous conditions, respectively. The results revealed a synergic effect in cytotoxicity by co-loading letrozole and cyclophosphamide with an efficacy increment in NLCPFA use in comparison with NLC. The NLCPFA resulted in the greatest drug internalization compared to the non-targeted formulation and the free drug. Additionally, downregulation of cyclin-D, cyclin-E, MMP-2, and MMP-9 and upregulating the expression of caspase-3 and caspase-9 genes were observed more prominently in the nanoformulation (particularly for NLCPFA) compared to the free drug. This exciting data indicated that niosome-based nanocarriers containing letrozole and cyclophosphamide with controlled release could be a promising platform for drug delivery with potential in breast cancer therapy.

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Novel folate-targeted docetaxel-loaded nanoparticles for tumour targeting: in vitro and in vivo evaluation

RSC Advances ◽

10.1039/c6ra04466b ◽

2016 ◽

Vol 6 (69) ◽

pp. 64306-64314 ◽

Cited By ~ 4

Author(s):

M. H. Han ◽

Z. T. Li ◽

D. D. Bi ◽

Y. F. Guo ◽

H. X. Kuang ◽

...

Keyword(s):

Breast Cancer ◽

Folic Acid ◽

Cancer Therapy ◽

Targeted Delivery ◽

Tumour Targeting ◽

Breast Cancer Therapy ◽

In Vivo Evaluation ◽

Targeted Delivery System

Cholesterol-PEG1000-FA (folic acid) was synthesized as a stabilizer to encapsulate DTX, for the construction of a promising targeted delivery system for breast cancer therapy.

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Folic acid modified copper oxide nanoparticles for targeted delivery in in vitro and in vivo systems

RSC Advances ◽

10.1039/c5ra08110f ◽

2015 ◽

Vol 5 (83) ◽

pp. 68169-68178 ◽

Cited By ~ 26

Author(s):

Dipranjan Laha ◽

Arindam Pramanik ◽

Sourav Chattopadhyay ◽

Sandip kumar Dash ◽

Somenath Roy ◽

...

Keyword(s):

Breast Cancer ◽

Folic Acid ◽

Cancer Therapy ◽

Copper Oxide ◽

Targeted Delivery ◽

Copper Oxide Nanoparticles ◽

Oxide Nanoparticles ◽

Breast Cancer Therapy

Targeted delivery of copper oxide nanoparticles for breast cancer therapy.

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Fabrication of curcumin-loaded folic acid-tagged metal organic framework for triple negative breast cancer therapy inin vitroandin vivosystems

New Journal of Chemistry ◽

10.1039/c8nj03350a ◽

2019 ◽

Vol 43 (1) ◽

pp. 217-229 ◽

Cited By ~ 13

Author(s):

Dipranjan Laha ◽

Kunal Pal ◽

Angshuman Ray Chowdhuri ◽

Pravat Kumar Parida ◽

Sumanta Kumar Sahu ◽

...

Keyword(s):

Breast Cancer ◽

Folic Acid ◽

Cancer Therapy ◽

Triple Negative Breast Cancer ◽

Triple Negative ◽

Metal Organic Framework ◽

Free Drug ◽

Therapeutic Activity ◽

Breast Cancer Therapy ◽

Metal Organic

Curcumin has shown therapeutic activity against triple-negative breast cancer (TNBC) cells, but it shows low efficacy and low bioavailability when administered as a free drug.

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Targeted Delivery of Cabazitaxel Using Cyclic Cell-Penetrating Peptide and Biomarkers of Extracellular Matrix for Prostate and Breast Cancer Therapy

Bioconjugate Chemistry ◽

10.1021/acs.bioconjchem.1c00319 ◽

2021 ◽

Author(s):

Shang Eun Park ◽

Naglaa Salem El-Sayed ◽

Kiumars Shamloo ◽

Sandeep Lohan ◽

Sumit Kumar ◽

...

Keyword(s):

Breast Cancer ◽

Extracellular Matrix ◽

Cancer Therapy ◽

Targeted Delivery ◽

Cell Penetrating Peptide ◽

Breast Cancer Therapy ◽

Cell Penetrating

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Folic acid conjugated curcumin loaded biopolymeric gum acacia microsphere for triple negative breast cancer therapy in invitro and invivo model

Materials Science and Engineering C ◽

10.1016/j.msec.2018.10.071 ◽

2019 ◽

Vol 95 ◽

pp. 204-216 ◽

Cited By ~ 31

Author(s):

Kunal Pal ◽

Shubham Roy ◽

Pravat Kumar Parida ◽

Ananya Dutta ◽

Souravi Bardhan ◽

...

Keyword(s):

Breast Cancer ◽

Folic Acid ◽

Cancer Therapy ◽

Triple Negative Breast Cancer ◽

Triple Negative ◽

Breast Cancer Therapy ◽

Gum Acacia

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Corrigendum to “Folic acid conjugated curcumin loaded biopolymeric gum acacia microsphere for triple negative breast cancer therapy in invitro and invivo model” [Mater. Sci. Eng. C (2019) 204–216]

Materials Science and Engineering C ◽

10.1016/j.msec.2020.110866 ◽

2020 ◽

Vol 111 ◽

pp. 110866

Author(s):

Kunal Pal ◽

Shubham Roy ◽

Pravat Kumar Parida ◽

Ananya Dutta ◽

Souravi Bardhan ◽

...

Keyword(s):

Breast Cancer ◽

Folic Acid ◽

Cancer Therapy ◽

Triple Negative Breast Cancer ◽

Triple Negative ◽

Breast Cancer Therapy ◽

Gum Acacia

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Surface functionalisation of poly-APO-b-polyol ester cross-linked copolymers as core–shell nanoparticles for targeted breast cancer therapy

Scientific Reports ◽

10.1038/s41598-020-78601-x ◽

2020 ◽

Vol 10 (1) ◽

Author(s):

Rida Tajau ◽

Rosiah Rohani ◽

Siti Selina Abdul Hamid ◽

Zainah Adam ◽

Siti Najila Mohd Janib ◽

...

Keyword(s):

Breast Cancer ◽

Drug Delivery ◽

Cancer Therapy ◽

Targeted Delivery ◽

Particle Diameter ◽

Core Shell ◽

Breast Cancer Therapy ◽

Polyol Ester ◽

Apo B ◽

Chemical Structures

AbstractPolymeric nanoparticles (NPs) are commonly used as nanocarriers for drug delivery, whereby their sizes can be altered for a more efficient delivery of therapeutic active agents with better efficacy. In this work, cross-linked copolymers acted as core–shell NPs from acrylated palm olein (APO) with polyol ester were synthesized via gamma radiation-induced reversible addition-fragmentation chain transfer (RAFT) polymerisation. The particle diameter of the copolymerised poly(APO-b-polyol ester) core–shell NPs was found to be less than 300 nm, have a low molecular weight (MW) of around 24 kDa, and showed a controlled MW distribution of a narrow polydispersity index (PDI) of 1.01. These properties were particularly crucial for further use in designing targeted NPs, with inclusion of peptide for the targeted delivery of paclitaxel. Moreover, the characterisation of the synthesised NPs using Fourier Transform-Infrared (FTIR) and Neutron Magnetic Resonance (NMR) analyses confirmed the possession of biodegradable hydrolysed ester in its chemical structures. Therefore, it can be concluded that the synthesised NPs produced may potentially contribute to better development of a nano-structured drug delivery system for breast cancer therapy.

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