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Ormeloxifene nanotherapy for cervical cancer treatment

Authors Chauhan N, Maher DM, Hafeez BB, Mandil H, Singh MM, Yallapu MM, Jaggi M, Chauhan SC

Received 9 January 2019

Accepted for publication 4 June 2019

Published 3 September 2019 Volume 2019:14 Pages 7107—7121


Checked for plagiarism Yes

Review by Single anonymous peer review

Peer reviewer comments 3

Editor who approved publication: Prof. Dr. Anderson Oliveira Lobo

Neeraj Chauhan1,2, Diane M Maher3, Bilal B Hafeez1,2, Hassan Mandil1, Man M Singh4, Murali M Yallapu1,2, Meena Jaggi1,2, Subhash C Chauhan1,2

1Department of Pharmaceutical Sciences, University of Tennessee Health Science Center, Memphis, TN 38163, USA; 2Department of Immunology and Microbiology, School of Medicine, University of Texas Rio Grande Valley, McAllen, TX 78504, USA; 3Sanford Research Center, USD, Sioux Falls, SD 57104, USA; 4Research and Development, Saraswati Dental College, Lucknow, Uttar Pradesh, India

Correspondence: Meena Jaggi; Subhash C Chauhan
Department of Immunology and Microbiology, School of Medicine, University of Texas Rio Grande Valley, McAllen, TX 78504, USA
Tel +1 956 296 1926; +1 956 296 5000

Background: Cervical cancer (CxCa) ranks as the fourth most prevalent women-related cancer worldwide. Therefore, there is a crucial need to develop newer treatment modalities. Ormeloxifene (ORM) is a non-steroidal, selective estrogen receptor modulator (SERM) that is used as an oral contraceptive in humans. Recent investigations suggest that ORM exhibits potent anti-cancer activity against various types of cancers. Nanoparticulates offer targeted delivery of anti-cancer drugs with minimal toxicity and promise newer approaches for cancer diagnosis and treatment. Therefore, the nanotherapy approach is superior compared to traditional chemotherapy, which is not site-specific and is often associated with various side effects.
Methods: Pursuing this novel nanotherapy approach, our lab has recently developed ORM-loaded poly [lactic-co-glycolic acid] (PLGA), an FDA-approved biodegradable polymer, nanoparticles to achieve targeted drug delivery and improved bioavailability. Our optimized PLGA-ORM nanoformulation showed improved internalization in both dose- and energy-dependent manners, through endocytosis-mediated pathways in both Caski and SiHa cell lines. Additionally, we employed MTS and colony forming assays to determine the short- and long-term effects of PLGA-ORM on these cells.
Results: Our results showed that this formulation demonstrated improved inhibition of cellular proliferation and clonogenic potential compared to free ORM. Furthermore, the PLGA-ORM nanoformulation exhibited superior anti-tumor activities in an orthotopic cervical cancer mouse model than free ORM.
Conclusion: Collectively, our findings suggest that our novel nanoformulation has great potential for repurposing the drug and becoming a novel modality for CxCa management.

Keywords: CxCa, ORM, PLGA, nanoformulation

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