Pluronic Polymer-Based Ormeloxifene Nanoformulations Induce Superior Anticancer Effects in Pancreatic Cancer Cells.


Journal

ACS omega
ISSN: 2470-1343
Titre abrégé: ACS Omega
Pays: United States
ID NLM: 101691658

Informations de publication

Date de publication:
21 Jan 2020
Historique:
received: 11 10 2019
accepted: 16 12 2019
entrez: 28 1 2020
pubmed: 28 1 2020
medline: 28 1 2020
Statut: epublish

Résumé

Utilization of safe cytotoxic agents with precise anticancer activity is considered as the prime focus of cancer therapeutics research. A greater incentive for such agents arises from the molecules/drugs that are already being used for other indications. Ormeloxifene (ORM) is a nonsteroidal, nonhormonal selective estrogen receptor modulator (SERM), which has been in human use for contraception purposes. Although in the recent past, many reports have suggested its emerging role as an anticancer agent, no significant attention was paid toward generating simple and safe nanoformulation(s) for improved therapeutic activity and tumor cell-specific delivery. Our aim is to develop nanoformulation(s) of ormeloxifene to improve its targeted delivery in tumor cells. We developed ormeloxifene nanoformulation(s) by utilizing various biocompatible polymers. The optimized formulations with pluronic polymers F127 and F68 show improved nanoparticle characteristics. These formulations show enhanced cellular uptake that allows ormeloxifene's intracellular availability. We further evaluated its improved anticancer activity by performing cell proliferation, flow cytometry, and immunoblotting assays. Overall, this study confirms possible novel nanoformulation(s) of ormeloxifene to be evolved as a new therapeutic modality for cancer treatment.

Identifiants

pubmed: 31984272
doi: 10.1021/acsomega.9b03382
pmc: PMC6977081
doi:

Types de publication

Journal Article

Langues

eng

Pagination

1147-1156

Subventions

Organisme : NCI NIH HHS
ID : R01 CA204552
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA206069
Pays : United States
Organisme : NCI NIH HHS
ID : R01 CA210192
Pays : United States

Informations de copyright

Copyright © 2020 American Chemical Society.

Déclaration de conflit d'intérêts

The authors declare no competing financial interest.

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Auteurs

Neeraj Chauhan (N)

Department of Immunology and Microbiology, School of Medicine, University of Texas Rio Grande Valley, McAllen, Texas 78504, United States.
Department of Pharmaceutical Sciences and Center for Cancer Research, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, South Dakota 57105, United States.

Amber Kruse (A)

Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, South Dakota 57105, United States.
Division of Natural Sciences, Mount Marty College, Yankton, South Dakota 57078, United States.

Hilary Newby (H)

Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, South Dakota 57105, United States.
Division of Natural Sciences, Augustana College, Sioux Falls, South Dakota 57105, United States.

Meena Jaggi (M)

Department of Immunology and Microbiology, School of Medicine, University of Texas Rio Grande Valley, McAllen, Texas 78504, United States.
Department of Pharmaceutical Sciences and Center for Cancer Research, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, South Dakota 57105, United States.

Murali M Yallapu (MM)

Department of Immunology and Microbiology, School of Medicine, University of Texas Rio Grande Valley, McAllen, Texas 78504, United States.
Department of Pharmaceutical Sciences and Center for Cancer Research, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, South Dakota 57105, United States.

Subhash C Chauhan (SC)

Department of Immunology and Microbiology, School of Medicine, University of Texas Rio Grande Valley, McAllen, Texas 78504, United States.
Department of Pharmaceutical Sciences and Center for Cancer Research, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Cancer Biology Research Center, Sanford Research/USD, Sioux Falls, South Dakota 57105, United States.

Classifications MeSH