Development and evaluation of talazoparib nanoemulsion for systemic therapy of BRCA1-mutant cancer

Neelesh Kumar Mehra, Rajeshwar R Tekmal, Srinath Palakurthi

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Aim: This is a debut study report on talazoparib (BMN-673)-loaded nanoemulsion (TZNE) for parenteral administration. Materials and Methods: TZNE (0.05% drug, 151.4±0.7 nm droplet size, polydispersity index of 0.120±0.010 and zeta potential of -33.30±1.22 mV) was designed, developed and characterized using in vitro studies. A cumulative in vitro release study was performed in physiological phosphate buffer solution at different pH (5.3, 6.5 and 7.4) using a dialysis method. Cytotoxicity and apoptosis assays were performed on MDA-MB-231, NCI/ADR-RES, 2008 C13, CP-70 and SKOV-3 cell lines using CellTiter® Blue. Quantitative and qualitative cell uptake was studied using fluorescent probe, coumarin-6 (C-6). Results: The drug release form TZNE nanoemulsion was slow and sustained for 24 h. Cytotoxicity and apoptosis were found to be concentration-dependent. The half-maximal inhibitory concentration of TZNE was 0.4852 and 1.35, 11.757 and 0.4696, and 1.169 and 0.7235 μM in MDA-MB-231, SKOV-3 and NCI/ADR-RES cells with 48 and 72 h incubation, respectively. Cellular uptake studies using fluorescent probe, coumarin-6 C-6, showed higher cellular uptake of TNZE compared with free C6. Results suggest that nanoemulsion could provide a new platform for systemic delivery of talazoparib.

Original languageEnglish (US)
Pages (from-to)4493-4503
Number of pages11
JournalAnticancer Research
Volume38
Issue number8
DOIs
StatePublished - Aug 1 2018

Fingerprint

Fluorescent Dyes
Apoptosis
Neoplasms
Dialysis
Buffers
Therapeutics
Phosphates
Cell Line
Pharmaceutical Preparations
talazoparib
coumarin 6
In Vitro Techniques
Drug Liberation

Keywords

  • BRCA1
  • Breast cancer
  • Cell uptake
  • Cytotoxicity
  • Nanoemulsion
  • Talazoparib

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Development and evaluation of talazoparib nanoemulsion for systemic therapy of BRCA1-mutant cancer. / Mehra, Neelesh Kumar; Tekmal, Rajeshwar R; Palakurthi, Srinath.

In: Anticancer Research, Vol. 38, No. 8, 01.08.2018, p. 4493-4503.

Research output: Contribution to journalArticle

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