Next Article in Journal
Synthesis of New Indanyl Nucleoside Analogues and their Biological Evaluation on Hepatitis C Virus (HCV) Replicon
Next Article in Special Issue
Quantitative Analysis of Tozadenant Using Liquid Chromatography-Mass Spectrometric Method in Rat Plasma and Its Human Pharmacokinetics Prediction Using Physiologically Based Pharmacokinetic Modeling
Previous Article in Journal
Green and Facile Assembly of Diverse Fused N-Heterocycles Using Gold-Catalyzed Cascade Reactions in Water
Previous Article in Special Issue
Anti-Idiotype DNA Aptamer Affinity Purification–High-Temperature Reversed-Phase Liquid Chromatography: A Simple, Accurate, and Selective Bioanalysis of Bevacizumab
Article Menu
Issue 5 (March-1) cover image

Export Article

Correction published on 7 May 2019, see Molecules 2019, 24(9), 1771.

Open AccessArticle

Quantitative Characterization of Olaparib in Nanodelivery System and Target Cell Compartments by LC-MS/MS

Dipartimento di Scienze Biomediche e Cliniche “Luigi Sacco”, Università degli Studi di Milano, Via G.B. Grassi 74, 20157 Milano, Italy
Dipartimento di Scienze Biomediche, Chirurgiche ed Odontoiatriche, Sezione di Tossicologia Forense, Università degli Studi di Milano, Via Mangiagalli 37, 20133 Milano, Italy
Author to whom correspondence should be addressed.
Molecules 2019, 24(5), 989;
Received: 25 January 2019 / Revised: 7 March 2019 / Accepted: 8 March 2019 / Published: 11 March 2019
(This article belongs to the Special Issue Biological Sample Analysis by Liquid Chromatography)
PDF [3025 KB, uploaded 7 May 2019]


Olaparib, an orally active inhibitor of poly(ADP-ribose)polymerase(PARP), is the drug of choice in the treatment of gBRCA1/2+ metastatic breast cancers. Unfortunately, Olaparib is poorly soluble with low bioavailability and tumor accumulation; nano-delivery could be a good choice to overcome these disadvantages. Here, a rapid and robust HPLC-ESI–MS/MS method for the quantification of Olaparib in ferritin nano-carriers led to the development of cells compartments, different tissues, plasma and urines and were validated to assess the effects of nano-delivery on cell compartment distribution of the drug. This method allows the quantification of Olaparib within the linear range of 0.1–10ng/mL in cells culture medium and cell cytoplasm, of 0.5–10ng/mL in nuclei, of 0.5–100ng/mL in plasma and urine and of 10–500ng/mL in tissue samples (kidney and liver). The limit of quantification was found to be 1.54 ng/mL for liver, 2.87 ng/mL for kidney, and lower than 0.48 ng/mL for all matrices. The method has been applied to quantify Ola encapsulated in ferritin-nano-carriers during the nano-drug development. The application of the method to human BRCA-mutated cell model to quantify the Olaparib distribution after incubation of free or ferritin-encapsulated Olaparib is also reported. This sensitive method allows the quantification of low concentrations of Olaparib released from nano-carriers in different cell compartments, leading to the determination of the drug release and kinetic profile of an essential parameter to validate nano-carriers. View Full-Text
Keywords: Olaparib; Olaparib nano-formulation; HPLC; bioanalysis; mass spectrometry; sample preparation Olaparib; Olaparib nano-formulation; HPLC; bioanalysis; mass spectrometry; sample preparation

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Ottria, R.; Ravelli, A.; Miceli, M.; Casati, S.; Orioli, M.; Ciuffreda, P. Quantitative Characterization of Olaparib in Nanodelivery System and Target Cell Compartments by LC-MS/MS. Molecules 2019, 24, 989.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top