A novel micelle-encapsulated platinum(II) anticancer agent

Journal of Controlled Release : Official Journal of the Controlled Release Society
Vithal B JadhavYoun Soo Sohn

Abstract

A hydrophobic and water-insoluble platinum(II) compound, cis-(cha)(2)Pt(NO(3))(2) was encapsulated by macromolecular micelles self-assembled from an amphiphilic cyclotriphosphazene [NP(MPEG750)(GlyPheLeu)(2)Et](3) (CP750). The micelle-encapsulated platinum(II) compound exhibited outstanding pharmacokinetics in rats by showing long blood circulation and much larger systemic exposure (AUC=43.5 μgh/ml) compared with the free carboplatin (AUC=4.32 μgh/ml). Biodistribution study of the micellar platinum(II) compound using male Sprague-Dawley rats has shown excellent tumor to tissue ratios of 4.03 at 2h post injection and 4.67 at 24h post injection. Furthermore, the micellar platinum(II) compound exhibited more than 6 times higher cellular uptake in human cervical (HeLa) and lung (A549) tumor cells compared with the free platinum compound. Also it is surprising that the micellar platinum(II) compound displayed specifically high cytotoxicity against the stomach tumor cells (SNU638), which are one of the least responsive to chemotherapeutic agents currently in clinical use. The acute toxicity study has shown that the LD(50) values of free and the micellar cis-(cha)(2)Pt(NO(3))(2) are approximately 70 mg/kg and 90 mg/kg, respectively. T...Continue Reading

Citations

Apr 15, 2014·Polymers·Ian Teasdale, Oliver Brüggemann
Nov 15, 2011·International Journal of Pharmaceutics·Yong Joo JunYoun Soo Sohn
Jul 30, 2015·Biomaterials Science·Jihoon KimWon Jong Kim
Jul 26, 2014·Journal of Inorganic Biochemistry·Prakash G AvajiYoun Soo Sohn
Oct 12, 2013·Advanced Drug Delivery Reviews·Hardeep S OberoiTatiana K Bronich
Sep 14, 2013·Colloids and Surfaces. B, Biointerfaces·Mahdieh RazmiHassan Mansuri-Torshizi
May 8, 2013·Journal of Controlled Release : Official Journal of the Controlled Release Society·Kaushik ThankiSanyog Jain
May 14, 2016·Macromolecular Bioscience·Helena HenkeIan Teasdale
Feb 7, 2017·Chemical Society Reviews·Nane VanparijsBruno G De Geest
Feb 23, 2011·Chemistry : a European Journal·Melissa D Krebs, Eben Alsberg
Apr 21, 2020·Journal of Vacuum Science and Technology. B, Nanotechnology & Microelectronics : Materials, Processing, Measurement, & Phenomena : JVST B·Kenneth S OgueriCato T Laurencin

❮ Previous
Next ❯

Related Concepts

Related Feeds

Aminoglycosides

Aminoglycoside is a medicinal and bacteriologic category of traditional Gram-negative antibacterial medications that inhibit protein synthesis and contain as a portion of the molecule an amino-modified glycoside. Discover the latest research on aminoglycoside here.

Aminoglycosides (ASM)

Aminoglycoside is a medicinal and bacteriologic category of traditional Gram-negative antibacterial medications that inhibit protein synthesis and contain as a portion of the molecule an amino-modified glycoside. Discover the latest research on aminoglycoside here.