Chitosan-modified PLGA polymeric nanocarriers with better delivery potential for tamoxifen.

Abstract:

:Breast cancer is believed as the second most common cause of cancer-related deaths in women for which tamoxifen is frequently prescribed. Despite many promises, tamoxifen is associated with various challenges like low hydrophilicity, poor bioavailability and dose-dependent toxicity. Therefore, it was envisioned to develop tamoxifen- loaded chitosan-PLGA micelles for potential safe and better delivery of this promising agent. The chitosan-PLGA copolymer was synthesised and characterised by Fourier Transform-Infrared, Ultraviolet-visible and Nuclear Magnetic Resonance spectroscopic techniques. The drug-loaded nanocarrier was characterised for drug-pay load, micrometrics, surface charge and morphological attributes. The developed system was evaluated for in-vitro drug release, haemolytic profile, cellular-uptake, anticancer activity by cytotoxicity assay and dermatokinetic studies. The developed nano-system was able to substantially load the drug and control the drug release. The in-vitro cytotoxicity offered by the system was significantly enhanced vis-a-vis plain drug, and there was no substantial haemolysis. The IC50 values were significantly decreased and the nanocarriers were uptaken by MCF-7 cells, noticeably. The carrier was able to locate the drug in the interiors of rat skin in considerable amounts to that of the conventional product. This approach is promising as it provides a biocompatible and effective option for better delivery of tamoxifen.

journal_name

Int J Biol Macromol

authors

Thakur CK,Thotakura N,Kumar R,Kumar P,Singh B,Chitkara D,Raza K

doi

10.1016/j.ijbiomac.2016.08.080

subject

Has Abstract

pub_date

2016-12-01 00:00:00

pages

381-389

issue

Pt A

eissn

0141-8130

issn

1879-0003

pii

S0141-8130(16)31400-3

journal_volume

93

pub_type

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