A dual pH/Redox responsive copper-ligand nanoliposome bioactive complex for the treatment of chronic inflammation.

Abstract

A novel dual pH/redox-responsive polymeric nanoliposome system (NLs) loaded with a copper-liganded bioactive complex was prepared and designed as a controlled delivery system for the management of inflammation. The NLs were synthesised after preparation of the copper-glyglycine-prednisolone succinate] ([(Cu(glygly)(PS)]) complex, and the dual pH/redox responsive biopolymer respectively. The methodology undertaken for the development of the drug delivery system involved coordination of the bioactive to Copper (II), preparation of dual pH/redox responsive biopolymer, and the synthesis of dual pH/redox nanoliposomes. Characterisations of the prepared copper-liganded bioactive [Copper-glyglycine-prednisolone succinate] ([(Cu(glygly)(PS)]) complex, dual pH/redox responsive biopolymer (Eudragit E100-cystamine) and [(Cu(glygly)(PS)]-loaded NLs were carried out using spectroscopic and physicochemical techniques. Results indicated a high inflammatory/oxidant inhibitory activity of [Cu(glygly)(PS)] in comparison to the free PS drug. The [Cu(glygly)(PS)] complex exhibited a significant free radical-scavenging activity (60.1±1.2%) and lipoxygenase (LOX-5) inhibitory activity (36.6±1.3%) in comparison to PS which resulted in activity of 4.4±1.4% and inhibition of 6.1±2.6% respectively. The [Cu(glygly)(PS)] loaded NLs demonstrated low release profiles of 22.9±5.4% in 6h at pH 7.4, in comparison to a significant accelerated release at pH 5 in a reducing environment of 75.9±3.7% over 6h duration. Results suggest that the novel copper-liganded bioactive delivery system with controlled drug release mechanism could serve as a potential drug delivery system candidate in the management of inflammation.

• Authors: Simphiwe Mavuso, Yahya E Choonara, Thashree Marimuthu, Pradeep Kumar, Lisa C du Toit, Pierre P D Kondiah, Viness Pillay
• Journal: International journal of pharmaceutics (Int J Pharm) Vol. 509 Issue 1-2 Pg. 348-359 (Jul 25 2016) ISSN: 1873-3476 [Electronic] Netherlands
• PMID: 27269194 (Publication Type: Journal Article)
• Copyright: Copyright © 2016 Elsevier B.V. All rights reserved.

Chemical References

• Acrylates
• Delayed-Action Preparations
• Eudragit E100
• Ligands
• Liposomes
• Polymers
• Copper
• Prednisolone

Topics

• Acrylates (chemistry)
• Copper (chemistry)
• Delayed-Action Preparations (chemical synthesis, pharmacology)
• Drug Delivery Systems (methods)
• Hydrogen-Ion Concentration
• Inflammation (drug therapy)
• Ligands
• Liposomes (chemistry)
• Nanoparticles (chemistry)
• Oxidation-Reduction
• Polymers (chemistry)
• Prednisolone (chemistry, pharmacology)