Multi-drug delivery of tuberculosis drugs by pi-back bonded gold nanoparticles with multiblock copolyesters

作者：Gajendiran Mani; Balashanmugam Pannerselvam; Kalaichelvan P T; Balasubramanian Sengottuvelan^*

来源：Materials Research Express, 2016, 3(6): 065401.

DOI：10.1088/2053-1591/3/6/065401

• multiblock copolymers
• polymer-gold nanoconjugates
• cytotoxicity
• controlled drug release
• tuberculosis

The effect of pi-back-bonding between AuNPs and the carbonyl group of multiblock copolyester on tuberculosis multi-drug delivery has been investigated. The carbonyl group of copolyester has vacant p orbitals and these vacant orbitals accept electron clouds from the filled d orbitals of Au-0 to form pi-back-bonding, which enhances the electron density for the carbonyl oxygen. This high electron density results in the strong binding of drug molecules with multiblock copolyesters and hence sustained drug release is achieved for a longer duration when compared to polymer systems without AuNPs. Anew series of tartarate-linked poly(lactic-co-glycolic acid) (PLGA)-polyethylene glycol (PEG)-based multiblock copolymers has been synthesized using a solvent-free melt reaction. The biocompatibility of multiblock copolyesters and AuNP nanoconjugates was investigated with an in vitro cytotoxicity study on the Vero cell line. Three major tuberculosis drugs, namely, rifampicin-, isoniazid-and pyrazinamide-loaded AuNP multiblock copolymer NPs were prepared by probe sonication followed by the self-assembly method. An in vitro drug release experiment was carried out and the amount of the three drugs released at various time intervals was determined simultaneously by the HPLC technique. The nanoconjugates exhibit 33%-40% RIF, 71%-95% INH, 77%-99% PYZ loading efficiencies, while the polymer NPs exhibit relatively lesser values. The nanoconjugates show sustained drug release for up to 264 h.

• 出版日期2016-6