Self-aggregation and the hemolytic effect limit the application of γ-cyclodextrin (γ-CD) in bioactive molecular delivery systems. In this study, γ-CD was modified by grafting onto bovine serum albumin protein (BSA), with epichlorohydrin (ECH) acting as the cross-linking agent. The effects of BSA concentration, reaction temperature, pH and time on the grafting rate were studied, and the γ-CD-BSA complex with a grafting rate of 99.5 ± 0.1% ± 0.06 ) % was achieved. The complex was confirmed using 1 H NMR and FT-IR spectra. Compared with γ-CD, the hemolytic effect and self-aggregation of γ-CD-BSA were significantly reduced, and the encapsulation efficiency of curcumin was increased by 10.8%. The results of scanning electron microscopy showed that both γ-CD and γ-CD-BSA nanoparticles were formed and the structure of the γ-CD-BSA complex was more uniform. The pH stability and salt stability of γ-CD-BSA were higher than γ-CD. The release rate of γ-CD-BSA was 15.2 ± 0.2% after 2 h at pH 1.2, and 57 ± 1% after 4 h at pH 7.2. The γ-CD-BSA nanoparticles could protect curcumin in acidic environments and release it in neutral environments. The results suggested a promising wall material for delivery of hydrophobic substances.
Jinguo Qiu,Mhd Anas Tomeh,Yi Jin,Bo Zhang,Xiubo Zhao
Anticancer peptides (ACPs) are promising antitumor drugs owning to their great cancer cell targeting and anticancer effects as well as low drug resistance. However, many of the ACPs have non-specific toxicity and can be easily degraded by the enzymes after administration. Therefore, drug delivery systems (DDSs) are required to shield these peptides from degradation and induce targeted delivery. In this paper, a high performance microfluidic device was used to fabricate the zeolitic imidazolate framework (ZIF-8) encapsulating an ACP (At3) recently developed by our group. The microfluidic device allowed for efficient and rapid mixing to generate ACP loaded nanoparticles (NPs) with controllable properties at high production rate (120 mL/min) and high encapsulation efficiency. The ZIF-8 NPs synthesised by microfluidic processing showed lower polydispersity index (PDI) than the conventional method, demonstrating an improved size uniformity. Encapsulating At3 into the ZIF-8 ( [email protected] ) significantly reduced the hemolytic effect and provided a pH-controlled release of At3 peptide. [email protected] showed higher anticancer effect than the unloaded peptide at the same concentration due to the enhanced cell uptake by the ZIF-8 NPs. The NPs were able to inhibit the growth of the multicellular tumour spheroids (MCTSs) and damage the mitochondrial membrane of the MCF-7 breast cancer cells. In vivo experiments demonstrated that the [email protected] NPs inhibited the growth of MCF-7 tumours in nude mice without changing the biochemical properties of the blood or the histopathological properties of vital organs. Therefore, the development of At3 loaded NPs provides an alternative approach in ACP delivery which can broaden the application of ACP-based cancer therapy.
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