The physical and chemical interactions with vancomycin (VAN) were accessed between graphene oxide (GO) and crumpled graphene oxide (CGO) to present the possible loading and release mechanisms. The improved hydrophilicity and surface charge were found on CGO through water contact angle and ζ-potential measurements. Fourier transform infrared and X-ray photoelectron spectroscopies confirmed the attachment of VAN onto CGO or GO through π–π stacking and hydrogen bonding. Both CGO–VAN and GO–VAN drug complexes showed pH-controlled release property. The high VAN loading and delayed release in CGO–VAN system were mainly due to the crumpled morphology.
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