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Berberine chloride was immobilized into MgAl LDH by ion-exchange and co-precipitation methods.The two methods favor different adsorption efficiency with slightly different physico-chemical properties.Berberine chloride-MgAl LDH biohybrids have the potential to be used as a controlled release formulation.Anti-bacterial assay for berberine chloride-MgAl indicates the efficacy of biohybrid as an efficient drug carrier.Hydrotalcite (HT), also known as a layered double hydroxide (LDH) compound, has been widely used in past years in the formulation of drugs due to its specific properties including good biocompatibility, null toxicity, high chemical stability and pH-dependent solubility which aid in drug controlled release. In this work, berberine chloride (BBC) class antibacterial agent was immobilized into magnesium-aluminum LDH in order to improve the drug efficiency as well as to achieve the controlled release property. BBC molecules were immobilized into MgAl LDH through a conventional ion exchange reaction and co-precipitation method. The ion-exchange experiments of BBC on MgAl LDH were investigated with particular attention paid to the influence of the layer charge, the nature of the intercalated anion and the morphology. The immobilization efficiency was dependent upon the LDH properties and the immobilization process. Characterization by powder x-ray diffraction, Fourier transform infrared spectroscopy, scanning electron microscopy and contact angle measurements revealed that the interaction of BBC with MgAl LDH occurs by adsorption rather than intercalation of BBC within LDH layers. In vitro anti-bacterial tests were carried out using disc diffusion assay to prove the effectiveness of these novel biohybrid beads as a controlled drug delivery method. Consequently, the BBC-LDH co-precipitated formulation revealed an enhanced anti-bacterial activity compared to the ion-exchanged formulation not only due to an improvement of chemical stability and retained amount of BBC molecules but also due to the release property.