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Abstract

The design of FA-PEO-Chol-coated liposomes resulted in a dramatic increase in the oral delivery of a moderate-size glycopeptide in the rat compared with uncoated liposomes or oral solution. It is speculated that the cause of the observed effect was due to binding of liposome-surface folic acid to receptors in the GI tract with subsequent receptor-mediated endocytosis of entrapped vancomycin by enterocytes.

Surface modification of monodisperse magnetite nanoparticles for improved intracellular uptake to breast cancer cells

“…The PEG-coated nanoparticles remained monodisperse as shown in the AFM image under height mode, and PEG was coated on the individual nanoparticles to form a core-shell structure as shown in the AFM image under phase mode. For PEG-FA coated nanoparticles, although some efforts have been performed to attach PEG-FA conjugate to polymer nanoparticles through chemical bonding [10][11][12][13], the protocols that have been developed so far are far from perfect. Those protocols are mainly based on the reaction between amino and carboxyl groups to form amide bonds, and the main drawback is that the reaction will definitely cause self-crosslinking of FA, which has both amino and carboxyl groups in its molecular structure.…”

Development and Stability Studies of Novel Liposomal Vancomycin Formulations

“…A change in amount of vancomycin to be encapsulated from 50 mg to 100 mg did not cause any appreciable change in the final encapsulation efficiency. To further improve the encapsulation efficiency of vancomycin, a modified dehydration-rehydration method [24] was used. In this method, a suspension of empty liposomes is lyophilized.…”

“…Due to poor encapsulation efficiency and poor stability of the prepared formulations using the above methods, it was decided to prepare subsequent formulations using a modified dehydration-rehydration method [24]. Both the conventional and PEGylated vancomycin liposomal formulations were prepared using the lipids DSPC, cholesterol, and MPEG-2000-DSPE in 3 : 1 : 0 and 3 : 1 : 0.02 molar ratios, respectively.…”

Current status of selected oral peptide technologies in advanced preclinical development and in clinical trials

“…Vancocin ® HCl is not well absorbed orally due to its large MW and hydrophilicity and is only licensed by that route to treat a single colonic condition, pseudomembranous colitis [57], and there have been few efforts to create other oral vancomycin formulations [58]. This is because of the narrow range of conditions that can be treated by local delivery and also because systemic delivery from an oral formulation cannot compete with i.v.…”