Formulation and Characterization of Bone-Targeting Vancomycin-Loaded Liposomes

<b>Background:</b> We report the successful formulation of a bone-targeted vancomycin-loaded liposomal carrier. <b>Method:</b> The basic liposomal structure is composed of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol, and dicetyl phosphate (DCP) in a molar r...

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Bibliographic Details
Main Authors: Basel Karzoun, Wala’a Albenayan, Shilpa Raut, Eman Atef
Format: Article
Language:English
Published: MDPI AG 2025-06-01
Series:Pharmaceutics
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Online Access:https://www.mdpi.com/1999-4923/17/6/792
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Summary:<b>Background:</b> We report the successful formulation of a bone-targeted vancomycin-loaded liposomal carrier. <b>Method:</b> The basic liposomal structure is composed of 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol, and dicetyl phosphate (DCP) in a molar ratio of 3:1:0.25, respectively. The dehydration–rehydration method was used to maximize the liposomal-encapsulation efficiency of vancomycin after the initial preparation using thin-film hydration. <b>Results:</b> Sodium alendronate was used as a targeting moiety and was successfully conjugated to DSPE–PEG–COOH via carbodiimide chemistry, as was confirmed using IR spectroscopy. The resulting conjugate, DSPE–PEG-alendronate, was subsequently used in the formulation of bone-targeting vancomycin-loaded liposomes. In vitro binding assays with hydroxyapatite demonstrated preferential binding of the surface-modified liposomes to hydroxyapatite crystals. Furthermore, ex vivo studies revealed that the surface-modified liposomes exhibited enhanced binding affinity to the tibial bone tissue of 4-week-old male CD1 mice, in comparison to unmodified liposomes. <b>Conclusions:</b> The successfully formulated surface-modified vancomycin loaded liposomes showed enhanced bone affinity with a great potential for targeting the antibiotic to infected bones.
ISSN:1999-4923