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AssigneesThe Johns Hopkins University, Kennedy Krieger Institute, Inc.
InventorsTao Yu, Kannie W. Y. Chan, Ming Yang, Michael T. McMahon, Justin Hanes
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Liposome-based mucus-penetrating particles (MPP) capable of loading hydrophilic agents including therapeutic, prophylactic and diagnostic agents such as the diaCEST MRI contrast agent barbituric acid (BA) were evaluated to determine how to optimize delivery. Polyethylene glycol (PEG)-coated liposomes containing ≧7 mol % PEG diffused only approximately 10-fold slower in human cervicovaginal mucus (CVM) compared to their theoretical speeds in water. 7 mol %-PEG liposomes provided improved vaginal distribution compared to 0 and 3 mol %-PEG liposomes.
A liposomal formulation, the liposome consisting of surface modified liposomes having a diameter of less than one micron, having enhanced mucosal penetration relative to liposomes that are not surface modified, having a molar ratio between surface modified lipid to non-surface modified lipid equivalent to between 3 and 11 mol % PEGylated liposomes to non-PEGylated liposomes.
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