Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 65, Issue 10, Pages 1331-1339Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.addr.2012.07.012
Keywords
Drug delivery; Protein binding; Endogenous drug carriers; Albumin; Drug absorption; Drug formulation; Fatty acids; Triglycerides; Lipid prodrugs; Reversible lipidization
Categories
Funding
- NCI NIH HHS [R01 CA126825] Funding Source: Medline
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Many drugs have decreased therapeutic activity due to issues with absorption, distribution, metabolism and excretion. The co-formulation or covalent attachment of drugs with fatty acids has demonstrated some capacity to overcome these issues by improving intestinal permeability, slowing clearance and binding serum proteins for selective tissue uptake and metabolism. For orally administered drugs, albeit at low level of availability, the presence of fatty acids and triglycerides in the intestinal lumen may promote intestinal uptake of small hydrophilic molecules. Small lipophilic drugs or acylated hydrophilic drugs also show increased lymphatic uptake and enhanced passive diffusional uptake. Fatty acid conjugation of small and large proteins or peptides has exhibited protracted plasma half-lives, site-specific delivery and sustained release upon parenteral administration. These improvements are most likely due to associations with lipid-binding serum proteins, namely albumin, LDL and HDL These molecular interactions, although not fully characterized, could provide the ability of using the endogenous carrier systems for improving therapeutic outcomes. Published by Elsevier B.V.
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