Lipid-Based Drug Carriers for Prodrugs to Enhance Drug Delivery
Journal Title: The AAPS Journal - Year 2015, Vol 17, Issue 1
Abstract
The combination of lipid drug delivery systems with prodrugs offers several advantages including improved pharmacokinetics, increased absorption, and facilitated targeting. Lipidization and use of lipid carriers can increase the pharmacological half-life of the drug, thus improving pharmacokinetics and allowing less frequent dosing. Lipids also offer advantages such as increased absorption through the intestines for oral drug absorption and to the CNS for brain delivery. Furthermore, the use of lipid delivery systems can enhance drug targeting. Endogenous proteins bind lipids in the blood and carry them to the liver to enable targeting of this organ. Drugs with significant side effects in the stomach can be specifically delivered to enterocytes by exploiting lipases for prodrug activation. Finally, lipids can be used to target the lymphatic system, thus bypassing the liver and avoiding first-pass metabolism. Lymphatic targeting is also important for antiviral drugs in the protection of B and T lymphocytes. In this review, both lipid-drug conjugates and lipid-based carriers will be discussed. An overview, including the chemistry and assembly of the systems, as well as examples from the clinic and in development, will be provided.
Authors and Affiliations
Jennica L. Zaro
Keywords
Related Articles
- EP ID EP680894
- DOI 10.1208/s12248-014-9670-z
- Views 51
- Downloads 0
Delivery of antibiotics to the eye using a positively charged polysaccharide as vehicle
The positively charged polysaccharide chitosan is able to increase precorneal residence time of ophthalmic formulations containing active compounds when compared with simple aqueous solutions. The purpose of the study wa...
Translational Pharmacokinetic-Pharmacodynamic Modeling from Nonclinical to Clinical Development: A Case Study of Anticancer Drug, Crizotinib
The online version of this article (doi:10.1208/s12248-012-9436-4) contains supplementary material, which is available to authorized users.
Population analysis of the pharmacokinetics and pharmacodynamics of RWJ-270201 (BCX-1812) in treating experimental influenza A and B virus in healthy volunteers
Our objective was to assess the pharmacokinetics and pharmacodynamics of RWJ-270201 (BCX-1812), an oral neuraminidase inibitor for the treatment of influenza A and B virus in healthy volunteers.
A Simplified PBPK Modeling Approach for Prediction of Pharmacokinetics of Four Primarily Renally Excreted and CYP3A Metabolized Compounds During Pregnancy
The online version of this article (doi:10.1208/s12248-013-9505-3) contains supplementary material, which is available to authorized users.
Mechanistic Models Describing Active Renal Reabsorption and Secretion: A Simulation-Based Study
The online version of this article (doi:10.1208/s12248-012-9437-3) contains supplementary material, which is available to authorized users.