Perspective and potential of oral lipid-based delivery to optimize pharmacological therapies against cardiovascular diseases.
Cardiovascular diseases (CVDs) remain the major cause of morbidity and mortality globally. Despite the large number of cardiovascular drugs available for pharmacological therapies, factors limiting the efficient oral use are identified, including low water solubility, pre-systemic metabolism, food intake effects and short half-life. Numerous in vivo proof-of-concepts studies are presented to highlight the viability of lipid-based delivery to optimize the oral delivery of cardiovascular drugs. In particular, the key performance enhancement roles of oral lipid-based drug delivery systems (LBDDSs) are identified, which include i) improving the oral bioavailability, ii) sustaining/controlling drug release, iii) improving drug stability, iv) reducing food intake effect, v) targeting to injured sites, and vi) potential for combination therapy. Mechanisms involved in achieving these features, range of applicability, and limits of available systems are detailed. Future research and development efforts to address these issues are discussed, which is of significant value in directing future research work in fostering translation of lipid-based formulations into clinical applications to reduce the prevalence of CVDs.
Ian Wark Research Institute, University of South Australia, Mawson Lakes Campus, Mawson Lakes, SA 5095, Australia.
Shasha
S
Rao
Ian Wark Research Institute, University of South Australia, Mawson Lakes Campus, Mawson Lakes, SA 5095, Australia.
Angel
A
Tan
Ian Wark Research Institute, University of South Australia, Mawson Lakes Campus, Mawson Lakes, SA 5095, Australia.
Nicky
N
Thomas
Ian Wark Research Institute, University of South Australia, Mawson Lakes Campus, Mawson Lakes, SA 5095, Australia,. Electronic address: clive.prestidge@unisa.edu.au.
Clive A
CA
Prestidge
D000284:Administration, Oral; D001682:Biological Availability; D002317:Cardiovascular Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000378:metabolism; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000639:trends; D004355:Drug Stability; D004655:Emulsions; D018565:Food-Drug Interactions; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D012996:Solutions; D013535:Suspensions
D002317:Cardiovascular Agents; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D012996:Solutions; D013535:Suspensions
Cardiovascular disease; Combined therapy; Controlled drug release; Lipid-based drug delivery; Oral bioavailability; Targeted delivery