Polymer-lipid hybrid systems: merging the benefits of polymeric and lipid-based nanocarriers to improve oral drug delivery

ABSTRACT

Introduction: A number of biobarriers limit efficient oral drug absorption; both polymer-based and lipid-based nanocarriers have demonstrated properties and delivery mechanisms to overcome these biobarriers in preclinical settings. Moreover, in order to address the multifaceted oral drug delivery challenges, polymer-lipid hybrid systems are now being designed to merge the beneficial features of both polymeric and lipid-based nanocarriers.

Areas covered: Recent advances in the development of polymer-lipid hybrids with a specific focus on their viability in oral delivery are reviewed. Three classes of polymer-lipid hybrids have been identified, i.e. lipid-core polymer-shell systems, polymer-core lipid-shell systems, and matrix-type polymer-lipid hybrids. We focus on their application to overcome the various biological barriers to oral drug absorption, as exemplified by selected preclinical studies.

Expert opinion: Numerous studies have demonstrated the superiority of polymer-lipid hybrid systems to their non-hybrid counterparts in providing improved drug encapsulation, modulated drug release, and improved cellular uptake. These features have encouraged their applications in the delivery of chemotherapeutics, proteins, peptides, and vaccines. With further research expected to optimize the manufacturing and scaling up processes and in-depth pre-clinical pharmacological and toxicological assessments, these multifaceted drug delivery systems will have significant clinical impact on the oral delivery of pharmaceuticals and biopharmaceuticals.

KEYWORDS:

• Bioavailability
• mucus and mucosal barriers
• oral drug delivery
• polymer-lipid hybrid
• proteins and peptides
• vaccine

Article highlights

• The plethora of polymer-lipid hybrid systems with diverse nanoarchitectures and developed for oral application are summarized and divided into three sub-categories based on structure.

• Specific polymer-lipid hybrid systems are identified that have been designed to overcome the major oral delivery barriers.

• Advantages of polymer-lipid hybrid systems over their non-hybrid polymeric or lipid-based counterparts are demonstrated.

• Oral delivery applications for polymer-lipid hybrid systems include hydrophobic compounds, poorly permeable small molecules, proteins, peptides and vaccines.

• Advantages and disadvantages of various polymer-lipid hybrid oral delivery systems are identified.

Declaration of interest

The authors were supported by The Australian Research Council (Discovery grant scheme, DP120101065), ITEK Pty. Ltd., and the Australian Biotech Ceridia Pty. Ltd. are greatly acknowledged for research funding and support. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.