An update on polymer-lipid hybrid systems for improving oral drug delivery

ABSTRACT

Introduction: A promising approach that has recently emerged to overcome the complex biobarriers and interrelated challenges associated with oral drug absorption is to combine the benefits of polymeric and lipid-based nanocarriers within one hybrid system. This multifaceted formulation strategy has given rise to a plethora of polymer-lipid hybrid (PLH) systems with varying nanostructures and biological activities, all of which have demonstrated the ability to improve the biopharmaceutical performance of a wide range of challenging therapeutics.

Areas covered: The multitude of polymers that can be combined with lipids to exert a synergistic effect for oral drug delivery have been identified, reviewed and critically evaluated. Specific focus is attributed to preclinical studies performed within the past 5 years that have elucidated the role and mechanism of the polymer phase in altering the oral absorption of encapsulated therapeutics.

Expert opinion: The potential of PLH systems has been clearly identified; however, improved understanding of the structure–activity relationship between PLH systems and oral absorption is fundamental for translating this promising delivery approach into a clinically relevant formulation. Advancing research within this field to identify optimal polymer, lipid combinations and engineering conditions for specific therapeutics are therefore encouraged.

KEYWORDS:

• Polymer-lipid hybrid
• oral drug delivery
• bioavailability
• poorly soluble drugs
• proteins and peptides
• vaccine
• lipid-based formulations
• polymeric nanoparticles
• nanocarriers

Article highlights

• The array of natural, semi-synthetic and synthetic polymers that can be combined with lipid drug delivery systems for improved biopharmaceutical performance are summarized and critically evaluated.

• The versatility of polymer-lipid hybrid systems with regards to structure, composition, and oral drug delivery properties/applications is demonstrated.

• The biopharmaceutical advantages offered by combining polymer and lipid systems are identified and discussed in detail, which include: improved gastrointestinal stability, promotion of mucosa interactions and enhanced solubilization.

• Opportunities and challenges for the translation of polymer-lipid hybrid systems into clinically and commercially relevant formulations are highlighted.

This box summarizes the key points contained in the article.

Declaration of interest

The authors have no 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. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was funded by the Australian Research Council’s Centre of Excellence in Convergent Bio-Nano Science and Technology (ARC CE140100036), the ÅForsk Foundation (16-463) and UniSA Ventures.