Solid lipid matrix mediated nanoarchitectonics for improved oral bioavailability of drugs

ABSTRACT

Introduction: Solid matrix mediated lipid nanoparticle formulations (LNFs) retain some of the best features of ideal drug carriers necessary for improving the oral absorption and bioavailability (BA) of both hydrophilic and hydrophobic drugs. LNFs with solid matrices may be typically categorized into three major types of formulations, viz., solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and lipid–drug conjugate nanoparticles (LDC-NPs). Solid matrix based LNFs are, potentially, the most appropriate delivery systems for poorly water soluble drugs in need of improved drug solubility, permeability, absorption, or increased oral BA. In addition, LNFs as matrices are able to encapsulate both hydrophobic and hydrophilic drugs in a single matrix based on their excellent ability to form cores and shells. Interestingly, LNFs also act as delivery devices to impart chemical stability to various orally administered drugs.

Areas covered: Aim of the review is to forecast the presentation of pharmacokinetic characteristics of solid lipid matrix based nanocarriers which are typically biocompatible, biodegradable and non-toxic carrier systems for efficient oral delivery of various drugs. Efficient delivery is broadly mediated by the fact that lipophilic drugs are readily soluble in lipidic substrates that are capable of permeating across the gut epithelium following oral administration, subsequently delivering the moiety of interest more efficiently across the gut mucosal membrane. This enhances the overall BA of many drugs facing oral delivery challenges by improving their pharmacokinetic profile. This article specifically focuses on the biopharmaceutical and pharmacokinetic aspects of such solid lipid matrix based nanoformulations and possible mechanisms for better drug absorption and improved BA following oral administration. It also briefly reviews methods to access the efficacy of LNFs for improving oral BA of drugs, regulatory aspects and some interesting lipid-derived commercial formulations, with a concluding remark.

Expert opinion: LNFs enhance the overall BA of many drugs facing oral delivery challenges by improving their pharmacokinetic profile.

KEYWORDS:

• Lipid nanoparticle formulations
• absorption
• pharmacokinetic
• oral delivery
• improved bioavailability

Article Highlights

• Solid lipid matrix-based nanoparticle formulations have recently emerged as potential drug carriers to improve drug absorption and bioavailability of many hydrophilic and hydrophobic drugs.

• LNFs act as a matrix to encapsulate not only hydrophobic drugs but also to entrap hydrophilic moieties as well in a single matrix system.

• LNFs as a delivery device to impart chemical stability of drug followed by improved oral BA.

• Solid matrix-based LNFs are the most appropriate delivery systems for poorly water-soluble drugs to improve their solubility, permeability, and absorption, eventually leading to increased oral bioavailability.

• Such lipid-based nanocarrier systems are biocompatible, biodegradable, non-toxic and physiologically compatible moieties for efficient oral delivery. This is due to the fact that lipophilic drugs are readily soluble in lipidic substrates and therefore capable to permeating across the gut epithelium. deliver the moiety of interest more significantly across the mucosal membrane via oral route.

• This overall enhances the oral bioavailability of many drugs facing oral delivery challenges via improving their pharmacokinetic profile.

This box summarizes key points contained in the article.

Acknowledgments

The authors are thankful to their respective organizations for providing the necessary literature support and digital library facilities. Acknowledgment also goes to all the authors of papers, books, and websites and all other published sources listed in the references that were used to prepare the contents of this 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 work was funded by a start-up research grant [File No: YSS/2015/000966/LS] from the Science and Engineering Research Board (SERB), Ministry of Science and Technology, Government of India, New Delhi, India.