Utilization of nanoemulsions to enhance bioactivity of pharmaceuticals, supplements, and nutraceuticals: Nanoemulsion delivery systems and nanoemulsion excipient systems

ABSTRACT

Introduction: The efficacy of many hydrophobic bioactives (pharmaceuticals, supplements, and nutraceuticals) is limited due to their relatively low or highly variable bioavailability. Nanoemulsions consisting of small lipid droplets (r < 100 nm) dispersed in water can be designed to improve bioavailability.

Areas covered: The major factors limiting the oral bioavailability of hydrophobic bioactive agents are highlighted: bioaccessibility, absorption and transformation. Two nanoemulsion-based approaches to control these processes and improve bioavailability are discussed: nanoemulsion delivery systems (NDS) and nanoemulsion excipient systems (NES). In NDS, hydrophobic bioactives are dissolved within the lipid phase of oil-in-water nanoemulsions. In NES, the bioactives are present within a conventional drug, supplement, or food, which is consumed with an oil-in-water nanoemulsion. Examples of NDS and NES utilization to improve bioactive bioavailability are given.

Expert opinion: Considerable progress has been made in nanoemulsion design, fabrication, and testing. This knowledge facilitates the design of new formulations to improve the bioavailability of pharmaceuticals, supplements, and nutraceuticals. NDS and NES must be carefully designed based on the major factors limiting the bioavailability of specific bioactives. Research is still required to ensure these systems are commercially viable, and to demonstrate their safety and efficacy using animal and human feeding studies.

KEYWORDS:

• Bioavailability
• delivery systems
• emulsions
• excipients
• nanoemulsions
• nutraceuticals

Article highlights

• Nanoemulsions can be designed to increase the bioavailability of lipophilic bioactive components in pharmaceuticals, supplements, and foods.

• NDS are designed to encapsulate lipophilic bioactive components within the interior of tiny lipid droplets.

• NES may contain no bioactive components themselves, but they are designed to improve the bioavailability of any lipophilic bioactive components present in pharmaceuticals, supplements, and foods ingested with them.

• NDS and NES can be designed to improve the bioavailability of lipophilic bioactives by creating compositions and structures within the GIT that alter the bioaccessibility, absorption, or stability of the bioactives.

• There is an opportunity to develop a new class of commercial products based on nanoemulsions that can be specifically designed to improve the efficacy of certain types of poorly soluble bioactive components.

This box summarizes key points contained in the article.

Declaration of interest

This material was partly based upon work supported by USDA-NRI Grants (2013-03795). This paper was also partly funded by the Deanship of Scientific Research (DSR), King Abdulaziz University, Jeddah, under grant no. G-299-130-1435-DSR. The authors, therefore, acknowledge with thanks DSR technical and financial 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.