Injectable Lipid Emulsions—Advancements, Opportunities and Challenges

Abstract

Injectable lipid emulsions, for decades, have been clinically used as an energy source for hospitalized patients by providing essential fatty acids and vitamins. Recent interest in utilizing lipid emulsions for delivering lipid soluble therapeutic agents, intravenously, has been continuously growing due to the biocompatible nature of the lipid-based delivery systems. Advancements in the area of novel lipids (olive oil and fish oil) have opened a new area for future clinical application of lipid-based injectable delivery systems that may provide a better safety profile over traditionally used long- and medium-chain triglycerides to critically ill patients. Formulation components and process parameters play critical role in the success of lipid injectable emulsions as drug delivery vehicles and hence need to be well integrated in the formulation development strategies. Physico-chemical properties of active therapeutic agents significantly impact pharmacokinetics and tissue disposition following intravenous administration of drug-containing lipid emulsion and hence need special attention while selecting such delivery vehicles. In summary, this review provides a broad overview of recent advancements in the field of novel lipids, opportunities for intravenous drug delivery, and challenges associated with injectable lipid emulsions.

The effect of phospholipid composition of reconstituted HDL on its cholesterol efflux and anti-inflammatory properties

“…The differences in lipid composition of various subclasses of HDL and how they relate to disease have been gaining attention in recent years (12)(13)(14). However, a single source of lipid is used for preparation of rHDL for most academic research and clinical development (2)(3)(4)(5)(15)(16)(17)(18). The fi rst lipid used to prepare rHDLs for human testing was soybean PC (soyPC), because this lipid was shown to be safe for parenteral nutrition products and is readily commercially available in infusion grade ( 18 ).…”

Nanoemulsions in Translational Research—Opportunities and Challenges in Targeted Cancer Therapy

“…Nanoemulsion is a heterogeneous system in which the oil phase is dispersed as droplets in an aqueous phase and stabilized by emulsifying agents (10,16). Emulsifying agents are amphiphilic surface-active molecules or surfactants that can reduce interfacial tension between two immiscible liquid phases of oil and water by preferentially adsorbing at their interfaces ( Fig.…”

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

“…Considering the formulation and physicochemical characteristics, nanoemulsions have been associated with a number of advantages such as a low surfactant concentration, a uniform and very small droplet size, low viscosity, and high solubilization capacity for lipophilic drugs. Additionally, the improved penetration through biological barriers, possible enhanced bioavailability and organ targeting could be expected with these systems [1][2][3][4][5][6]. Although lipid nanoemulsions have been traditionally employed for parenteral nutrition and intravenous delivery of lipophilic drugs -with several approved products on the market -the additional efforts are required to optimize nanoemulsion formulation, stability, and overall drug delivery [1,7].…”