Recent Advances in Improving the Bioavailability of Hydrophobic/Lipophilic Drugs and Their Delivery via Self-Emulsifying Formulations

Formulations based on emulsions for enhancing hydrophobic and lipophilic drug delivery and its bioavailability have attracted a lot of interest. As potential therapeutic agents, they are integrated with inert oils, emulsions, surfactant solubility, liposomes, etc.; drug delivering systems that use emulsion formations have emerged as a unique and commercially achievable accession to override the issue of less oral bioavailability in connection with hydrophobic and lipophilic drugs. As an ideal isotropic oil mixture of surfactants and co-solvents, it self-emulsifies and forms fine oil in water emulsions when acquainted with aqueous material. As droplets rapidly pass through the stomach, fine oil promotes the vast spread of the drug all over the GI (gastrointestinal tract) and conquers the slow disintegration commonly seen in solid drug forms. The current status of advancement in technologies for drug carrying has promulgated the expansion of innovative drug carriers for the controlled release of self-emulsifying pellets, tablets, capsules, microspheres, etc., which got a boost for drug delivery usage with self-emulsification. The present review article includes various kinds of formulations based on the size of particles and excipients utilized in emulsion formation for drug delivery mechanisms and the increase in the bioavailability of lipophilic/hydrophobic drugs in the present time.

1. Introduction

The improvements in combinatorial chemistry show an enormous rise in a variety of less water-soluble drugs. At least forty novel pharmacologically active lipophilic/hydrophobic moieties exhibit very low aqueous solubility. Nevertheless, a unique challenge regarding drugs is presented to pharmaceutical scientists: orally administrated drugs have innate low aqueous solubility, leading to inadequate oral bioavailability with higher inter- and intra-subject changeability and scarcity of dose proportionality [1]. Numerous formulation perspectives are currently being applied to handle challenges related to formulations of biopharmaceutical class system (BCS) drugs; this includes compound pre-dissolution in suitable solvents followed by capsule filing with this formulation [2], or as solid solution formulations that utilize water-soluble polymers [3]. Although these perspectives will help resolve the matter related to the primary dissolution of drug matter in a liquid phase inside the GI tract up to specific proportions, momentous restrictions such as the precipitation issue of drug molecules in the dispersal of formulations during the crystallization of drugs in the polymer-based matrix are still unsolved.
For the same reasons, assessment of physical stability is critical and has been evaluated using techniques such as X-ray crystallography or differential scanning calorimetry. Several formulation modes, such as carrier technology, provide an innovative methodology for enhancing solubility in drug molecules with low solubilities. Advancements in oral drug molecule bioavailability use lipid-based formulations that have now become attraction points. Perhaps the most adaptable excipient class members presently available are lipids, providing a strong eventuality as a formulator in improving and controlling the lipophilic drug’s absorption where ordinary formulation methods failed or when the drug molecule itself is an oil molecule (i.e., Dronabinol, ethyl icosapentate). In addition, with a low affinity for precipitation of lipophilic drugs in the GI tract during dilution, such formulations will favor partitioning kinetics in the lipid droplets to be retained [4].
The literature review indicates that the application of carrier technology is a perspective of scientific interest in lipid-based oral formulations and strengthens the ambidexterity in addressing the issues complementary to oral drug delivery of poorly soluble molecules [2,3,4,5,6]. Novel methods such as self-emulsification modes have also intensified the solubility of inadequately soluble drugs and have some advantages. The introduction of this self-emulsification concept and present-day advances in polymer science have led to application advancements with lipid-based self-emulsifying formulations in various drug delivery views comprising drug targeting. This article endeavors to review the far-reaching awareness of emulsion-forming drug delivery systems (DDS) for the bioavailability enhancement of hydrophobic/lipophilic drugs by cherishing numerous formulations. The present-day architectural innovations and the advancement of self-nano-emulsifying and self-micro-emulsifying formulations have also been considered. Thus, this review’s main focus is on improving the bioavailability or solubility of hydrophobic/lipophilic drugs via self-emulsifying formulations (SEF).


Excipients mentioned in this article beside others: Vitamin E TPGS

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Ameta, R.K.; Soni, K.; Bhattarai, A. Recent Advances in Improving the Bioavailability of Hydrophobic/Lipophilic Drugs and Their Delivery via Self-Emulsifying Formulations. Colloids Interfaces 2023, 7, 16.

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