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

Abstract

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.

Modification with Conventional Surfactants to Improve a Lipid-Based Ionic-Liquid-Associated Transcutaneous Anticancer Vaccine

“…The HLB value represents the surfactant’s propensity to incorporate in water or oil and form an emulsion. Surfactants with low HLB values tend to be more soluble in oil, whereas those with high HLB numbers tend to be more soluble in water [ 37 , 38 ]. Those properties of nonionic surfactants allowed them to load higher amounts of drug than ionic surfactants ( Table S1 ).…”

“…Compared with surfactant-free formulations, all nonionic surfactants showed significantly increased ( p < 0.001) drug-loading capacity, whereas ionic surfactants had no such effect. Nonionic surfactants have varying HLB values (e.g., S-20 = 8.6, S-80 = 4.3, T-20 = 16.72, T-80 = 15, Brij-35 = 16.9, squalene = 8.4, PEG = 20), and a reasonable range for emulsification is between 3.6 and 8.0 [ 33 , 37 , 38 ]. Due to S-20’s HLB being in a good range (HLB = 8.6) for emulsification formulations, which enabled S-20 to develop more sustainable formulations, as well as the possibility that S-20 has a potentially better drug-loading capacity compared to Tween and other surfactants.…”

“…Due to S-20’s HLB being in a good range (HLB = 8.6) for emulsification formulations, which enabled S-20 to develop more sustainable formulations, as well as the possibility that S-20 has a potentially better drug-loading capacity compared to Tween and other surfactants. ( Figure 2 A) [ 38 ]. However, it is currently challenging to adequately describe how LBILs may affect pharmaceutical formulations, because the HBL values of LBILs have not yet been studied.…”

The anti‐inflammatory activity of flavonoids and alkaloids from Sophora flavescens alleviates psoriasiform lesions: Prenylation and methoxylation beneficially enhance bioactivity and skin targeting

“…These chemicals exert a wide spectrum of bioactivities against cancer cells, viruses, bacteria, and inflammation (J. J. Li et al, 2020). The oral bioavailability of flavonoids and alkaloids is generally low due to their poor solubility and extensive first‐pass metabolism (Ameta et al, 2023; Zhao et al, 2019). However, topical delivery of flavonoids and alkaloids represents a simple, efficient way to treat psoriatic skin lesions.…”

Effect of water supplementation of Magic oil at different growing periods on growth performance, carcass traits, blood biochemistry, and ileal histomorphology of broiler chickens

“…Essential oils need to be nano formulated with a small droplet size (20-500 nm) to avoid evaporation and maintain biological function by enhancing cellular uptake and bioavailability of numerous hydrophobic drugs. This results in increasing their solubility, physical stability, and dissolution rate, and bioavailability ( Salman et al, 2021 ; Singh et al, 2021 ; Ameta et al, 2023 ).…”