Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)

Abstract

Background: High lipophilicity and poor aqueous solubility are the endemic problems of new drug molecules. Sixty to seventy percent of these drugs are unable to solubilize completely in aqueous media, or have very low permeability. This hampers their oral absorption and further leads to their poor bioavailability. Various researches are in progress to overcome these limitations. Novel technologies like nano-carrier systems have become popular for improving the solubility of drugs. Main body: Lipid-based formulations, among nano systems, are taking pace for the enhancement of solubility, oral absorption, and hence the bioavailability of drugs. Among the lipid formulations, self-emulsification systems are gaining popularity by offering various advantages to delivery systems. Self-emulsifying drug delivery systems (SEDDS) are isotropic blends of oil and surfactant/co-surfactants. These ingredients upon gentle agitation in aqueous media results in the formation of o/w emulsion. In spite of many works published in SEDDS, the major concerns of this article are to discuss the various approaches to formulate a good lipid-based carrier system for poorly aqueous soluble drugs, role of various polymers, and their categories used in the formulation along-with the modern technologies used for enhancing the stability of liquid SEDDS. This review majorly focuses upon the problems related to the poor aqueous solubility of the newer lipid molecules and the solutions to overcome their solubility and in addition bioavailability. Conclusion:As per the researches done in formulation and optimization of SEDDS for the enhancement of bioavailability of lipophilic molecules, it can be stated that the aqueous solubility as well as bioavailability can be increased by many folds compared to their marketed or other oral formulations.

Discovery, Synthesis, and Optimization of 1,2,4-Triazolyl Pyridines TargetingMycobacterium tuberculosis

“…Antitubercular drugs tend to be more lipophilic compared to other antimicrobials; 24 thus we were curious whether the trends in potency observed within the 3-thio-1,2,4-triazole series correlated to lipophilicity. We calculated the LogP values of all the analogs using the SwissADME online data 25, 26, 27 and plotted these values against IC 50 in Mtb . We observed that all compounds that were active against Mtb have cLogP values clustered between 3.1 and 6.5 (Figure 3).…”

Lipid-Based Drug Delivery System (LBDDS): An Emerging Paradigm to Enhance Oral Bioavailability of Poorly Soluble Drugs

“…Surfactant in the formulation plays a predominant role to increase the absorption of lipophilic drugs. Ethoxylated lipid surfactants such as Gelucire®, Labrasol® and Cre-mophor® had proved that they inhibit the P-GP modulated drug efflux [111][112][113]. The selection of surfactants is restricted since not very many are satisfactory for oral delivery.…”

In Silico Taste–Toxicity Study of New Hypothetical Hetero-Abiraterone Derivatives

“…Acceptable balance between lipid and water phases permits suitability of absorption, drug design and formulation. This required balance mainly depends upon chemical structure [16].…”