Recent trends of self-emulsifying drug delivery system for enhancing the oral bioavailability of poorly water-soluble drugs

Tran, Phuong Ha-Lien; Park, Jeong Sook

doi:10.1007/s40005-021-00516-0

Cited by 35 publications

(20 citation statements)

References 135 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Based on these results, lidocaine was dissolved in an ointment in an amorphous form. The amorphous form generally has higher solubility and bioavailability than those of the crystalline form [ 53 , 54 ]. Therefore, the amorphous form is expected to improve bioavailability by enhancing skin permeability.…”

Section: Discussionmentioning

confidence: 99%

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

et al. 2021

View full text Add to dashboard Cite

Lidocaine, a commonly used local anesthetic, has recently been developed into a number of ointment products to treat hemorrhoids. This study examined its efficient delivery to the dermis through the pharmaceutical improvement of hemorrhoid treatment ointments. We attempted to increase the amount of skin deposition of lidocaine by forming a nanoemulsion through the self-nanoemulsifying effect that occurs when glycerol monostearate (GMS) is saturated with water. Using Raman mapping, the depth of penetration of lidocaine was visualized and confirmed, and the local anesthetic effect was evaluated via an in vivo tail-flick test. Evaluation of the physicochemical properties confirmed that lidocaine was amorphous and evenly dispersed in the ointment. The in vitro dissolution test confirmed that the nanoemulsifying effect of GMS accelerated the release of the drug from the ointment. At a specific concentration of GMS, lidocaine penetrated deeper into the dermis; the in vitro permeation test showed similar results. When compared with reference product A in the tail-flick test, the L5 and L6 compounds containing GMS had a significantly higher anesthetic effect. Altogether, the self-nanoemulsifying effect of GMS accelerated the release of lidocaine from the ointment. The compound with 5% GMS, the lowest concentration that saturated the dermis, was deemed most appropriate.

show abstract

Section: Discussionmentioning

confidence: 99%

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

et al. 2021

View full text Add to dashboard Cite

show abstract

“…In addition to greatly improving the water solubility, physicochemical stability, and oral bioavailability of lipophilic compounds, SEDDSs are thermodynamically stable and easily produced (Betageri 2019;Singh et al 2020). The production of SEDDSs relies on spontaneous emulsification, using oil, surfactants, and solvents, but it differs from conventional emulsification (Tran and Park 2021). The preparation of SEDDSs is carried out initially making a isotropic mixture of oil and surfactant at a gentle agitation followed by dilution within an aqueous phase, whereas in conventional emulsification all components are mixture at once to form an emulsion (Tran and Park 2021;Zhao et al 2020).…”

Section: Introductionmentioning

confidence: 99%

Promising self-emulsifying drug delivery system loaded with lycopene from red guava (Psidium guajava L.): in vivo toxicity, biodistribution and cytotoxicity on DU-145 prostate cancer cells

et al. 2021

View full text Add to dashboard Cite

Background Self-emulsifying drug delivery systems (SEDDSs) have attracted attention because of their effects on solubility and bioavailability of lipophilic compounds. Herein, a SEDDS loaded with lycopene purified from red guava (nanoLPG) was produced. The nanoemulsion was characterized using dynamic light scattering (DLS), zeta potential measurement, nanoparticle tracking analysis (NTA), transmission electron microscopy (TEM), Fourier-transform infrared spectroscopy (FTIR), lycopene content quantification, radical scavenging activity and colloidal stability in cell culture medium. Then, in vivo toxicity and tissue distribution in orally treated mice and cytotoxicity on human prostate carcinoma cells (DU-145) and human peripheral blood mononuclear cells (PBMC) were evaluated. Results NanoLPG exhibited physicochemical properties with a size around 200 nm, negative zeta-potential, and spherical morphology. The size, polydispersity index, and zeta potential parameters suffered insignificant alterations during the 12 month storage at 5 °C, which were associated with lycopene stability at 5 °C for 10 months. The nanoemulsion showed partial aggregation in cell culture medium at 37 °C after 24 h. NanoLPG at 0.10 mg/mL exhibited radical scavenging activity equivalent to 0.043 ± 0.002 mg Trolox/mL. The in vivo studies did not reveal any significant changes in clinical, behavioral, hematological, biochemical, and histopathological parameters in mice orally treated with nanoLPG at 10 mg/kg for 28 days. In addition, nanoLPG successfully delivered lycopene to the liver, kidney and prostate in mice, improved its cytotoxicity against DU-145 prostate cancer cells—probably by pathway independent on classical necrosis and apoptosis—and did not affect PBMC viability. Conclusions Thus, nanoLPG stands as a promising and biosafe lycopene delivery system for further development of nanotechnology-based health products. Graphical Abstract

show abstract

“…By enhancing the permeability of phospholipid membranes, Tween 80 improves skin penetration for transdermal drug delivery [ 35 , 36 ]. Tween 80 is also known to improve the bioavailability of a drug after oral administration [ 37 , 38 , 39 , 40 ]. Tween 80 may modulate the intestinal membrane permeability leading to improved oral bioavailability [ 40 ].…”

Section: Resultsmentioning

confidence: 99%

“…Tween 80 may modulate the intestinal membrane permeability leading to improved oral bioavailability [ 40 ]. Studies have indicated that Tween 80 may inhibit efflux transporters such as P-glycoprotein (P-gp), multidrug resistance-associated protein (MRP2), and breast cancer resistance protein (BCRP) and improve oral absorption [ 38 , 39 , 41 ]. The low oral bioavailability of nafamostat is likely due to its high polarity, which would limit gastrointestinal permeability.…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetics of Nafamostat, a Potent Serine Protease Inhibitor, by a Novel LC-MS/MS Analysis

Kim

et al. 2022

Molecules

View full text Add to dashboard Cite

Nafamostat, a synthetic serine protease inhibitor, has been used for the treatment of inflammatory diseases such as pancreatitis. Recently, an increasing number of studies have shown the promising antiviral effects of nafamostat for the treatment of coronavirus disease-19 (COVID-19). This study aimed to develop a novel liquid chromatography–tandem mass spectrometry (LC-MS/MS) analysis and to characterize the pharmacokinetics of nafamostat in rats. Nafamostat in the rat plasma was extracted by solid phase extraction, and 13C6-nafamostat was used as an internal standard. The quantification limit of nafamostat in the rat plasma was 0.5 ng/mL. The LC-MS/MS method was fully validated and applied to characterize the pharmacokinetics of nafamostat in rats. Following intravenous injection (2 mg/kg), nafamostat in the plasma showed a multiexponential decline with an average elimination half-life (t1/2) of 1.39 h. Following oral administration of nafamostat solutions (20 mg/kg) in 10% dimethyl sulfoxide (DMSO) and in 10% DMSO with 10% Tween 80, nafamostat was rapidly absorbed, and the average oral bioavailability was 0.95% and 1.59%, respectively. The LC-MS/MS method and the pharmacokinetic information of nafamostat could be helpful for the further preclinical and clinical studies of nafamostat.

show abstract

Recent trends of self-emulsifying drug delivery system for enhancing the oral bioavailability of poorly water-soluble drugs

Cited by 35 publications

References 135 publications

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

Promising self-emulsifying drug delivery system loaded with lycopene from red guava (Psidium guajava L.): in vivo toxicity, biodistribution and cytotoxicity on DU-145 prostate cancer cells

Pharmacokinetics of Nafamostat, a Potent Serine Protease Inhibitor, by a Novel LC-MS/MS Analysis

Contact Info

Product

Resources

About