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. 2020 Dec 9;12(12):1194. doi: 10.3390/pharmaceutics12121194

Table 3.

Examples of preclinical studies reporting enhanced dissolution and bio-availability of drugs upon their incorporation into SNEDDSs.

Class Drug Components In Vitro/Vivo Observation References
ANTI-CANCER Docetaxel Capryol® 90, Labrasol®, Transcutol® HP AUC0-t and Cmax increased 6.4 and 6.5-fold, respectively compared to docetaxel aqueous solution. [196]
Erlotinib Labrafil® M2125 CS, Labrasol®, Transcutol® HP, Aerosil® 200, Dextran 40 AUC0–t and Cmax increased 2.1 and 2.4-fold, respectively in case of dextran-based solid SEDDS compared to erlotinib powder. [197]
Paclitaxel Sesame oil, Labrasol®, Sodium deoxycholate AUC0–t and Cmax increased to 2.7 and 3.99-fold, respectively compared to drug suspension. [194]
Lycopene LCT, Tween® 85, Cremophor® RH, Gelucire® AUC0–t and Cmax increased 2.3 and 2.85-fold, respectively compared to Lycovit®. [198]
Methotrexate Ethyl oleate, Tween® 80, Propylene glycol AUC0–24 and Cmax increased 1.57 and 1.68-fold, respectively compared to native drug. [199]
Irinotecan Capmul® CM-C8, Cremophor® EL, Pluronic L-121 AUC0–t and Cmax increased 4.2 and 1.7-fold, respectively compared to drug suspension. [200]
CARDIOVASCULAR AND ANTI-HYPERTENSIVE Carvedilol Labrafil® M1944CS, Tween® 80, Transcutol® Relative bio-availability enhanced by 4.1 times compared with tablet. [201]
Felodipine Miglyol® 812, Cremophor® RH 40, Tween® 80, Transcutol® HP, Silicon dioxide AUC0–t increased 2-fold compared to conventional tablets. [202]
Clinidipine Capryol® 90, Tween® 80, Transcutol® The absorption of the drug was enhanced from liquid-SEDDS as 99 % of the drug was transported from mucosal to serosal side of the rat intestine within 90 min from SEDDS in comparison to only 42.2% from that of the pure drug suspension. [203]
Valsartan Triacetin or Castor oil, Tween® 80, PEG 600 For triacetin-SNEDDS 5 and 2.4-fold increase in Cmax and AUC, respectively; for castor oil SNEDDS 8 and 3.6-fold increase in Cmax and AUC, respectively. [204]
Rosuvastatin Peceol®, Tween® 80, Transcutol® HP In vivo pharmacokinetic studies revealed 1.8 and 5.7-fold enhancement in AUC0-t and Cmax, respectively, and 0.33-fold reduction in Tmax of drug from the SNEDDS vis-à-vis the pure drug suspension. [173]
Atenolol Tartaric acid, Captex®, Span® 80, Oleic acid Ex vivo intestinal permeability studies revealed that atenolol SDEDDS exhibited better drug permeation compared to atenolol or atenolol-tartaric acid suspension. [205]
Ramipril Sefsol, Tween® 80, Carbitol 2.29-fold improvement in oral bio-availability compared with free drug suspension. [104]
ANTI-DIABETIC Insulin Miglyol®, Cremophor® RH40, MCM C-10, Ethanol AUC0–t increased 2.7-fold compared to insulin solution. [206]
Glibenclamide Cotton oil, Tween® 80, Propylene glycol AUC0–t increased 1.4-fold compared to free drug. [207]
Trans-cinnamic acid Isopropyl myristate, Cremophor® EL, PEG 400 The efficacy of trans-cinnamic acid in both hyperglycemia and glucolipid metabolic disorder was enhanced in SNEDDS compared to the drug suspension. [208]
Gliclazide Capryol® 90, Cremophor® EL, Akoline® MCM Enhancement in oral bio-availability as compared to the free drug. [209]
Exenatide Cremophor® EL, Labrafil® 1944, Capmul®-PG 8, propylene glycol 14.6-fold higher relative bio-availability versus subcutaneous exenatide solution. [210]
ANTIOXIDANT Quercetin Capmul®, Tween® 20, Ethanol 23.7-fold increase in the cell uptake of quercetin when incorporated in SEDDS compared to free drug. [211]
Resveratrol Miglyol® 812, Montanox, Labrasol®, Gelucire®, Ethanol The absorptive fluxes through the intestinal epithelium from the nano-emulsions were significantly increased compared to an ethanolic control solution. [212]
Genistein Labrafac® lipophile 1349, Maisine®-35, Cremophor® EL, Labrasol®, Transcutol® 95% of drug release in 5 min. [213]
Retinol acetate Soybean oil, Capmul®, Cremophor® EL Improved in dissolution rate. [214]
Coenzyme Q10 Lauroglycol® FCC, Witepsol® H335, Solutol® HS 15 5-fold improvement in oral bio-availability compared to free drug. [39]
ANTI-VIRAL,
ANTI-BACTERIAL, ANTI-FUNGAL, AND ANTIPROTOZOAL
Darunavir Lauroglycol® 90, Tween® 80, Transcutol® HP Enhancement in AUC0-t, oral bio-availability and Cmax, 1.45,5.8 and 7.5-fold, respectively compared to free drug. [215]
Nelfinavir mesylate Maisine® 35-1, Tween® 80, Transcutol® HP 4.5-fold improvement in permeability and 3.6-fold improvement in bio-availability. [113]
Lopinavir Maisine®, Tween®-80, Transcutol® HP Enhanced oral bio-availability (3.9-fold) compared to the pure drug. [216]
Acyclovir Sunflower oil, Tween® 60, Glycerol 3.5-fold increase in oral bio-availability compared to the pure drug suspension. [217]
Rifampicin Capmul® MCM C, Cremophor®-EL, Labrasol® 3.72 and 5.22-fold improvement in AUC0–t and Cmax, respectively compared to drug suspension. [218]
Amphotericin B Peceol®, PEG-200, Distearoylphos-phatidylethanolamine Amphotericin B-SEDD treatment significantly decreases total fungal colony forming unit concentrations compared to non-treated controls without significant changes in plasma creatinine levels in the A. fumigatus infected rats. [219]
Satranidazole Oleic acid, Tween® 20, PEG 400 SNEDDSs formulations showed a drug release of greater than 70% in 45 minutes whereas marketed preparation showed more than 70% of drug release in 90 min. [220]