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. 2021 Jul 21;29(9):999–1012. doi: 10.1016/j.jsps.2021.07.015

Table 2.

Recent studies aiming to improve oral bioavailability of poorly bioavailable drugs.

Drug Composition research outcome
Olanzapine The NLCs were composed of glyceryl tripalmitate (solid lipid), castor oil (liquid lipid), Pluronic F-68 and soy lecithin (surfactants). In rats, NLC formulation was more than 5½-fold increase in oral bioavailability when compared to olanzapine suspension (Jawahar et al. 2018).
Raloxifene hydrochloride The NLCs were composed of glyceryl monostearate (solid lipid) and Capmul MCM C8 (liquid lipid) and polyvinyl alcohol (surfactant). In dogs, NLC optimized formulation was 3.75 fold enhancement in oral bioavailability when compared to raloxifene hydrochloride suspension (Shah et al. 2016).
Rosuvastatin Lauric acid or stearic acid (solid lipid) and Capryol-90 or oleic acid (liquid lipid) and PEG-25-stearate (surfactant). In rats, NLC formulations were six to nine fold improvement in the bioavailability of rosuvastatin when compared to Aqueous dispersion. Mixture of long chain fatty acid and medium chain fatty acids exhibited 1.5-fold increase in bioavailability when compared to only medium chain fatty acid (Pokharkar, Patil-Gadhe, and Kaur 2018).
Telmisartan Glyceryl monostearate (solid lipid), oleic acid (liquid lipid) and Tween 20 (surfactant). in rats, bioavailability of the telmisartan loaded NLC was increased by 2.17 and 3.46 fold compared to that of the marketed formulation and pure drug suspension, respectively (Thapa et al. 2018).
Olmesartan medoxomil Gelucire 44/14 (solid lipid, Capmul MCM EP (liquid lipid) and TPGS (surfactant). in rats, bioavailability of olmesartan medoxomil loaded NLC was increased by about 5 fold compared to that of the pure drug suspension (Kaithwas et al. 2017).
Fenofibrate Precirol ATO 5 (solid lipid), Captex100 (liquid lipid) and tween-80 (surfactant). in beagle dogs, bioavailability of Fenofibrate loaded NLCs suspension and solidified NLCs pellets revealed 3.6- and 3.5-fold respectively increase in bioavailability when compared to commercial product (Lipanthyl™ capsule) (Tian et al. 2013).
Atorvastatin Gelucire 43/01 (solid lipid), Capryol PGMC (propylene glycol monocaprylate type I; liquid lipid) and Pluronic F68 (surfactant). In rats, bioavailability of atorvastatin loade NLCs revealed 3.6- and 2.1-fold increase in bioavailability when compared to atorvastatin suspension and commercial product (Lipitor ™) (Elmowafy et al. 2017),
Ezetimibe Monosteol™ (solid lipid), Capryol™ 90 (liquid lipid), Kolliphor® EL (surfactant) and Transcutol® HP (Cosurfactant). In rats, bioavailability of ezetimibe loaded NLCs revealed 2.5- and 1.6-fold increase in bioavailability when compared to atorvastatin suspension and commercial product (Lipitor ™) (Shevalkar and Vavia 2019).
Amisulpride Gelucire®43/01(solid lipid), Capryol™90 (liquid lipid) and Tween-80 (surfactant) The relative bioavailability of NLCs capsules was found to be 252.78% when compared to Amipride® tablets (Assasy et al., 2019).
Simvastatin Stearic acid (solid lipid), oleic acid (liquid lipid) and Pluronic F-68 (surfactant). After oral administration of a single dose of simvastatin loaded NLC, 4-fold increase in bioavailability was observed, as compared to the simvastatin suspension (Fathi et al. 2018).