Review Article

Nanostructured Lipid Carriers for Improved Delivery of Therapeutics via the Oral Route

Table 2

NLCs and their role in improving the oral bioavailability of pharmaceuticals.

Drug/bioactive moleculeActivityModelEnhancement of oral bioavailabilityReferences

Candesartan cilexetil (CC)AntihypertensiveIn situ model for determining drug absorption2-fold increase in oral bioavailability[125]
Gypenosides (GPS)Anti-inflammatoryIn situ intestinal perfusion/in vivo pharmacokinetic studies8.5-fold increase in bioavailability of the GPS-SGC-NLCs[126]
Nimodipine (NMP)Calcium channel blockerIn situ intestinal perfusion/in vivo pharmacokinetic studies161% increased bioavailability than nimodipine suspension[127]
Ezetimibe (EMB)AntihyperlipidemicIn vivo pharmacokinetic studies2.63-and 2.33-fold increase in oral bioavailability in comparison with EMB suspension and marketing product[128]
Ritonavir (RTV)Highly active antiretroviral therapy (HAART)In vivo pharmacokinetic study2.86-fold augmentation in oral bioavailability of RTV in comparison to RTV suspension[129]
Felodipine (FDP)AntihypertensiveIn vivo pharmacokinetic studiesA 2-fold oral bioavailability enhancement of FDP in comparison to marketed formulation[130]
Apixaban (APX)AnticoagulantIn vivo pharmacokinetic study2.67-fold increase in oral bioavailability of APX in comparison to pure drug suspension[131]
Levosulpiride (LSP)DyspepsiaIn vivo pharmacokinetic study4.38-fold improvement in oral bioavailability of LSP than drug dispersion[132]
Amisulpride (AMS)AntipsychoticIn vivo pharmacokinetic studyThe relative bioavailability of AMS-NLCs capsules was found to be 252.78% as equated with commercial Amipride® tablets[133]
Triptolide (TP)AntiinflammatoryIn vivo pharmacokinetic studyLonger residence time, sustained drug release, 1.54 times increased bioavailability than free drug[134]
ErgosterolAntidiabetic nephropathyIn vivo pharmacokinetic studyThe comparative oral bioavailability of ERG-NLCs was 277.56% higher than that of pure ergosterol[135]
Raloxifene (RLN)AnticancerIn vivo pharmacokinetic studyA 4.79-fold increase in oral bioavailability of RLN equated to RLN suspension[136]
Raloxifene (RLX)OsteoporosisIn vivo pharmacokinetic study3.19-fold enhancement in oral bioavailability of RLX in comparison to free RLX suspension[137]
FenofibrateAntihyperlipidemicIn vivo pharmacokinetic studyFour times increase in oral bioavailability[138]
Transferulic acid (TFA)Antioxidative, anti-inflammatory, and cardioprotectiveIn vivo pharmacokinetic studyAugmented oral bioavailability than TFA-SLNs[139]
Ticagrelor (TGL)Antiplatelet activityIn vivo pharmacokinetic/pharmacodynamic studyThe oral bioavailability of TGL-NLC was augmented by 254.99% in comparison to raw TGL[140]