Table 1. Drug delivery through oral route by NLC .
Drug | Purpose | Solid lipid | Liquid lipid | Surfactants | Formulation method | Outcome | Ref. |
Nisoldipine | Increase oral bioavailability of the hypertensive agent | Trimyristin | Oleic acid | Egg lecithin E 80 and poloxamer 188 | Hot homogenization technique followed by ultrasonication | Drug loaded in NLC showed a prolonged drug release rate. Oral bioavailability increased by 2.46 and 1.09-fold in respect to suspension and SLN in rats. | 44 |
Sulforaphane | Increase oral efficacy of anticancer agent | Precirol ATO 5 | Vitamin E | Poloxamer 188 and tween 80 | Melt emulsification method followed by ultrasonication | Optimized NLC show higher ex vivo drug permeability, improved cytotoxicity. Drug release is increased by more than 2-fold. 5-fold increase in relative bioavailability in comparison to suspension during in vivo studies in albino Wistar rats. | 45 |
Insulin | Evaluate the impact of surfactant on peptide protection in gastric environment | Stearic acid | Peceol and oleic acid | Kolliphor RH 40, Brij L23, tegosoft PC41, and tegosolve 90 MB | Solvent diffusion method | PEG ether (Brij l23) shows the highest and PEG ester (tegosoft PC41 and tegosolve 90 MB) shows the lowest protection from GI proteases. | 46 |
Rifabutin | Oral delivery of antimycobacterial drug in Crohn’s disease | Precirol ATO 5 | Oleic acid | Tween 80 and epikuron 145 | Hot high shear homogenization technique | In vitro, cellular studies show efficient macrophage uptake, increased permeation, and selective release in macrophages. NLC helped in achieving therapeutic concentration at a fast rate. | 26 |
Quetiapine Fumarate | Increase bioavailability of antipsychotic a and reduce hepatic metabolism by lymphatic drug targeting | Precirol ATO 5 | Oleic acid | Poloxamer 188 and phospholipon 90 G | Hot emulsification and ultrasonication technique | Pharmacokinetic study on rats shows an approximately 4-fold increase in AUC in rats than suspension. The experiment also shows lymphatic uptake of quetiapine fumarate in rats. | 47 |
Lopinavir | Deliver antiretroviral drug orally | Compritol 888 ATO | Oleic acid | Poloxamer 188 and Tween 80 | Hot high shear homogenization technique | Optimized NLC formulation shows higher cellular uptake in caco-2 cell line and 7-fold increase bioavailability in rats than drug suspension. | 27 |
Cedrol | Increase bioavailability of antileishmanial drug | Compritol 888 ATO | Triolein | Pluronic F68 and soya lecithin | Hot melt emulsification ultrasonication method | In vivo studies show 2-fold increase in selectivity index (CC50/IC50) in both wild and drug-resistant leishmania and 2 to 3 fold and 3 to 5 fold increase of bioavailability in wild and drug-resistant leishmania respectively. | 48 |
Adefovir dipivoxil | Oral delivery of antiviral drug for hepatitis B | Precirol ATO 5 | Capmul MCM | Cremophor RH40 and pluronic F68 | Solvent emulsification diffusion technique | In vivo, studies in Swiss albino mice demonstrate high uptake of the drug by liver cells, which will make NLC an appropriate liver targeting carrier. | 49 |
Amphotericin B | Preparation of enteric-coated NLC for stability of antiviral drug in gastric pH | Glyceryl monostearate | Castor oil and labrasol |
Tween 80, cremophor RH40 and PEG400 | Hot high-pressure homogenization | Eudragit L100-55 coated nanoparticle shows a more than 4-fold increase in solubility than the free drug. Uncoated particle shows high drug solubility but is susceptible to acid degradation. | 22 |
Fluconazole | Local delivery of antifungal drug for oral Candiasis by mucoadhesion | Stearic acid | Oleic acid | Pluronic F127 and lecithin | Emulsification and sonication technique | Optimized NLC were coated with chitosan results in sustained release of drug with prolonged antifungal effect due to mucoadhesion of NLC particles. | 50 |
Berberine | Selenium coated NLC of antidiabetic phytomedicine for type 2 diabetes | Precirol ATO 5 | Oleic acid | Tween 80 | Hot melt dispersion and homogenization technique | Coating resulted in a 6.63-fold enhancement of oral bioavailability in rats than a solution with sustained release of the drug. | 51 |