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| Drug | Disease/activity | NLC components | Model | Outcomes | References |
|
| Thymoquinone (TQ) | Antioxidant, anti-inflammatory, and neuroprotective | Hydrogenated palm oil, lecithin, Lipoid GmbH, olive oil | Pharmacokinetic/pharmacodynamic | Enhanced intestinal absorption via the oral route of TQ. Higher bioavailability was observed via the oral route than i.v. administered TQ-NLCs. Due to lower AUC0-∞, oral administration had slower absorption and better bioavailability compared to intravenous administration | [164] |
| Bromelain (BR) | Antiarthritic activity | Soya lecithin, stearic acid, palmitic acid, myristic acid | Pharmacodynamic studies | BR and Br-NLCs, after oral administration, significantly lessened the complete Freund’s adjuvant- (CFA-) induced paw inflammation around the lateral tibial joint and soft tissue thickening as equated to (CFA) control | [165] |
| Chrysin (CHN) | Antitumor activity | Capmul PG-12, GMS, and S 100 | Cellular uptake studies and in vivo pharmacokinetics studies | CHN-loaded biotin-modified NLC (Bio-NLC) displayed excellent uptake by Caco-2 cell lines compared to plain NLCs. CHN-Bio-NLCs showed a 7.46-fold increase in AUC0-∞ in comparison to CHN suspension | [166] |
| Auraptene (APN) | Benign prostate hyperplasia | Compritol, almond oil, phospholipid | Histopathological investigations, oxidative stress, inflammation, and apoptotic assessments | APN-NLCs demonstrated superlative results by safeguarding testosterone-induced BPH in animal models from oxidative stress, inflammation, and apoptosis | [167] |
| Amphotericin B (AmpB) | Antifungal activity | Chitosan, beeswax, coconut oil, soya lecithin | Mucoadhesion studies | ChiAmpB-NLC enhanced the adsorption of positively charged chitosan to negatively charged porcine gastric mucin protein | [168] |
| Perphenazine (PPZ) | Schizophrenia | Glyceryl monostearate 900 K, Dynasan 118, oleic acid | In vivo pharmacokinetic studies | The oral bioavailability of PPZ-loaded NLC-6 and NLC-12 was enhanced about 3.12- and 2.49-fold, respectively, compared to the plain drug suspension | [169] |
| Silymarin (SLM) | Hepatoprotective, antidiabetic | Cetyl palmitate (CP) Capryol 90, Lauroglycol 90, Labrafac PG, Labrafac WL 1349, Labrafil M 1944 CS, Precirol ATO 5, oleic acid, hemp oil, borage oil | Transcellular passive permeability by the parallel artificial membrane permeability Assay (PAMPA) and cell uptake studies (Caco-2) | Amplified the passive permeation of SLM by around 10-fold, CP as a solid lipid increased NLC cellular uptake by Caco-2 cells | [170] |
| Berberine (BB) | Antidiabetic | Oleic acid, glyceryl distearate | Cellular uptake, pharmacokinetic/pharmacodynamic studies | 396.87% and 663.65% augmented oral bioavailability of BB-NLCs and selenium conjugated-BB-NLCs as compared with BB solution. More profound hypoglycemic effect of Se-BB-NLCs than BB-NLCs and BB solution. Fast cellular uptake was seen in Se-BB-NLCs and BB-NLCs than in the BB solution | [171] |
| Ezetimibe (EZE) | Hypercholesterolemia | Geleol™, Compritol® 888 ATO, Precirol® ATO 5, Monosteol™, Transcutol® HP, Peceol™, Lauroglycol™ FCC | In vivo pharmacokinetic/pharmacodynamic studies | After oral administration, EZE-NLC showed increased oral bioavailability in comparison to a drug suspension and tablet. A substantial decline in cholesterol levels was observed in a rat model administered with EZE-NLCs | [172] |
| Rosuvastatin (RST) | Hypercholesterolemia and dyslipidemia | Precirol® ATO 5, oleic acid | In vivo pharmacokinetic and pharmacodynamic model | 1.65-fold increased absorption of RST-NLC as compared to RST tablet powder indicated oral solubility enhancement | [173] |
| Atorvastatin (AT) | Hypercholesterolemia | Gelucire® 43/01, glyceryl monostearate (GMS), Compritol® 888 ATO, and Capryol® PGMC | In vivo pharmacokinetic/dynamic studies | A 3.6- and 2.1-fold upsurge in bioavailability as equated to AT suspension and market product, AT-NLC-1 significantly reduced rats’ serum levels of total cholesterol (TC), triglyceride (TG), low-density lipoprotein (LDL) and raised high-density lipoprotein (HDL) levels | [174] |
| Naringenin (NGN) | Nonalcoholic fatty liver Disease | Stearic acid, oleic acid | Transepithelial transport, in vivo pharmacokinetic studies | High permeability coefficients of NGN-NLC indicated improved transport of NGN via MDCK cells, NGN-NLCs augmented 1.2-fold oral bioavailability | [175] |
| Adefovir dipivoxil (AD) | Hepatitis B | Cremophor RH 40, Pluronic F68 (poloxamer 188), egg yolk L-α phosphatidylcholine (PC) | In vivo hepatoprotective evaluation | Oral administered AD-NLC exhibited higher uptake as indicated by radioiodinated rose Bengal dye to the thioacetamide-induced liver injury | [176] |
| Temazepam (TZP) | Insomnia | Capryol® 90, Labrasol®, Compritol®888, ATO, oleic acid | In vivo gamma scintigraphy imaging and brain biodistribution study | TZP-NLCs accumulated at higher concentrations than the TZP suspension, as evident from gamma scintigraphy. TZP-NLCs augmented relative drug bioavailability by 292.7% after oral administration in comparison to TZP suspension | [177] |
| Olmesartan (OLM) | Hypertension | Compritol 888, Peceol, Maisine 35-1, Lauroglycol FCC, Lauroglycol 90, stearic acid, GMS, IPM, cetyl palmitate, oleic acid, and ethyl oleate | Cellular uptake and transport studies, in vivo pharmacokinetics, in vivo biodistribution study | High cellular uptake for OLM-NLCs and OLM-ConA-NLCs compared to a drug suspension. 2.88- and 4.62-fold improvement in oral bioavailability was evident for OLM-NLCs and OLM-ConA-NLCs in comparison to drug suspension, 37% reduction in blood pressure was observed for drug-loaded NLCs in comparison to pure drug suspension | [178] |
| Isradipine (ISD) | Hypertension | Glyceryl monostearate, glycerol distearate, glycerol dibehenate, PEG-8 beeswax, PEG-75 stearate, propylene glycol dicaprylocaprate, propylene glycol monocaprylate, and macrogol 15 hydroxy stearate | In vitro permeation/in vivo pharmacodynamic study | Verapamil (a P-gp efflux inhibitor) significantly enhanced the permeation of ISD from NLCs through the rat intestine by inhibiting the drawing back of the drug inside the intestine. ISD solubility was augmented due to micelle formation owing to the lipid digestion of NLC components | [152] |
| Quercetin (QCT) | Nutraceutical delivery | Glyceryl monostearate, polyglycerol-6 monostearate | In vitro antioxidant activity | Improved solubility and antioxidant activity of QCT-NLCs, which also lessened the lipid oxidation as compared to emulsion | [179] |
| Quercetin and piperine | Oral squamous cell carcinoma | Glyceryl behenate, squalene | In vivo pharmacokinetic study | Enhanced biodistribution of both drugs in oral cavity parts upon oral administration of drug-loaded NLCs | [180] |
| Eplerenone | Chronic central serous chorioretinopathy | Cremophor® RH40, Miglyol®81N2 | Ex vivo permeation study | Twofold higher drug permeation through the rabbit intestine compared to aqueous drug suspension after 24 h | [181] |
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