Table 1.
Characteristics and in vivo bioavailability of liposomal formulations for various water-insoluble drugs.
| Drugs (Therapeutic Category) | Liposome Composition | Encapsulation Efficiency (%) | Physical Forms | Study Subject | Relative BA (fold) | Comparator | Reference |
|---|---|---|---|---|---|---|---|
| BCS Class II drugs | |||||||
| Apigenin (herbal supplement) | Phospholipid 90H | 93.3% | Solid: proliposome (mannitol) | Rat | 1.5 | Free drug suspension | [16] |
| Carbamazepine (antiepilectic) | Drug:DMPG (1:1) | ND | Solid: co-precipitate | Rabbitt | 1.2 (NS) | Tegretol suspenstion | [17] |
| Carvedilol (cardiovascular) | EPC:CH:Labrasol (65:15:20) | 79.8% | Liquid: liposome dispersion | Rat | 2.3 | Free drug suspension | [18] |
| Docetaxel (anticancer) | EPC:SA (1:0.2) with SDC and coating with Eudragit L100/S100 (4:1) | 33.6% | Solid: Freeze-dried liposomes (trehalose, mannitol) | Rat | 3.1 | Free drug solution in polysorbate 80/ethanol/saline (20:13:67) | [19] |
| Dronedarone (antiarrhythmic) | DMPG Na:CH (1:2) | 84% | Solid: proliposomes (MCC) | Rat | 1.5 | Free drug suspension | [20] |
| Fenofibrate (antilipidemic) | SPC:SDC (4:1) | 88.2% | Liquid: liposomal dispersion | Dog | 5.1 | Micronized fenofibrate in capsule | [21] |
| Flutamide (antiandrogen) | SPC:CH (4:1 w/w) | 70.6% | Liquid: liposomal dispersion | Rat | 0.9 | Free drug suspension | [22] |
| Halofantrine (antimalarial) | DSPC:Drug (3:1) Coating with CAP | ND | Solid: proliposomes (enteric coating) | Rat | 1.4 | Free drug suspension | [23] |
| Indomethacin (NSAID) | DSPC:DCP:CH (8:2:1) coating with chitosan | ND | Liquid: liposomal dispersion | Rat | 1.8 | Free drug solution | [24] |
| Isradipine (calcium antagonist) | HSPC:CH (1:1) | 96.8% | Solid: proliposomes (mannitol) | Rat | 2.0 | Free drug suspension | [25] |
| Lovastatin (antilipidemic) | SPC:CH (9:1) | 85.8% | Solid: proliposomes (silicified MCC) | Rat | 1.6 | Free drug suspension | [26] |
| Nisoldipine (calcium channel blocker) | DMPC:CH (4:1) | 85.6% | Solid: proliposome (MCC) | Rat | 3.0 | Free drug suspension | [27] |
| Piroxicam (NSAID) | DMPG | ND | Solid: solid dispersion | Rat | 1.3 (NS) | Free drug suspension | [28] |
| Raloxifen (estrogen receptor modulator) | HSPC:CH with DCP or SA | 94.2% (cationic) 93.2% (anionic) 93.9% (neutral) |
Solid: proliposomes (mannitol) | Rat | 3.4 (cationic); 2.6 (anionic); 2.4 (neutral) |
Free drug suspension (processed without lipids) | [29] |
| Sorafenib tosylate (anticancer) | DPPC:DPPG:TPGS:CH (8:1:2:4) Coating with Glycol chitosan & Eudragit S100 | 94.6% (uncoated) 96.6% (glycol chitosan-coated) 89.7% (double layer coated) |
Liquid: liposome dispersion | Rat | 2.9 (uncoated); 3.0 (glycol chitosan-coated); 5.1 (EudragitS100/glycol chitosan coated) |
Free drug | [30] |
| Silymarin (hepatoprotective) | Phospholipid (82% PC) | 92.6% | Solid: proliposomes (mannitol) | Dog | 3.4 | Powder | [31] |
| Dehydrosilymarin (hepatoprotective) | SPC 0.3 g CH 0.075 g IPM 0.2 g Sodium cholate 0.2 g |
70–80% | Solid: proliposomes (mannitol) | Rabbit | 2.2 | Free drug suspension | [32] |
| Tacrolimus (immunosuppressant) | DSPC:CH (4:1) | approx. 70–80% | Solid: proliposomes | Rat | 1.9 | Free drug suspension | [33] |
| Vinpocetine (Cardiovascular) | SPC:CH (9:1, w/w) | 86.3% | Solid: proliposomes (sorbitol) | Rabbit | 3.5 | Free drug suspension | [34] |
| Zaleplon (hypnotic) | HSPC:CH (1:1) with DCP or SA | 93.8% (cationic) 92.5% (anionic) 94.6% (neutral) |
Solid: proliposomes (mannitol) | Rat | 4.6 (cationic) 3.0 (anionic) 2.0 (neutral) |
Free drug suspension (processed without lipids) | [35] |
| BCS class IV drugs | |||||||
| Curcumin (herbal supplement) | SPC:SDC (85:15 w/w) Coating with Silica | 93.3% | Liquid: liposome dispersion | Rat | 2.3 (uncoated); 3.3 (silica-coated) |
Free drug suspension | [36] |
| SPC:CH:TPGS:drug (20:2:12:1) Coating with TMC | 86.7% | Liquid: liposome dispersion | Rat | 6.7 (uncoated); 10.6 (TMC-coated) |
Free drug suspension | [37] | |
| SPC:SDC (70:25 w/w) Coating with TMC and CMCS | ND | Liquid: liposome dispersion | Rat | 6.3 (CMCS/TMC-coated); 2 (TMC-coated) |
Uncoated liposomes | [38] | |
| Cyclosporine A (immunosuppressant) | ePC:Cremophor EL (10:0.5) | 96.3% | Solid: proliposomes (lactose) | Rat | 9.6 | Free drug suspension | [39] |
| SPC:SDC (3:1) | 94.0% | Liquid: liposome dispersion | Rat | 1.2 (NS) | Sandimmune Neoral®® | [40] | |
| SPC:CH (20:1) Coating with OACS | 98.0% | Liquid: liposome dispersion | Rat | 1.7 (uncoated); 3.4 (OACS-coated) |
Free drug suspension | [41] | |
| EPC:CH (28:5) with Pluronic F127 | 90.0% | Liquid: liposome dispersion | Rat | 1.8 | Unmodified liposomes | [42] | |
| Daidzein (natural compound) | SPC:CH:DSPEPEG2000 (55:40:5) | 80.2% | Solid: freeze dried liposomes with 3% sucrose | Rat | 2.5 | Free drug suspension | [43] |
| Lopinavir (antiviral) | HSPC, CH (7:3) | Approx. 89% | Solid: proliposome (mannitol) | Rat | 2.2 | Free drug suspension | [44] |
| Paclitaxel (anticancer) | SPC:CH:SA (24.5:11.5:2 w/w) Coating with PAA and then PAH | 81.3% | Solid: freeze dried liposomes with mannitol | Rat | 4.0 (double-layer coated) | Free drug suspension | [45] |