Liposome formulation of vilanterol trifenatate
a technology of vilanterol trifenatate and liposome, which is applied in the direction of liposomal delivery, medical preparations, organic active ingredients, etc., can solve the problems of difficult or unpleasant administration of dry powder inhalation for some patients, children and elderly patients,
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example 1
[0093]Preparation Method 1:
Preparation of vilanterol trifenatate solution: NaCl (0.9 g) was added to a beaker containing 100 ml purified water. To this NaCl solution, 117 μLof hydrochloric acid was added. Vilanterol trifenatate (7.03 mg) was added to 70 ml of the solution, then sonicated for 10 min to dissolve. Then, the solution containing vilanterol trifenatate was filtered using a 0.22 μm-filter membrane.
[0094]Mixing vilanterol trifenatate solution with lipid solution: DPPC (44.57 mg), DSPG (5.49 mg), and cholesterol (13.20 mg) were combined in a 50-ml round-bottom flask followed by the addition of 18 ml of chloroform and 2 ml of methanol to dissolve the DPPC and DSPG with gentle shaking. The solvent was removed using a rotary evaporator at 65° C., until a thin film of dried lipid was deposited on the walls of the flask. Finally, 20 ml of the prepared vilanterol trifenatate solution was added to the round-bottom flask containing the thin layer of dried lipid. The temperature was ...
example 2
[0096]In accordance with the preparation method described above, four different samples were prepared with high encapsulation efficiency and different drug to lipid ratios. The encapsulation efficiency of each of the four samples was over 97%, and the encapsulation efficiency of each of sample 2 and sample 4 was 100%. The average particle sizes of the liposomes were in the range of about 120 nm to about 320 nm.
[0097]Sample 1: NaCl (0.9 g) was added to a beaker containing 100 ml purified water. To this NaCl solution, 117 μLof hydrochloric acid was added. Vilanterol trifenatate (7.03 mg) was added to 70 ml of the solution, then sonicated for 10 min to dissolve. Then, the solution containing vilanterol trifenatate was filtered using a 0.22-μm filter membrane. Then DPPC (178.95 mg), DSPG (21.78 mg), and cholesterol (52.90 mg) were combined in a 50-ml round-bottom flask, followed by addition of 18 ml of chloroform and 2 ml of methanol to dissolve the DPPC and DSPG with gentle shaking. Th...
example 3
[0102]All four samples prepared in above example 2 were evaluated for drug-loading using HPLC, and the particle size was measured using a Malvern Nano ZS90 particle size analyzer. As shown in table 1, the encapsulation efficiency of each of the four samples was above 95%. Furthermore, the average particle size recorded was in the range of about 120 nm to about 320 nm.
TABLE 1Parameter list of the samplesParameterSample 1Sample 2Sample 3Sample 4Drug to lipid ratio1:1001:501:301:50Drug-loading (μg / ml)100.1886.58105.72110.28Average particle size261.6286.07311.23125.27(nm)Encapsulation efficiency97.6710098.21100(%)
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