Abstract：
:To investigate the possibility of liquid proliposomes being carriers for oral delivery, nimodipine liquid proliposomes-based soft capsules (NPSC) were prepared. Nimodipine proliposomes were characterized by transmission electron microscopy (TEM), conversion rate from proliposomes to liposomes, entrapment efficiency, particle size, and zeta potential. Accelerated stability testing of NPSC was carried out for 3 months at 40±2°C, 75±5% RH. The concentration of nimodipine in plasma of New Zealand rabbits of NPSC, nimodipine soft capsules, and hydrated liposomes was studied. Results showed that nimodipine proliposomes were automatically converted into liposomes when exposed to a water phase in 30 s. The average diameter was 378.6±26.5 nm in distilled water with entrapment efficiency (EE%) of 84.7±5.9%, while the average diameter was 316.9±34.6 nm in 0.1 M hydrochloric acid solution with EE% of 72.8±4.7%. Accelerated stability test showed that there was no change in drug content, particle size, and EE% except for a decrease in dissolution of nimodipine. In vivo experiments, areas under the plasma level-time curve of NPSC and nimodipine-hydrated liposomes increased 2.41 and 2.34 times more than that of nimodipine soft capsules, peak concentration increased 2.87 and 2.92 times, time of peak concentration from 0.75 to 2 and 1 h, respectively. Nimodipine-hydrated liposomes presented similar pharmacokinetic parameters compared with NPSC. Results suggested that NPSC offered a potential way to improve oral delivery of nimodipine.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Sun C,Wang J,Liu J,Qiu L,Zhang W,Zhang Ldoi
10.1208/s12249-013-9924-6subject
Has Abstractpub_date
2013-03-01 00:00:00pages
332-8issue
1issn
1530-9932journal_volume
14pub_type
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