Document Detail


Liquid proliposomes of nimodipine drug delivery system: preparation, characterization, and pharmacokinetics.
MedLine Citation:
PMID:  23319300     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Chuandi Sun; Ji Wang; Jianping Liu; Lu Qiu; Wenli Zhang; Lei Zhang
Publication Detail:
Type:  Journal Article     Date:  2013-01-15
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  14     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-26     Completed Date:  2013-08-12     Revised Date:  2014-01-23    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  332-8     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium Channel Blockers / administration & dosage*,  pharmacokinetics
Liposomes*
Male
Microscopy, Electron, Transmission
Nimodipine / administration & dosage*,  pharmacokinetics
Rabbits
Spectrophotometry, Ultraviolet
Chemical
Reg. No./Substance:
0/Calcium Channel Blockers; 0/Liposomes; 57WA9QZ5WH/Nimodipine
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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