Document Detail

Preparation and in vitro evaluation of liposomal chloroquine diphosphate loaded by a transmembrane pH-gradient method.
MedLine Citation:
PMID:  18573626     Owner:  NLM     Status:  MEDLINE    
This study developed an active loading method for encapsulating chloroquine diphosphate (CQ) into liposomes. The effects of different formulation factors on the encapsulation efficiency (EE) and the size of CQ liposomes were investigated. These factors included the internal phase of liposomes, the external phase of liposomes, the ratio of drug to soybean phosphatidylcholine (drug/SPC), the ratio of cholesterol to soybean phosphatidylcholine (Chol/SPC), and the incubation temperature and time. The EE (93%) was obtained when using drug/SPC (1:50 mass ratio), SPC/Chol (1:5 mass ratio) at 0.10 M citrate-sodium citrate buffer (pH 3.6). As 5 mol% methoxypoly(ethylene glycol)(2,000) cholesteryl succinate (CHS-PEG(2000)) or distearoyl phosphatidylethanolamine-poly (ethylene glycol)(2,000) (DSPE-PEG(2000)) was added, the size of particle was reduced and the EE was improved. Freeze-drying with 5% trehalose as a cryoprotectant was carried out to achieve long-term stability. The drug release studies were performed in vitro simulating the desired application conditions, such as physiological fluids (pH 7.4), tumor tissues (pH 6.5) and endosomal compartments (pH 5.5). The release of CQ from the liposomes prepared via remote loading showed the significant pH-sensitivity and retention properties, which favored the application of liposomal CQ at tumor tissues and endosomal compartments.
Liyan Qiu; Na Jing; Yi Jin
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Publication Detail:
Type:  Journal Article     Date:  2008-05-16
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  361     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2008 Sep 
Date Detail:
Created Date:  2008-08-04     Completed Date:  2008-10-10     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  56-63     Citation Subset:  IM    
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
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MeSH Terms
Chemistry, Pharmaceutical
Chloroquine / administration & dosage,  analogs & derivatives*,  chemistry
Cholesterol / chemistry
Drug Carriers / chemistry*
Drug Stability
Drug Storage
Excipients / chemistry*
Hydrogen-Ion Concentration
Particle Size
Phosphatidylcholines / chemistry
Polyethylene Glycols / chemistry
Proton-Motive Force
Soybeans / chemistry
Time Factors
Reg. No./Substance:
0/Drug Carriers; 0/Excipients; 0/Liposomes; 0/Phosphatidylcholines; 0/Polyethylene Glycols; 50-63-5/chloroquine diphosphate; 54-05-7/Chloroquine; 57-88-5/Cholesterol

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

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