PMID- 18798089
OWN - NLM
STAT- MEDLINE
DCOM- 20090420
LR  - 20231213
IS  - 1520-5762 (Electronic)
IS  - 0363-9045 (Linking)
VI  - 35
IP  - 3
DP  - 2009 Mar
TI  - Preparation and body distribution of freeze-dried powder of ursolic acid 
      phospholipid nanoparticles.
PG  - 305-10
LID - 10.1080/03639040802302165 [doi]
AB  - Ursolic acid (UA) is a poor soluble natural triterpenoid. It has a wide variety 
      of antitumor activities. We extracted it from Crataegus pinnatifida for the first 
      time. To achieve a high bioavailability, targeting effect, stability, and an 
      intravenous (i.v.) administration, the UA phospholipid nanopowders (UA-PL-NP) 
      were prepared, characterized, and evaluated. With soybean phospholipid as the 
      carrier and poloxamer 188 as emulsifier, the UA nanoparticle suspension was 
      prepared by solvent emulsification-evaporation and ultrasonic dispersion. The 
      UA-PL-NP was obtained by freeze drying. The body distribution in mice was studied 
      after i.v. administration of UA-PL-NP and an UA control solution (UA-Sol). The 
      entrapment efficiency (EE) and UA concentration in vitro and in vivo were 
      analyzed by high-performance liquid chromatography (HPLC). The results showed 
      that the UA-PL-NP had an average diameter of 273.8 nm with a zeta potential of 
      -23.2 mV. The EE was up to 86.0%, and the drug loading (DL) was 12.8%. After i.v. 
      administration of UA-PL-NP with low, middle and high doses, UA concentration in 
      the livers of mice obviously increased during tested period and was highest in 
      tested organs at 4 h. The AUC(0-12) ratio of UA-PL-NP in liver to that in plasma 
      was much higher than that of UA-Sol, and the liver AUC(0-12) ratio of UA-PL-NP to 
      UA-Sol was 8.6. These results indicate the UA-PL-NP have a good targeting to the 
      liver after i.v. administration. Therefore, the UA-PL-NP is demonstrated to be 
      available as an i.v. and liver targeting system for lipophilic antitumor 
      triterpenoids.
FAU - Zhou, Xiao Ju
AU  - Zhou XJ
AD  - State Key Laboratory of Virology, College of Pharmacy, Wuhan University, Wuhan, 
      P.R., China.
FAU - Hu, Xian Ming
AU  - Hu XM
FAU - Yi, Yi Mu
AU  - Yi YM
FAU - Wan, Jing
AU  - Wan J
LA  - eng
PT  - Journal Article
PL  - England
TA  - Drug Dev Ind Pharm
JT  - Drug development and industrial pharmacy
JID - 7802620
RN  - 0 (Antineoplastic Agents, Phytogenic)
RN  - 0 (Drug Carriers)
RN  - 0 (Phospholipids)
RN  - 0 (Triterpenes)
RN  - 106392-12-5 (Poloxamer)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents, Phytogenic/isolation & purification/*pharmacokinetics
MH  - Area Under Curve
MH  - Biological Availability
MH  - Chromatography, High Pressure Liquid
MH  - Crataegus/*chemistry
MH  - Drug Carriers/chemistry
MH  - Drug Delivery Systems
MH  - Freeze Drying
MH  - Injections, Intravenous
MH  - Liver/metabolism
MH  - Male
MH  - Mice
MH  - *Nanoparticles
MH  - Phospholipids/chemistry
MH  - Poloxamer/chemistry
MH  - Glycine max/chemistry
MH  - Tissue Distribution
MH  - Triterpenes/isolation & purification/*pharmacokinetics
MH  - Ursolic Acid
EDAT- 2008/09/18 09:00
MHDA- 2009/04/21 09:00
CRDT- 2008/09/18 09:00
PHST- 2008/09/18 09:00 [pubmed]
PHST- 2009/04/21 09:00 [medline]
PHST- 2008/09/18 09:00 [entrez]
AID - 902503368 [pii]
AID - 10.1080/03639040802302165 [doi]
PST - ppublish
SO  - Drug Dev Ind Pharm. 2009 Mar;35(3):305-10. doi: 10.1080/03639040802302165.