PMID- 24882406
OWN - NLM
STAT- MEDLINE
DCOM- 20150120
LR  - 20190720
IS  - 1347-5215 (Electronic)
IS  - 0918-6158 (Linking)
VI  - 37
IP  - 6
DP  - 2014
TI  - Development and evaluation of optimized sucrose ester stabilized oleanolic acid 
      nanosuspensions prepared by wet ball milling with design of experiments.
PG  - 926-37
AB  - The aim of this study was to develop optimized sucrose ester (SE) stabilized 
      oleanolic acid (OA) nanosuspensions (NS) for enhanced delivery via wet ball 
      milling by design of experiments (DOE). In this study, SEOA NS batches were 
      prepared by wet ball milling method. Mean particle sizes and polydispersity 
      indices were determined using a nanosizer. The percent encapsulation efficiency, 
      saturation solubility and in vitro dissolution rate were obtained with analyses 
      using HPLC. Preparation methods were optimized by DOE using the Minitab software. 
      The in vitro bioefficacy was obtained by methyl thiazolyl tetrazolium (MTT) 
      measurements in A549 human non small cell lung cancer cell line. The in vivo 
      pharmacokinetics profile was determined using LC-electrospray ionization 
      (ESI)-MS/MS. The study produced spherical SEOA NS particles (ca. 100 nm in 
      diameter) which were found to be able to increase OA saturation solubility 
      considerably. Optimized SEOA-GBD NS (milled at 600 rpm for 3 h, sucrose 
      monolaurate (SEL) : sucrose monopalmitate (SEP) at 9 : 1, w/w; SE : OA at 1 : 1, 
      w/w) was found to be physically stable over 14 d at 4 degrees C. The NS showed much 
      higher dissolution rate, cytotoxicity and bioavailability when compared with the 
      free drug. Thus, the prepared OA as SE stabilized NS particles by wet ball 
      milling enhanced the saturation solubility, in vitro dissolution rate, 
      bioefficacy and in vivo bioavailability of OA. The use of sugar esters may also 
      be potentially applied to other hydrophobic drugs.
FAU - Li, Wenji
AU  - Li W
AD  - Department of Pharmacy, National University of Singapore.
FAU - Ng, Ka-yun
AU  - Ng KY
FAU - Heng, Paul Wan Sia
AU  - Heng PW
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Japan
TA  - Biol Pharm Bull
JT  - Biological & pharmaceutical bulletin
JID - 9311984
RN  - 0 (Drug Carriers)
RN  - 0 (Esters)
RN  - 05Q7CD0E49 (sucrose monolaurate)
RN  - 3OSQ643ZK5 (sucrose monopalmitate)
RN  - 57-50-1 (Sucrose)
RN  - 6SMK8R7TGJ (Oleanolic Acid)
SB  - IM
MH  - Administration, Oral
MH  - Animals
MH  - Cell Line, Tumor
MH  - Cell Survival/drug effects
MH  - Dose-Response Relationship, Drug
MH  - Drug Carriers/*chemistry
MH  - Drug Compounding/*methods
MH  - Drug Stability
MH  - Esters
MH  - Freeze Drying
MH  - Humans
MH  - Male
MH  - Microscopy, Electron, Transmission
MH  - Nanostructures/*chemistry
MH  - Oleanolic Acid/administration & dosage/*chemistry/pharmacokinetics/pharmacology
MH  - Particle Size
MH  - Rats, Sprague-Dawley
MH  - Solubility
MH  - Sucrose/*analogs & derivatives/chemistry
MH  - Surface Properties
EDAT- 2014/06/03 06:00
MHDA- 2015/01/21 06:00
CRDT- 2014/06/03 06:00
PHST- 2014/06/03 06:00 [entrez]
PHST- 2014/06/03 06:00 [pubmed]
PHST- 2015/01/21 06:00 [medline]
AID - DN/JST.JSTAGE/bpb/b13-00864 [pii]
AID - 10.1248/bpb.b13-00864 [doi]
PST - ppublish
SO  - Biol Pharm Bull. 2014;37(6):926-37. doi: 10.1248/bpb.b13-00864.