PMID- 24398695
OWN - NLM
STAT- MEDLINE
DCOM- 20150105
LR  - 20211021
IS  - 1573-904X (Electronic)
IS  - 0724-8741 (Linking)
VI  - 31
IP  - 6
DP  - 2014 Jun
TI  - Comparative studies on the influences of primary emulsion preparation on 
      properties of uniform-sized exenatide-loaded PLGA microspheres.
PG  - 1566-74
LID - 10.1007/s11095-013-1262-6 [doi]
AB  - PURPOSE: It is well known that primary emulsion (W1/O) preparation process (by 
      ultrasonication or homogenization) plays an important role in the properties of 
      drug-loaded microspheres, such as encapsulation efficiency, release behavior and 
      pharmacodynamics. However, its involved mechanism has not been intensively and 
      systematically studied, partly because that broad size distribution of the 
      resultant particles prepared by conventional preparation can greatly disturb the 
      analysis and reliability of the results. Here, we focused on the relevant 
      studies. METHODS: In order to eliminate the disturbance caused by broad size 
      distribution, uniform-sized exenatide-loaded poly(DL-lactic-co-glycolic acid) 
      (PLGA) microspheres were prepared by Shirasu Porous Glass (SPG) premix membrane 
      emulsification. The properties of microspheres whose W1/O was formed by 
      ultrasonication (UMS) and homogenization (HMS) were compared including in vitro 
      release, pharmacology and so forth. RESULTS: HMS exhibited fast release rate and 
      hyperglycemic efficacy within first 14 days, but declined afterwards. 
      Comparatively, UMS showed slower polymer degradation, more acidic microclimate pH 
      (mupH) in vitro, and stable drug release with sustained efficacy during 1 month in 
      vivo. CONCLUSIONS: HMS was desirable for the 2-week-sustained release in vivo, 
      while UMS was more appropriate for the longer time release (about 1 month). These 
      comparative researches can provide guidance for emulsion-microsphere preparation 
      routs in pharmaceutics.
FAU - Qi, Feng
AU  - Qi F
AD  - National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of 
      Biopharmaceutical Production & Formulation Engineering, Institute of Process 
      Engineering, Chinese Academy of Sciences, Beijing, 100190, People's Republic of 
      China.
FAU - Wu, Jie
AU  - Wu J
FAU - Hao, Dongxia
AU  - Hao D
FAU - Yang, Tingyuan
AU  - Yang T
FAU - Ren, Yu
AU  - Ren Y
FAU - Ma, Guanghui
AU  - Ma G
FAU - Su, Zhiguo
AU  - Su Z
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20140108
PL  - United States
TA  - Pharm Res
JT  - Pharmaceutical research
JID - 8406521
RN  - 0 (Emulsions)
RN  - 0 (Excipients)
RN  - 0 (Hypoglycemic Agents)
RN  - 0 (Peptides)
RN  - 0 (Venoms)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - 9P1872D4OL (Exenatide)
SB  - IM
MH  - Animals
MH  - Drug Compounding
MH  - Drug Stability
MH  - Drug Storage
MH  - Emulsions
MH  - Excipients
MH  - Exenatide
MH  - Hydrogen-Ion Concentration
MH  - Hypoglycemic Agents/administration & dosage/*chemistry/pharmacokinetics
MH  - Lactic Acid
MH  - Male
MH  - Microspheres
MH  - Particle Size
MH  - Peptides/administration & dosage/*chemistry/pharmacokinetics
MH  - Polyglycolic Acid
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Venoms/administration & dosage/*chemistry/pharmacokinetics
EDAT- 2014/01/09 06:00
MHDA- 2015/01/06 06:00
CRDT- 2014/01/09 06:00
PHST- 2013/07/16 00:00 [received]
PHST- 2013/12/09 00:00 [accepted]
PHST- 2014/01/09 06:00 [entrez]
PHST- 2014/01/09 06:00 [pubmed]
PHST- 2015/01/06 06:00 [medline]
AID - 10.1007/s11095-013-1262-6 [doi]
PST - ppublish
SO  - Pharm Res. 2014 Jun;31(6):1566-74. doi: 10.1007/s11095-013-1262-6. Epub 2014 Jan 
      8.