PMID- 21048339
OWN - NLM
STAT- MEDLINE
DCOM- 20110314
LR  - 20190706
IS  - 1347-5223 (Electronic)
IS  - 0009-2363 (Linking)
VI  - 58
IP  - 11
DP  - 2010 Nov
TI  - Preparation, characterization, and pharmacodynamics of exenatide-loaded 
      poly(DL-lactic-co-glycolic acid) microspheres.
PG  - 1474-9
AB  - Exenatide (synthetic exendin-4), a 39-amino acid peptide, was encapsulated in 
      poly(DL-lactic-co-glycolic acid) (PLGA) microspheres as a sustained release 
      delivery system for the therapy of type 2 diabetes mellitus. The microspheres 
      were prepared by a double-emulsion solvent evaporation method and the particle 
      size, surface morphology, drug encapsulation efficiency, in vitro release 
      profiles and in vivo hypoglycemic activity were evaluated. The results indicated 
      that the morphology of the exenatide PLGA microspheres presented as a spherical 
      shape with smooth surface, and the particle sizes distributed from 5.8 to 13.6 
      microm. The drug encapsulation efficiency tested by micro-bicinchoninic acid (BCA) 
      assay was influenced by certain parameters such as inner and outer aqueous phase 
      volume, PLGA concentration in oil phase, polyvinyl alcohol (PVA) concentrations 
      in outer aqueous phase. Moreover, in vitro release behaviors were also affected 
      by some parameters such as polymer type, PLGA molecular, internal aqueous phase 
      volume, PLGA concentration. The pharmacodynamics in streptozotocin (STZ)-induced 
      diabetic mice suggested that, exenatide microspheres have a significant 
      hypoglycemic activity within one month, and its controlling of plasma glucose was 
      similar to that of exenatide solution injected twice daily with identical 
      exenatide amount. In conclusion, this microsphere could be a well sustained 
      delivery system for exenatide to treat type 2 diabetes mellitus.
FAU - Liu, Bin
AU  - Liu B
AD  - Jilin University, Changchun, China.
FAU - Dong, Qingguang
AU  - Dong Q
FAU - Wang, Mengshu
AU  - Wang M
FAU - Shi, Lin
AU  - Shi L
FAU - Wu, Yongge
AU  - Wu Y
FAU - Yu, Xianghui
AU  - Yu X
FAU - Shi, Yanyu
AU  - Shi Y
FAU - Shan, Yaming
AU  - Shan Y
FAU - Jiang, Chunlai
AU  - Jiang C
FAU - Zhang, Xizhen
AU  - Zhang X
FAU - Gu, Tiejun
AU  - Gu T
FAU - Chen, Yan
AU  - Chen Y
FAU - Kong, Wei
AU  - Kong W
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Japan
TA  - Chem Pharm Bull (Tokyo)
JT  - Chemical & pharmaceutical bulletin
JID - 0377775
RN  - 0 (Delayed-Action Preparations)
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  - Delayed-Action Preparations/*chemistry
MH  - Diabetes Mellitus, Experimental/*drug therapy
MH  - Exenatide
MH  - Hypoglycemic Agents/*administration & dosage/pharmacokinetics/*therapeutic use
MH  - Lactic Acid/*chemistry
MH  - Mice
MH  - Microspheres
MH  - Particle Size
MH  - Peptides/*administration & dosage/pharmacokinetics/*therapeutic use
MH  - Polyglycolic Acid/*chemistry
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Venoms/*administration & dosage/pharmacokinetics/*therapeutic use
EDAT- 2010/11/05 06:00
MHDA- 2011/03/15 06:00
CRDT- 2010/11/05 06:00
PHST- 2010/11/05 06:00 [entrez]
PHST- 2010/11/05 06:00 [pubmed]
PHST- 2011/03/15 06:00 [medline]
AID - JST.JSTAGE/cpb/58.1474 [pii]
AID - 10.1248/cpb.58.1474 [doi]
PST - ppublish
SO  - Chem Pharm Bull (Tokyo). 2010 Nov;58(11):1474-9. doi: 10.1248/cpb.58.1474.