PMID- 20493221
OWN - NLM
STAT- MEDLINE
DCOM- 20101203
LR  - 20181201
IS  - 1873-4995 (Electronic)
IS  - 0168-3659 (Linking)
VI  - 146
IP  - 2
DP  - 2010 Sep 1
TI  - Issues in long-term protein delivery using biodegradable microparticles.
PG  - 241-60
LID - 10.1016/j.jconrel.2010.05.011 [doi]
AB  - Recently, a variety of bioactive protein drugs have been available in large 
      quantities as a result of advances in biotechnology. Such availability has 
      prompted development of long-term protein delivery systems. Biodegradable 
      microparticulate systems have been used widely for controlled release of protein 
      drugs for days and months. The most widely used biodegradable polymer has been 
      poly(d,l-lactic-co-glycolic acid) (PLGA). Protein-containing microparticles are 
      usually prepared by the water/oil/water (W/O/W) double emulsion method, and 
      variations of this method, such as solid/oil/water (S/O/W) and water/oil/oil 
      (W/O/O), have also been used. Other methods of preparation include spray drying, 
      ultrasonic atomization, and electrospray methods. The important factors in 
      developing biodegradable microparticles for protein drug delivery are protein 
      release profile (including burst release, duration of release, and extent of 
      release), microparticle size, protein loading, encapsulation efficiency, and 
      bioactivity of the released protein. Many studies used albumin as a model 
      protein, and thus, the bioactivity of the release protein has not been examined. 
      Other studies which utilized enzymes, insulin, erythropoietin, and growth factors 
      have suggested that the right formulation to preserve bioactivity of the loaded 
      protein drug during the processing and storage steps is important. The protein 
      release profiles from various microparticle formulations can be classified into 
      four distinct categories (Types A, B, C, and D). The categories are based on the 
      magnitude of burst release, the extent of protein release, and the protein 
      release kinetics followed by the burst release. The protein loading (i.e., the 
      total amount of protein loaded divided by the total weight of microparticles) in 
      various microparticles is 6.7+/-4.6%, and it ranges from 0.5% to 20.0%. 
      Development of clinically successful long-term protein delivery systems based on 
      biodegradable microparticles requires improvement in the drug loading efficiency, 
      control of the initial burst release, and the ability to control the protein 
      release kinetics.
CI  - Copyright 2010 Elsevier B.V. All rights reserved.
FAU - Ye, Mingli
AU  - Ye M
AD  - Departments of Biomedical Engineering and Pharmaceutics, Purdue University, West 
      Lafayette, Indiana 47907, USA.
FAU - Kim, Sungwon
AU  - Kim S
FAU - Park, Kinam
AU  - Park K
LA  - eng
GR  - CA129287/CA/NCI NIH HHS/United States
GR  - GM067044/GM/NIGMS NIH HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20100519
PL  - Netherlands
TA  - J Control Release
JT  - Journal of controlled release : official journal of the Controlled Release 
      Society
JID - 8607908
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Proteins)
RN  - 0 (Recombinant Proteins)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
SB  - IM
MH  - Animals
MH  - Delayed-Action Preparations/*chemistry
MH  - Drug Compounding/*methods/trends
MH  - Humans
MH  - Lactic Acid/*chemistry
MH  - Polyglycolic Acid/*chemistry
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Proteins/*administration & dosage
MH  - Recombinant Proteins/administration & dosage
EDAT- 2010/05/25 06:00
MHDA- 2010/12/14 06:00
CRDT- 2010/05/25 06:00
PHST- 2010/03/15 00:00 [received]
PHST- 2010/05/10 00:00 [revised]
PHST- 2010/05/10 00:00 [accepted]
PHST- 2010/05/25 06:00 [entrez]
PHST- 2010/05/25 06:00 [pubmed]
PHST- 2010/12/14 06:00 [medline]
AID - S0168-3659(10)00360-3 [pii]
AID - 10.1016/j.jconrel.2010.05.011 [doi]
PST - ppublish
SO  - J Control Release. 2010 Sep 1;146(2):241-60. doi: 10.1016/j.jconrel.2010.05.011. 
      Epub 2010 May 19.