PMID- 25578370
OWN - NLM
STAT- MEDLINE
DCOM- 20151110
LR  - 20181202
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 480
IP  - 1-2
DP  - 2015 Mar 1
TI  - Critical attributes of formulation and of elaboration process of PLGA-protein 
      microparticles.
PG  - 27-36
LID - S0378-5173(15)00010-1 [pii]
LID - 10.1016/j.ijpharm.2015.01.008 [doi]
AB  - Low drug loading, burst effect during release and drug inactivation account for 
      the main drawbacks of protein microencapsulation in poly(d,l-lactic-co-glycolic) 
      acid (PLGA) matrix by the water-in oil-in water (W/O/W) solvent evaporation 
      method. Thus, the current study was set to invest the critical attributes of 
      formulation and of elaboration process which determine protein loading into 
      microparticles as well as its further release, using albumin as protein model. 
      NaCl concentration in the external aqueous phase, poly(vinyl alcohol) (PVA) 
      concentration and mostly viscosity of both the internal aqueous phase and the 
      organic phase were critical attributes for improving drug loading, with polymer 
      molecular weight and hydrophobicity likewise directly related to albumin loading. 
      In such a way, when using 0.5% PVA as internal aqueous phase the highest albumin 
      loading was achieved. Optimized microparticles exhibited a sustained in vitro 
      release of albumin over 130 days. The influence of the microencapsulation process 
      on albumin stability and biological activity was evaluated by carrying out cell 
      proliferation assays on PC12 cells with albumin released from microparticles. 
      Such assay demonstrated that the microencapsulation procedure optimized in this 
      study did not affect the biological stability of the microencapsulated protein.
CI  - Copyright (c) 2015 Elsevier B.V. All rights reserved.
FAU - Martin-Sabroso, C
AU  - Martin-Sabroso C
AD  - Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, 
      Complutense University of Madrid, Spain.
FAU - Fraguas-Sanchez, A I
AU  - Fraguas-Sanchez AI
AD  - Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, 
      Complutense University of Madrid, Spain.
FAU - Aparicio-Blanco, J
AU  - Aparicio-Blanco J
AD  - Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, 
      Complutense University of Madrid, Spain.
FAU - Cano-Abad, M F
AU  - Cano-Abad MF
AD  - Clinical Pharmacology, Health Research Institute, La Princesa University 
      Hospital, Madrid, Spain; Teofilo Hernando Institute, Madrid, Spain; Department of 
      Pharmacology and Therapeutics, Faculty of Medicine, Autonomous University of 
      Madrid, Spain.
FAU - Torres-Suarez, A I
AU  - Torres-Suarez AI
AD  - Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, 
      Complutense University of Madrid, Spain; Institute of Industrial Pharmacy, 
      Complutense University of Madrid, Spain. Electronic address: galaaaa@ucm.es.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20150108
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Albumins)
RN  - 0 (Delayed-Action Preparations)
RN  - 0 (Solvents)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - 451W47IQ8X (Sodium Chloride)
SB  - IM
MH  - Albumins/*administration & dosage/chemistry
MH  - Animals
MH  - Cell Proliferation/drug effects
MH  - Chemistry, Pharmaceutical/methods
MH  - Delayed-Action Preparations
MH  - Drug Liberation
MH  - Hydrophobic and Hydrophilic Interactions
MH  - Lactic Acid/*chemistry
MH  - *Microspheres
MH  - Molecular Weight
MH  - PC12 Cells
MH  - Polyglycolic Acid/*chemistry
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Rats
MH  - Sodium Chloride/chemistry
MH  - Solvents/chemistry
OTO - NOTNLM
OT  - Albumin
OT  - Critical attributes
OT  - Microparticles
OT  - Poly(lactic-co-glycolic) acid
OT  - Protein microencapsulation
OT  - Quality by design
EDAT- 2015/01/13 06:00
MHDA- 2015/11/11 06:00
CRDT- 2015/01/13 06:00
PHST- 2014/10/13 00:00 [received]
PHST- 2015/01/04 00:00 [revised]
PHST- 2015/01/07 00:00 [accepted]
PHST- 2015/01/13 06:00 [entrez]
PHST- 2015/01/13 06:00 [pubmed]
PHST- 2015/11/11 06:00 [medline]
AID - S0378-5173(15)00010-1 [pii]
AID - 10.1016/j.ijpharm.2015.01.008 [doi]
PST - ppublish
SO  - Int J Pharm. 2015 Mar 1;480(1-2):27-36. doi: 10.1016/j.ijpharm.2015.01.008. Epub 
      2015 Jan 8.