PMID- 19646519
OWN - NLM
STAT- MEDLINE
DCOM- 20100202
LR  - 20181201
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 382
IP  - 1-2
DP  - 2009 Dec 1
TI  - Improved cellular uptake of chitosan-modified PLGA nanospheres by A549 cells.
PG  - 198-204
LID - 10.1016/j.ijpharm.2009.07.023 [doi]
AB  - The authors have previously developed poly(DL-lactic-co-glycolic acid) (PLGA) 
      nanospheres (NSs) as a nanoparticulate drug carrier for pulmonary administration. 
      The present study demonstrates that chitosan (CS)-modified PLGA NSs (CS-PLGA NSs) 
      are preferentially taken up by human lung adenocarcinoma cells (A549). PLGA NSs 
      prepared using a water-oil-water emulsion solvent evaporation method were 
      surface-modified by adsorption of CS. The physicochemical parameters of PLGA NS, 
      including average size and surface charge, were measured to identify which 
      parameter influenced cellular uptake of PLGA NS. Uptake was confirmed using 
      fluorescence spectrophotometry and was visualized in A549 cells with confocal 
      laser scanning microscopy (CLSM). The cytotoxicities of non- and CS-PLGA NS 
      systems were compared in vitro by MTS assay. Cellular uptake of PLGA NS increased 
      with decreasing diameter to the submicron level and with CS-mediated surface 
      modification. Cellular uptake of PLGA NS was energy dependent, as shown by a 
      reduction in uptake at lower incubation temperatures and in hypertonic growth 
      medium used as an inhibitor of clathrin-coated pit endocytosis. CS-PLGA NSs were 
      taken up by A549 cells in an energy-dependent manner, suggesting a 
      clathrin-mediated endocytic process. CS-PLGA NS demonstrated low cytotoxicity, 
      similar to non-PLGA NS.
FAU - Tahara, Kohei
AU  - Tahara K
AD  - Laboratory of Pharmaceutical Engineering, School of Pharmaceutical Science, Aichi 
      Gakuin University, 1-100, Kusumoto, Chikusa, Nagoya, Aichi 464-8650, Japan.
FAU - Sakai, Takeshi
AU  - Sakai T
FAU - Yamamoto, Hiromitsu
AU  - Yamamoto H
FAU - Takeuchi, Hirofumi
AU  - Takeuchi H
FAU - Hirashima, Naohide
AU  - Hirashima N
FAU - Kawashima, Yoshiaki
AU  - Kawashima Y
LA  - eng
PT  - Journal Article
DEP - 20090729
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Clathrin)
RN  - 0 (Drug Carriers)
RN  - 0 (Hypertonic Solutions)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - 9012-76-4 (Chitosan)
SB  - IM
MH  - Adenocarcinoma/*metabolism
MH  - Biological Transport, Active
MH  - Cell Line, Tumor
MH  - Cell Survival/drug effects
MH  - Chemistry, Pharmaceutical
MH  - Chitosan/chemistry/*metabolism/toxicity
MH  - Clathrin/metabolism
MH  - Coated Pits, Cell-Membrane/metabolism
MH  - Dose-Response Relationship, Drug
MH  - *Drug Carriers
MH  - Endocytosis
MH  - Humans
MH  - Hypertonic Solutions
MH  - Kinetics
MH  - Lactic Acid/chemistry/*metabolism/toxicity
MH  - Lung Neoplasms/*metabolism
MH  - Microscopy, Confocal
MH  - *Nanospheres
MH  - Particle Size
MH  - Polyglycolic Acid/chemistry/*metabolism/toxicity
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Spectrometry, Fluorescence
MH  - Surface Properties
MH  - Technology, Pharmaceutical/methods
MH  - Temperature
EDAT- 2009/08/04 09:00
MHDA- 2010/02/03 06:00
CRDT- 2009/08/04 09:00
PHST- 2009/04/23 00:00 [received]
PHST- 2009/06/25 00:00 [revised]
PHST- 2009/07/22 00:00 [accepted]
PHST- 2009/08/04 09:00 [entrez]
PHST- 2009/08/04 09:00 [pubmed]
PHST- 2010/02/03 06:00 [medline]
AID - S0378-5173(09)00495-5 [pii]
AID - 10.1016/j.ijpharm.2009.07.023 [doi]
PST - ppublish
SO  - Int J Pharm. 2009 Dec 1;382(1-2):198-204. doi: 10.1016/j.ijpharm.2009.07.023. 
      Epub 2009 Jul 29.