PMID- 22074176
OWN - NLM
STAT- MEDLINE
DCOM- 20120920
LR  - 20151119
IS  - 1521-0464 (Electronic)
IS  - 1071-7544 (Linking)
VI  - 19
IP  - 1
DP  - 2012 Jan
TI  - Evaluation of biosafety and intracellular uptake of Cremophor EL free paclitaxel 
      elastic liposomal formulation.
PG  - 11-20
LID - 10.3109/10717544.2011.621990 [doi]
AB  - The present study examines the acute, sub-acute toxicity, and cytotoxicity of 
      paclitaxel elastic liposomal formulation in comparison to a marketed Cremophor EL 
      (polyoxyethylated castor oil):ethanol (1:1, v/v) based formulation. In the 
      previous study, Cremophor EL free paclitaxel elastic liposomal formulation was 
      developed and characterized. Cytotoxicity of formulation was evaluated by MTT 
      assay using A549 cell lines. Percentage intracellular uptake of paclitaxel 
      elastic liposomal and marketed formulation was determined using a fluorescence 
      activating cell sorting assay (FACS) and fluorescence microscopy techniques. 
      Single and repeated dose toxicity measurement showed no mortality, hematological, 
      biochemical, or histopathological changes up to a dose of 120 mg/kg for 
      paclitaxel elastic liposomal formulation, in comparison the marketed formulation 
      showed toxicity at a dose of 40 mg/kg. Maximum tolerated dose (MTD) for 
      paclitaxel elastic liposomal and marketed formulation was found to be 160 mg/kg 
      and 40 mg/kg, respectively. Results of FACS analysis showed a 94.6 +/- 2.5% 
      intracellular uptake of fluorescence marker acridine orange (AO) loaded in 
      elastic liposomes; in comparison the AO solution showed only a 19.8 +/- 1.1% 
      uptake. Paclitaxel elastic liposomal formulation seems to be a better alternative 
      for safe and effective delivery of paclitaxel. This study proves the safety and 
      higher intracellular uptake of paclitaxel elastic liposomal formulation.
FAU - Utreja, Puneet
AU  - Utreja P
AD  - Department of Pharmaceutical Sciences and Drug Research, Punjabi University, 
      Patiala, India.
FAU - Jain, Subheet
AU  - Jain S
FAU - Tiwary, A K
AU  - Tiwary AK
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20111110
PL  - England
TA  - Drug Deliv
JT  - Drug delivery
JID - 9417471
RN  - 0 (Liposomes)
RN  - 0 (Pharmaceutical Vehicles)
RN  - 6D4M1DAL6O (cremophor EL)
RN  - P88XT4IS4D (Paclitaxel)
RN  - PDC6A3C0OX (Glycerol)
SB  - IM
MH  - Animals
MH  - Cell Line, Tumor
MH  - Chemistry, Pharmaceutical
MH  - Drug Evaluation, Preclinical/methods
MH  - *Elasticity
MH  - Female
MH  - Glycerol/adverse effects/*analogs & derivatives/metabolism
MH  - Humans
MH  - Intracellular Fluid/*metabolism
MH  - Liposomes
MH  - Male
MH  - Mice
MH  - Paclitaxel/adverse effects/*metabolism
MH  - Pharmaceutical Vehicles/adverse effects
MH  - Random Allocation
MH  - Toxicity Tests, Acute/methods
EDAT- 2011/11/15 06:00
MHDA- 2012/09/21 06:00
CRDT- 2011/11/15 06:00
PHST- 2011/11/15 06:00 [entrez]
PHST- 2011/11/15 06:00 [pubmed]
PHST- 2012/09/21 06:00 [medline]
AID - 10.3109/10717544.2011.621990 [doi]
PST - ppublish
SO  - Drug Deliv. 2012 Jan;19(1):11-20. doi: 10.3109/10717544.2011.621990. Epub 2011 
      Nov 10.