PMID- 20564384
OWN - NLM
STAT- MEDLINE
DCOM- 20101028
LR  - 20181201
IS  - 1520-6017 (Electronic)
IS  - 0022-3549 (Linking)
VI  - 99
IP  - 8
DP  - 2010 Aug
TI  - Enhanced oral bioavailability of paclitaxel formulated in vitamin E-TPGS 
      emulsified nanoparticles of biodegradable polymers: in vitro and in vivo studies.
PG  - 3552-60
LID - 10.1002/jps.22113 [doi]
AB  - This work evaluates the effects of paclitaxel loaded polymeric nanoparticles 
      (NPs) composed of poly(D,L-lactic-co-glycolic acid) (PLGA) with vitamin E TPGS as 
      emulsifier for oral chemotherapy. NPs prepared by a modified solvent 
      extraction/evaporation technique were observed in spherical shape of 200-300 nm 
      diameter with a high drug encapsulation efficiency (EE) of 80.9%. The 
      TPGS-emulsified PLGA NPs formulation of paclitaxel was found of great advantages 
      over that of Taxol. The in vitro viability experiment showed that the NP 
      formulation could be 1.28, 1.38, 1.12 times more effective than Taxol(R) after 
      24, 48, 72 h incubation with MCF-7 human breast cancer cell line at 2.5 microg/mL 
      paclitaxel concentration. In vivo evaluation confirmed the advantages of the 
      TPGS-emulsified PLGA NP formulation versus Taxol in promoting oral 
      bioavailability of paclitaxel. Such a NP formulation achieved more than 10 times 
      higher oral bioavailability than Taxol, which resulted 9.74-fold higher 
      therapeutic effect and 12.56-fold longer sustainable therapeutic time than Taxol. 
      The present proof-of-concept experimental data proved that the formulation of 
      vitamin E TPGS emulsified PLGA NPs is a promising approach for paclitaxel oral 
      administration. Oral chemotherapy by NPs formulation is feasible.
CI  - (c) 2010 Wiley-Liss, Inc. and the American Pharmacists Association
FAU - Zhao, Lingyun
AU  - Zhao L
AD  - Department of Chemical & Biomolecular Engineering, National University of 
      Singapore, Singapore. chefess@nus.edu.sg
FAU - Feng, Si-Shen
AU  - Feng SS
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - J Pharm Sci
JT  - Journal of pharmaceutical sciences
JID - 2985195R
RN  - 0 (Antineoplastic Agents, Phytogenic)
RN  - 0 (Antioxidants)
RN  - 0 (Drug Carriers)
RN  - 0 (Excipients)
RN  - 0 (Polymers)
RN  - 1406-18-4 (Vitamin E)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
RN  - O03S90U1F2 (tocophersolan)
RN  - P88XT4IS4D (Paclitaxel)
SB  - IM
MH  - Absorbable Implants
MH  - Animals
MH  - Antineoplastic Agents, Phytogenic/administration & dosage/*pharmacokinetics
MH  - Antioxidants/*chemistry
MH  - Biological Availability
MH  - Chemistry, Pharmaceutical
MH  - Chromatography, High Pressure Liquid
MH  - Drug Carriers
MH  - Electrochemistry
MH  - Excipients
MH  - Humans
MH  - Lactic Acid
MH  - Light
MH  - Microscopy, Electron, Scanning
MH  - Nanoparticles
MH  - Paclitaxel/administration & dosage/*pharmacokinetics
MH  - Particle Size
MH  - Polyethylene Glycols/chemistry
MH  - Polyglycolic Acid
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Polymers
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Scattering, Radiation
MH  - Vitamin E/*analogs & derivatives/chemistry
EDAT- 2010/06/22 06:00
MHDA- 2010/10/29 06:00
CRDT- 2010/06/22 06:00
PHST- 2010/06/22 06:00 [entrez]
PHST- 2010/06/22 06:00 [pubmed]
PHST- 2010/10/29 06:00 [medline]
AID - S0022-3549(15)32535-1 [pii]
AID - 10.1002/jps.22113 [doi]
PST - ppublish
SO  - J Pharm Sci. 2010 Aug;99(8):3552-60. doi: 10.1002/jps.22113.