PMID- 20585163
OWN - NLM
STAT- MEDLINE
DCOM- 20100921
LR  - 20181201
IS  - 1361-6528 (Electronic)
IS  - 0957-4484 (Linking)
VI  - 21
IP  - 28
DP  - 2010 Jul 16
TI  - Delivery of phytochemical thymoquinone using molecular micelle modified poly(D, L 
      lactide-co-glycolide) (PLGA) nanoparticles.
PG  - 285104
LID - 10.1088/0957-4484/21/28/285104 [doi]
AB  - Continuous efforts have been made in the development of potent benzoquinone-based 
      anticancer drugs aiming for improved water solubility and reduced adverse 
      reactions. Thymoquinone is a liposoluble benzoquinone-based phytochemical that 
      has been shown to have remarkable antioxidant and anticancer activities. In the 
      study reported here, thymoquinone-loaded PLGA nanoparticles were synthesized and 
      evaluated for physico-chemical, antioxidant and anticancer properties. The 
      nanoparticles were synthesized by an emulsion solvent evaporation method using 
      anionic molecular micelles as emulsifiers. The system was optimized for maximum 
      entrapment efficiency using a Box-Behnken experimental design. Optimum conditions 
      were found for 100 mg PLGA, 15 mg TQ and 0.5% w/v poly(sodium 
      N-undecylenyl-glycinate) (poly-SUG). In addition, other structurally related 
      molecular micelles such as poly(sodium N-heptenyl-glycinate) (poly-SHG), 
      poly(sodium N-undecylenyl-leucinate) (poly-SUL), and poly(sodium 
      N-undecylenyl-valinate) (poly-SUV) were also examined as emulsifiers. All 
      investigated molecular micelles provided excellent emulsifier properties, leading 
      to maximum optimized TQ entrapment efficiency, and monodispersed particle sizes 
      below 200 nm. The release of TQ from molecular micelle modified nanoparticles was 
      investigated by dialysis and reached lower levels than the free drug. The 
      antioxidant activity of TQ-loaded nanoparticles, indicated by IC50 (mg ml( - 1) 
      TQ for 50% 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity), was highest 
      for poly-SUV emulsified nanoparticles (0.030 +/- 0.002 mg ml( - 1)) as compared 
      to free TQ. In addition, it was observed that TQ-loaded nanoparticles emulsified 
      with poly-SUV were more effective than free TQ against MDA-MB-231 cancer cell 
      growth inhibition, presenting a cell viability of 16.0 +/- 5.6% after 96 h.
FAU - Ganea, Gabriela M
AU  - Ganea GM
AD  - Department of Chemistry, Louisiana State University, Baton Rouge, LA 70803, USA.
FAU - Fakayode, Sayo O
AU  - Fakayode SO
FAU - Losso, Jack N
AU  - Losso JN
FAU - van Nostrum, Cornelus F
AU  - van Nostrum CF
FAU - Sabliov, Cristina M
AU  - Sabliov CM
FAU - Warner, Isiah M
AU  - Warner IM
LA  - eng
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20100628
PL  - England
TA  - Nanotechnology
JT  - Nanotechnology
JID - 101241272
RN  - 0 (Antioxidants)
RN  - 0 (Benzoquinones)
RN  - 0 (Biphenyl Compounds)
RN  - 0 (Emulsions)
RN  - 0 (Micelles)
RN  - 0 (Picrates)
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
RN  - O60IE26NUF (thymoquinone)
SB  - IM
MH  - Analysis of Variance
MH  - Antioxidants/pharmacology
MH  - Benzoquinones/chemistry/*pharmacology
MH  - Biphenyl Compounds/metabolism
MH  - Cell Death/drug effects
MH  - Cell Line, Tumor
MH  - Cell Survival/drug effects
MH  - Drug Delivery Systems/*methods
MH  - Emulsions
MH  - Humans
MH  - Lactic Acid/*chemistry
MH  - *Micelles
MH  - Nanoparticles/*chemistry/ultrastructure
MH  - Picrates/metabolism
MH  - Polyglycolic Acid/*chemistry
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
EDAT- 2010/06/30 06:00
MHDA- 2010/09/23 06:00
CRDT- 2010/06/30 06:00
PHST- 2010/06/30 06:00 [entrez]
PHST- 2010/06/30 06:00 [pubmed]
PHST- 2010/09/23 06:00 [medline]
AID - S0957-4484(10)52650-3 [pii]
AID - 10.1088/0957-4484/21/28/285104 [doi]
PST - ppublish
SO  - Nanotechnology. 2010 Jul 16;21(28):285104. doi: 10.1088/0957-4484/21/28/285104. 
      Epub 2010 Jun 28.