PMID- 22745556
OWN - NLM
STAT- MEDLINE
DCOM- 20130124
LR  - 20220311
IS  - 1178-2013 (Electronic)
IS  - 1176-9114 (Print)
IS  - 1176-9114 (Linking)
VI  - 7
DP  - 2012
TI  - Effects of polymer molecular weight on relative oral bioavailability of curcumin.
PG  - 2957-66
LID - 10.2147/IJN.S32630 [doi]
AB  - BACKGROUND: Polylactic-co-glycolic acid (PLGA) nanoparticles have been used to 
      increase the relative oral bioavailability of hydrophobic compounds and 
      polyphenols in recent years, but the effects of the molecular weight of PLGA on 
      bioavailability are still unknown. This study investigated the influence of 
      polymer molecular weight on the relative oral bioavailability of curcumin, and 
      explored the possible mechanism accounting for the outcome. METHODS: Curcumin 
      encapsulated in low (5000-15,000) and high (40,000-75,000) molecular weight PLGA 
      (LMw-NPC and HMw-NPC, respectively) were prepared using an emulsification-solvent 
      evaporation method. Curcumin alone and in the nanoformulations was administered 
      orally to freely mobile rats, and blood samples were collected to evaluate the 
      bioavailability of curcumin, LMw-NPC, and HMw-NPC. An ex vivo experimental gut 
      absorption model was used to investigate the effects of different molecular 
      weights of PLGA formulation on absorption of curcumin. High-performance liquid 
      chromatography with diode array detection was used for quantification of curcumin 
      in biosamples. RESULTS: There were no significant differences in particle 
      properties between LMw-NPC and HMw-NPC, but the relative bioavailability of 
      HMw-NPC was 1.67-fold and 40-fold higher than that of LMw-NPC and conventional 
      curcumin, respectively. In addition, the mean peak concentration (C(max)) of 
      conventional curcumin, LMw-NPC, and HMw-NPC was 0.028, 0.042, and 0.057 mug/mL, 
      respectively. The gut absorption study further revealed that the HMw-PLGA 
      formulation markedly increased the absorption rate of curcumin in the duodenum 
      and resulted in excellent bioavailability compared with conventional curcumin and 
      LMw-NPC. CONCLUSION: Our findings demonstrate that different molecular weights of 
      PLGA have varying bioavailability, contributing to changes in the absorption rate 
      at the duodenum. The results of this study provide the rationale for design of a 
      nanomedicine delivery system to enhance the bioavailability of water-insoluble 
      pharmaceutical compounds and functional foods.
FAU - Tsai, Yin-Meng
AU  - Tsai YM
AD  - Institute of Traditional Medicine, School of Medicine, National Yang-Ming 
      University, Taipei, Taiwan. thtsai@ym.edu.tw
FAU - Chang-Liao, Wan-Ling
AU  - Chang-Liao WL
FAU - Chien, Chao-Feng
AU  - Chien CF
FAU - Lin, Lie-Chwen
AU  - Lin LC
FAU - Tsai, Tung-Hu
AU  - Tsai TH
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20120615
PL  - New Zealand
TA  - Int J Nanomedicine
JT  - International journal of nanomedicine
JID - 101263847
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - IT942ZTH98 (Curcumin)
SB  - IM
MH  - Absorption/drug effects
MH  - Administration, Oral
MH  - Animals
MH  - Biological Availability
MH  - Chromatography, High Pressure Liquid
MH  - Curcumin/*administration & dosage/*pharmacokinetics
MH  - Intestine, Small/metabolism
MH  - Lactic Acid/*chemistry/*pharmacology
MH  - Male
MH  - Molecular Weight
MH  - Nanoparticles/administration & dosage/*chemistry
MH  - Particle Size
MH  - Polyglycolic Acid/*chemistry/*pharmacology
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Rats, Sprague-Dawley
MH  - Reproducibility of Results
MH  - Tissue Distribution
PMC - PMC3384366
OTO - NOTNLM
OT  - PLGA
OT  - absorption
OT  - duodenum
OT  - molecular weight
OT  - poly(lactic-co-glycolic acid)
OT  - relative oral bioavailability
EDAT- 2012/06/30 06:00
MHDA- 2013/01/25 06:00
PMCR- 2012/06/15
CRDT- 2012/06/30 06:00
PHST- 2012/06/30 06:00 [entrez]
PHST- 2012/06/30 06:00 [pubmed]
PHST- 2013/01/25 06:00 [medline]
PHST- 2012/06/15 00:00 [pmc-release]
AID - ijn-7-2957 [pii]
AID - 10.2147/IJN.S32630 [doi]
PST - ppublish
SO  - Int J Nanomedicine. 2012;7:2957-66. doi: 10.2147/IJN.S32630. Epub 2012 Jun 15.