PMID- 23251090
OWN - NLM
STAT- MEDLINE
DCOM- 20130408
LR  - 20211021
IS  - 1178-2013 (Electronic)
IS  - 1176-9114 (Print)
IS  - 1176-9114 (Linking)
VI  - 7
DP  - 2012
TI  - Formation of ion pairing as an alternative to improve encapsulation and 
      anticancer activity of all-trans retinoic acid loaded in solid lipid 
      nanoparticles.
PG  - 6011-20
LID - 10.2147/IJN.S38953 [doi]
AB  - This work aims to develop solid lipid nanoparticles (SLNs) loaded with retinoic 
      acid (RA) to evaluate the influence of two lipophilic amines, stearylamine (SA) 
      and benethamine (BA), and one hydrophilic, triethylamine (TA), on 
      drug-encapsulation efficiency (EE) and cytotoxicity in cancer cell lines. The 
      SLNs were characterized for EE, size, and zeta potential. The mean particle size 
      decreased from 155 +/- 1 nm (SLNs without amine) to 104 +/- 4, 95 +/- 1, and 96 +/- 1 nm 
      for SLNs prepared with SA, BA, and TA, respectively. SA-RA-loaded SLNs resulted 
      in positively charged particles, whereas those with TA and BA were negatively 
      charged. The EEs were significantly improved with the addition of the amines, and 
      they increased from 36% +/- 6% (without amine) to 97% +/- 2%, 90% +/- 2%, and 100% +/- 1% 
      for SA, TA, and BA, respectively. However, stability studies showed higher EE for 
      BA-RA-loaded SLNs than TA-RA-loaded SLNs after 30 days. The formulations 
      containing SA loaded or unloaded (blank SLNs) with RA were cytotoxic in normal 
      and cancer cell lines. In contrast, the blank SLNs containing TA or BA did not 
      show cytotoxicity in human breast adenocarcinoma cells (MCF-7), while RA-loaded 
      SLNs with the respective amines were significantly more cytotoxic than free RA. 
      Furthermore, the cytotoxicity of BA-RA-loaded SLNs was significantly higher than 
      TA-RA-loaded SLNs. These findings are in agreement with the data obtained in the 
      evaluation of subdiploid DNA content and cell-cycle analysis, which showed better 
      anticancer activity for BA-RA-loaded SLNs than TA-RA-loaded SLNs and free RA. 
      Taken together, these findings suggest that the BA-RA-loaded SLN formulation is a 
      promising alternative for the intravenous administration of RA in the treatment 
      of cancer.
FAU - Carneiro, Guilherme
AU  - Carneiro G
AD  - Department of Pharmaceutics, Faculty of Pharmacy, Federal University of Minas 
      Gerais, Belo Horizonte, Brazil.
FAU - Silva, Elton Luiz
AU  - Silva EL
FAU - Pacheco, Layssa Alves
AU  - Pacheco LA
FAU - de Souza-Fagundes, Elaine Maria
AU  - de Souza-Fagundes EM
FAU - Correa, Natassia Caroline Resende
AU  - Correa NC
FAU - de Goes, Alfredo Miranda
AU  - de Goes AM
FAU - de Oliveira, Monica Cristina
AU  - de Oliveira MC
FAU - Ferreira, Lucas Antonio Miranda
AU  - Ferreira LA
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20121212
PL  - New Zealand
TA  - Int J Nanomedicine
JT  - International journal of nanomedicine
JID - 101263847
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Ions)
RN  - 0 (Lipids)
RN  - 0 (Nanocapsules)
RN  - 5688UTC01R (Tretinoin)
SB  - IM
MH  - Antineoplastic Agents/administration & dosage
MH  - Cell Line, Tumor
MH  - Crystallization/methods
MH  - Diffusion
MH  - Drug Synergism
MH  - Humans
MH  - Ions
MH  - Lipids/*chemistry
MH  - Nanocapsules/*chemistry/*ultrastructure
MH  - Neoplasms, Experimental/*drug therapy/*pathology
MH  - Treatment Outcome
MH  - Tretinoin/*administration & dosage/*chemistry
PMC - PMC3525049
OTO - NOTNLM
OT  - all-trans retinoic acid
OT  - antitumor activity
OT  - cancer
OT  - ion pairing
OT  - solid lipid nanoparticles
OT  - treatment
EDAT- 2012/12/20 06:00
MHDA- 2013/04/09 06:00
PMCR- 2012/12/12
CRDT- 2012/12/20 06:00
PHST- 2012/12/20 06:00 [entrez]
PHST- 2012/12/20 06:00 [pubmed]
PHST- 2013/04/09 06:00 [medline]
PHST- 2012/12/12 00:00 [pmc-release]
AID - ijn-7-6011 [pii]
AID - 10.2147/IJN.S38953 [doi]
PST - ppublish
SO  - Int J Nanomedicine. 2012;7:6011-20. doi: 10.2147/IJN.S38953. Epub 2012 Dec 12.