PMID- 24992316
OWN - NLM
STAT- MEDLINE
DCOM- 20150514
LR  - 20140901
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 473
IP  - 1-2
DP  - 2014 Oct 1
TI  - Development of tamoxifen-phospholipid complex: novel approach for improving 
      solubility and bioavailability.
PG  - 1-9
LID - S0378-5173(14)00485-2 [pii]
LID - 10.1016/j.ijpharm.2014.06.056 [doi]
AB  - In the present study, tamoxifen-phospholipid complex (TMX-PLC) was developed and 
      evaluated for its impact on solubility and bioavailability of tamoxifen. TMX-PLC 
      was prepared by solvent evaporation method and characterized. FTIR revealed the 
      disappearance of the characteristic peaks of TMX in the complex, which can be due 
      to weakening, removal or shielding by the phospholipid molecule. This phenomenon 
      could be due to packing of TMX in the hydrophobic cavity of phospholipid and 
      being held by van der Waals forces and hydrophobic interactions. This observation 
      was confirmed by DSC and PXRD. TMX-PLC exhibited increased solubility, 
      dissolution rate with decreased distribution coefficient indicating its increased 
      hydrophilicity. Oral bioavailability of TMX and TMX-PLC were evaluated in 
      Sprague-Dawley (SD) rats. TMX-PLC exhibited considerable enhancement in the 
      bioavailability with an increase in Cmax (0.85 vs. 0.40 mug/mL), t1/2 (22.47 vs. 
      13.93 h), and AUC0-infinity (15.29 vs. 8.62 mug h/mL) with 212.25% relative 
      bioavailability. This enhancement can be attributed to the improvement of the 
      aqueous solubility of the complex and a probable decrease in its extent of 
      intestinal and hepatic metabolism. Thus, phospholipid complexation holds a 
      promising potential for increasing oral bioavailability of TMX.
CI  - Copyright (c) 2014 Elsevier B.V. All rights reserved.
FAU - Jena, Sunil Kumar
AU  - Jena SK
AD  - Department of Pharmaceutical Technology (Formulations), National Institute of 
      Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S Nagar-160062, 
      Punjab, India.
FAU - Singh, Charan
AU  - Singh C
AD  - Department of Pharmaceutical Technology (Formulations), National Institute of 
      Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S Nagar-160062, 
      Punjab, India.
FAU - Dora, Chander Parkash
AU  - Dora CP
AD  - Department of Pharmaceutical Technology (Formulations), National Institute of 
      Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S Nagar-160062, 
      Punjab, India.
FAU - Suresh, Sarasija
AU  - Suresh S
AD  - Department of Pharmaceutical Technology (Formulations), National Institute of 
      Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S Nagar-160062, 
      Punjab, India. Electronic address: ssuresh@niper.ac.in.
LA  - eng
PT  - Journal Article
DEP - 20140630
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Antineoplastic Agents, Hormonal)
RN  - 0 (Phosphatidylcholines)
RN  - 094ZI81Y45 (Tamoxifen)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents, Hormonal/blood/*chemistry/*pharmacokinetics
MH  - Area Under Curve
MH  - Biological Availability
MH  - Female
MH  - Phosphatidylcholines/*chemistry/*pharmacokinetics
MH  - Rats, Sprague-Dawley
MH  - Solubility
MH  - Tamoxifen/blood/*chemistry/*pharmacokinetics
OTO - NOTNLM
OT  - Oral bioavailability
OT  - Phospholipid
OT  - Solubility
OT  - Tamoxifen
OT  - Tamoxifen-phospholipid complex
EDAT- 2014/07/06 06:00
MHDA- 2015/05/15 06:00
CRDT- 2014/07/04 06:00
PHST- 2014/05/14 00:00 [received]
PHST- 2014/06/27 00:00 [revised]
PHST- 2014/06/28 00:00 [accepted]
PHST- 2014/07/04 06:00 [entrez]
PHST- 2014/07/06 06:00 [pubmed]
PHST- 2015/05/15 06:00 [medline]
AID - S0378-5173(14)00485-2 [pii]
AID - 10.1016/j.ijpharm.2014.06.056 [doi]
PST - ppublish
SO  - Int J Pharm. 2014 Oct 1;473(1-2):1-9. doi: 10.1016/j.ijpharm.2014.06.056. Epub 
      2014 Jun 30.