PMID- 32723273
OWN - NLM
STAT- MEDLINE
DCOM- 20211021
LR  - 20211021
IS  - 1875-5704 (Electronic)
IS  - 1567-2018 (Linking)
VI  - 18
IP  - 2
DP  - 2021
TI  - Quetiapine Fumarate Loaded Nanostructured Lipid Carrier for Enhancing Oral 
      Bioavailability: Design, Development and Pharmacokinetic Assessment.
PG  - 184-198
LID - 10.2174/1567201817999200728135119 [doi]
AB  - AIMS: The study aimed at developing and characterizing Nanostructured Lipid 
      Carriers (NLC) of Quetiapine Fumarate (QF) by Design of Experiment (DoE) for the 
      enhancement of bioavailability. BACKGROUND: QF, an anti-psychotic drug, has an 
      oral bioavailability of 9% due to hepatic first- pass metabolism necessitating 
      the use of high doses. Its side effects are dose -related and enhancement in 
      bioavailability would result in minimization of side effects. OBJECTIVE: The 
      objective of the study was the enhancement of bioavailability of the NLC of QF by 
      preferential lymphatic uptake. METHODS: Hot emulsification-ultrasonication was 
      the method of formulation using PrecirolATO5 and Oleic acid as solid and liquid 
      lipids respectively. Poloxamer188 and Phospholipon90G were used as surfactant and 
      stabilizer respectively. Solid:liquid lipid ratio and Phospholipon90G amount were 
      independent variables and percent Entrapment Efficiency (%EE), Particle Size (PS) 
      dependent variables during optimization by Central Composite Design. RESULTS: The 
      optimized formulation showed a %EE of 77.21%, PS of 140.2 nm and surface charge 
      of - 19.9mV. Higuchi kinetic model was followed during the in-vitro release. TEM 
      revealed spherical, smooth nanoparticles. A pharmacokinetic study in rats showed 
      AUC0-infinity of QF-NLC to be 3.93 times that of QF in suspension, suggesting 
      significant enhancement in bioavailability. An increase in AUC0-infinity in 
      cycloheximide untreated rats' group of QF-NLC by 2.43 times as compared to 
      cycloheximide treated group, confirmed lymphatic absorption of QF- NLC. 
      CONCLUSION: The results validated DoE as an appropriate tool for developing QF 
      loaded NLC and proved NLC to be a promising delivery system for the enhancement 
      of oral bioavailability of QF.
CI  - Copyright(c) Bentham Science Publishers; For any queries, please email at 
      epub@benthamscience.net.
FAU - Agarwal, Shweta
AU  - Agarwal S
AD  - Department of Pharmaceutical Sciences, IKG Punjab Technical University, 
      Kapurthala, Punjab, India.
FAU - HariKumar, S L
AU  - HariKumar SL
AD  - CUJ, Ranchi, India.
FAU - Negi, Poonam
AU  - Negi P
AD  - School of Pharmaceutical Sciences, Shoolini University, Solan, H.P, India.
FAU - Upadhyay, Navneet
AU  - Upadhyay N
AD  - School of Pharmaceutical Sciences, Shoolini University, Solan, H.P, India.
FAU - Garg, Rajeev
AU  - Garg R
AD  - Department of Pharmaceutics, Amar Shaheed Baba Ajit Singh Jujhar Singh Memorial, 
      College of Pharmacy, Bela, Ropar, Punjab, India.
LA  - eng
PT  - Journal Article
PL  - United Arab Emirates
TA  - Curr Drug Deliv
JT  - Current drug delivery
JID - 101208455
RN  - 0 (Drug Carriers)
RN  - 0 (Lipids)
RN  - 2S3PL1B6UJ (Quetiapine Fumarate)
SB  - IM
MH  - Animals
MH  - Drug Carriers
MH  - Lipids/chemistry
MH  - *Nanoparticles
MH  - *Nanostructures
MH  - Particle Size
MH  - Quetiapine Fumarate
MH  - Rats
OTO - NOTNLM
OT  - NLC
OT  - Quetiapine fumarate
OT  - bioavailability
OT  - nanostructured lipid carrier
OT  - pharmacokinetic
OT  - phospholipon90G
EDAT- 2020/07/30 06:00
MHDA- 2023/02/25 06:00
CRDT- 2020/07/30 06:00
PHST- 2020/03/19 00:00 [received]
PHST- 2020/04/22 00:00 [revised]
PHST- 2020/05/28 00:00 [accepted]
PHST- 2020/07/30 06:00 [pubmed]
PHST- 2023/02/25 06:00 [medline]
PHST- 2020/07/30 06:00 [entrez]
AID - CDD-EPUB-108570 [pii]
AID - 10.2174/1567201817999200728135119 [doi]
PST - ppublish
SO  - Curr Drug Deliv. 2021;18(2):184-198. doi: 10.2174/1567201817999200728135119.