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Drug Dev Ind Pharm. 2017 Sep;43(9):1557-1565. doi: 10.1080/03639045.2017.1326931. Epub 2017 May 30.

Nanoparticulation improves bioavailability of Erlotinib.

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a Department of Biochemistry and Molecular Biology , Yonsei University College of Medicine , Seoul , Korea.
c Department of Health, Social, Clinical Pharmacy , College of Pharmacy, Chung-Ang University , Seoul , Korea.
d Bio-Synectics, Inc. , Seoul , Korea.
e Department of Biological and Chemical Engineering , Hongik University , Sejong , Korea.
b Integrated Genomic Research Center for Metabolic Regulation , Seoul , Korea.



Nanoparticulation using fat and supercritical fluid (NUFSTM) is a drug delivery platform technology enabling efficient and effective formulation of poorly soluble drugs. We performed experiments to examine whether NUFS™ could improve poor bioavailability and reduce fed-fasted bioavailability variances of erlotinib (Ert).


NUFS-Ert was prepared using NUFS™ technology; its physical properties were characterized, and drug release was measured. Furthermore, in vitro and in vivo efficacy tests and pharmacokinetic analysis were performed.


NUFS-Ert nanoparticles had an average size of 250 nm and were stable for 2 months at 40 °C, 4 °C, and room temperature. The dissolution rate of NUFS-Ert increased in bio-relevant dissolution media. NUFS-Ert was more potent in inhibiting EGF signaling and in suppressing the proliferation of A549, a human non-small cell lung cancer cell line. Furthermore, A549 xenografts in BALB/c nude mice treated with NUFS-Ert regressed more efficiently than those in the mice treated with vehicle or Tarceva®. In addition, experimental lung metastasis was more efficiently inhibited by NUFS-Ert than by Tarceva®. The relative bioavailability of NUFS-Ert compared with that of Tarceva® was 550% and the ratio of the area under the concentration-time curve (AUC) of fed state to the AUC of fasted state was 1.8 for NUFS-Ert and 5.8 for Tarceva®.


NUFS-Ert could improve poor bioavailability and reduce fed-fasted bioavailability variances of Ert. NUFS-Ert was more efficacious than Tarceva®.


Bioavailability; Erlotinib; NUFS-Ert; fed-fasted variance; pharmacokinetics

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