Nanostructured lipid carriers as oral delivery systems for improving oral bioavailability of nintedanib by promoting intestinal absorption

[Display omitted] The aim of this study was to fabricate nanostructured lipid carriers, NLCs, of nintedanib (BIBF) to improve its oral bioavailability. Two types of NLCs loaded with BIBF (BIBF-NLCs-1 and BIBF-NLCs-2) were prepared by the melt-emulsification technique. BIBF-NLCs-1 and BIBF-NLCs-2 sho...

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Bibliographic Details
Published in:International journal of pharmaceutics 2020-08, Vol.586, p.119569, Article 119569
Main Authors: Zhu, Yunjing, Liang, Xue, Lu, Cong, Kong, Yihan, Tang, Xing, Zhang, Yu, Yin, Tian, Gou, Jingxin, Wang, Yanjiao, He, Haibing
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Bioavailability
Biological Availability
Caco-2 Cells
Carcinoma, Lewis Lung - drug therapy
Cell Line, Tumor
Drug Carriers - chemistry
Drug Delivery Systems
Humans
Indoles - administration & dosage
Indoles - pharmacokinetics
Indoles - pharmacology
Intestinal Absorption
Lipids - chemistry
Male
Mice
Mice, Inbred C57BL
Nanostructured lipid carriers
Nanostructures
Nintedanib
Oral
Particle Size
Protein Kinase Inhibitors - administration & dosage
Protein Kinase Inhibitors - pharmacokinetics
Protein Kinase Inhibitors - pharmacology
Rats
Rats, Sprague-Dawley
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Summary:[Display omitted] The aim of this study was to fabricate nanostructured lipid carriers, NLCs, of nintedanib (BIBF) to improve its oral bioavailability. Two types of NLCs loaded with BIBF (BIBF-NLCs-1 and BIBF-NLCs-2) were prepared by the melt-emulsification technique. BIBF-NLCs-1 and BIBF-NLCs-2 showed nanoscale particle sizes of 142.70 ± 0.85 nm and 7.99 ± 0.06 nm, and both were positive zeta potential. Study on Caco-2 cells showed that BIBF-NLCs-1 exhibited distinct advantages at the cytological level. The oral bioavailability of BIBF-NLCs-1 and BIBF-NLCs-2 was extremely improved 3.13-fold and 2.39-fold respectively compared with BIBF solution (BIBF-Sol). And in vivo anti-tumor efficiency study in mice bearing LLC lung tumor indicated that BIBF-NLCs-1 and BIBF-NLCs-2 had excellent tumor inhibition. Besides, the two NLCs did not increase the risk of liver damage and can even reduce the incidence of gastrointestinal irritation of BIBF to some extent. In summary, NLCs are a potential oral delivery system to improve the bioavailability of BIBF by promoting intestinal absorption.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2020.119569