Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions

Ting-ting Liu,1–3 Li-Qiu Mu,1–3 Wei Dai,1–3 Chuan-bang Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–3 1Department of Pharmacy, The Second Xiangya Hospital, 2Institute of Clinical Pharmacy, Central South University, 3Key Laboratory for New Techn...

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Autores principales: Liu TT, Mu LQ, Dai W, Wang CB, Liu XY, Xiang DX
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Publicado: Dove Medical Press 2016
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spelling oai:doaj.org-article:b3737b59196b4a27aa17410356593fed2021-12-02T00:10:20ZPreparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions1178-2013https://doaj.org/article/b3737b59196b4a27aa17410356593fed2016-06-01T00:00:00Zhttps://www.dovepress.com/preparation-characterization-and-evaluation-of-antitumor-effect-of-bru-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ting-ting Liu,1–3 Li-Qiu Mu,1–3 Wei Dai,1–3 Chuan-bang Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–3 1Department of Pharmacy, The Second Xiangya Hospital, 2Institute of Clinical Pharmacy, Central South University, 3Key Laboratory for New Technology of Chinese Medicine Preparations of Hunan Province, Changsha, People’s Republic of China Abstract: The purpose of this study was to prepare Brucea javanica oil cationic nanoemulsions (BJO-CN) with BJO as drug as well as oil phase and chitosan as cationic inducer, to explore the practical suitability of using cationic nanoemulsions for oral delivery of mixed oil, and to test its bioavailability and antitumor effect. BJO-CN was prepared by chitosan solution stirring method and then characterized physicochemically. The obtained BJO-CN had a spherical morphology with a positive zeta potential of 18.9 mV and an average particle size of 42.36 nm, showing high colloidal stability. The drug loading of BJO-CN was 91.83 mg·mL-1, determined by high-performance liquid chromatography with precolumn derivatization. Pharmacokinetic studies revealed that, compared with BJO emulsion (BJO-E) (the dosage of BJO-CN and BJO-E was equal to 505 mg·kg-1, calculated by oleic acid), BJO-CN exhibited a significant increase in the area under the plasma drug concentration–time curve over the period of 24 hours and relative bioavailability was 1.6-fold. Furthermore, the antitumor effect of BJO-CN in the orthotopic mouse model of lung cancer was evaluated by recording the median survival time and the weight of lung tissue with tumor, hematoxylin and eosin staining, and immunohistochemical technique. Results of anticancer experiments illustrated that, even though the administrated dosage in the BJO-CN group was half of that in the BJO-E group, BJO-CN exhibited similar antitumor effect to BJO-E. Moreover, BJO-CN had good synergistic effect in combination therapy with vinorelbine. These results suggested that cationic nanoemulsions are an effective and promising delivery system to enhance the oral bioavailability and anticancer effect of BJO. Keywords: oleic acid, chitosan, combined chemotherapy, orthotopic mouse model of lung cancer, pharmacokineticsLiu TTMu LQDai WWang CBLiu XYXiang DXDove Medical PressarticleBrucea Javanica Oilchitosancationic nanoemulsionorthotopic mouse model of lung cancerantitumorMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2016, Iss default, Pp 2515-2529 (2016)
institution DOAJ
collection DOAJ
language EN
topic Brucea Javanica Oil
chitosan
cationic nanoemulsion
orthotopic mouse model of lung cancer
antitumor
Medicine (General)
R5-920
spellingShingle Brucea Javanica Oil
chitosan
cationic nanoemulsion
orthotopic mouse model of lung cancer
antitumor
Medicine (General)
R5-920
Liu TT
Mu LQ
Dai W
Wang CB
Liu XY
Xiang DX
Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions
description Ting-ting Liu,1–3 Li-Qiu Mu,1–3 Wei Dai,1–3 Chuan-bang Wang,1–3 Xin-Yi Liu,1–3 Da-Xiong Xiang1–3 1Department of Pharmacy, The Second Xiangya Hospital, 2Institute of Clinical Pharmacy, Central South University, 3Key Laboratory for New Technology of Chinese Medicine Preparations of Hunan Province, Changsha, People’s Republic of China Abstract: The purpose of this study was to prepare Brucea javanica oil cationic nanoemulsions (BJO-CN) with BJO as drug as well as oil phase and chitosan as cationic inducer, to explore the practical suitability of using cationic nanoemulsions for oral delivery of mixed oil, and to test its bioavailability and antitumor effect. BJO-CN was prepared by chitosan solution stirring method and then characterized physicochemically. The obtained BJO-CN had a spherical morphology with a positive zeta potential of 18.9 mV and an average particle size of 42.36 nm, showing high colloidal stability. The drug loading of BJO-CN was 91.83 mg·mL-1, determined by high-performance liquid chromatography with precolumn derivatization. Pharmacokinetic studies revealed that, compared with BJO emulsion (BJO-E) (the dosage of BJO-CN and BJO-E was equal to 505 mg·kg-1, calculated by oleic acid), BJO-CN exhibited a significant increase in the area under the plasma drug concentration–time curve over the period of 24 hours and relative bioavailability was 1.6-fold. Furthermore, the antitumor effect of BJO-CN in the orthotopic mouse model of lung cancer was evaluated by recording the median survival time and the weight of lung tissue with tumor, hematoxylin and eosin staining, and immunohistochemical technique. Results of anticancer experiments illustrated that, even though the administrated dosage in the BJO-CN group was half of that in the BJO-E group, BJO-CN exhibited similar antitumor effect to BJO-E. Moreover, BJO-CN had good synergistic effect in combination therapy with vinorelbine. These results suggested that cationic nanoemulsions are an effective and promising delivery system to enhance the oral bioavailability and anticancer effect of BJO. Keywords: oleic acid, chitosan, combined chemotherapy, orthotopic mouse model of lung cancer, pharmacokinetics
format article
author Liu TT
Mu LQ
Dai W
Wang CB
Liu XY
Xiang DX
author_facet Liu TT
Mu LQ
Dai W
Wang CB
Liu XY
Xiang DX
author_sort Liu TT
title Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions
title_short Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions
title_full Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions
title_fullStr Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions
title_full_unstemmed Preparation, characterization, and evaluation of antitumor effect of Brucea javanica oil cationic nanoemulsions
title_sort preparation, characterization, and evaluation of antitumor effect of brucea javanica oil cationic nanoemulsions
publisher Dove Medical Press
publishDate 2016
url https://doaj.org/article/b3737b59196b4a27aa17410356593fed
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