Enhancement of the oral bioavailability of isopropoxy benzene guanidine though complexation with hydroxypropyl-β-cyclodextrin

被引：8

作者：

Lu, Yixing ^{[1
,2
]}

Yang, Liuye ^{[1
,2
]}

Zhang, Wanying ^{[1
,2
]}

Xie, Shiting ^{[1
,2
]}

Zhao, Feifei ^{[1
,2
]}

Peng, Xianfeng ^{[3
]}

Qin, Zonghua ^{[3
]}

Zeng, Dongping ^{[1
,2
]}

Zeng, Zhenling ^{[1
,2
]}

机构：

[1] South China Agr Univ, Coll Vet Med, Natl Risk Assessment Lab Antimicrobial Resistance, Guangdong Prov Key Lab Vet Pharmaceut Dev & Safet, Guangzhou 510642, Peoples R China

[2] Guangdong Lab Lingnan Modern Agr, Guangzhou, Peoples R China

[3] Guangzhou Insighter Biotechnol Co Ltd, Guangzhou, Peoples R China

来源：

DRUG DELIVERY | 2022年 / 29卷 / 01期

关键词：

Isopropoxy benzene guanidine; hydroxypropyl-beta-cyclodextrin; dissolution; bioavailability; pharmacokinetics; INCLUSION COMPLEX; 2-HYDROXYPROPYL-BETA-CYCLODEXTRIN;

D O I：

10.1080/10717544.2022.2118400

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Isopropoxy benzene guanidine (IBG) is a novel substituted benzene guanidine analogue with antibacterial activity against multidrug-resistant bacteria. However, the bioavailability of IBG is not optimal due to its finite aqueous solubility, thus hampering its potential therapeutic exploitation. In this study, we prepared IBG/hydroxypropyl-beta-CD (IBG/HP-beta-CD) complex, and characterized it by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffraction, and scanning electron microscopy. Physicochemical characterization indicated that the crystal morphology of IBG transformed into an amorphous state, thus forming IBG/HP-beta-CD inclusion complexes. Complexation with HP-beta-CD significantly improve the aqueous solubility, pharmaceutical properties, absorption, and bioavailability of IBG.

引用

页码：2824 / 2830

页数：7

共 28 条

[1] Preparation and in vitro characterization of rosuvastatin calcium incorporated methyl beta cyclodextrin and Captisol(R) inclusion complexes [J].

Al-Heibshy, Fawaz N. S. ;

Basaran, Ebru ;

Ozturk, Naile ;

Demirel, Muzeyyen .

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2020, 46 (09) :1495-1506

[2] Preparation and characterization of a synthetic curcumin analog inclusion complex and preliminary evaluation of in vitro antileishmanial activity [J].

Alves Pinto, Luciana Matos ;

Adeoye, Oluwatomide ;

Thomasi, Sergio Scherrer ;

Francisco, Ana Paula ;

Carvalheiro, Manuela Colla ;

Cabral-Marques, Helena .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2020, 589

[3] Antibiotic development - economic, regulatory and societal challenges [J].

Ardal, Christine ;

Balasegaram, Manica ;

Laxminarayan, Ramanan ;

McAdams, David ;

Outterson, Kevin ;

Rex, John H. ;

Sumpradit, Nithima .

NATURE REVIEWS MICROBIOLOGY, 2020, 18 (05) :267-274

[4] Cyclodextrin-Drug Inclusion Complexes: In Vivo and In Vitro Approaches [J].

Carneiro, Simone Braga ;

Costa Duarte, Fernanda Ilary ;

Heimfarth, Luana ;

Siqueira Quintans, Jullyana de Souza ;

Quintans-Junior, Lucindo Jose ;

da Veiga Junior, Valdir Florencio ;

Neves de Lima, Adley Antonini .

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 2019, 20 (03)

[5] Antimicrobial Resistance in ESKAPE Pathogens [J].

De Oliveira, David M. P. ;

Forde, Brian M. ;

Kidd, Timothy J. ;

Harris, Patrick N. A. ;

Schembri, Mark A. ;

Beatson, Scott A. ;

Paterson, David L. ;

Walker, Mark J. .

CLINICAL MICROBIOLOGY REVIEWS, 2020, 33 (03)

[6] Formation of inclusion complex of enrofloxacin with 2-hydroxypropyl-β-cyclodextrin [J].

Ding, Yili ;

Pang, Yuchang ;

Vara Prasad, Chamakura V. N. S. ;

Wang, Bingyun .

DRUG DELIVERY, 2020, 27 (01) :334-343

[7] 2-hydroxypropyl-β-cyclodextrin (HP-β-CD):: A toxicology review [J].

Gould, S ;

Scott, RC .

FOOD AND CHEMICAL TOXICOLOGY, 2005, 43 (10) :1451-1459

[8] Emergence of plasmid-mediated high-level tigecycline resistance genes in animals and humans [J].

He, Tao ;

Wang, Ran ;

Liu, Dejun ;

Walsh, Timothy R. ;

Zhang, Rong ;

Lv, Yuan ;

Ke, Yuebin ;

Ji, Quanjiang ;

Wei, Ruicheng ;

Liu, Zhihai ;

Shen, Yingbo ;

Wang, Gang ;

Sun, Lichang ;

Lei, Lei ;

Lv, Ziquan ;

Li, Yun ;

Pang, Maoda ;

Wang, Liyuan ;

Sun, Qiaoling ;

Fu, Yulin ;

Song, Huangwei ;

Hao, Yuxin ;

Shen, Zhangqi ;

Wang, Shaolin ;

Chen, Gongxiang ;

Wu, Congming ;

Shen, Jianzhong ;

Wang, Yang .

NATURE MICROBIOLOGY, 2019, 4 (09) :1450-1456

[9]

Higuchi T, 1965, Phase Solubility Studies, P117

[10] Enhanced oral bioavailability of koumine by complexation with hydroxypropyl-β-cyclodextrin: preparation, optimization, ex vivo and in vivo characterization [J].

Hu, Qing ;

Fu, Xiaoling ;

Su, Yanping ;

Wang, Yanfang ;

Gao, Sihuan ;

Wang, Xiaoqin ;

Xu, Ying ;

Yu, Changxi .

DRUG DELIVERY, 2021, 28 (01) :2415-2426

← 1 2 3 →