文献类型：期刊文献

英文题名：In situ phase transition of microemulsions for parenteral injection yielding lyotropic liquid crystalline carriers of the antitumor drug bufalin

作者：Li, Yawen[1,2];Angelova, Angelina[3];Liu, Jianwen[1,2];Garamus, Vasil M.[4];Li, Na[5,6];Drechsler, Markus[7];Gong, Yabin[8];Zou, Aihua[1,2,9]

机构：[1]East China Univ Sci & Technol, Sch Chem & Mol Engn, State Key Lab Bioreactor Engn, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem & Mol Engn, Inst Appl Chem, Shanghai 200237, Peoples R China;[3]Univ Paris Saclay, Univ Paris Sud, Inst Gallen Paris Sud, CNRS,UMR 8612,LabEx LERMIT, F-92296 Chatenay Malabry, France;[4]Helmholtz Zentrum Geesthacht, Ctr Mat & Coastal Res, D-21502 Geesthacht, Germany;[5]Natl Ctr Prot Sci Shanghai, Shanghai 200237, Peoples R China;[6]Shanghai Inst Biochem & Cell Biol, Shanghai 200237, Peoples R China;[7]Univ Bayreuth, Bavarian Polymerinst BPI, Keylab Electron & Opt Microscopy, D-95440 Bayreuth, Germany;[8]Yueyang Hosp Integrated Tradit Chinese & Western, Shanghai 200437, Peoples R China;[9]East China Univ Sci & Technol, Shanghai, Peoples R China

年份：2019

卷号：173

起止页码：217

外文期刊名：COLLOIDS AND SURFACES B-BIOINTERFACES

收录：;EI(收录号：20184105914394);WOS:【SCI-EXPANDED(收录号:WOS:000454377300027)】；

基金：We gratefully acknowledge the support of this work by the National Natural Science Foundation of China (Grant No. 21573070).

语种：英文

外文关键词：Bufalin; Encapsulation; In situ phase transition; Liquid crystalline carrier; SAXS; Drug release; Bioavailability

摘要：In this work, we used the small angle X-ray scattering (SAXS) method for controlled preparation of in situ forming sustained-release carriers for the antitumor drug bufalin (BUF), which has very poor solubility and a considerable cardiotoxicity in a non-encapsulated state. To that aim, we exploited the pseudo-ternary phase diagram of an oil(O)/surfactant(S)/water(W) system containing medium chain capric/caprylic triglycerides (MCT) and a co-surfactant blend of Macrogol (15)-hydroxystearate (Solutol HS 15) and sorbitan monooleate (Span 80). Two compositions with different oil contents (sample B and C) were selected from the microemulsion region of the phase diagram in order to study the effect of the aqueous environment on their structural behavior. A phase transition from a microemulsion (ME) to a liquid crystalline phase (LC) was established by SAXS upon progressive dilution. The drug bufalin (BUF) was encapsulated in the microemulsions with low viscosity, whereas the release of the drug occurred from the in situ generated lamellar liquid crystalline structures. The formulations were characterized by SAXS, dynamic light scattering (DLS), cryogenic transmission electron microscopy (Cryo-TEM), rheology, drug loading and encapsulation efficiency, and in vitro release profiles. A correlation was suggested between the structures of the in situ phase-transition formed LC-ME formulations, the differences in their viscosities and drug release profiles. The performed cytotoxicity, cell apoptosis and pharmacokinetic experiments showed an enhanced bioavailability of BUF after encapsulation. These results suggest potential clinical applications for the obtained safe in skit phase-transition sustained-release formulations of BUF.