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Brief

Chinese Traditional and Herbal Drugs is supervised by Chinese Pharmaceutical Association and sponsored by Tianjin Institute of Pharmaceutical Research and Chinese Pharmaceutical Association. Launched in 1970, the journal is an academic journal with a broad scope in publishing research papers, brief reports, reviews, dissertations, and special treatises on the recent achievements of basic study, production, quality control, and clinic application on traditional Chinese medicine and Chinese materia medica. The journal is included in CA, JST and CSCD.
Editorial Board

Editor-in-Chief
Tang Lida

Director
Chen Changqing

A new seco-triterpene from roots of Rosa laevifgata

LIU Yi-han;TIAN Yun-gang;LONG Hua;LI Gui;LIU Zhu-xiang;WEI Hua

Chinese Traditional and Herbal Drugs,2018,Vol 49,No. 24

A new diterpene glycoside associated from marine-derived Penicillium sp. H1

WANG Cong;LIU Chun-juan;LEI Fu-hou;TAN Xue-cai;LI Xiao-yan;WANG Jing-zhen

Chinese Traditional and Herbal Drugs,2018,Vol 49,No. 24

Preparation and characteristics of TPGS-CS/PTX polymeric micelles and its in vivo intestinal absorption in rats

CHEN Tian-e;WANG Ge;CHEN Min-ting;ZHANG Wei;FENG Jian-fang

Chinese Traditional and Herbal Drugs,2018,Vol 49,No. 24

Objective To obtain the intestinal absorption of TPGS-CS/PTX polymeric micelles in rats, a drug-loaded micelle system was established by a kind of amphiphilic copolymer, namely, D-α-tocopherol polyethylene glycol 1000 succinate-chitosan (TPGS-CS) prepared by grafting D-α-tocopherol polyethyleneglycol 1000 succinate (TPGS) as the donor of the micelle hydrophobic group on chitosan (CS) as bioadhesive material, with loading paclitaxel as model drug. Methods TPGS was activated by its hydroxy-terminal carboxylation with succinic anhydride (SA) and 4-dimethylaminopyridine (DMAP). The TPGS-CS copolymer was prepared by the amidation of free amino groups on CS. The chemical structure of the TPGS-CS grafted copolymer was characterized by Fourier transform-infrared spectroscopy (FT-IR) and Nuclear magnetic resonance spectroscopy (NMR). The polymer micelle loading paclitaxel was selected as model drug and TPGS-CS/PTX was prepared by ultrasonic emulsification method. The encapsulation efficacy (EE) and drug loading (DL) were determined by high performance liquid chromatography (HPLC). The particle size, Zeta potential, and size distribution of the micelle system were measured by dynamic light scattering (DLS). The surface morphology of the micelles was investigated by Transmission electron microscopy (TEM). The in vivo intestinal absorption rate (Ka) of paclitaxel-loaded TPGS-CS micelle was calculated in rats. Results The results of FT-IR and 1H NMR indicated that the copolymer (TPGS-CS) was synthesized. The TEM result showed that the formed particles were uniform in shape without aggregation. The Ka of TPGS-CS/PTX was 20 percent higher in comparison to the reference preparation, which indicated that this polymeric micelles could increase bioavailability. Conclusion The proposed TPGS-CS copolymer was successfully synthesized in this experiment, and the drug-loaded micelles prepared by ultrasonic emulsification exhibited good characteristics as compared with the reference preparation. The Ka of paclitaxel was increased to some extent to promote oral absorption of the drug.