RGD and cell penetrating peptides co-modiifed paclitaxel loaded liposome inhibit the A549 cells / 中国生化药物杂志

Objective To prepare RGD and TAT co-modified paclitaxel loaded liposome(RGD/TAT-LP-PTX)for A 549 cells targeting.Method The co-modified liposome was prepared by film-ultrasonic method. The appearance,particle size,Zeta potential were evaluated. The cellular uptake by A 549 cells in vitro was used to evaluate the targeting efficiency. The anti-proliferation efficiency of RGD/TAT-LP-PTX was evaluated by MTT assay. Results The particle diameter of the co-modified liposome was (118.5±11.4) nm with the Zeta potential of (21.58±2.42 )mV. The entrapment efficiency of PTX was 86.5%. The result demonstrated that the co-modified liposome uptaken by A 549 were 2.1, 2.8 times higher than that of TAT-LP and RGD-LP, respectively. The RGD/TAT-LP-PTX shows the highest anti-proliferation efficiency. Conclusion The co-modified liposome might serve as a promising tumor delivery system of antitumor drugs.

The study of RGD modiifed paclitaxel and curcumin loaded liposome for the treatment of ovarian carcinoma in vitro and in vivo / 中国生化药物杂志

Objective To prepare RGD conjugated paclitaxel and curcumin loaded liposome and evaluate their properties and effect on the treatment of ovarian carcinoma in vitro and in vivo . Method The liposomes were prepared by thin film hydration method. The particle size,Zeta potential and entrapment efficiency were evaluated. The efficiency of cellular uptake on A 2780 cells in vitrowas evaluated. Flowcytometry were used to observe the apoptosis morphous.A 2780 cells werexenografted in athymic mice to establish the animal model, which were used to evaluate the effect of anti-cancer. Results The particle diameter of the RGDLP-PTX/Cu was (94.8±11.2) nm with the Zeta potential of (-3±2.45) mV. The entrapment efficiency of PTX and Gen were 81.8%and 84.6%respectively. The result demonstrated that RGDLP uptaken by A 2780 were 3.6 times higher than that of LP. The apoptosis assay、the inhibition of the inhibition of tumor in vivoconfirmed strong inhibitory effect ofRGDLP-PTX/Cu. Conclusion RGDLP-PTX/Cu were easy to prepare and it is a potential delivery system for the treatment of ovarian carcinoma.

Safety, Pharmacokinetic and Pharmacodynamic Studies of Batifiban Injection Following Single- and Multiple-Dose Administration to Healthy Chinese Subjects / 华中科技大学学报（医学）（英德文版）

Batifiban,a synthetic cyclic peptide,is a potent platelet glycoprotein GPⅡb/Ⅲa an-tagonist which may be useful in the treatment and prevention of acute coronary syndromes. The pharmacokinetics and pharmacodymanic (inhibition of platelet aggregation) effects,and tolerability of batifiban were investigated in healthy subjects following single bolus injection with doses of 55,110,or 220 μg/kg,or multiple doses of an bolus followed intravenous infusion for 24 h (180 μg/kg of batifiban and areas under the curve were found to be proportional to doses. Batifiban was rapidly eliminated with a half-life of approximately 2.5 h. Significant differences were noted for plasma lev-els of batifiban and areas under the curve between males and females. No significant differences in the terminal half-life were found between males and females. Batifiban reversibly inhibited ex vivo platelet aggregation in a dose- and concentration-dependent manner,consistent with its mechanism as a GP Ⅱb/Ⅲa antagonist. Single and multiple intravenous doses of batifiban were found to be safe and well tolerated in healthy subjects. These results support a bolus injection plus intravenous infusion regimen of batifiban for the treatment and prevention of acute coronary syndromes.