Preparation and detection of VEGF chitosan microspheres with different concentrations / 中华医学美学美容杂志

Objective To evaluate the effects of chitosan microspheres as the ball wall,pre pared by emulsion cross-linked VEGF chitosan microspheres.Methods 1 ％ chitosan aqueous solution as the aqueous solution and genipin as a cross-linking agent were used to detect the drug loading rate and cumulative release rate of drug-loaded microspheres by ELISA.Results VEGF chitosan microsphere size was about 5.25-20.34 μm;electron microscopy showed that microspheres surface was smooth,decentralized,and had small adhesions each other.The highest encapsulation efficiency was (56.33±3.42) ％ and the highest drug loading rate was (18.75±0.32) ng/mg.In vitro release experiments showed that the concentration of VEGF increased gradually with the passage of time.The release rate of microspheres was (32.32±2.31)％ on the first day and (86.42±1.68)％ on the 21st day.The cumulative release rate was 88.7％.Conclusions Genipin can be used to prepare chitosan microspheres loaded with different concentrations of VEGF with good performance and simple preparation process.The drug-loading rate and entrapment efficiency of the obtained microspheres are both high.

Optimization of preparation of curcumin-loaded TPGS/F127/P123 mixed micelles by uniform design methodology / 中草药

Objective: The preparation process of curcumin-loaded TPGS/F127/P123 mixed micelles was optimized with uniform design method to improve the poor solubility of curcumin in water, aiming to increase entrapment efficiency (EE), drug-loading (DL), and reduce the precipitated drug (PD). Methods: Curcumin-loaded TPGS/F127/P123 mixed micelles were prepared by thin-film hydration method with modification. Before using the uniform design, a number of preliminary experiments were conducted to identify the controlled factors such as the amount of curcumin, the dosage of TPGS, and the ratio of F127/P123. The formulation was operated by uniform design of three factors and seven levels, and its results were fitted by polynomial linear equation, the response surface, and the contour line in order to choose and verify the optimal preparation process. Results: In the optimum formulation, the dosage of curcumin was 14.0 mg, TPGS 150.0 mg, and the ratio of F127/P123 was 68: 32. The solubility of optimum formulation was (3.47 ± 0.14) mg/mL, EE (87.15 ± 4.39)%, DL (4.70 ± 0.17)%, and PD (0.33 ± 0.12)% in 48 h. Conclusion: The solubility of curcumin in TPGS/F127/P123 mixed micelles was improved after the optimization of the uniform design method, and EE and DL were also improved.

Preparation and evaluation of GEN-VES-TPGS1000 nano-micelles / 中草药

Objective: To prepare GEN-VES-TPGS nano-micelles and improve the oral bioavailability of genistein (GEN). Methods: GEN-VES-TPGS nano-micelles, made by film hydration, were evaluated with particle size, entrapment efficiency, and drug-loading as indexes. Single factor experiment was used to optimize the formulation and productive technology, including dosages of TPGS, VES, GEN, hydration volume, temperature, and time. Morphology of nano-micelles, release rate in vitro, and pharmacokinetics in rat were investigated. Results: The results showed GEN-VES-TPGS nano-micelles presented with good clarity, appropriate particle diameter (43.50 ± 1.65) nm, negative charge, when the dosages of TPGS, VES, GEN were 200, 30, and 6 mg, respectively. Meanwhile, a condition of 15 mL, 50 ℃ at 3 h to hydrate was necessary to prepare. In this setting, the encapsulation efficiency of the nano-micelles was (98.99 ± 0.69)% and drug-loading rate was (2.57 ± 0.04)%. The pharmacokinetic results in rats showed the oral bioavailability of GEN-VES-TPGS nano-micelles was 162.96% of the GEN APIs. Conclusion: The prepared GEN-VES-TPGS nano-micelles have small particle size and good stability, and increase the oral bioavailability of GEN evidently.

Investigation of anticancer drug 5-Fu loaded porous metal-organic frameworks of MIL-53 / 中国药学杂志

OBJECTIVE: To study the drug release and cytotoxicity in vitro of 5-fluorouracil (5-Fu)-loaded porous metal-organic frameworks of MIL-53. METHODS: MIL-53 was hydrothermally synthesized, and the synthetic MIL-53 was characterized by TEM, XRD, IR and TG. 5-Fu was loaded into MIL-53, and the release pattern and cytotoxicity were investigated. RESULTS: The structure of MIL-53 was confirmed. The diameter of MIL-53 was at nanometer level and MIL-53 displayed better thermo-stabilization. The highest drug loading rate was 0.431 g · g-1 MIL-53 for 5-Fu. The drug release profile of 5-Fu-loaded MIL-53 displayed a clear biphasic release pattern. Cytotoxicity test showed that MIL-53 had good biocompatility at lower concentrations. CONCLUSION: MIL-53 is a promising platform for drug delivery due to its large pore sizes for drug encapsulation and good biocompatility at lower concentrations.

Determination of Drug Loading Rate of Butyl-5-Aminosalicylic Acid-Pectin Conjugates by HPLC / 中国药房

OBJECTIVE:To establish an HPLC method for the determination of the drug loading rate of butyl-5-aminosalicylic acid-pectin conjugate.METHODS:The conjugate was hydrolyzed with base solution and neutralized with acid before being determined by HPLC.Kromasil C18 column was used as chromatographic column with mobile phase consisted of water(containing 0.15% triethylamine and 0.15% acetic acid)-methanol(95∶5,V/V).The detection wavelength was set at 240 nm.RESULTS:The calibration curve of 5-aminosalicylic acid was linear over the range of 1～100 ?g?mL-1(r=0.999 9) at an average recovery of 99.90%.Both intra-day and inter-day RSD were less than 2.25%.The drug loading rate of the conjugate was 12.76 %(n=3).CONCLUSION:The method is simple,rapid,accurate,and suitable for the determination of drug-loading rate of conjugate.