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The "vicious cycle" established between tumor growth and osteolysis aggravates the process of breast cancer bone metastasis, leading to life-threatening skeletal-related events that severely reduce survival and quality of life. To effectively interrupt the "vicious cycle", innovative therapeutic strategies that not only reduce osteolysis but also relieve tumor burden are urgently needed. Herein, a bone-seeking moiety, alendronate (ALN), functionalized coordination polymer nanoparticles (DZ@ALN) co-delivering cisplatin prodrug (DSP) and antiresorptive agent zoledronate (ZOL)
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Polymorphism of drug is known to influence the stability, dissolution, bioavailability and other performance characteristics of the products. Therefore, the crystal form of the drug must be identified and determined in order to ensure consistent product performance. Even if the identification and characterization of crystal forms are performed thoroughly and the effective crystal form is selected for preparation, it is important to ensure that the effective crystal form in the final product remains unchanged. Therefore, it is essential to quantitate the content of the effective crystal form in the product to control the quality and performance of them. X-ray powder diffraction, FT-Raman, mid-IR, near-IR, terahertz pulsed spectroscopy, solid-state NMR spectroscopy, and DSC are the quantitative methods of crystal form used in the recent 10 years. This review briefly highlights the basic principles and the progress of these methods and discusses the perspective as they apply to pharmaceutical research and development.
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AIM To study the release mechanism of fenoprofen calcium (FC) from hydroxypropylmethylcellulose (HPMC) matrices. METHODS The release of FC and the erosion properties of hydrophillic matrices containing HPMC was examined at different paddle speed. The release mechanism of FC was further confirmed by evaluating the n value in Peppas equation. RESULTS The results indicate that the release of FC and the erosion of matrices exhibit zero order kinetic equation, and it exhibits line relationship between them. CONCLUSION In the first 40 min, FC mainly released by diffusion and erosion from HPMC matrix, while it was controlled by the rate of tablet erosion after 50 min.
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Objective To study the uptaking characteristics of puerarin in Caco-2 model system. Methods The transepithelial transporting character of puerarin across Caco-2 cells was investigated by changing the concentration, temperature of drug and using appropriate inhibitors. Results The transport of puerarin across Caco-2 cell monolayers was directional. With the increase of the concentration of pue-rarin, the permeability direction ratio (PDR) was decreased from 2.1 to 1.4. With the increase of temperature, PDR was increased. When the metabolic inhibitors, KCN and 2,4-dinitrophenol, were added, the PDR was decreased from 1.7 to 1.0 and 1.2, respectively. When 100 mg/L Verapamil was added, the permeability coefficient of apical to basolateral was increased from (0.84?0.18)?10-7 cm/s to (1.01?0.17)?10-7 cm/s, and the permeability coefficient of basolateral to apical was decreased from (1.43?0.18)?10-7 cm/s to (1.11?0.24)?10-7 cm/s. Conclusion The evacuation by P-glycoprotein affects the puerarin transepithelial transport across Caco-2 cells.
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AIM: In order to prepare the self-microemulsifying soft capsule(SMESC)of pueraria lobata isoflavone and investigate its dissolution property. METHODS: Through solubility experiment,self-microemulsification in vitro,phase diagram and the stability of solution,the optimum formulation was selected for pueraria lobata isoflavone.The dissolution of SMESC was measured taking the commercial tablet as reference. RESULTS: In the selected formulation,Tween-80,1,2-Propanediol and ethyl oleate were screened as emulsifier,co-emulsifier and oil phase,respectively.The optimized proportion was 65∶20∶15 .The dissolution of SMESC in the condition of distilled water,pH6.8 phosphate buffer and 0.1 mol/L HCl were more than 90% in 10 min,while those of the commercial tablet were less than 40% in 90 min. CONCLUSION:In comparison with the commercial tablet,the dissolution of pueraria lobata isoflavone is sufficiently improved at various conditions.