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.

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.

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.

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.

Objective:To investigate the relationship of the expression of VEGF-C and the metastasis of the lymphoid nodes in laryngeal cancer.Methods:Using immunohistochemistry method, the expression of VEGF-C in the tumor tissues and the density of lymphatic in adjacent tissue of laryngeal carcinoma were detected.Results:The expression of VEGF-C in laryngeal carcinoma was higher than in vocal cord polyp and in lymphoid node-positive was higher than in node-negative. Density of lymphatic capillary in adjacent tissue of laryngeal carcinoma was much higher than in normal laryngeal tissue and in lymphoid node-positive was higher than in node-negative.Conclusion:VEGF-C protein expression is close to lymphatic metastasis.

Objective To study the expression of Snail in laryngeal carcinoma and to explore its relationship with invasion and metastasis in subgroup laryngeal carcinoma cells. Method The expression of Snail protein was examined by immunohistochemistry staining in the tissue of laryngeal carcinoma. The statistical evaluation was performed to detect the correlation between the Snail protein expression and clinical features. In different subgroups of laryngeal carcinoma cells (CD 44+CD 133+cells, CD 44 and CD 133-cells), the expression of Snail and adhesion molecules E-cadherin were detected by RT-PCR,Western blot test and immunochemical staining which were studied in the correlation with invasion and metastasis. Results The result of immunohistochemical staining revealed that Snail was moderately or highly expressed in the tissue of laryngeal carcinoma significantly and higher than those in adjacent non-cancerous tissues(P<0.01). Expression of Snail was highly correlated with lymph node metastasis, tumor differentiation and clinical classification(P<0.05).However, it was not related to the age , gender and clinical type. RT-PCR and Western blot test results confirmed that the expression level of Snail was significantly higher in CD 44+CD 133+laryngeal cancer cells than in CD 44-and CD 133-laryngeal cancer cells, otherwise the expression level of E-cadherin in CD 44+CD 133+laryngeal cancer cells was significantly lower than in the CD 44-and CD 133-laryngeal cancer cells. Cell immunohistochemical staining confirmed the expression of Snail and E-cadherin were negatively correlated in CD 44+CD 133+laryngeal cancer cells. Conclusion Over expression of Snail in laryngeal carcinoma is closely related to the development of laryngeal cancer and lymph node metastasis. The expression of Snail in the CD 44+CD 133+laryngeal cancer cell subgroup is negatively correlated with adhesion molecules E-cadherin, which is a close correlation with invasion and metastasis of laryngeal cancer cells.

T cell immune checkpoint pathways contribute to tumor immune escape. Many studies have shown that immune checkpoint is demonstrably correlated with tumor grade or prognosis in several types of malignancies and immune checkpoint has become a new biological index for tumor detection and prognosis. Immune checkpoint inhibitors have shown promising tumor outcomes in clinical trials for some advanced solid tumors and it will become a new target for cancer immunotherapy. In this review we will explore the correlation between expressions of immune checkpoint-associated genes and proteins in immune microenviroment and prognosis of head and neck squamous cell carcinoma, and specifically will discuss how this pathway can be manipulated with immune therapeutic drugs.

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)