Self-assembly of CXCR4 antagonist peptide-docetaxel conjugates for breast tumor multi-organ metastasis inhibition

As a representative chemotherapeutic drug, docetaxel (DTX) has been used for breast cancer treatment for decades. However, the poor solubility of DTX limits its efficacy, and the DTX based therapy increases the metastasis risk due to the upregulation of C-X-C chemokine receptor type 4 (CXCR4) expression during the treatment. Herein, we conjugated CXCR4 antagonist peptide (CTCE) with DTX (termed CTCE-DTX) as an anti-metastasis agent to treat breast cancer. CTCE-DTX could self-assemble to nanoparticles, targeting CXCR4-upregulated metastatic tumor cells and enhancing the DTX efficacy. Thus, the CTCE-DTX NPs achieved promising efficacy on inhibiting both bone-specific metastasis and lung metastasis of triple-negative breast cancer. Our work provided a rational strategy on designing peptide-drug conjugates with synergistic anti-tumor efficacy.

Some technological studies on obtaining granular drug formulation from “Shimshin-6” traditional prescription / Монголын эм зүй, эм судлал

Introduction@#Amenorrhea has still been listed as one of common diseases among women in Mongolia. Some traditional prescription for amenorrhea, used commonly in Mongolian traditional medicine, needs more attention to dig out its scientific proof of therapeutic effect on pathogenesis of some diseases. Therefore, we aimed to research Shimshin-6 traditional prescription to develop a granule formulation for amenorrhea and other female reproductive diseases, and study its qualitative and quantitative characteristics.@*Material and method@#In this study, Shimshin-6 traditional prescription was randomly collected from 5 pharmaceutical manufacturers named as “Х-1, Х-2, Х-3, Х-4 and Х-5”. The collected prescriptions were granulated and optimized by a wet-granulation method. Then, granule spill weight and flow quality were detected in obtained granule formulation.@*Result@#20 types of granule formulation from Shimshin-6 were obtained by using 8% and 10% of gelatin, 6% and 8% of polyvinylpyrrolidone as a binder in these formulations. As a result, the suitable binder in this formulation was detected 6% of polyvinylpyrrolidone after researching the granule spill weight and flow rate. For the granule formulations of X-1, X-2 and X-5 prescriptions, the polyvinylpyrrolidone was chosen as the suitable binder due to the result from granule spill weight of the formulation. As for the X-3 and X-4 prescriptions, gelatin was the suitable binder in these formulations. After studying the flow quality of newly obtained granule formulations from “Х- 1, Х-2, Х-3, Х-4 and Х-5”, the most suitable binder was polyvinylpyrrolidone.@*Conclusion@#Altogether, these results showed that the most suitable binder for granulating Shimshin-6 traditional medicine was 6% of polyvinylpyrrolidone due to the results from granule spill weight and flow rate.

Topical antimicrobial therapy: Current status and challenges

Topically applied antibacterial agents are widely used. Opinions regarding the clinical efficacy of topical antibiotics are conflicting, and for most indications, alternative oral therapies are available. Topical application has many potential advantages over systemic therapy that includes high and sustained concentrations of drug directly at the infected site, low quantity of antibiotic needed, better compliance, fewer systemic side effects and potentially less chance of antimicrobial resistance. Despite these advantages, an important concern has been the difficulty in monitoring antibiotic dosage and duration of therapy. Most topical preparations are applied on sites with pre-existing normal bacterial flora, and the detrimental effect of antibiotic on the 'good' bacteria is difficult to control. Unnecessary exposure of the resident microflora to high drug levels may select drug-resistant phenotypes. The number of antibiotics available and the quality and composition of the formulations recommended for topical drug delivery are improving. Their role in the prevention and treatment of locally invasive infections is established for many clinical conditions. However, there is still a lacuna in the availability of pharmacokinetic (PK) knowledge of these topical preparations and translation of the same to clinical practice. In addition, reporting the clinical outcome following the use of these agents and its analysis considering the recently proposed epidemiological cut-off value-based cut-offs are also areas which merit further research. In this review, we highlight the clinical utility and the PK aspects of topical antimicrobials in various infections. We also discuss the limitations of the current antimicrobial susceptibility testing (AST) protocols and new methods for AMST for topical agents.

Application of Chitosan and it's Derivatives on Oral Drug Preparation / 中国海洋药物

Chitosan and it's derivatives have good biologic and particular physical and chemical properties. They have a wide applied foreground on drug preparations. This study introduced the recent advances of them based on widely researching the information and the actual works, and provided reference for the study of oral drug preparations.