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Objective To evaluate the quality of coenzyme Q10 emulsion with improved formulation and technology and establish an assay method. Methods Coenzyme Q10 emulsion with a high oil concentration was prepared and analyzed by HPLC. The physical and chemical properties of the emulsion were characterized, and the entrapment efficiency was determined. The stability of sterilization, freeze-thaw and dilution was investigated. The photodegradation test as well as the influencing factors, acceleration and long-term stability tests were carried out. Results The particle size, Zeta potential, pH value, content and entrapment efficiency of coenzyme Q10 emulsion were (239.5±0.8) nm、(−32.28±2.04) mV、(5.86±0.02)、 (100.59±1.24) % and (98.5±1.1) %, respectively. The stability of sterilization, freeze-thaw and dilution was good. The photolysis rate was directly proportional to the dilution ratio and inversely proportional to the drug loading. Coenzyme Q10 emulsion should be prepared in light free environment and stored at a low temperature. The pH value dropped 0.61 when it was kept in darkness at (40±2) ℃ for 10 days. It exhibited good stability both in the accelerated and long-term test. Conclusion The physicochemical properties of coenzyme Q10 emulsion with a high oil concentration meet the quality requirements for intravenous injection with good stability.
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OBJECTIVE： To evaluate the influential factors for drug-induced liver injury （DILI） caused by routine lung cancer chemotherapy plan and the rationality of hepatoprotective drugs. METHODS： The information of lung cancer patients receiving routine chemotherapy in our hospital from Feb. 1st， 2018 to Jan. 31st， 2019 were selected. The occurrence of DILI induced by different routine chemotherapy plans， the correlation of each influential factor with DILI and the rationality of hepatoprotective drugs were analyzed retrospectively. RESULTS： A total of 325 patients were involved in this study， among which 126 patients （38.77％） suffered from DILI， involving 109 first-level cases （33.54％） and 17 second-level cases （5.23％）. Routine chemotherapy plan included etoposide+cisplatin， gemcitabine+cisplatin， docetaxel+platinum， pemetrexed disodium+platinum. The clinical classification of DILI included hepatocyte injury type 44 cases （14.52％）， cholestasis type 38 cases （12.54％） and mixed type 37 cases （12.21％）. Totally 174 patients （53.54％） received hepatoprotective drugs during chemo-therapy， among whom 49 patients （28.16％） suffered from first-level DILI and 6 patients （3.45％） second-level DILI， with total incidence of 31.61％. Among patients without hepatoprotective drugs， 60 patients （39.74％） suffered from first-level DILI， and 11 patients （7.28％） suffered from second-level DILI， with total incidence of 47.02％. The incidence of DILI in patients without hepatoprotective drugs was significantly higher than those with hepatoprotective drugs （P＜0.05）. Among patients with hepatoprotective drugs， 23 patients （13.22％） used hepatoprotective drugs unreasonably， including 5 patients （2.87％） received 3 kinds or more hepatoprotective drugs； 3 patients （1.72％） received drugs with same mechanism repeatedly； 11 patients （6.32％） received 3 kinds or more drugs and drug with same mechanism repeatedly； 4 patients （2.30％） used drugs contrary to contraindication. Influential factor correlation analysis showed that there was a positive correlation between DILI and the dosage of chemotherapeutic drugs， treatment course and KPS before chemotherapy （P＜0.05）. CONCLUSIONS： KPS before chemotherapy， dosage of chemotherapeutic agents and treatment course are the main factors of DILI. There is still unreasonable use of drugs such as repeated use， unreasonable drug combination， violation of drug contraindications. The use of hepatoprotective drugs during chemotherapy can reduce the risk of DILI occurrence. Clinicians should be more aware of the methods and indications of hepatoprotective drugs in order to improve the effectiveness and safety of drug use.
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Transporter-targeted nanoparticulate drug delivery systems (nano-DDS) have emerged as promising nanoplatforms for efficient drug delivery. Recently, great progress in transporter-targeted strategies has been made, especially with the rapid developments in nanotherapeutics. In this review, we outline the recent advances in transporter-targeted nano-DDS. First, the emerging transporter-targeted nano-DDS developed to facilitate oral drug delivery are reviewed. These include improvements in the oral absorption of protein and peptide drugs, facilitating the intravenous-to-oral switch in cancer chemotherapy. Secondly, the recent advances in transporter-assisted brain-targeting nano-DDS are discussed, focusing on the specific transporter-based targeting strategies. Recent developments in transporter-mediated tumor-targeting drug delivery are also discussed. Finally, the possible transport mechanisms involved in transporter-mediated endocytosis are highlighted, with special attention to the latest findings of the interactions between membrane transporters and nano-DDS.
ABSTRACT
Docetaxel (DXT)is a member of the taxane drug class,which is used to treat breast cancer,lung cancer,gastric cancer,prostate cancer and so on.Docetaxel can be used as a single agent or in combination with other chemotherapeutic drugs.Many side effects of docetaxel have been reported in recent years.New dosage forms are developed to reduce toxicity and increase efficacy.An overview of these novel formulations of docetaxel and clinical progress will be discussed by consulting 43 literatures.