1.Research progress on local anesthetic drug delivery systems based on covalent modification strategies
Jia-xing YAO ; Zi-fu LIU ; Yue-qin ZHENG
Acta Pharmaceutica Sinica 2024;59(12):3215-3221
This review introduced the research progress of covalent modification strategies in local anesthetic drug delivery systems. As a commonly used and multimodal analgesic drug, local anesthetics have limited duration of action and potential toxicity in clinical application. In order to prolong the analgesic effect and reduce systemic toxicity, researchers are committed to the development of sustained-release local anesthetics with long-lasting dose-controlled-release functions. When it comes to the delivery of local anesthetics, the covalent modification strategy is a key approach. By covalently binding drugs to large molecule carriers, covalent modification strategies can improve drug stability, targeting and delivery efficiency. Macromolecular prodrugs can modulate the kinetic process of the drug, so that the drug is released in the form of the active ingredient and achieve better therapeutic effects. In recent years, stimulus-responsive macromolecular prodrugs have become a research hotpot for local anesthetic drug delivery systems, and the stimulus-responsive performance of macromolecular prodrugs can rapidly release drugs under internal and external stimulus conditions, and maintain low toxicity and high efficiency in blood circulation and normal tissues. These emerging research directions provide important guidance for prolonging the analgesic effect of local anesthetics and reducing systemic toxicity, and provide new idea for the development of more effective drug delivery systems in the future.
2.Antibacterial Activity Observation of TGC, MH and PB on the Pan-resistant Acinetobacter Baumannii in Vitro
Hua ZHANG ; Jie ZHAN ; Jinrong CANG ; Zi FU ; Qiaodi GUI ; Ying LIU ; Miao CHEN ; Yanyan GONG
Journal of Modern Laboratory Medicine 2015;(4):93-95
Objective To observe tigecycline (TGC),minocycline (MH)and polymyxin B (PB)in vitro antibacterial activity of pan-resistant Acinetobacter baumannii (PDR-Ab)for clinical treatment,provide the basis for infection control.Methods Collected 76 patients’clinical specimens used for no repeat count of isolation and identification with pan-resistant Acineto-bacter baumannii in Shaanxi Provincial People’s Hospital from October 2013 to March 2013.Used tigecycline,minocycline and polymyxin B to do susceptibility testing with disk diffusion method (KB).Results 76 pan-resistant Acinetobacter bau-mannii ,sensitive to the rate for tigecycline and polymyxin B were 100% sensitivity rate of minocycline and intermediary rates were 67.11%,27.63%.Conclusion Tigecycline,minocycline and polymyxin B for the Pan-resistant Acinetobacter bau-mannii had good in vitro antibacterial activity.It provide a reference for clinical pan-resistant Acinetobacter baumannii infec-tions caused by diseases treatment.
6.Late course accelerated hyperfractionation radiotherapy for nasopharyngeal carcinoma
Xia-Yun HE ; Zi-Qiang PAN ; Shao-Qin HE ; Su-Lan HUAN ; Ci-Xi FU ; Tai-Fu LIU ;
Chinese Journal of Radiation Oncology 2005;0(06):-
Objective To study the efficacy of late course accelerated fractionation(LCAF) radio- therapy in the treatment of nasopharyngeal carcinoma(NPC).The end-po s were local control,radiation-in- duced complications,factors influencing survival.Methods From December 1995 to April 1998,178 NPC patients were admitted for radiation treatment.The radiation beam used was ~(60)Co?or 6 MV X-ray.For the first two-thirds of the treatment,two daily fractions of 1.2 Gy were given to the primary lesion ,with an interval of≥6 hours,5 days per week to a total dose of 48 Gy/40 fractions,over a period of 4 weeks.For the last one third of the treatment,i.e.beginning from the 5th week,an accelerated hyperfractionation schedule was carried out.The dose per fraction was increased to 1.5 Gy,2 fractions per day with an interval of≥6 hours,the total dose for this part of the protocol was 30 Gy/20 fractions over 2 weeks.Thus the total dose was 78 Gy in 60 fractions in 6 weeks.Results All patients completed the treatment.Acute mucosi- tis:none in 2 patients,Grade 1 in 43,Grade 2 in 78,Grade 3 in 52,and Grade 4 in 3 patients.Local control rate:the 5-year nasopharyngeal local control rate was 87.7%,and the cervical lymph node local control rate was 85.7%.The 5-year distant metastasis rate was 26.1%,and 5-year survivals was 67.9%. Sixteen patients had radiation-induced cranial nerve palsy.Conclusions With this treatment schedule, patient's tolerance is good,local control and 5 year survivals are better than control groups of conventional fractionation and hyperfractionation radiotherapy.Radiation-related late complication does not increase.Ran- domized clinical trials are being carried out to further confirm the efficacy of LCAF for nasopharyngeal carci- noma.
7.Corticosteroid?induced Osteonecrosis of the Femoral Head:Detection, Diagnosis, and Treatment in Earlier Stages
Liu LI?HUA ; Zhang QING?YU ; Sun WEI ; Li ZI?RONG ; Gao FU?QIANG
Chinese Medical Journal 2017;(21):2601-2607
Objective: This review aimed to provide a current recommendation to multidisciplinary physicians for early detection, diagnosis, and treatment of corticosteroid?induced osteonecrosis of the femoral head (ONFH) based on a comprehensive analysis of the clinical literature. Data Sources: For the purpose of collecting potentially eligible articles, we searched for articles in the PubMed, Cochrane Library, Embase, and CNKI databases up to February 2017, using the following key words: "corticosteroid", "osteonecrosis of the femoral head","risk factors", "diagnosis", "prognosis", and "treatment". Study Selection: Articles on relationships between corticosteroid and ONFH were selected for this review. Articles on the diagnosis, prognosis, and intervention of earlier?stage ONFH were also reviewed. Results: The incidence of corticosteroid?induced ONFH was associated with high doses of corticosteroids, and underlying diseases in certain predisposed individuals mainly occurred in the first 3 months of corticosteroid prescription. The enhanced awareness and minimized exposure to the established risk factors and earlier definitive diagnosis are essential for the success of joint preservation. When following up patients with ONFH, treatment should be started if necessary. Surgical treatment yielded better results than conservative therapy in earlier?stage ONFH. The ideal purpose of earlier intervention and treatment is permanent preservation of the femoral head without physical restrictions in daily living. Conclusions: Clinicians should enhance their precaution awareness of corticosteroid?induced ONFH. For high?risk patients, regular follow?up is very important in the 1st year after high?dose prescription of corticosteroids. Patients with suspected ONFH should be referred to orthopedists for diagnosis and treatment in its earlier stage to preserve the joint.
8.Impact factors for hidden blood loss after primary total knee arthroplasty.
Fu-qiang GAO ; Zi-jian LI ; Ke ZHANG ; Yan-qing LIU ; Hua TIAN ; Yan LIU ; Zhong-jun LIU
Chinese Journal of Surgery 2011;49(5):419-423
OBJECTIVETo investigate the relative factors for hidden blood loss (HBL) after primary total knee arthroplasty (TKA).
METHODSA retrospective study of 422 consecutive patients who underwent primary TKA between October 2007 and August 2009 was carried on. There were 60 male and 362 female patients with a mean age of 65.7 years. The HBL was calculated according to Gross formula. The effect of patient gender, age, body mass index (BMI), pre-operative diagnosis, unilateral or simultaneous bilateral TKA, tourniquet time, type of prosthesis, postoperative anticoagulation method and deep vein thrombosis (DVT) on the postoperative HBL were analyzed.
RESULTSThe HBL in patients underwent unilateral TKA was significantly lower than that in those underwent simultaneous bilateral TKA [(1284 ± 207) ml vs. (2248 ± 504) ml, P = 0.000]. Unvaried analysis showed that the HBL were associated with BMI, tourniquet time, prosthesis type and postoperative anticoagulation method. Multivariate linear regression analysis showed that the impact factors of postoperative HBL include BMI, tourniquet time and prosthesis type.
CONCLUSIONSBMI, bilateral simultaneous TKA, tourniquet time and intercondylar open prosthesis impact the HBL after primary TKA. However, the influence of gender, age, diagnosis, postoperative anticoagulation method and DVT on the HBL are not significant.
Adolescent ; Adult ; Aged ; Aged, 80 and over ; Arthroplasty, Replacement, Knee ; Female ; Humans ; Male ; Middle Aged ; Osteoarthritis, Knee ; surgery ; Postoperative Hemorrhage ; Regression Analysis ; Retrospective Studies ; Young Adult
9.Hydrogen rich water protects against myocardial ischemia/reperfusion injury in rats
Zan WANG ; Li LIU ; Zhe ZHANG ; Xiao-Yu SUN ; Xiang-Zi LI ; Zhi-Lin LI ; Fu-Lin LIU ; Yu-Juan ZHOU
Chinese Journal of Tissue Engineering Research 2018;22(8):1229-1234
BACKGROUND: Increasing evidence has indicated that low-concentration hydrogen or hydrogen rich water or hydrogen saturated saline exerts a protective effect on various diseases, such as myocardial ischemia/reperfusion injury. OBJECTIVE: To explore the protective effect of hydrogen rich water on myocardial ischemia/reperfusion injury. METHODS: Forty-eight Wistar rats were equally randomized into control and hydrogen-rich groups, and then subdivided into ischemic preconditioning, ischemia, and ischemia/reperfusion groups (n=8 rats in each subgroup). The myocardial ischemia/reperfusion model was established in the heart of each rat by the following procedures: reverse perfusion for 10 minutes, room temperature for 20 minutes, and reperfusion for 20 minutes. The control rats was perfused with pre-oxygenated (95% O2plus 5% CO2) 37 ℃ K-R solution and the hydrogen-rich group was perfused with pre-oxygen-equilibrated (95% O2plus 5% CO2) 37 ℃ K-R solution plus hydrogen-rich water (0.6 mmol/L, pH=7.3). Subsequently, the heart was removed, the pathological changes of the myocardial tissues were observe by hematoxylin-eosin staining, the activities of lactic dehydrogenase and creatine kinase in the myocardial tissues were determined, and the levels of tumor necrosis factor-α and interleukin-1β were detected by ELISA. RESULTS AND CONCLUSION: In the control group, the activity of lactic dehydrogenase at the ischemic and ischemia/reperfusion stages was significantly higher than that at the ischemic preconditioning stage (P < 0.05), and the activity of creatine kinase at the ischemia/reperfusion stage was significantly higher than that at the ischemic preconditioning and ischemic stages (P < 0.05). In the hydrogen-rich group, there was no significant difference in the activities of lactic dehydrodenase and creatine kinase at each stage, but the activities of at the ischemia/reperfusion stage was significantly lower than those in the control group (P < 0.05). In the two groups, the order of the levels of tumor necrosis factor-α and interleukin-1β was as follows: the ischemia/reperfusion stage > ischemic stage > ischemic preconditioning stage (P < 0.05). The levels of above factors in the hydrogen-rich group were significantly lower than those in the control group (P < 0.05). Our findings imply that hydrogen rich water has protective effect on myocardial ischemia/reperfusion injury of the rat hearts in vitro,which may be by reducing the expression of tumor necrosis factor-α and interleukin-1β, and further alleviating the inflammatory response.
10.Risk factors for lower limb swelling after primary total knee arthroplasty.
Fu-Qiang GAO ; Zi-Jian LI ; Ke ZHANG ; David HUANG ; Zhong-Jun LIU
Chinese Medical Journal 2011;124(23):3896-3899
BACKGROUNDTotal knee arthroplasty (TKA) is a successful surgical technique for patients with advanced knee osteoarthritis; however, some peri-operative complications can not be predicted or avoided completely. This study aimed to investigate the factors affecting limb swelling after primary total knee arthroplasty, to guide and improve patient rehabilitation.
METHODSUsing a hospital database, we retroactively analyzed the mean changes in limb circumferences of 286 consecutive patients who underwent primary unilateral total knee arthroplasty between October 2007 and August 2009. The lower limb circumference change was calculated and analyzed statistically. The influence of age, gender, body mass index, the presence of deep vein thrombosis, methods of anti-coagulation, operation time, hidden blood loss, and type of prosthesis on post-operative lower limb swelling was studied.
RESULTSSwelling was most pronounced from the third to the fifth post-operative day and usually occurred in both lower limbs. Swelling was significantly more pronounced in the operated limb than in the non-operated limb. The swelling above the knee was also significantly greater than that below the knee. The change in limb circumference at 10 cm above the knee was significantly different between the patients with body mass index ≤ 25 kg/m(2) and those with body mass index > 25 kg/m(2). However, the change in limb circumference at 10 cm below the knee was not significantly different between the two groups. There was no statistically significant difference in limb swelling between different age groups (P > 0.05). Similarly, gender, methods of anti-coagulation, the presence of deep vein thrombosis, the type of prosthesis, and operation time did not significantly affect post-operative limb swelling. Multivariate linear regression showed that the factors affecting post-operative limb swelling were body mass index and hidden blood loss.
CONCLUSIONSLower limb swelling after total knee arthroplasty is related to early post-operative hidden blood loss. The patient's hemoglobin level should be monitored. The degree of limb swelling is correlated with the patient's body mass index and the amount of hidden blood loss. Early intramuscular deep vein thrombosis formation has little effect on limb swelling.
Adult ; Aged ; Aged, 80 and over ; Arthroplasty, Replacement, Knee ; adverse effects ; Edema ; etiology ; Female ; Humans ; Lower Extremity ; surgery ; Male ; Middle Aged ; Postoperative Period ; Retrospective Studies ; Risk Factors ; Young Adult