The aim of the study is to prepare flurbiprofen axetil nanoemulsion-in situ gel system (FBA/NE-ISG) and observe its ocular pharmacokinetics, rheological behavior, TEM images, irritation and cornea retention. Production of nanoemulsion was based on high-speed shear and homogenization process, and then mixed with gellan gum to prepare FBA/NE-ISG. Rheological study showed that FBA/NE-ISG possesses strong gelation capacity and its viscosity and elastic modulus increases by 2 Pa*s and 5 Pa respectively when mixed with artificial tear at the ratio of 40 : 7. TEM images suggested no significant changes in particle morphology of the pre and post gelation. Good ocular compatibility of FBA/NE-ISG was testified by the irritation test based on histological examination. In vivo fluorescence imaging system was applied to investigate the characteristics of cornea retention, and the results indicated that the nanoemulsion-in situ gel (NE-ISG) prolonged the cornea retention time significantly since K(NE-ISG) (0.008 5 min(-1) was much lower compared with flurbiprofen sodium eye drops (FB-Na, 0.03% w/v) of which the K(Eye drops) was 0.105 2 min(-1), indicated that the cornea retention time of NE-ISG was prolonged significantly. Pharmacokinetics of FBA/NE-ISG in rabbit aqueous humor was studied by cornea puncture, the MRT (12.3 h) and AUC(0-12h) (126.8 microg x min x mL(-1)) of FBA/NE-ISG was 2.7 and 2.9 times higher than that of the flurbiprofen sodium eye drops respectively, which meant that the ocular bioavailability was improved greatly by the novel preparation. Therefore, FBA/NE-ISG can enhance the ocular bioavailability by prolonging drug corneal retention significantly. What's more, encapsulated by emulsion droplets prodrug flurbiprofen (FBA) instead of flurbiprofen (FB) can reduce the ocular irritation.

The aim of the study is to prepare flurbiprofen axetil nanoemulsion-in situ gel system (FBA/NE- ISG) and observe its ocular pharmacokinetics, rheological behavior, TEM images, irritation and cornea retention. Production of nanoemulsion was based on high-speed shear and homogenization process, and then mixed with gellan gum to prepare FBA/NE-ISG. Rheological study showed that FBA/NE-ISG possesses strong gelation capacity and its viscosity and elastic modulus increases by 2 Pa?s and 5 Pa respectively when mixed with artificial tear at the ratio of 40∶7. TEM images suggested no significant changes in particle morphology of the pre and post gelation. Good ocular compatibility of FBA/NE-ISG was testified by the irritation test based on histological examination. In vivo fluorescence imaging system was applied to investigate the characteristics of cornea retention, and the results indicated that the nanoemulsion-in situ gel (NE-ISG) prolonged the cornea retention time significantly since KNE-ISG (0.008 5 min-1) was much lower compared with flurbiprofen sodium eye drops (FB-Na, 0.03% w/v) of which the KEye drops was 0.105 2 min-1, indicated that the cornea retention time of NE-ISG was prolonged significantly. Pharmacokinetics of FBA/NE-ISG in rabbit aqueous humor was studied by cornea puncture, the MRT (12.3 h) and AUC0→12 h (126.8 ?g?min?mL-1) of FBA/NE-ISG was 2.7 and 2.9 times higher than that of the flrubiprofen sodium eye drops respectively, which meant that the ocular bioavailabilitywas improved greatly by the novel preparation. Therefore, FBA/NE-ISG can enhance the ocular bioavailability by prolonging drug corneal retention significantly. What’s more, encapsulated by emulsion droplets prodrug flurbiprofen (FBA) instead of flurbiprofen (FB) can reduce the ocular irritation.

Aim: To prepare novel cubosome system for effective ocular drug delivery with dexamethasone(DEX) as model drug, and investigate its pharmacokinetic profile in rabbit aqueous humor. Methods: DEX cubosomes was prepared by the method of high-pressure homogenization, and its particle size was determined by the laser particle sizer, and the microstructure observed by cryo-TEM. In addition, Draize method was used to evaluate the ocular irritation of DEX cubosomes. Finally, aqueous humor microdialysis was utilized to evaluate its pharmacokinetics in rabbits. Results: Average diameter of DEX cubosomes was about 200 nm, and the cubic structure of the particles was evident under the cryo-TEM. It was indicated by Draize scores that this dosage form exhibited excellent ocular tolerance. Results of pharmacokinetic profiles in aqueous humor showed that AUC_(0→240) and c_(max) of the rabbit group administered with DEX cubosomes were significantly higher than those of the control group( DEX sodium phosphate eye drops), with AUC_(0→240) of the formulation Fl( 10% oil content) and F2(20% oil content) is being about 1. 8 and 2. 9 times higher than those of the control group, respectively( P <0. 05). Conclusion: The novel ocular drug delivery system of DEX cubosomes was capable of increasing significantly the drug concentration in aqueous humor, and improving the ocular bioavailability.

The aim was to prepare a novel ocular cationic microemulsion-in situ gel (CM-ISG) system with vitamin A palmitate (VAP) as model drug, and investigate the corneal retention behavior and corneal irritation of the system. VAP/CM was prepared by a process based on supply of energy, and the before-and-after gelation rheology of VAP/CM-ISG was investigated. In vitro VAP release and gel dissolution of both VAP/CM-ISG and Oculotect Gel was determined. And in vitro corneal retention behavior of both formulations was evaluated by captive bubble technique. Ocular irritation test was carried out based on the Draize method. Images of TEM showed that homogenous VAP/CM was made, and no significant differences of particle size were found between the VAP/CM and VAP/CM in Poloxamer 407 gel. Rheology study illustrated that VAP/CM reduced the phase transition temperature of Poloxamer 407 gel by 1.5 degrees C, and the elastic modulus increased about 15.7 times. The in vitro release and gel dissolution profile of both formulations exhibited the characteristics of zero order kinetics. Comparing with Oculotect Gel, desorption kinetics study of VAP/CM-ISG exhibited longer corneal retention time and smaller contact angle. Irritation test showed a good ocular compatibility of VAP/CM-ISG. Therefore, VAP/CM-ISG combined both advantages of the cationic microemulsion and in situ gel system, provided better wettability and longer ocular retention time. It might be a promising ocular drug delivery system.
Animals ; Cornea ; drug effects ; metabolism ; Delayed-Action Preparations ; Drug Carriers ; Drug Delivery Systems ; Emulsions ; Ophthalmic Solutions ; Poloxamer ; chemistry ; Rabbits ; Random Allocation ; Viscosity ; Vitamin A ; administration & dosage ; analogs & derivatives ; pharmacokinetics ; toxicity

The aim of the study is to prepare flurbiprofen axetil nanoemulsion-in situ gel system (FBA/NE-ISG) and observe its ocular pharmacokinetics, rheological behavior, TEM images, irritation and cornea retention. Production of nanoemulsion was based on high-speed shear and homogenization process, and then mixed with gellan gum to prepare FBA/NE-ISG. Rheological study showed that FBA/NE-ISG possesses strong gelation capacity and its viscosity and elastic modulus increases by 2 Pa*s and 5 Pa respectively when mixed with artificial tear at the ratio of 40 : 7. TEM images suggested no significant changes in particle morphology of the pre and post gelation. Good ocular compatibility of FBA/NE-ISG was testified by the irritation test based on histological examination. In vivo fluorescence imaging system was applied to investigate the characteristics of cornea retention, and the results indicated that the nanoemulsion-in situ gel (NE-ISG) prolonged the cornea retention time significantly since K(NE-ISG) (0.008 5 min(-1) was much lower compared with flurbiprofen sodium eye drops (FB-Na, 0.03% w/v) of which the K(Eye drops) was 0.105 2 min(-1), indicated that the cornea retention time of NE-ISG was prolonged significantly. Pharmacokinetics of FBA/NE-ISG in rabbit aqueous humor was studied by cornea puncture, the MRT (12.3 h) and AUC(0-12h) (126.8 microg x min x mL(-1)) of FBA/NE-ISG was 2.7 and 2.9 times higher than that of the flurbiprofen sodium eye drops respectively, which meant that the ocular bioavailability was improved greatly by the novel preparation. Therefore, FBA/NE-ISG can enhance the ocular bioavailability by prolonging drug corneal retention significantly. What's more, encapsulated by emulsion droplets prodrug flurbiprofen (FBA) instead of flurbiprofen (FB) can reduce the ocular irritation.
Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; adverse effects ; pharmacokinetics ; Aqueous Humor ; metabolism ; Biological Availability ; Cornea ; cytology ; drug effects ; Emulsions ; Female ; Flurbiprofen ; administration & dosage ; adverse effects ; analogs & derivatives ; pharmacokinetics ; Gels ; Male ; Nanoparticles ; Ophthalmic Solutions ; Rabbits ; Rheology ; Viscosity

OBJECTIVETo explore causes of shoulder pain and propose prevention measures in treating acromioclavicular joint dislocation.

METHODSFrom January 2005 to January 2013, 86 patients with acromioclavicular joint dislocation (Tossy III) were treated with hook plate fixation, and were divided into two groups. Bsaed on recovery of shoulder function mostly, the patients who suffered from rest pain, motion pain were named as shoulder pain group, while the patients without pain were named as painless group. In shoulder pain group, there were 21 cases including 15 males and and 6 females ranging the age from 22 to 62 years old with an average of (40.6±11.2) years old. There were 8 cases were on the left side and 13 cases were on the right side. In painless group, there were 65 cases including 36 males and and 29 females ranging the age from 19 to 65 years old with an average of (40.0±11.3) years old. There were 33 cases were on the left side and 32 cases were on the right side. The time from injury to operation ranged from 3 h to 8 d with an average of 34.6 h. Shoulder function of all patients were normal before injuried. Postoperative pain, activity of daily living (ADL), range of motion, deltoid muscle strength were compared. Anteflexion,rear protraction, abduction and upthrow of shoulder joint were also compared. Postoperative complications between two groups were observed and compared.

RESULTSAll patients were followed up from 12 to 48 months with an average of 18.5 months. Constant-Murley score were used to evaluate clinical efficacy at the least following up, and 13 cases got an excellent results, 5 moderate, 2 good and 1 poor in shoulder pain group ; while 61 cases were obtained excellent results, 3 moderate and 1 good in painless group. There were significantly differences between two groups in Constant-Murley score and activity of shoulder joint (P<0.05). In shoulder pain group, 3 cases were disconnected, 1 case occurred stress fracture, 9 cases were subacromial impingement syndrome, 5 cases occurred subluxation, 1 case occurred plate breakage and 11 cases were acromioclavicular arthritis.

CONCLUSIONChosing individual clavicular hook plate, fulfilling anatomic reset, paying attention to the repair of articular capsule ligament, and reducing hook and bone antagonism between stress is the key point of preventing and decreasing postoperative shoulder pain.

Acromioclavicular Joint ; injuries ; physiopathology ; surgery ; Adult ; Bone Plates ; adverse effects ; Case-Control Studies ; Female ; Fracture Fixation, Internal ; instrumentation ; methods ; Humans ; Male ; Middle Aged ; Postoperative Complications ; etiology ; Range of Motion, Articular ; Shoulder Dislocation ; complications ; physiopathology ; surgery ; Shoulder Pain ; etiology ; Treatment Outcome ; Young Adult

Hot Temperature ; Humans ; Occupational Exposure ; Occupational Medicine ; standards

Polymyxin E shows effective treatment of the infection induced by resistant gramnegative bacteria, but its nephrotoxicity severely limits the clinical application of this drug. In this work, methoxypolyethylene glycols 2000 (mPEG2K)-polymyxin E (PME) was synthesized via chemical grafting reaction and had been characterized. The antimicrobial activity and cytotoxicity of mPEG2K-PME in vitro were investigated on Escherichia coli and HK-2 cells, separately. Intra-abdominal infection model was further established in order to study the therapeutic effect and the toxic effect on kidney of mice. The results showed that mPEG2K-PME exhibited significant inhibitory effect on Escherichia coli and had a lower toxicity on HK-2 cells in vitro. At the same time, mPEG2K-PME had a good efficacy in the treatment of Escherichia coli infected mice in vivo. Moreover, nephrotoxicity caused by mPEG2K-PME was significantly reduced compared to free PME. mPEG2K-PME is promising in development of new preparations with high efficiency and low toxicity.

Objective To evaluate the effect of popliteal fossa fixed method to reduce the setup errors in patients with postoperative cervical carcinoma by CBCT of TrueBeam Linear accelerator.Methods 30 cases of postoperative cervical cancer patients were randomly divided into two groups,group A with popliteal fossa fixed method by trapezoidal fixation,group B with traditional vacuum pad fixation.CBCT was used to record both setup errors and rotational errors,Stroom extension formula was used to calculate the PTV expansion value coming from the two different fixation methods.Results There was significant difference in setup errors between group A and group B.The setup errors in the left-right direction (X),cranial-caudal direction (Y) and anterior-posterior direction (Z) were (0.19±0.14) cm,(0.17±0.12) cm and (0.13±0.11) cm in group A,respectively.On the contrary,the setup errors in X,Y and Z were (0.24±0.19) cm,(0.25±0.21) cm and (0.22±0.18) cm in group B,respectively.The rotational errors were 0.05°±0.02° in group A,comparing with 0.5°±0.21° in group B (P =0.00).The PTV expanded margin in group A was 0.56 cm in X direction,0.51 cm in Y direction,0.40 cm in Z direction,in comparing with 0.73 cm,0.78 cm and 0.67 cm in group B,respectively.Group A remarkably reduced the PTV,pelvis,small intestine,bladder and rectum irradiated volumes [(1 167±271) mm3 vs (1 379±297) mm3,(84±12) mm3 vs (130±17) mm3,(81±51) mm3 vs (117±64)mm3,(62±40) mm3 vs (75±47) mm3,(21±16) mm3 vs (31±21) mm3].Conclusion Popliteal fossa fixed method can reduce setup errors and improve the stability of positioning,more suitable in precise radiotherapy for postoperative cervical cancer patients,which has the value of further validation.

BACKGROUND: High molecular materials have been proved to enhance the mechanical properties of calcium phosphate bone cement, as well as attenuate the injectability of composite materials. It thereby influences the clinical application of composite materials.OBJECTIVE: To observe the compressive strength and injectability of silk fihroin compound calcium phosphate bone cement, to evaluate the effect of silk fibroin on calcium phosphate, and to investigate the feasibility of applying silk fibroin as an injectable hone substitute to repair hone defects.DESIGN, TIME AND SETTING: Controlled study was performed in the central laboratory of Analysis and Testing Center, Soochow University from September to December in 2007.MATERIALS: Calcium phosphate cement was purchased from Shanghai Rebone Biomaterials Co., Ltd; silk fibroin was offered by Institute of Material & Engineering, Soochow University.METHODS: Six groups were set with different mass fractions (0.5%, 1%, 1.5%, 2%, 2.5%, 3%) of silk fibroin, which were mixed with bone cement at a certain liquid/solid ratio of 0.4 mL/g to prepare the calcium phosphate composite. The calcium phosphate cement without silk fibroin was served as control group.MAIN OUTCOME MEASURES: The compressive strength and injectability were determined. The characteristic microstructure was observed using scanning electron microscope.RESULTS: The compressive strength increased firstly and then decreased with the addition of silk fibroin. The compressive strength of the experimental groups was remarkably higher than the control group when the silk fibroin content was 1%-2.5% (P<0.05). The injectability of the paste diminished with the addition of silk fibroin, which was statistically different when the silk fibroin content was 1.5%-3% (P<0.05). Scanning electron microscope result revealed that the silk fihroin penetrated throughout calcium phosphate crystals, which were tightly connected.CONCLUSION: Silk fibroin can improve the compressive strength of silk fibroin/calcium phosphate cement composites without significant influence of manipulation, and can widen the application field of calcium phosphate bone substitute.