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1.
China Pharmacy ; (12): 1487-1491, 2019.
Article in Chinese | WPRIM | ID: wpr-816911

ABSTRACT

OBJECTIVE: To prepare Baicalin-loaded Polyethylene glycol-derivatized phosphatidylethanolamine (BAI@PEG-PE) nanomicelles, and to characterize it and study its cytotoxicity. METHODS: BAI@PEG-PE nanomicelles were prepared by film hydration method and their appearance characteristics were observed. The particle size, polydispersity index, Zeta potential, drug-loading amount and encapsulation efficiency of the nanomicelles were detected. Drug release of BAI raw material and BAI@PEG-PE nanomicelles in pH 7.4 phosphate buffer were compared within 1-84 h. Using coumarin 6 as fluorescent probe, the distribution of PEG-PE nanomicelles in H9c2 cardiomyocytes were observed. H9c2 cardiomyocytes were divided into model group, BAI raw material group and BAI@PEG-PE nanomicelles group. After treated with serum-free DMEM medium containing no or corresponding drugs for 0.5 h, isoproterenol was used to induce cardiomyocyte apoptosis. Nuclear morphology, cell apoptosis rate and protein expression of Bcl-2 and Bax were compared with among 3 groups. RESULTS: Prepared BAI@PEG-PE nanomicelles were uniform globular shape. The particle size was (16.7±0.8) nm, PDI was 0.11±0.01 and Zeta-potential was (-18.4±0.6) mV; drug-loading amount was (7.84±0.65)%, encapsulation efficiency was (85.7±4.9)% (n=3). Accumulative release rate was 76.5% within 84 h. BAI raw material was released completely within 24 h. PEG-PE nanomicelles could strengthen the intake of coumarin 6 in H9c2 cardiomyocytes, mainly gathering around mitochondria. Compared with model group, the apoptosis morphology of cardiomyocytes were improved significantly in BAI raw material group and BAI@PEG-PE nanomicelles group; apoptosis rate was decreased significantly; protein expression of Bcl-2 was increased significantly; protein expression of Bax was decreased significantly with statistical significance (P<0.05 or P<0.01). Above effects of BAI@PEG-PE nanomicelles group were more significant (P<0.05 or P<0.01). CONCLUSIONS: BAI@PEG-PE nanomicelles are prepared successfully, and show significant sustained-release effect and myocardial targeting, and can prevent cardiomyocyte apoptosis.

2.
Cancer Research and Clinic ; (6): 306-309, 2008.
Article in Chinese | WPRIM | ID: wpr-383741

ABSTRACT

Objective To investigate the FDG PET-CT image characteristics of bone metastases from lung cancer and the clinical value of 18F-fluorodeoxyglucose(FDG)PET-CT for diagnosis to bone metastases from lung cancer.Methods 32 cases of bone metastasis from lung cancer examined by FDG PET-CT had been studied.All of them were proved by pathology after operation or biopsy.Their FDG PET-CT diagnosis were analyzed by comparing with CT diagnosis. Results All of 115 lesions of 32 cases showed intense uptake of 18F-FDG. SUV mean was 7.47±3.48. 115 lesions located in 42 pieces of bones. Most importantly.16 lesions of occult bone metastases of 12 cases were found.The most related bone were ribs(26/115,22.61%),thoracic vertebral(21/115,18.26%),iliac bone(18/115,15.65%)and lumbar vertebral(16/115,13.91%).96 lesions(83.48%)showed lytic type on CT images,1 lesion(0.87%)showed sclerotic type,and 2 lesions(1.74%)showed mixture type.Conclusion The FDG PET-CT can early detect bone metastases from lung cancer.show their exact location,and have superiority in the screen of bone metastases from lung cancer.

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