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China Pharmacy ; (12): 943-949, 2022.
Article in Chinese | WPRIM | ID: wpr-923596


OBJECTIVE To optimize the pr eparation technology of the baicalin lipid nano foam aerosol (BC-LN-FA). METHODS Baicalin lipid nanoparticle (BC-LN)and BC-LN-FA were prepared by the thin film dispersion method and homogeneous emulsification method ,respectively,using baicalin (BC) as the model drug. The preparation technology was optimized by Box-Behnken design-response surface methodology using particle size and encapsulation efficiency (EE)as indexes ,with dosage , emulsifier dosage ,co-emulsifier dosage and homogenization time as factors. The morphology ,particle size ,polymerdispersity index(PDI),EE,the viscosity ,the foam dissolution rate and in vitro transdermal release of BC-LN-FA were characterized. RESULTS The optimal technology included 25 mg BC ,40 mg emulsifier (mass ratio of stearic acid-soybean lecithin-glycerol was 1∶1∶1),30 mg co-emulsifier (mass ratio of octadecanol-lactic acid was 1∶1),homogenization time of 20 min. Results of 3 times of validation tests showed that particle size of prepared BC-LN-FA was (151.70±2.40)nm,EE was (68.62±1.16)%;the deviation of them from the predicted value (particle size of 150.80 nm,EE of 67.02%)were 0.60% and 2.39% respectively. The BC-LN-FA prepared by the optimal process was light yellow opalescence ,uniform in particle size and round-like in shape. The viscosity,the foam dissolution rate ,the content of BC and PDI were (122.92±5.09)mPa·s,(65.32±3.22)%,(7.01±0.12)% and(0.199±0.006),respectively. At 48 h,the cumulative release rates of BC-LN-FA in phosphate buffer saline (PBS)at pH 7.4, 6.8,5.0 were(54.12±2.69)%,(57.85±4.25)% and(59.47±1.83)%,respectively;those of free BC in PBS at pH 7.4 was only (15.04±1.43)%. CONCLUSIONS The optimized technology is stable and feasible. Prepared BC-LN-FA has a uniform particle size,high digestion rate and certain viscosity.

Acta Pharmaceutica Sinica B ; (6): 271-282, 2021.
Article in English | WPRIM | ID: wpr-881136


The chemotherapy combined with photothermal therapy has been a favorable approach for the treatment of breast cancer. In present study, nanoparticles with the characteristics of photothermal/matrix metalloproteinase-2 (MMP-2) dual-responsive, tumor targeting, and size-variability were designed for enhancing the antitumor efficacy and achieving "on-demand" drug release markedly. Based on the thermal sensitivity of gelatin, we designed a size-variable gelatin nanoparticle (GNP) to encapsulate indocyanine green (ICG) and doxorubicin (DOX). Under an 808 nm laser irradiation, GNP-DOX/ICG responded photothermally and swelled in size from 71.58 ± 4.28 to 160.80 ± 9.51 nm, which was beneficial for particle retention in the tumor sites and release of the loaded therapeutics. Additionally, GNP-DOX/ICG showed a size reduction of the particles to 33.24 ± 4.11 nm and further improved drug release with the degradation of overexpressed MMP-2 in tumor. In the subsequently performed

Article in Chinese | WPRIM | ID: wpr-805158


Objective@#To determine the HIV infection of a 13-year-old leukemia patient Wei using molecular tracing technique.@*Methods@#Three blood samples were collected from the persons who were associated with HIV positive blood donation member Lang. The viral load was tested and pol gene was sequenced and analyzed. At the same time using HyPhy2.2.4 and Cytoscape 3.6.1 to establish the molecular network with these 3 samples sequences and other HIV subtypes sequences obtained from Luzhou.@*Results@#The HIV-1 viral load test result of the three patients were: Lang 933 CPS /ml (treated, blood donor), Wei (blood recipitent) 89 813 CPS /ml, Deng (blood recipitent) 85 158 CPS /ml. The subtype of HIV-1 of these three samples were all recombinant HIV CRF01_AE, and the pol gene similarity was 98.8% (Lang and Wei), 99.7% (Lang and Deng), and 99.1% (Wei and Deng), respectively. The gene sequences of the three samples were linked into clusters (the gene distance was less than 0.004).@*Conclusions@#The patient Wei with leukemia was infected with HIV-1 due to blood transfusion during the seroconversion period, and the three patients were more likely to be infected with the same HIV-1 strain. It is necessary to popularize the use of high-sensitivity nucleic acid detection method in blood collection and supply institutions, which can effectively improve the safety of blood use.