Aim Ciprofloxacin polylactic acid microspheres (CFX-PLA-MS) were preparedusing solvent evaporation method from a solid-in-oil-in-water emulsion system. Methods Orthogonalexperiment was used to optimize the method of C...Aim Ciprofloxacin polylactic acid microspheres (CFX-PLA-MS) were preparedusing solvent evaporation method from a solid-in-oil-in-water emulsion system. Methods Orthogonalexperiment was used to optimize the method of CFX-PLA-MS preparation. Microspheres werecharacterized in terms of morphology, size, encapsulation efficiency, drug loading and in vitro drugrelease. Results The physical state of CFX-PLA-MS was determined by scanning electron microscopy(SEM) and differential scanning calorimetry (DSC) . Microspheres formed were spherical with smoothsurfaces. Drug was enveloped in microspheres without mixing physically with PLA. The averageparticle size was 280.80 ± 0.15 μm, with over 90% of microspheres falling in the range of 250 -390 μm. The encapsulation efficiency was 65.8% ± 0.58% and the drug loading was 34.1% ± 0.51% .In vitro release study revealed a profile of sustained release of Ciprofloxacin from CFX-PLA-MS. Theaccumulated release percentage and half-life (T_(1/2) of Ciprofloxacin microspheres were 84.0% in53.2 h, and 31.9 h, respectively. Higuchi equation was Q= -0.0043 + 0.003 9 t^(1/2), r = 0.9941.Conclusion Ciprofloxacin microspheres have been successfully prepared and sustained release of CFXfrom microspheres is achieved.展开更多
Aim In vitro dissolution test and pharmacokinetics in beagle dogs wereconducted to assess the formulation of tretinoin in self-emulsifying systems. Methods Theconcentrations of tretinoin were determined by HPLC. A cro...Aim In vitro dissolution test and pharmacokinetics in beagle dogs wereconducted to assess the formulation of tretinoin in self-emulsifying systems. Methods Theconcentrations of tretinoin were determined by HPLC. A crossover study was performed in four fastingbeagle dogs with the formulation of self-emulsifying systems and commercial capsules. Results Theresults showed that the dissolution rate in 15 min of tretinoin in self-emulsifying systems washigher than 80% while that of the commercial capsules was lower than 5% . The area under the plasmaconcentration-time curve (AUC) of the self-emulsifying formulation was significantly higher andC_(max) was approximately two times greater than those of commercial capsule, respectively, Inaddition, the time taken to reach peak was shorter (2 h to 1.25 h) for self-emulsifying formulationof tretinoin. Conclusion The self-emulsifying drug delivery systems.can significantly increasetretinoin in vitro dissolution and in vivo absorption.展开更多
The key to improve the therapeutic efficacy for cancer treatment is to increase the delivery of drugs to tumors.For this purpose, tumor-microenvironment stimuliresponsive materials have great potential. Here, we prepa...The key to improve the therapeutic efficacy for cancer treatment is to increase the delivery of drugs to tumors.For this purpose, tumor-microenvironment stimuliresponsive materials have great potential. Here, we prepared a new nanomedicine by bonding the conjugate of honokiol(HNK) and 5,6-dimethylxanthenone-4-acetic acid(DMXAA)to a glutathione(GSH)-responsive nanocarrier, poly(α-lipoic acid) polyethylene glycol. The nanomedicine would disintegrate due to the high level of GSH at the tumor sites,achieving the co-delivery of HNK and DMXAA, and realizing the combination therapy through close-range killing by HNK and long-range striking by DMXAA together. In a murine 4T1 breast tumor model, this strategy exhibited high tumor inhibition rate of 93%, and provided a valuable therapeutic choice for cancer therapy.展开更多
基金National Natural Science Foundation of Guangdong Province (020885,980504).
文摘Aim Ciprofloxacin polylactic acid microspheres (CFX-PLA-MS) were preparedusing solvent evaporation method from a solid-in-oil-in-water emulsion system. Methods Orthogonalexperiment was used to optimize the method of CFX-PLA-MS preparation. Microspheres werecharacterized in terms of morphology, size, encapsulation efficiency, drug loading and in vitro drugrelease. Results The physical state of CFX-PLA-MS was determined by scanning electron microscopy(SEM) and differential scanning calorimetry (DSC) . Microspheres formed were spherical with smoothsurfaces. Drug was enveloped in microspheres without mixing physically with PLA. The averageparticle size was 280.80 ± 0.15 μm, with over 90% of microspheres falling in the range of 250 -390 μm. The encapsulation efficiency was 65.8% ± 0.58% and the drug loading was 34.1% ± 0.51% .In vitro release study revealed a profile of sustained release of Ciprofloxacin from CFX-PLA-MS. Theaccumulated release percentage and half-life (T_(1/2) of Ciprofloxacin microspheres were 84.0% in53.2 h, and 31.9 h, respectively. Higuchi equation was Q= -0.0043 + 0.003 9 t^(1/2), r = 0.9941.Conclusion Ciprofloxacin microspheres have been successfully prepared and sustained release of CFXfrom microspheres is achieved.
文摘Aim In vitro dissolution test and pharmacokinetics in beagle dogs wereconducted to assess the formulation of tretinoin in self-emulsifying systems. Methods Theconcentrations of tretinoin were determined by HPLC. A crossover study was performed in four fastingbeagle dogs with the formulation of self-emulsifying systems and commercial capsules. Results Theresults showed that the dissolution rate in 15 min of tretinoin in self-emulsifying systems washigher than 80% while that of the commercial capsules was lower than 5% . The area under the plasmaconcentration-time curve (AUC) of the self-emulsifying formulation was significantly higher andC_(max) was approximately two times greater than those of commercial capsule, respectively, Inaddition, the time taken to reach peak was shorter (2 h to 1.25 h) for self-emulsifying formulationof tretinoin. Conclusion The self-emulsifying drug delivery systems.can significantly increasetretinoin in vitro dissolution and in vivo absorption.
基金supported by the Ministry of Science and Technology of China (2018ZX09711003-012)the National Natural Science Foundation of China (51873206, 51673189, 51829302, 51503202, 51833010 and 51520105004)the Program of Scientific Development of Jilin Province (20190103033JH)
文摘The key to improve the therapeutic efficacy for cancer treatment is to increase the delivery of drugs to tumors.For this purpose, tumor-microenvironment stimuliresponsive materials have great potential. Here, we prepared a new nanomedicine by bonding the conjugate of honokiol(HNK) and 5,6-dimethylxanthenone-4-acetic acid(DMXAA)to a glutathione(GSH)-responsive nanocarrier, poly(α-lipoic acid) polyethylene glycol. The nanomedicine would disintegrate due to the high level of GSH at the tumor sites,achieving the co-delivery of HNK and DMXAA, and realizing the combination therapy through close-range killing by HNK and long-range striking by DMXAA together. In a murine 4T1 breast tumor model, this strategy exhibited high tumor inhibition rate of 93%, and provided a valuable therapeutic choice for cancer therapy.
