Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN...Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressurehomogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology,particle size with polydispersi-ty index (PI) and zeta potential were examined by atomic forcemicroscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability andin vitro drug release were also studied. The transdermal drug delivery through porcine ear skin wasevaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with theaverage size of (95.5 - 186.2) nm, the zeta potential of (-26.3- -15.7) mV and the entrapmentefficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had goodstability, the release profile in vitro fitted Higuchi equation. In comparison with conventionalhydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition withinporcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is preparedwith stable physicochemical properties. The release profile and improved drug permeation into skinmake it be a promising vehicle for transdermal drug delivery.展开更多
In the present study,we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion(SD)that facilitated solubility and dissolution rate of the poorly water soluble drug and...In the present study,we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion(SD)that facilitated solubility and dissolution rate of the poorly water soluble drug and compare with binary SD with single poloxamer.Lidocaine(LIC)was selected as a model drug,and poloxamer 188(P188)and poloxamer 407(P407)were utilized as single and mixed carriers.Depending on DSC and the dissolution testing,the appropriate ratio of SD prepared by melting method was optimized.Ternary and binary SD was characterized by DSC,XRD,SEM and FTIR.In vitro dissolution study,phase solubility study and saturated solubility study were performed to clarify solubilization from apparent phenomena and inherent reason.Moreover,stability study under different relative humidity(RH)was investigated.Physical characterizations of binary and ternary SD exhibited the formation of eutectic mixture and the presence of molecular interaction.Compared with the pure LIC,the dissolution rate and solubility of LIC in binary and ternary SDs were enhanced.The phase solubility study revealed an AL-type curve.Furthermore,the stability test indicated that ternary and binary SD was stable.The results of this study demonstrated that SD with mixed poloxamers could improve dissolution rate and solubility of poorly water-soluble drug.展开更多
文摘Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressurehomogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology,particle size with polydispersi-ty index (PI) and zeta potential were examined by atomic forcemicroscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability andin vitro drug release were also studied. The transdermal drug delivery through porcine ear skin wasevaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with theaverage size of (95.5 - 186.2) nm, the zeta potential of (-26.3- -15.7) mV and the entrapmentefficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had goodstability, the release profile in vitro fitted Higuchi equation. In comparison with conventionalhydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition withinporcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is preparedwith stable physicochemical properties. The release profile and improved drug permeation into skinmake it be a promising vehicle for transdermal drug delivery.
基金National Natural Science Fund of China(Grant No.30801552&81274095)the third key project funded by Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization(Grant No.012092002006-10)the 55th postdoctoral project(Grant No.021062001001).
文摘In the present study,we aimed to probe the possibility of using mixed poloxamers as carriers to prepare ternary solid dispersion(SD)that facilitated solubility and dissolution rate of the poorly water soluble drug and compare with binary SD with single poloxamer.Lidocaine(LIC)was selected as a model drug,and poloxamer 188(P188)and poloxamer 407(P407)were utilized as single and mixed carriers.Depending on DSC and the dissolution testing,the appropriate ratio of SD prepared by melting method was optimized.Ternary and binary SD was characterized by DSC,XRD,SEM and FTIR.In vitro dissolution study,phase solubility study and saturated solubility study were performed to clarify solubilization from apparent phenomena and inherent reason.Moreover,stability study under different relative humidity(RH)was investigated.Physical characterizations of binary and ternary SD exhibited the formation of eutectic mixture and the presence of molecular interaction.Compared with the pure LIC,the dissolution rate and solubility of LIC in binary and ternary SDs were enhanced.The phase solubility study revealed an AL-type curve.Furthermore,the stability test indicated that ternary and binary SD was stable.The results of this study demonstrated that SD with mixed poloxamers could improve dissolution rate and solubility of poorly water-soluble drug.
