The present study aimed to develop and optimize chitosan coated solid lipid nanoparticles(chitosan-SLNs)encapsulated with methazolamide. Chitosan-SLNs were successfully prepared by a modified oil-in-water emulsificati...The present study aimed to develop and optimize chitosan coated solid lipid nanoparticles(chitosan-SLNs)encapsulated with methazolamide. Chitosan-SLNs were successfully prepared by a modified oil-in-water emulsification-solvent evaporation method with glyceryl monostearate as the solid lipid and phospholipid as the surfactant. Systematic screening of formulation factors was carried out. The optimized formula for preparation was screened by orthogonal design as well as Box-Behnken design with entrapment efficiency, particle size and zeta potential as the indexes. The entrapment efficiency of the optimized formulation(methazolamide-chitosan-SLNs)prepared was(58.5± 4.5)%,Particle size(247.7 ± 17.3) nm and zeta potential(33.5 ±3.9) mV. Transmission electron microscopy showed homogeneous spherical particles in the nanometer range. A prolonged methazolamide in vitro release profile was obtained in the optimized chitosan-SLNs suspension compared with methazolamide solution. No ocular damages were observed in the susceptibility test on albino rabbits. The results suggest that the combination of orthogonal design and Box-Behnken design is efficient and reliable in the optimization of nanocarriers, and chitosanSLNs is a potential carrier for ophthalmic administration.展开更多
Purpose:.To test the safe clinical application of sufentanil as topical ophthalmic drops by examining treated rabbit eyes for ophthalmic irritation signs or short-time toxic reactions.Methods:.Twenty-four rabbits were...Purpose:.To test the safe clinical application of sufentanil as topical ophthalmic drops by examining treated rabbit eyes for ophthalmic irritation signs or short-time toxic reactions.Methods:.Twenty-four rabbits were randomly divided into 8groups(n=3): The ocular toxicity at 14 d after eye drop administration was evaluated in groups 1 to 4, and at 30 d postadministration in groups 5 to 8..Groups 1 and 5 were treated with blank vehicle and served as normal controls..The left eyes of rabbits in groups 2 and 6 were exposed to low-dose sufentanil(5 μg, 2 drops within 5 min), groups 3 and 7 received moderate-dose sufentanil.(7.5 μg, 3 drops within 10 min),and groups 4 and 8 received high-dose sufentanil(10 μg,.4drops within 15 min). As self-controls, the right eyes of each rabbit were administered an equivalent amount of sodium chloride(9 g / L) at the same drop intervals. At 14 and 30 d after exposure to sufentanil,.ophthalmic irritation signs were evaluated and corneas were stained with fluorescein and observed by slit-lamp microscopy..Corneal endothelial counts were performed and toxic reactions were evaluated.Results: Multiple parameters were compared in the control and experimental groups by visual inspection and slit-lamp examination at 14 and 30 d after sufentanil administration..No evidence of irritation signs(including corneal opacity,.conjunctival congestion, or edema), eye secretions, iris abnormalities,.or temporal eye closure were noted..Corneal endothelial cell counts did not significantly differ between the control and experimental groups..Light microscopy revealed no pathological or morphological injury to the cornea, conjunctiva, iris, ciliary body, retina, or optic nerve in either group.The same observation outcomes were noted at 14 and 30 d after administration.Conclusion:.Single ocular administration of sufentanil at a dose of 5-10 μg in rabbits yields no ocular irritation or toxic responses at 14 or 30 d following eye drop delivery.展开更多
基金supported by grants from the National Natural Science Foundation of China(81100977)
文摘The present study aimed to develop and optimize chitosan coated solid lipid nanoparticles(chitosan-SLNs)encapsulated with methazolamide. Chitosan-SLNs were successfully prepared by a modified oil-in-water emulsification-solvent evaporation method with glyceryl monostearate as the solid lipid and phospholipid as the surfactant. Systematic screening of formulation factors was carried out. The optimized formula for preparation was screened by orthogonal design as well as Box-Behnken design with entrapment efficiency, particle size and zeta potential as the indexes. The entrapment efficiency of the optimized formulation(methazolamide-chitosan-SLNs)prepared was(58.5± 4.5)%,Particle size(247.7 ± 17.3) nm and zeta potential(33.5 ±3.9) mV. Transmission electron microscopy showed homogeneous spherical particles in the nanometer range. A prolonged methazolamide in vitro release profile was obtained in the optimized chitosan-SLNs suspension compared with methazolamide solution. No ocular damages were observed in the susceptibility test on albino rabbits. The results suggest that the combination of orthogonal design and Box-Behnken design is efficient and reliable in the optimization of nanocarriers, and chitosanSLNs is a potential carrier for ophthalmic administration.
文摘Purpose:.To test the safe clinical application of sufentanil as topical ophthalmic drops by examining treated rabbit eyes for ophthalmic irritation signs or short-time toxic reactions.Methods:.Twenty-four rabbits were randomly divided into 8groups(n=3): The ocular toxicity at 14 d after eye drop administration was evaluated in groups 1 to 4, and at 30 d postadministration in groups 5 to 8..Groups 1 and 5 were treated with blank vehicle and served as normal controls..The left eyes of rabbits in groups 2 and 6 were exposed to low-dose sufentanil(5 μg, 2 drops within 5 min), groups 3 and 7 received moderate-dose sufentanil.(7.5 μg, 3 drops within 10 min),and groups 4 and 8 received high-dose sufentanil(10 μg,.4drops within 15 min). As self-controls, the right eyes of each rabbit were administered an equivalent amount of sodium chloride(9 g / L) at the same drop intervals. At 14 and 30 d after exposure to sufentanil,.ophthalmic irritation signs were evaluated and corneas were stained with fluorescein and observed by slit-lamp microscopy..Corneal endothelial counts were performed and toxic reactions were evaluated.Results: Multiple parameters were compared in the control and experimental groups by visual inspection and slit-lamp examination at 14 and 30 d after sufentanil administration..No evidence of irritation signs(including corneal opacity,.conjunctival congestion, or edema), eye secretions, iris abnormalities,.or temporal eye closure were noted..Corneal endothelial cell counts did not significantly differ between the control and experimental groups..Light microscopy revealed no pathological or morphological injury to the cornea, conjunctiva, iris, ciliary body, retina, or optic nerve in either group.The same observation outcomes were noted at 14 and 30 d after administration.Conclusion:.Single ocular administration of sufentanil at a dose of 5-10 μg in rabbits yields no ocular irritation or toxic responses at 14 or 30 d following eye drop delivery.
