The clinical application of solid lipid particles(SLPs)is hampered due to the need for advanced nano/micro-suspension production technology.This research aims to establish a pilot-scale production line employing high-...The clinical application of solid lipid particles(SLPs)is hampered due to the need for advanced nano/micro-suspension production technology.This research aims to establish a pilot-scale production line employing high-speed shears as emulsification equipment.The primary purpose is to manufacture nano/micro-suspensions using solid lipid particles(SLPs).The study also exhaustively introduces and analyzes the regulatory schemes for process parameters and formulations at various stages of production.The process and formulation endured optimization through orthog-onal or single-factor tests at various production steps:laboratory research,small-scale trial production,and pilot production.Quality standards for the product were determined,and key parameters were obtained at each stage.The laboratory research demonstrated that the optimal SLPs comprised 15 mL 3%polyvinyl alcohol(PVA)per 1.0 g tilmicosin and 2.5 g carnauba wax(WAX).During small-scale production,modifications were made to the volume of the aqueous phase,emulsifier concentration,and emulsification strength,setting them to 16 mL,5%,and 2200 r/min,respectively.In the pilot production stage,the shear time was considered optimal at eight min.The impurity,content,polydispersion coefficient(PDI),and size of the pilot product were<3%,5%,0385 and 2.64μm,respectively.Among the several parameters studied,heating temperature,drug-lipid ratio,and emulsifier concentration were identified as the main factors affecting product quality,and they were regulated at 100℃,1:3,and 5%,respectively.A novel hot melt emulsification shear method aided the development of a new solid lipid-based suspension from its preliminary stages in the laboratory to pilot production.This innovation is expected to enhance solid lipid-based suspensions'industrial evolution extensively.展开更多
Metal‒organic frameworks(MOFs)are porous materials that combine high stability,large surface areas,excellent porosity,and low toxicity.The rapid development of these drugs has opened new opportunities to enhance drug ...Metal‒organic frameworks(MOFs)are porous materials that combine high stability,large surface areas,excellent porosity,and low toxicity.The rapid development of these drugs has opened new opportunities to enhance drug efficacy with reduced adverse effects.To enhance the pharmacological effects of poorly soluble,easily degraded,lowpermeability drugs can be covalently bound,adsorbed,or encapsulated in MOF nanopores.This strategy prevents premature release during transport and allows release at the target site,triggered by bond breakage or MOF structure collapse in pathological microenvironments,together with surface functional modifications.In this review,we initially summarize the antibacterial capabilities,easy functional modifications,and flexible structural properties of MOFs,as well as the standard classification of MOFs for drug delivery and their synthesis methods.We subsequently discuss functional modifications for active targeting and several pathological responsiveness tactics for targeted drug delivery,including the pH response,ion response,ATP response,redox response,magnetic reactivity,and light response.Finally,the incumbent challenges and future directions of the use of MOFs for drug delivery are proposed.This review aims to help researchers more clearly understand the properties and stimulus‐responsive mechanisms of MOFs to design more effective and targeted nanosystems for drug delivery.展开更多
基金supported by the Fundamental Research Funds for the Central Universities(2662020DKPY008)the National Natural Science Foundation of China(grant No.31772797)。
文摘The clinical application of solid lipid particles(SLPs)is hampered due to the need for advanced nano/micro-suspension production technology.This research aims to establish a pilot-scale production line employing high-speed shears as emulsification equipment.The primary purpose is to manufacture nano/micro-suspensions using solid lipid particles(SLPs).The study also exhaustively introduces and analyzes the regulatory schemes for process parameters and formulations at various stages of production.The process and formulation endured optimization through orthog-onal or single-factor tests at various production steps:laboratory research,small-scale trial production,and pilot production.Quality standards for the product were determined,and key parameters were obtained at each stage.The laboratory research demonstrated that the optimal SLPs comprised 15 mL 3%polyvinyl alcohol(PVA)per 1.0 g tilmicosin and 2.5 g carnauba wax(WAX).During small-scale production,modifications were made to the volume of the aqueous phase,emulsifier concentration,and emulsification strength,setting them to 16 mL,5%,and 2200 r/min,respectively.In the pilot production stage,the shear time was considered optimal at eight min.The impurity,content,polydispersion coefficient(PDI),and size of the pilot product were<3%,5%,0385 and 2.64μm,respectively.Among the several parameters studied,heating temperature,drug-lipid ratio,and emulsifier concentration were identified as the main factors affecting product quality,and they were regulated at 100℃,1:3,and 5%,respectively.A novel hot melt emulsification shear method aided the development of a new solid lipid-based suspension from its preliminary stages in the laboratory to pilot production.This innovation is expected to enhance solid lipid-based suspensions'industrial evolution extensively.
基金supported by the National Natural Science Foundation of China(Grant No.32273064)Project 2662023DKPY004 supported by the Fundamental Research Funds for the Central Universities.
文摘Metal‒organic frameworks(MOFs)are porous materials that combine high stability,large surface areas,excellent porosity,and low toxicity.The rapid development of these drugs has opened new opportunities to enhance drug efficacy with reduced adverse effects.To enhance the pharmacological effects of poorly soluble,easily degraded,lowpermeability drugs can be covalently bound,adsorbed,or encapsulated in MOF nanopores.This strategy prevents premature release during transport and allows release at the target site,triggered by bond breakage or MOF structure collapse in pathological microenvironments,together with surface functional modifications.In this review,we initially summarize the antibacterial capabilities,easy functional modifications,and flexible structural properties of MOFs,as well as the standard classification of MOFs for drug delivery and their synthesis methods.We subsequently discuss functional modifications for active targeting and several pathological responsiveness tactics for targeted drug delivery,including the pH response,ion response,ATP response,redox response,magnetic reactivity,and light response.Finally,the incumbent challenges and future directions of the use of MOFs for drug delivery are proposed.This review aims to help researchers more clearly understand the properties and stimulus‐responsive mechanisms of MOFs to design more effective and targeted nanosystems for drug delivery.
