Preparation and in vitro Release of Donepezil Hydrochloride Microspheres

[Objectives]To prepare donepezil hydrochloride microspheres and evaluate their quality.[Methods]The donepezil hydrochloride microspheres were prepared by emulsification-solvent evaporation method.The morphology was observed by scanning electron microscopy and the particle size distribution was determined by Laser Diffraction Method.The encapsulation efficiency,drug loading capacity,and in vitro release were determined by HPLC.[Results]The prepared donepezil hydrochloride microspheres were spherical with the average particle diameter of 15.927 μm.The drug loading capacity was 35.62%.The encapsulation efficiency was 90.32%.The drug release in vitro lasted for14 d.The release curve accorded with the first-order kinetic equation.[Conclusions]The prepared donepezil hydrochloride microspheres performed good sustained release effect in vitro,and it was expected to be used for research on Parkinson's disease.

Identification of key genes and active anti-inflammatory ingredients in Panax medicinal plants by climate-regulated callus culture combined with gene-component-efficacy gray correlation analysis

Objective:We aimed to establish a novel strategy for identifying key genes and active anti-inflammatory ingredients in Panax medicinal plants.Methods:First,fresh roots of 2-year-old Panax plants,including P.ginseng C.A.Mey.,P.quinquefolium L.,P.notoginseng(Burk.)F.H.Chen,P.japonicus C.A.Mey.,P.japonicus Mey.var.major(Burk.)C.Y.Wu et K.M.Feng,were selected as explants,and callus formation was induced under three experimental temperatures(17,24,and 30℃).Second,high-performance liquid chromatography-mass spectrometry was used to analyze the saponin content of the callus.Nitric oxide reduction efficacy was used for“component-efficacy”gray correlation analysis to find the active anti-inflammatory ingredients.Quantitative reverse-transcription polymerase chain reaction(qRT-PCR)was used to determine the inflammatory factors and verify the active ingredients’anti-inflammatory effects.Finally,qRT-PCR was used to detect the expression of key genes in the callus,and“gene-component”gray correlation analysis was used to examine the relationships between the regulatory pathway of the genes and the components.Results:Among the three experimental temperatures(17,24,and 30℃),the lowest temperature(17℃)is the most suitable for generating Panax callus.Lower-latitude native Panax notoginseng is more adaptable under high culture temperatures(24℃and 30℃)than other Panax plants.The ginsenoside contents of the callus of P.notoginseng and P.japonicus were the highest under similar climate conditions(17℃).Major anti-inflammatory components were G-Rh1,G-Rb1,G-Rg3,and G-Rh6/FloralGKa.CYP76A47 contributed to the accumulation of anti-inflammatory components.Conclusions:This study provides a strategy for the gene-component-efficacy correlational study of multi-component,multi-functional,and multi-purpose plants of the same genus.

Polydiacetylene-based poly-ion complex enabling aggregation-induced emission and photodynamic therapy dual turn-on for on-demand pathogenic bacteria elimination

Poly-ion complex(PIC)integrating non-antibiotic theranostics holds great promise in the combat against drug-resistant bacteria.Photosensitizers with aggregation-induced emission(AIE)characteristic are particularly intriguing theranostic agents,but incorporating them into antibacterial PIC to enable both fluorescence and reactive oxygen species(ROS)generation turn-on is deemed a great challenge.Here we report the development of a PIC that can dually boost the fluorescence and ROS generation in the presence of pathogen bacteria.The PIC is constructed based on an anionic polydiacetylene poly(deca-4,6-diynedioic acid)(PDDA),which completely degrades in the presence of ROS.A cationic polymer quaternized poly(2-(dimethylamino)ethyl methacrylate)(PQDMA)that can disrupt bacterial membrane is co-loaded together with a highly efficient AIE photosensitizer TPCI in the PIC.PIC is nonfluorescent initially in that PDDA can quench the AIE of TPCI in PIC.When pathogenic bacteria are present,they can disturb the assembly of PIC to release TPCI,whose fluorescence turns on sensitively to indicate the existence of bacteria.The on-demand irradiation can be subsequently applied to excite TPCI,which generates ROS to degrade PDDA and deform the PIC.As a result,TPCI and PQDMA are completely released to eliminate bacteria through a synergy of turned-on photodynamic therapy(PDT)and membrane disruption.The highly efficient detection and inhibition against both Gramnegative and Gram-positive bacteria have validated this polydiacetylene-based PIC system as an effective non-antibiotic antibacterial theranostic platform as well as a new strategy to enable“turn-on”fluorescence sensing and imaging of AIE fluorophores.