Preparation of Sustained-release Silybin Microspheres by Spherical Crystallization Technique

Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding polymers. A differential scanning calorimeter and an X-ray diffractometer were used to investigate the dispersion state of silybin in the microspheres. The shape, surface morphology, and internal structure of the microspheres were observed using a scanning electron microscope. Characterization of the microspheres, such as average diameter, size distribution and bulk density of the microspheres was investigated. Results The particle size of the microspheres was determined mainly by the agitation speed. The dissolution rate of silybin from microspheres was enhanced by increasing the amount of the dispersing agents, and sustained by the retarding agents. The release rate of microspheres was controlled by adjusting the combination ratio of the dispersing agents to the retarding agents. The resuits of X-ray diffraction and differential scanning calorimetry analysis indicated that silybin was highly dispersed in the microspheres in amorphous state. The release profiles and content did not change after a three-month accelerated stability test at 40 ℃ and 75% relative humidity. Conclusion Sustained-release silybin microspheres with a solid dispersion structure were prepared successfully in one step by a spherical crystallization technique combined with solid dispersion technique. The preparation process is simple, reproducible and inexpensive. The method is efficient for designing sustained-release microspheres with water-insoluble drugs.

The effect of far field flow on a spherical crystal growth in the undercooled melt

The effect of convective flow on a spherical crystal growth in the undercooled melt with a moderate far field flow is studied. The asymptotic solution of the evolution of the interface of the spherical crystal growth is obtained by the matched asymptotic expansion method. The analytic result shows that the convective flow in the undercooled melt has a strong effect on the evolution of spherical crystal growth. The convective flow induced by the far field flow makes the interface of the growing spherical crystal enhance its growth velocity in the upstream direction of the far field flow and inhibit growth in the downstream direction, and the interface of the decaying spherical crystal further decay in the upstream direction and inhibit decay in the downstream direction. The maximum growth velocity of the interface of the spherical crystal influenced by the far field flow is obtained.

Characterization of physiochemical and biological properties of spherical protein crystals for sustained release

This study presents an exploration on extending the action of therapeutic proteins by crystallization strategy without new molecular entities generation.Recombinant human interferon a-2b(rhIFN),a model protein drug in this case,was crystallized using a hanging drop vapor diffusion method.A novel chelating technique with metal ions was employed to promote crystals formation.The physico-chemical characterization of the protein crystals,including morphology,particle size,X-ray diffraction,circular dichroism and biological potency evaluations were performed.In addition,the in vitro release behavior of rhIFN from crystal lattice suggested an exciting possibility of protein crystals as a longacting formulation.The work described here demonstrates the possibility of spherical crystals of biomacromolecules for controllable delivery application of therapeutic proteins.

Kinetics of Spherical Interface in Crystal Growth

The growth kinetics of spherical NiAl and CuZr crystals are studied by using molecular dynamics simulations. The growth rates of crystals are found to increase with the grain radius. The simulations show that the interface thickness and the Jackson α-faetor increase as the growth proceeds, indicating that the interface becomes increasingly rough during growth. Due to the increasing interface roughening, the fraction of repeatable growth sites at interface f is proposed to actually increase in growth. An attachment rate, which is defined as the fraction of atoms that join the crystal interface without leaving, is used to approximate f, displaying a linear increase. With this approximation, we predict the growth rates as a function of the crystal radius, and the results qualitatively agree with those from the direct simulations.

The effect of two-dimensional shear flow on the stability of a crystal interface in a supercooled melt

A model is developed based on the time-related thermal diffusion equations to investigate the effects of twodimensional shear flow on the stability of a crystal interface in the supercooled melt of a pure substance. Similar to the three-dimensional shear flow as described in our previous paper, the two-dimensional shear flow can also be found to reduce the growth rate of perturbation amplitude. However, compared with the case of the Laplace equation for a steady-state thermal diffusion field, due to the existence of time partial derivatives of the temperature fields in the diffusion equation the absolute value of the gradients of the temperature fields increases, therefore destabilizing the interface. The circular interface is more unstable than in the case of Laplace equation without time partial derivatives. The critical stability radius of the crystal interface increases with shearing rate increasing. The stability effect of shear flow decreases remarkably with the increase of melt undercooling.

Linear stability analysis on a spherical particle growing from a binary melt under the far-field flow

The solutions of temperature and solute fields around a spherical crystal growing from a binary melt under the far-field flow are obtained.Based on the results,a linear stability analysis on the spherical interface growing from the binary melt under the far-field flow is performed.It is found that the constitutional supercooling effect ahead of the spherical crystal interface under the far-field flow is enhanced compared with that without the flow.The growth rate of the perturbation amplitude at the up-wind side of the spherical crystal interface is larger than that at the down-wind side.The critical stability radius of the crystal interface decreases with the increasing far-field flow velocity.Under the far-field flow,the whole spherical interface becomes more unstable compared with that without the flow.

OPTICAL OPTIMIZATION FOR LIQUID CRYSTAL TEST BY LASER-CCD SYSTEM

For the narrowband of liner charge-coupled device （CCD） receiver and the imaging rule that cylindrical lens system can compress round facula into narrow and long one, the system is simplified and light force can concentrate on a strip facula, Considered the effective CCD length and selection of lens parameters, the system can be optimized. Correspondingly to the CCD pixels, the ray is composed of much angle information. By widening the parallel ray or increasing the lens aperture, luminous flux can be ensured when oblique incidence. Meanwhile, the effective working range can also be improved. Based on the experimental data, cylindrical system could be applied in accurate angle measurement. It has been proved feasible that the cylindrical system can be used in anchor behavior study for liquid crystal （LC） case. The low-power He-Ne laser cylindrical system can carry out the previous effect in high power laser spherical system.

Highly Selective Photocatalytic Conversion of Glucose on Holo-Symmetrically Spherical Three-Dimensionally Ordered Macroporous Heterojunction Photonic Crystal

Photocatalytic conversion of biomass is considered an effective,clean,and environmentally friendly route to obtain high-valued chemicals and hydrogen.However,the limited conversion efficiency and poor selectivity are still the main bottlenecks for photocatalytic biomass conversion.Herein,we report the highly selective photocatalytic conversion of glucose solution on holosymmetrically spherical three-dimensionally ordered macroporous TiO_(2)-CdSe heterojunction photonic crystal structure(s-TCS).The obtained s-TCS photocatalysts show excellent stability and strong light harvesting,uniform mass diffusion and exchange,and efficient photogenerated electrons/holes separation and utilization.The optimized s-TCS-4 photocatalyst displays the highest photocatalytic performance for glucose oxidation and hydrogen production.The glucose conversion,lactic acid selectivity,and yield on s-TCS-4 are about 95.9%,94.3%,and 96.4%,respectively.The photocatalytic production of lactic acid for s-TCS-4(18.5 g/L)is 2.3 times higher than the pure spherical TiO_(2) photonic crystal without CdSe(s-TiO_(2),8.1 g/L),and the hydrogen production rate of s-TCS-4 is 9.4 times that of s-TiO_(2).For the first time,we reveal that the photocatalytic conversion of glucose to lactic acid is a third-order and four-electron-involved reaction.This work could shed some new light on the efficient photocatalysis conversion of biomass to highly value-added products with high selectivity and yield,and simultaneously sustainable hydrogen evolution.

Design spherical particles of potassium peroxymonosulfate compound salt with high stability and good powder properties via an agglomeration-dissolution mechanism

With the outbreak of COVID-19,disinfection protection has become a necessary measure to prevent infection.As a new type of disinfectant,potassium peroxymonosulfate compound salt(PMS)has the advantages of good bactericidal effect,non-toxicity,high safety and stability.However,the current PMS products with irregular particle shapes lead to poor flowability,high hygroscopicity,poor stability of reactive oxygen species(ROS)and serious caking problems.In this work,an agglomeration-dissolution mechanism was designed to prepare spherical PMS particles with large size(>300μm)and high sphericity(up to 90%),effectively addressing the above problems.Shaping(dissolution and abrasion)is the key to improving sphericity,which is mainly controlled by the design of the heating mode,residence time and stirring rate.Compared with the irregular PMS particles,the large spherical particles present better flowability(angle of repose decreased by 35.80%,Carr's index decreased by 64.29%,Hausner's ratio decreased by 19.14%),lower hygroscopicity(decreased by 38.0%),lower caking ratio(decreased by 84.50%),and higher stability(the monthly loss of ROS was reduced by 61.68%).The agglomeration-dissolution mechanism demonstrates the crystallization,agglomeration,dissolution and abrasion process of inorganic salt crystals,providing an opportunity to prepare high-end inorganic crystal materials with high-quality morphologies.