Preparation Of Folic Acid Coupling Aloe Chitosan Nanoparticles And Preliminary Study Of Its Targeted Anti-tumor Activity

ObjectiveMalignant tumors are present-day threats to human health the number onekiller, cancer incidence rates have been on an upward trend, cancer treatment isone of the hotspots of study by scholars today. The antitumor activity ofpolysaccharide from aloe vera, this paper mainly medicines, natural non-toxicbiodegradable chitosan as carrier, folic acid as the ligand, preparation of aloechitosan nanoparticles by ionic cross-linking. Also visit aloe chitosannanoparticle characterization and in vitro drug-release performances; Surfacemodified nanoparticle surface and connection of folic acid, so that it hastargeted and used infrared spectroscopy test connection. By making thenanoparticles containing fluorescent dye fluorescein isothiocyanate (FITC) toinvestigate the SMMC-7721of tumor cell uptake properties of nanoparticles,prove that the coupling of folic acid nanoparticles have targeted, so performanceis better than the ordinary non-coupled folate intake of nanoparticles. Bydetermined by MTT method to investigate blank nanoparticles toxicity for tumorcells SMMC-7721, and proved that nanoparticles materials non-toxic;comparison of aloe chitosan nanoparticles, folate conjugated chitosannanoparticles and aloe raw in vitro inhibitory effects on tumor cell SMMC-7721activity, prove aloe chitosan nanoparticles, folic acid coupling chitosan nanoparticles with aloe reversed-phased also has anti-tumor effect, at the sametime that folate conjugated chitosan nanoparticles of aloe has targeted, betterthan ordinary aloe chitosan nanoparticles and aloe. By acridine orange (AO)staining, more intuitive to show the safety, non-toxic blank coupled folatechitosan nanoparticle vector; Packet of folate conjugated chitosan nanoparticlescontaining aloe polysaccharide has obvious inhibitory effect on tumor cellproliferation of SMMC-7721.MethodsPreparation of aloe chitosan nanoparticles by ionic crosslinking method.With drug and chitosan volume ratio, pH, stirring speed as factors, theencapsulation efficiency of nanoparticles as evaluation index; The responsesurface method was used to study the best combination of variables and theresponse value, screening the best prescription and technology; The aloechitosan nanoparticles in vitro release study. Using EDC and NHS to connectthe folic acid and nanoparticles and to detect the connection of folic acid andnanoparticles by infrared. Investigated by MTT assay blank nanoparticles affectcell viability and proved non-toxic materials, compare the original drug aloe,aloe chitosan nanoparticles, folate-conjugated chitosan nanoparticles for tumorcell viability inhibition of SMMC-7721effects. Nanoparticles containingfluorescent dye fluorescein isothiocyanate (FITC), study of tumor cellsSMMC-7721for ordinary nanoparticles and nanoparticles coupled folic acidintake. By acridine orange (AO) staining, visit blank folic acid coupled chitosannanoparticles with packs containing aloe vera of folate-coupled chitosannanoparticles on proliferation of tumor cells.ResultThe chitosan nanoparticles size is uniform, complete structure, for thespherical or class spherical by ionic crosslinking method. Preparation of aloe chitosan nanoparticles using the response surface method was designed andoptimized prescription process is: the drug quantity and amount of chitosan ratiois0.14, pH3.0, mixing speed is294r/min. In terms of nanoparticle coating rateand forecast deviation is smaller. Aloe chitosan nanoparticles with slow releaseproperties, in vitro release process accord with Ritger-Peppas model. Detectedby infrared absorption spectrum of folic acid and nanoparticles to connectcoupling. Determined by MTT experiment results show that aloe chitosannanoparticles and folic acid coupling aloe chitosan on tumor cell SMMC-7721has obvious inhibitory effect, blank nanoparticles to cells almost no inhibition.Cells on the uptake of nanoparticles effect is obvious, especially the coupling offolic acid aloe chitosan nanoparticles is more outstanding. Acridine orange blankfolic acid coupling with the results of the experiment of chitosan on theproliferation of tumor cells had no effect, the package of aloe folic acid couplingchitosan nanoparticles have obvious inhibitory effect on cell proliferation.ConclusionPreparation of aloe chitosan nanoparticles by ionic crosslinking method,and using the response surface method and optimization design is feasible,nanoparticles have remarkable sustained-release property, good nanoparticleuptake in tumor cells, the nanoparticles coupled folate uptake significantly moretargeted, has obvious inhibitory effect on tumor cells, nanoparticles materialsnon-toxic, with the great prospect.