Synthesis And Release Behavior Of Zein-based Composite Microparticles

The development of micro/nanoparticles technology has great significance toimprove the efficacy of the drug molecules and nutrients. As drug delivery systems,micro/nanoparticles have been developed to overcome disadvantages of conventionaldrug dosage forms and reduce the side effects of free drugs. A large number ofpolymers, synthetic and natural have been used to prepare micro/nanoparticles, eachwith its own advantages/disadvantages profile. Natural polymers as drug deliverysystems have some advantages, such as biodegradability, biocompatibility, plentifulsupply and low cost. Hydrophilic polymers, such as gelatin, casein, albumin, can beused for controlled release over shorter periods and maybe better at entrappingwater-soluble drugs compared with lipophilic polymers. Instead, hydropholic polymersystems, as controlled release systems, may offer other favourable prospects such as tolocalize the delivery of drug to particular sites, to stabilize rapidly metabolized drugs,to maintain relatively constant therapeutic blood levels of the drug for a desired periodand to increase patient comfort. In this study, two microparticles drug delivery systemsof water-soluble drugs using hydrophobic protein zein, water-soluble chitosan andCaCO3was prepared by the solvent-nonsolvent phase separation method andcharacterized by dynamic light scattering, fourier infrared spectrum, transmissionelectron microscopy and scanning electron microscope. The sustained release of drugsfrom the microparticles was confirmed in different medium.Firstly, this paper introduces the sources, composition and properties of Zein. Thecurrent research status of Zein and application in various fields such as food,bio-pharmaceutical, and industrial production were summarized.Secondly, the Zein-based composite nanoparticles (NSZ/CS) was prepared usingwater-soluble chitosan. The optimum conditions for preparation of NSZ/CS were givenbased on the size and PDI of nanoparticles. Furthermore, the obtained NSZ/CS wascharacterized by DLS, FT-IR, TEM, SEM and other characterization method. Theencapsulation efficiency and controlled release of NSZ/CS/RB and NSZ/CS/Dox wasinvestigated in different PBS medium and simulated gastrointestinal fluid.Thirdly, we devised a simple method to incorporate water-soluble drugs(RB andDox·HCl)into Zein-based composite microparticles (ZCa) and to regulate the size of the particles by different solutions. Characterization was carried out by evaluating theparticlesize, encapsulation efficiency, and controlled release of compositemicroparticles ZCa. The controlled release properties of encapsulated water-solubledrugs in different medium with or without presence of enzymes was also studied.In conclusion, A novel microparticles delivery system of water-soluble drug usinghydrophobic protein Zein was prepared by the solvent-nonsolvent phase separationmethod. Zein-based biocompatible composite nanospheres (NSZ/CS) and compositemicroparticles (ZCa) were prepared successfully. The effect of various constituents onthe nanoparticles fabrication and the drug loading and release properties of compositemicroparticles was investigated. The results showed the water-soluble RB andDox·HCl could be effectively loaded in the composite microparticles (NSZ/CS andZCa) with a high encapsulation efficiency, and the drug release could be effectivelysustained, indicating the composite microparticles were suitable for delivery ofwater-soluble drugs.