The Preparation And Characteration Of Shell Type And Matrix Type Alginate/polyacrylamide Microspheres Loaded With Andrographolide

Acute upper respiratory tract infection is a pediatric multi-disease in China,and its predisposing factors are variable,resulting in a variety of therapeutic drugs.Compared with other therapeutic drugs commonly used upper respiratory tract infection,the antibacterial and antiviral synergy of andrographolide make it more effective,however because of its oral bitterness,it has poor compliance with treatment for children.In order to solve this problem,currently we have developed mature dosage forms include injections,drops,suspensions,tablets,etc.,but they still do not mask bitterness well.Therefore,aiming at the goal of developing new dosage forms for children,it is proposed to study a novel microencapsulation formulation that can effectively mask the bitter taste of andrographolide and is highly effective and load-controlled in this study.In this article,Sodium Alginate?SA?,a natural polymer material,was selected as the skeleton material for the preparation of gel microspheres in this study,and polyacrylamide?PAAm?was polymerized and cross-linked by acrylamide?Am?.As a filler material,Andrographolide?Andro?was used as a drug model molecule to prepare an interpenetrating network structure by adding acrylamide monomer molecules in two ways on the basis of electrostatic droplet preparation of gel microspheres.Scanning electron microscopy?SEM?,Fourier transform infrared spectroscopy?FT-IR?and other methods were used to characterize the appearance and structure of the gel microspheres.The performance parameters such as compressive strength and swelling rate were tested and the antibacterial and biocompatible properties of the gel microspheres were evaluated.The main findings are as follows:1.Shell-type Ca-Alg/PAAm microspheres were prepared by electrostatic droplet method.The optimal formulation of shell-type Ca-Alg/PAAm microspheres were determined by single factor experiments and orthogonal design experiments:C_Alg=20 g/L,m_Am=80 g/L,m_MBA=6g/L.The SEM results show that there are obvious shell layers in the gel microspheres,and the shell thickness increases with the addition of Am.FT-IR results showed that Am polymerized and PAAm was formed.Under the optimal formulation,the maximum compressive stress of the gel microspheres subjected to 75%compression was 0.289 MPa,and the water swelling rate was 35%.The results of in vitro release experiments with andrographolide as a drug model show that compared with Ca-Alg microspheres,the release of shell type Ca-Alg/PAAm microspheres at 1 h was reduced by 46.534 mg/L,indicating that it was good The drug slow release effect and bitterness masking effect and the encapsulation efficiency was66.70%.2.Adding Am to Alg solution to prepare the matrix-type Ca-Alg/PAAm microspheres.The optimal formulation were determined by single factor experiments and orthogonal design experiments:C_Alg=20 g/L,m_Am=120 g/L,m_MBA=6 g/L.The SEM results show that the gel microspheres are solid spherical and have the same shell as the shell-type microspheres.Under the optimal formulation,the maximum compressive stress of compressing 75%of the matrix microspheres was 0.467 MPa,and the water swelling rate was 29%.The results of in vitro release experiments with andrographolide as a drug model show that compared with shell-type Ca-Alg/PAAm microspheres,the release of matrix-type Ca-Alg/PAAm microspheres at 1 h was reduced by 4.562 mg/L,indicating that it was good The drug slow release effect and bitterness masking effect and the encapsulation efficiency was 64.80%.The parameters indicate that the matrix-type Ca-Alg/PAAm microspheres are more suitable for masking the bitterness of andrographolide.3.The gram-negative bacterium E.coli and gram-positive bacterium Staphylococcus aureus were selected as experimental strains,and L929 mouse fibroblasts were selected as experimental cells.The results showed that:the Andro gel microspheres inhibited Staphylococcus aureus and E.coli,and the prepared two gel microspheres have good biocompatibility;Am residue test results showed that there was no residue of Am monomer in gel microspheres.Therefore,it has good biocompatibility and can be used as an oral preparation carrier material.