The Study On Preparation And Quality Evaluation Of Aloe Emodin Niosome

Aloe emodin,a kind of anthiaquinone components,was extracted from dried concentrated solution of liliaceous plant curacao Aloe Aloe barbadensis Miller,the cape Aloe Aloe ferox Miller and other belong to relatives of plant leaves,reportedly has anti-bacterial,anti-inflammatory activity,immunosuppressive action,purgative effect and Anti-tumor activity.The anti-tumor characteristics which have become a hot topic concerned about by pharmaceutical researchers at home and abroad.Relevant reports indicated Aloe emodin can induce apoptosis of cancer cells,including tongue,liver,lung,gastric,melanin fine muscle and neural ectoderm cancer cells.AE,a hydrophobic drug,was found to crystallize in water,low bioavailability,it is difficult to achieve the effective plasma drug concentration,therefore,to improve the drug solubility,has become the urgent problem at present.Nonionic Surfactant Vesicle(NSV),also known as lipid vesicles,similar to the structure of liposomes,As the drug carrier,is formed self-assembly by non-ionic surfactant and cholesterol with closed bilayer structure.Which can package hydrophilic or lipophilic drugs,so as to improve the solubility of lipophilic drugs,and has high affinity,natural liver and spleen targeting and sustained-release long-lasting advantages.The purpose of this project is to use a non-ionic surfactant vesicles drug system,wrapped in aloe emodin,to increase solubility,and it can be slowly released in the body to reach the target site,and thus play a curative effect.This article is divided into four parts:Firstly,we investigated the pre-formulation studies of AE,mainly includes the establishing the method and methodology of HPLC to determine the content of aloe emodin;Screening the method of measuring encapsulation rate,the results showed that the membrane filter technique is simple,accurate and suitable for measuring the entrapment efficiency rate of the drug that does not dissolve in water.Meanwhile,measuring the apparent solubility of AE in common reagents,and apparent oil-water partition coefficient,The results showed that the solubility in acetone was better,LogP is 3.36.Secondly,we investigated the prescription and process factors including types of nonionic surfactants,proportion of cholesterol and nonionic surfactant,drug dosage,types of hydration medium,injection speed,stirring speed,bath temperature by single factor.The results showed that when surfactant was Tween 60,cholesterol/Tween 60 was 15%,the dosage of AE was 2mg,hydration medium was saline,the highest entrapment efficiency reached 90.0 ±3.0%,the particle size of the vesicle was approximately 200.0±2.0nm,zeta potential was about-1.5.In addition,the methods and the prescription of precursor of aloe emodin vesicle was investigated,mainly adopted the spray drying and freeze drying and screening the types and dosage of auxiliary,The results showed that preparing the precursor of aloe emodin vesicle with 3%A as excipients by spray diying.The final sample was reconstituted with sterile water and measured the particle size,Its size was 200 ±2.0nm,comparing with the particle size of the non-drying vesicles,there has little changes.That illustrated that properties of aloe emodin vesicle have no change.Finally,we investigated the physico-chemical properties and quality evaluation of the aloe emodin vesicles through the appearance,pH value,entrapment efficiency rate,determination of the content,particle size and size distribution,zeta potential,the leakage rate,the cumulative release rate of the vesicles,etc.Results:Aloe emodin vesicles showed homogeneously and clear,yellow translucent liquid,the pH is about 7.0 ±0.2,the entrapment efficiency rate is about 90%,per milliliter containing content of aloe emodin is 0.25 mg/mL,particle size is about 200.0± 3.0 nm,PDI is 0.17,potential value is 1,5,the leakage rate is smaller,compared with reference substance of aloe emodin,the release of vesicle is relatively slow,have obviously sustained effect.In addition,it conducted a preliminary study in rats plasma concentrations,Which found that Aloe emodin niosomes can significantly improve the absorption in the body.