Study On Preparation Of Cinnamaldehyde Liposomes And Its Physicochemical Properties

Cinnamaldehyde,a volatile essential oil extracted from cinnamon,has been widely used as a food additive.Meanwhile,it has received more and more attention due to its various physiological activities,such as anti-bacterial,anti-inflammatory,anti-oxidation,anti-diabetes,anti-platelet aggregation,anti-cancer,anti-apoptosis,anti-virus and other effects.However,its application is limited because of solubility,stability,volatility,etc.Developing a suitable dosage form is a common methods of improving the above problems.As a novel dr?g delivery carrier,liposome has received more and more attention with its biodegradability,good biocompatibility,physical insertion modes without changing the structural function of the drug.In this thesis,we use natural phospholipids and cholesterol as main raw materials to prepare cinnamaldehyde liposome and investigated its physical and chemical properties.Firstly,we established methods for detecting content and related substances.Pre-prescription studies on cinnamaldehyde was conducted.Determining HPLC quantitative detection conditions of cinnamaldehyde.In the concentration range of5-80?g/mL,the linearity of calibration plots of cinnamaldehyde was good(R~2=0.9996).The intra-day and inter-day precision RSD is less than 2%.The recovery rate is between 98%and 102%.It is in line with liquid analysis requirements.According to this methods,the solubility of cinnamaldehyde in water was 1.4mg/mL.The oil-water partition coefficient log P was 1.6.These results provide a basis for subsequent cinnamaldehyde dosage form design and formulation optimization.The effects of different preparation methods and prescription factors on the particle size,PDI and encapsulation efficiency of cinnamaldehyde liposomes were investigated.We separated free drugs not encapsulated in liposomes and established encapsulation efficiency methods by ultrafiltration centrifugation.After compared the three preparation methods,Considering comprehensive,we finally selected the film hydration method with higher encapsulation efficiency and smaller particle size for subsequent experiments.Single factor experiments were used to investigate phospholipid drug ratio,phospholipid cholesterol ratio,hydration temperature,and hydration pH.These factors are selected to obtain the optimal prescription through orthogonal design.The optimal prescription was phospholipid:cinnamaldehyde:cholesterol mass ratio 4:1:2.The cinnamaldehyde liposome is a uniform colloid with blue opalescence.TEM showed that it was round and nearly spherical.The particle size was between 100 and 110nm or so.PDI was less than 0.2.Encapsulation efficiency was above 85 percent.The short-term stability study showed that liposomes were good at 4?within one month.In summary,we prepared a cinnamaldehyde liposome with a small particle size and a high encapsulation efficiency,which provide a feasible method for expanding the application range of cinnamaldehyde.