Preparation And Characterization Of Chitosan Microcapsules Loaded With Adriamycin And Its Pharmacodynamics

Background Microencapsulation has been widely used in many fields. It has the following advantages:Covering up the bad taste of the drug, improving drug stability, reducing the drug stimulation on the stomach, wrapping bioactive substances and so on. Preparation methods of microencapsulation includes physical chemical, mechanical and chemical method, In this paper, chitosan (CS) is chosen as the capsule wall material and adriamycin (ADM) as model drug. Chitosan not only has extensive sources, non-toxic, excellent film properties, preventing hypertension, inhibitting bacterial activity and anti-tumor properties; Adriamycin is a broad-spectrum anti-tumor, inhibiting RNA, but it has strong toxicity, poor patient tolerance. Bying microencapsulation, ADM can not only reduce its toxicity, but also can improve the stability and bioavailability.Objective Bying the preparation of chitosan microcapsules loaded with adriamycin, its release mechanism in vitro and pharmacodynamics are studied. It can provide theoretical support and experimental basis in chitosan as a carrier for the microencapsulation of drugs.Methods HPLC method was established to measure the concentration of ADM. By Minitab response surface design of experiments and optimization and single legal coacervation, chitosan microcapsules loaded with adriamycin is prepared, the morphology, size distribution, the drug loading and encapsulation efficiency are characterized on each batch of microcapsules. The cumulative release rate in vitro is determined. The study on the drug through the chitosan microcapsules into the capsule and release mechanism in vitro assess the impact of all relevant factors. H22hepatoma cells in the Netherlands as a tumor mouse model of drug-loaded microcapsules, preliminary pharmacodynamic is researched.Results1. The established content analysis method has been validated, ADM has a good linear relationship (r=0.9997) in the1.01-50.4μg· ml-1concentration range.2. The optimized conditions of preparing adriamycin-chitosan microcapsules are0.2%chitosan concentration,2:3core wall ratio,7%surfactant content and45℃; The average diameter of microcapsules12.51±1.26μm,the span0.65, The mean loading (%)20.6±0.21and encapsulation rate (%)90.73±0.40. Microcapsule quality are in line with the China Pharmacopoeia2010edition of microcapsule preparation parameters.3. The results show that the nature of chitosan, the particle diameter of microcapsules, the amount of crosslinking agent, environmental factors such as the medium for sustained release microcapsules in vitro produce different effects.4. Experimental results show that the inhibitory effect of ADM microencapsulated better, not only extended the ADM action time, while reducing its relative toxicity of the spleen and thymus, in order to achieve the purpose of long-term treatment, and low toxicity.Conclusion The prepared CS microcapsules loaded with adriamycin has a good slow-release properties and can significantly improve tumor inhibition rate at the same time, reducing the side effects of ADM.