Preparation of Methotrexate Sustained-Release Microspheres
ZHANG Li-na1,2, ZHANG Qian2, SUN Shan-shan2, DING Lin2, WANG Hui-yun2, QUAN Xian-gao2*
1. School of Medicine and Life Science,University of Jinan , Jinan 250022, China; 2. School of Pharmaceutical Science, Jining Medical University, Rizhao 276826, China
Abstract��OBJECTIVE To prepare a novel methotrexate sustained-release microspheres system, and study its in vitro release properties. METHODS The CS-montmorillonite (CS-MMT) intercalative composites were prepared by using chitosan and montmorillonite. The novel drug sustained-release system was prepared with CS-MMT as the carrier material and methotrexate as the model drug. The microspheres were characterized by Fourier transform infrared spectrometer (FTIR), electric microscope, UV-spectrophotometer (UV), as well as Malvernlaser particle size analyzer. The influences of the amount of composite materials, dosage of emulsifiers, ratio of oil/water and dosage of crosslinking agent on the drug loading and entrapment rate of microspheres were investigated. And in vitro release experiment was used to study the drug release properties of the microspheres. RESULTS The shape and size of the microspheres were uniform. The drug loading, average particle size and Zeta potential were 31.6%, 557.4 nm and 20.8 mV respectively under the optimal conditions, ie, ratio of water/oil of 1��5, amount of glutaraldehyde(aqueous phase)of 6%, dosage of emulsifiers (oil phase) of 7%, CS-MMT/CS ratio of 1��4, and MTX/CS ratio of 1��3. Methotrexate sustained-release system was pH-sensitive and tended to show a larger release percentage in hydrochloric acid solution. CONCLUSION CS-MMT can be used as a slow-release excipient. CS-MMT microspheres are good controlled-release carrier for drugs, with pH sensitivity.
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2017, Vol. 52 
