介孔二氧化硅和中空介孔二氧化硅载体用于提高难溶性药物溶出度的比较
|
摘要
目的研究介孔二氧化硅(mesoporous silica nanoparticles,MSN)和中空介孔二氧化硅(hollow mesoporous silica nanoparticles,HMSN)两种载体对提高难溶性药物缬沙坦(valsartan,VAL)和尼莫地平(nimodipine,NMP)的载药量以及改善药物溶出度作用的比较。方法采用溶剂挥干法制备VAL-MSN、VAL-HMSN、NMP-MSN和NMP-HMSN四种固体分散体,以紫外分光光度法测定样品的载药量。采用X射线衍射法表征药物的存在状态。以溶出度为评价指标,对原料药、无定型药物以及载药体系的溶出速率进行了比较。结果 VAL-HMSN和NMP-HMSN的载药量分别为(34.76±1.36)%和(38.30±1.38)%,而VAL-MSN和NMP-MSN的载药量分别为(23.54±1.72)%和(22.93±1.08)%。X射线衍射实验表明药物在载体中以非晶体状态存在。溶出实验结果显示无定型药物的溶出度最低,HMSN和MSN载药体系的溶出度均比原料药有所提高。结论 HMSN和MSN相比,HMSN载药体系的载药量更高,但溶出度较MSN载药体系低。
Objective To compare the effects of mesoporous silica nanoparticles(MSN)and hollow mesoporous silica nanoparticles(HMSN)to improve the drug loading efficiencies and drug dissolution rate of the insoluble drugs Valsartan(VAL)and Nimodipine(NMP).Methods Four solid dispersions including VAL-MSN,VAL-HMSN,NMP-MSN and NMP-HMSN were prepared by solvent evaporation method.The drug contents of the samples were measured by UV-vis method.The X-ray diffraction(XRD)was used to characterize the existence state of the drugs.Taking dissolution as the evaluation criteria,the dissolution ratesof VAL and NMP were compared among raw drugs,amorphous drugs and preparations.Results The contents of VAL-HMSN and NMP-HMSN were(34.76±1.36)% and(38.30±1.38)%,respectively,while the contents of VAL-MSN and NMP-MSN were(23.54±1.72)% and(22.93±1.08)%,respectively.The result of XRD illustrated that the existence state of the drugs was in a non-crystalline state.The results of dissolution tests showed that the amorphous drugs showed the lowest dissolution rate,and both HMSN and MSN preparations improved the dissolution rates compared with the raw drugs.Conclusion Compared with MSN,drug loading HMSN preparations have a higher drug loading efficiency,but a lower dissolution rate.
Objective To compare the effects of mesoporous silica nanoparticles(MSN)and hollow mesoporous silica nanoparticles(HMSN)to improve the drug loading efficiencies and drug dissolution rate of the insoluble drugs Valsartan(VAL)and Nimodipine(NMP).Methods Four solid dispersions including VAL-MSN,VAL-HMSN,NMP-MSN and NMP-HMSN were prepared by solvent evaporation method.The drug contents of the samples were measured by UV-vis method.The X-ray diffraction(XRD)was used to characterize the existence state of the drugs.Taking dissolution as the evaluation criteria,the dissolution ratesof VAL and NMP were compared among raw drugs,amorphous drugs and preparations.Results The contents of VAL-HMSN and NMP-HMSN were(34.76±1.36)% and(38.30±1.38)%,respectively,while the contents of VAL-MSN and NMP-MSN were(23.54±1.72)% and(22.93±1.08)%,respectively.The result of XRD illustrated that the existence state of the drugs was in a non-crystalline state.The results of dissolution tests showed that the amorphous drugs showed the lowest dissolution rate,and both HMSN and MSN preparations improved the dissolution rates compared with the raw drugs.Conclusion Compared with MSN,drug loading HMSN preparations have a higher drug loading efficiency,but a lower dissolution rate.
引文
[1] SAHOO S K,LABHASETWAR V.Nanotech approaches to drug delivery and imaging[J].Drug Discovery Today,2003,8(24):1112-1120.
[2] SLOWING I I,VIVERO-ESCOTO J L,WU C W,et al.Mesoporous silica nanoparticles as controlled release drug delivery and gene transfection carriers[J].Advanced Drug Delivery Reviews,2008,60(11):1278-1288.
[3] KRESGE C T,LEONOWICZ M E,ROTH W J,et al.Ordered mesoporous molecular sieves synthesized by a liquid-crystal template mechanism[J].Nature,1992,359:710-712.
[4] KIM J M,RYOO R.Synthesis of MCM-48 single crystals[J].Chem Commun,1998,2(2):259-260.
[5] KILPEL INEN M,RIIKONEN J,VLASOVA M A,et al.In vivo delivery of a peptide ghrelin antagonist with mesoporous silicon microparticles[J].Journal of Controlled Release,2009,137(2):166-170.
[6] SLOWING IGOR I,TREWYN BRIAN G,GIRI SUPRATIM,et al.Mesoporous silica nanoparticles for drug delivery and biosensing applications[J].Advanced Functional Materials,2007,17(8):1225-1236.
[7] LI Z Z,WEN L X,SHAO L,et al.Fabrication of porous hollow silica nanoparticles and their applications in drug release control[J].Journal of Controlled Release,2004,98(2):245-254.
[8] LIU C,YIN H B,WANG A L,et al.Size-controlled preparation of hollow silica spheres and glyphosate release[J].Transactions of Nonferrous Metals Society of China,2012,22(5):1161-1168.
[9] FANG X L,ZHAO X J,FANG W J,et al.Self-templating synthesis of hollow mesoporous silica and their applications in catalysis and drug delivery[J].Nanoscale,2013,5(6):2205-2218.
[10] ZHU Y F,SHI J L,CHEN H R,et al.A facile method to synthesize novel hollow mesoporous silica spheres and advanced storage property[J].Microporous and Mesoporous Materials,2005,84(1):218-222.
[2] SLOWING I I,VIVERO-ESCOTO J L,WU C W,et al.Mesoporous silica nanoparticles as controlled release drug delivery and gene transfection carriers[J].Advanced Drug Delivery Reviews,2008,60(11):1278-1288.
[3] KRESGE C T,LEONOWICZ M E,ROTH W J,et al.Ordered mesoporous molecular sieves synthesized by a liquid-crystal template mechanism[J].Nature,1992,359:710-712.
[4] KIM J M,RYOO R.Synthesis of MCM-48 single crystals[J].Chem Commun,1998,2(2):259-260.
[5] KILPEL INEN M,RIIKONEN J,VLASOVA M A,et al.In vivo delivery of a peptide ghrelin antagonist with mesoporous silicon microparticles[J].Journal of Controlled Release,2009,137(2):166-170.
[6] SLOWING IGOR I,TREWYN BRIAN G,GIRI SUPRATIM,et al.Mesoporous silica nanoparticles for drug delivery and biosensing applications[J].Advanced Functional Materials,2007,17(8):1225-1236.
[7] LI Z Z,WEN L X,SHAO L,et al.Fabrication of porous hollow silica nanoparticles and their applications in drug release control[J].Journal of Controlled Release,2004,98(2):245-254.
[8] LIU C,YIN H B,WANG A L,et al.Size-controlled preparation of hollow silica spheres and glyphosate release[J].Transactions of Nonferrous Metals Society of China,2012,22(5):1161-1168.
[9] FANG X L,ZHAO X J,FANG W J,et al.Self-templating synthesis of hollow mesoporous silica and their applications in catalysis and drug delivery[J].Nanoscale,2013,5(6):2205-2218.
[10] ZHU Y F,SHI J L,CHEN H R,et al.A facile method to synthesize novel hollow mesoporous silica spheres and advanced storage property[J].Microporous and Mesoporous Materials,2005,84(1):218-222.