【摘要】：目的新型樹狀大分子(PAMAM-co-0.25OEG,PGD)作穩(wěn)定劑制備多烯紫杉醇(Docetaxel,DTX)納米粒,以提高多烯紫杉醇的溶解度和生物利用度。方法將多烯紫杉醇(DTX)、PGD按藥載比8:1,采用超聲沉淀聯(lián)合高壓均質(zhì)法制備DTX-PGD納米粒,動(dòng)態(tài)光散射測(cè)定載藥納米粒粒徑及電位;考察37℃條件下,DTX-PGD納米粒在生理鹽水、5%葡萄糖、PBS及血漿中的穩(wěn)定性及DTX-PGD納米粒的溶血性。X射線粉末衍射法測(cè)定DTX在納米粒中的晶型形式。透析法測(cè)定DTX-PGD納米粒的體外釋放度,MTT法檢測(cè)DTX-PGD納米粒對(duì)4T1細(xì)胞的殺傷作用。結(jié)果多烯紫杉醇在水中的溶解度提高到1.6 mg/m L(原藥在水中幾乎不溶),納米粒載藥量達(dá)65.7%。DTX-PGD納米粒粒徑270.7 nm,PDI值為0.112,電位28.6 m V。DTX-PGD納米粒在5%葡萄糖及血漿中穩(wěn)定存在。掃描電鏡觀察納米粒為片狀,XRD圖譜顯示,多烯紫杉醇在納米粒中以晶體形式存在。DTX-PGD納米粒在PBS緩沖液中釋放緩慢,有較好的緩釋效果。溶血實(shí)驗(yàn)得知,DTX-PGD納米粒無(wú)溶血現(xiàn)象,可采用靜脈注射法給藥。MTT結(jié)果表明,DTX-PGD納米粒對(duì)4T1細(xì)胞較多烯紫杉醇溶液具有更強(qiáng)的殺傷作用。結(jié)論 PGD樹狀大分子可以作為一種有效的穩(wěn)定劑應(yīng)用到多烯紫杉醇納米粒的制備中,DTX-PGD納米粒有望作為一種新型的藥物輸送系統(tǒng)應(yīng)用到癌癥的臨床治療中。
[Abstract]:Aim to prepare docetaxel (Docetaxel,DTX) nanoparticles by using new dendrimer (PAMAM-co-0.25OEG,PGD) as stabilizer in order to improve the solubility and bioavailability of docetaxel. Methods DTX-PGD nanoparticles were prepared by ultrasonic precipitation combined with high pressure homogenization with docetaxel (DTX), PGD at a drug loading ratio of 8 渭 1. The particle size and potential of drug-loaded nanoparticles were measured by dynamic light scattering (DLS). The stability of DTX-PGD nanoparticles in normal saline, 5% glucose, PBS and plasma and the hemolysis of DTX-PGD nanoparticles were investigated at 37 鈩，

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