載10-羥基喜樹(shù)堿的葉酸受體靶向相變超聲造影劑的制備及一般特性
發(fā)布時(shí)間:2018-03-14 08:11
本文選題:-羥基喜樹(shù)堿 切入點(diǎn):葉酸 出處:《中國(guó)介入影像與治療學(xué)》2017年03期 論文類(lèi)型:期刊論文
【摘要】:目的制備一種載10-羥基喜樹(shù)堿(10-HCPT)的葉酸受體靶向相變納米粒超聲造影劑(FR-HCPT-PNPCA),評(píng)價(jià)其載藥及在體外的相變能力、對(duì)腫瘤細(xì)胞的靶向能力等一般特性。方法通過(guò)雙步乳化法制備以脂質(zhì)為殼膜材料、液態(tài)氟碳為內(nèi)核,且包裹抗癌藥物10-HCPT的納米粒,采用高效液相色譜研究其藥物包封率和載藥量,在體外通過(guò)加熱法研究其相變產(chǎn)生微泡的能力,并在肝癌細(xì)胞株7721細(xì)胞上研究其體外尋靶能力。結(jié)果成功制備出載10-HCPT的靶向相變納米粒FR-HCPT-PNPCA,其藥物包封率為70.42%,載藥量為20.05%。當(dāng)加熱至70℃時(shí),顯微鏡下可以觀察到明顯的相變并產(chǎn)生微氣泡,且大量納米粒可特異性地黏附于肝癌細(xì)胞周?chē)。結(jié)論 FR-HCPT-PNPCA載藥率高,性質(zhì)穩(wěn)定,靶向腫瘤能力強(qiáng),有望成為一種集腫瘤診治于一體的多功能超聲分子探針,具有良好的應(yīng)用前景。
[Abstract]:Objective to prepare FR-HCPT-PNPCAA, a kind of folic acid receptor targeting phase change nano-particle ultrasound contrast agent (FR-HCPT-PNPCAA) loaded with 10-hydroxycamptothecin (10-HCPTT), and to evaluate its drug loading and phase transformation ability in vitro. Methods the nanoparticles with lipids as shell material and liquid fluorocarbon as core and encapsulated with anticancer drug 10-HCPT were prepared by two-step emulsification. High performance liquid chromatography (HPLC) was used to study the encapsulation efficiency and drug loading, and the ability of phase change to produce microbubbles was studied by heating method in vitro. The target finding ability of FR-HCPT-PNPCAA was studied on the hepatoma cell line 7721 in vitro. Results the target phase change nanoparticles FR-HCPT-PNPCAA carrying 10-HCPT were successfully prepared. The encapsulation efficiency of FR-HCPT-PNPCAA was 70.42 and the drug loading capacity was 20.05.When heated to 70 鈩,
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