高等学校化学学报
高等學校化學學報
고등학교화학학보
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES
2014年
9期
1982-1987
,共6页
王爽%兀晓文%李海平%张人杰%侯万国
王爽%兀曉文%李海平%張人傑%侯萬國
왕상%올효문%리해평%장인걸%후만국
类水滑石%葫芦素%剥离-共组装法%纳米杂化物%缓释
類水滑石%葫蘆素%剝離-共組裝法%納米雜化物%緩釋
류수활석%호호소%박리-공조장법%납미잡화물%완석
Hydrotalcite-like compound%Cucurbitacin%Delamination-coassembling method%Nanohybrid%Release
采用剥离-共组装法制备了电中性疏水药物葫芦素( CA)插层类水滑石( HTlc)纳米杂化物.先用胆酸钠( Ch)包覆修饰葫芦素,再与剥离的HTlc薄片共组装,形成CA-Ch-HTlc纳米杂化物.采用小角X射线散射、傅里叶变换红外吸收光谱、透射和扫描电子显微镜、Zeta电位和元素分析等技术对样品进行了表征.所制备纳米杂化物的载药量达到7.06%,表明该方法可以实现电中性疏水药物在HTlc上的有效负载.依据胆酸离子和葫芦素尺寸及纳米杂化物通道高度推测,胆酸离子在HTlc层间为双层排列,其长轴几乎垂直于HTlc层板;葫芦素分子插入(或“溶入”)胆酸离子双层中. CA-Ch-HTlc纳米杂化物具有良好的药物缓释效果,其药物释放过程符合准二级动力学方程.
採用剝離-共組裝法製備瞭電中性疏水藥物葫蘆素( CA)插層類水滑石( HTlc)納米雜化物.先用膽痠鈉( Ch)包覆脩飾葫蘆素,再與剝離的HTlc薄片共組裝,形成CA-Ch-HTlc納米雜化物.採用小角X射線散射、傅裏葉變換紅外吸收光譜、透射和掃描電子顯微鏡、Zeta電位和元素分析等技術對樣品進行瞭錶徵.所製備納米雜化物的載藥量達到7.06%,錶明該方法可以實現電中性疏水藥物在HTlc上的有效負載.依據膽痠離子和葫蘆素呎吋及納米雜化物通道高度推測,膽痠離子在HTlc層間為雙層排列,其長軸幾乎垂直于HTlc層闆;葫蘆素分子插入(或“溶入”)膽痠離子雙層中. CA-Ch-HTlc納米雜化物具有良好的藥物緩釋效果,其藥物釋放過程符閤準二級動力學方程.
채용박리-공조장법제비료전중성소수약물호호소( CA)삽층류수활석( HTlc)납미잡화물.선용담산납( Ch)포복수식호호소,재여박리적HTlc박편공조장,형성CA-Ch-HTlc납미잡화물.채용소각X사선산사、부리협변환홍외흡수광보、투사화소묘전자현미경、Zeta전위화원소분석등기술대양품진행료표정.소제비납미잡화물적재약량체도7.06%,표명해방법가이실현전중성소수약물재HTlc상적유효부재.의거담산리자화호호소척촌급납미잡화물통도고도추측,담산리자재HTlc층간위쌍층배렬,기장축궤호수직우HTlc층판;호호소분자삽입(혹“용입”)담산리자쌍층중. CA-Ch-HTlc납미잡화물구유량호적약물완석효과,기약물석방과정부합준이급동역학방정.
A nanohybrid of cucurbitacin(CA), a charge-neutral and poorly water-soluble drug, intercalated hydrotalcite-like compounds( HTlc) was synthesized via a delamination-coassembling method. CA molecules were initially incorporated into the micelles of sodium cholate( Ch) , and the resulting negatively charged CA-loaded micelles and the positively charged delaminated HTlc nanosheets were then coassembled together into the CA-Ch-HTlc nanohybrid. The so-obtained nanohybrid was characterized by small angle X-ray scattering, Fourier transform infrared, transmission and scanning electron microscopy, zeta potential and elemental analyses. The results showed that the loading of CA in the nanohybrid was 7. 06%, indicating that this route could be used to achieve the effective intercalation of charge-neutral and poorly water-soluble drugs into the HTlc gallery. Based on the sizes of Ch and CA, and the gallery heights of the nanohybrid, a possible orienta-tion of Ch anions and CA molecules in the HTlc gallery was proposed. The Ch anions are arranged as a slightly tilted bilayer with their long axis approximately perpendicular to the brucite-like layer, and the CA molecules are encapsulated in the bilayer as a consequence of the hydrophobic interactions. The in vitro release of CA from the nanohybrid was examined, and the results showed that the nanohybrid had a good drug controlled release performance and its drug release process obeyed pseudo-second order kinetics model.