傳(chuan)統注(zhu)(zhu)射(she)(she)劑在臨床中(zhong)廣泛使用，但(dan)同時也暴露(lu)出不少(shao)問題，例如使用風險(xian)高、用藥(yao)(yao)不便、藥(yao)(yao)效(xiao)維持時間短、患者依從性低等(deng)(deng)，因為(wei)使得新型注(zhu)(zhu)射(she)(she)劑成(cheng)為(wei)新的臨床需求。近些年，脂(zhi)質體注(zhu)(zhu)射(she)(she)劑、混(hun)懸注(zhu)(zhu)射(she)(she)劑、微乳注(zhu)(zhu)射(she)(she)劑、納米粒注(zhu)(zhu)射(she)(she)劑、微球注(zhu)(zhu)射(she)(she)劑、凝(ning)膠注(zhu)(zhu)射(she)(she)劑以(yi)及包(bao)合(he)物(wu)注(zhu)(zhu)射(she)(she)劑等(deng)(deng)新型注(zhu)(zhu)射(she)(she)給(gei)藥(yao)(yao)系統的開發，實現藥(yao)(yao)物(wu)的緩控釋，減(jian)少(shao)給(gei)藥(yao)(yao)頻次(ci)、提高藥(yao)(yao)物(wu)療效(xiao)、降(jiang)低毒副作用。

1、脂(zhi)肪(fang)乳(ru)(ru)(ru)(ru)注射(she)劑(ji)(ji)(ji)脂(zhi)肪(fang)乳(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)（Fat emulsions）又稱為(wei)脂(zhi)質(zhi)乳(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)（Lipid emulsions）或亞微(wei)(wei)乳(ru)(ru)(ru)(ru)（Submicron emulsions），是以植物油作為(wei)油相，輔以磷(lin)脂(zhi)為(wei)主(zhu)要(yao)乳(ru)(ru)(ru)(ru)化(hua)劑(ji)(ji)(ji)，甘油為(wei)等滲調節劑(ji)(ji)(ji)，經乳(ru)(ru)(ru)(ru)化(hua)制得的粒(li)(li)徑在100~600 nm的水包(bao)油（O/W）乳(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)微(wei)(wei)粒(li)(li)給藥(yao)系(xi)統。一般而言，乳(ru)(ru)(ru)(ru)滴微(wei)(wei)粒(li)(li)中不含藥(yao)的脂(zhi)肪(fang)乳(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)常用(yong)做腸外營養劑(ji)(ji)(ji)，而載(zai)藥(yao)脂(zhi)肪(fang)乳(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)則作為(wei)藥(yao)物載(zai)體使用(yong)。

圖1脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)的(de)(de)(de)(de)(de)(de)(de)結構第一個即用(yong)型(xing)營(ying)(ying)養脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)Intralipid于(yu)1961年(nian)(nian)實(shi)現工(gong)業(ye)化(hua)(hua)生產(chan)(chan)并在瑞典上(shang)(shang)(shang)市(shi)，此后，營(ying)(ying)養型(xing)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)隨著(zhu)(zhu)(zhu)油(you)(you)(you)(you)(you)(you)(you)(you)(you)相(xiang)的(de)(de)(de)(de)(de)(de)(de)改(gai)變(bian)不(bu)斷地(di)(di)(di)(di)發展，主(zhu)要(yao)變(bian)化(hua)(hua)為(wei)(wei)(wei)(wei)油(you)(you)(you)(you)(you)(you)(you)(you)(you)相(xiang)從單純的(de)(de)(de)(de)(de)(de)(de)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)改(gai)為(wei)(wei)(wei)(wei)中鏈(lian)油(you)(you)(you)(you)(you)(you)(you)(you)(you)、橄欖油(you)(you)(you)(you)(you)(you)(you)(you)(you)、魚(yu)(yu)油(you)(you)(you)(you)(you)(you)(you)(you)(you)以及多(duo)種油(you)(you)(you)(you)(you)(you)(you)(you)(you)的(de)(de)(de)(de)(de)(de)(de)混(hun)合(he)物。營(ying)(ying)養型(xing)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)成(cheng)功上(shang)(shang)(shang)市(shi)以后，醫(yi)藥(yao)(yao)行(xing)業(ye)在20世紀70年(nian)(nian)代將其(qi)(qi)應用(yong)作(zuo)為(wei)(wei)(wei)(wei)難溶性藥(yao)(yao)物靜脈注(zhu)(zhu)射(she)的(de)(de)(de)(de)(de)(de)(de)載(zai)(zai)體(ti)，即載(zai)(zai)藥(yao)(yao)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)。載(zai)(zai)藥(yao)(yao)型(xing)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)除活性成(cheng)分(fen)(fen)(fen)外(wai)，其(qi)(qi)處方(fang)組成(cheng)與營(ying)(ying)養型(xing)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)基(ji)(ji)本一致。地(di)(di)(di)(di)塞(sai)米(mi)(mi)(mi)松(song)棕櫚酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)酯(zhi)(zhi)(zhi)(zhi)和前列(lie)地(di)(di)(di)(di)爾(er)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)于(yu)1988年(nian)(nian)上(shang)(shang)(shang)市(shi)，隨后開(kai)發了多(duo)種載(zai)(zai)藥(yao)(yao)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)，例如地(di)(di)(di)(di)西洋、丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)、依托咪酯(zhi)(zhi)(zhi)(zhi)、氟(fu)比洛(luo)(luo)芬(fen)酯(zhi)(zhi)(zhi)(zhi)、氯(lv)維(wei)地(di)(di)(di)(di)平、阿瑞匹坦。表(biao)1已上(shang)(shang)(shang)市(shi)的(de)(de)(de)(de)(de)(de)(de)部分(fen)(fen)(fen)營(ying)(ying)養乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)商品名(ming)油(you)(you)(you)(you)(you)(you)(you)(you)(you)相(xiang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)其(qi)(qi)他成(cheng)分(fen)(fen)(fen)Intralipid大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)Abbolipid大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/紅花(hua)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)Deltalipid大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)Salvilipid大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)LipofundinN大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)，生育酚(fen)(fen)(fen)(fen)(fen)Lipofundin MCT大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/中鏈(lian)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)，生育酚(fen)(fen)(fen)(fen)(fen)Lipovenoes PLR大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)Lipovenoes MCT大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/中鏈(lian)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)橄欖油(you)(you)(you)(you)(you)(you)(you)(you)(you)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)橄欖油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)氨基(ji)(ji)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)、葡萄(tao)糖ω-3魚(yu)(yu)油(you)(you)(you)(you)(you)(you)(you)(you)(you)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)魚(yu)(yu)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)ω-3魚(yu)(yu)油(you)(you)(you)(you)(you)(you)(you)(you)(you)中/長(chang)鏈(lian)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)魚(yu)(yu)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/中鏈(lian)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)表(biao)2已上(shang)(shang)(shang)市(shi)的(de)(de)(de)(de)(de)(de)(de)部分(fen)(fen)(fen)載(zai)(zai)藥(yao)(yao)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)商品名(ming)藥(yao)(yao)物油(you)(you)(you)(you)(you)(you)(you)(you)(you)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)國(guo)外(wai)上(shang)(shang)(shang)市(shi)國(guo)產(chan)(chan)化(hua)(hua)Liple前列(lie)地(di)(di)(di)(di)爾(er)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)PC/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)1988（日本）1998Limethason地(di)(di)(di)(di)塞(sai)米(mi)(mi)(mi)松(song)棕櫚酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)酯(zhi)(zhi)(zhi)(zhi)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)1988（日本）2010Diprivan丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)1989（美國(guo)）1999Lipo-NSAID氟(fu)比洛(luo)(luo)芬(fen)酯(zhi)(zhi)(zhi)(zhi)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)1992（日本）2004Etomidaat-Lipuro依托咪酯(zhi)(zhi)(zhi)(zhi)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/MCT蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉2001（德國(guo)）2002Diazepam-Lipuro地(di)(di)(di)(di)西泮(pan)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/MCT蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉（歐洲）-VitalipideVit A，D2，E，K1大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)（歐洲）2005Propofol MCT丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)/MCT蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)2005（歐洲）2013Cleviprex丁酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)氯(lv)維(wei)地(di)(di)(di)(di)平大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)2008（美國(guo)）-ALYPROST前列(lie)地(di)(di)(di)(di)爾(er)大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)PC/PG2013（日本）-Cinvanti阿瑞匹坦大(da)(da)(da)(da)(da)(da)豆(dou)(dou)(dou)(dou)油(you)(you)(you)(you)(you)(you)(you)(you)(you)蛋(dan)(dan)(dan)黃(huang)卵(luan)(luan)(luan)(luan)(luan)(luan)磷(lin)(lin)(lin)(lin)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)/油(you)(you)(you)(you)(you)(you)(you)(you)(you)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉2017（美國(guo)）-2、注(zhu)(zhu)射(she)用(yong)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)中助(zhu)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)的(de)(de)(de)(de)(de)(de)(de)加入能(neng)顯著(zhu)(zhu)(zhu)降(jiang)低油(you)(you)(you)(you)(you)(you)(you)(you)(you)、水兩相(xiang)界面(mian)的(de)(de)(de)(de)(de)(de)(de)表(biao)面(mian)張(zhang)力(li)，僅需(xu)利用(yong)攪拌、超(chao)聲、均質等(deng)簡(jian)單方(fang)法(fa)即可制(zhi)備(bei)出粒(li)度分(fen)(fen)(fen)布均勻的(de)(de)(de)(de)(de)(de)(de)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)。但目前上(shang)(shang)(shang)市(shi)的(de)(de)(de)(de)(de)(de)(de)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)產(chan)(chan)品很少(shao)，主(zhu)要(yao)受限于(yu)如下幾點(dian)：（1）制(zhi)備(bei)粒(li)徑為(wei)(wei)(wei)(wei)10~100nm的(de)(de)(de)(de)(de)(de)(de)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)需(xu)要(yao)更(geng)高(gao)濃度的(de)(de)(de)(de)(de)(de)(de)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)，過多(duo)的(de)(de)(de)(de)(de)(de)(de)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)會(hui)(hui)刺激注(zhu)(zhu)射(she)部位(wei)；（2）納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)不(bu)耐(nai)(nai)稀釋，如果水相(xiang)過多(duo)則會(hui)(hui)影(ying)響納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)的(de)(de)(de)(de)(de)(de)(de)理化(hua)(hua)特(te)性。目前獲(huo)FDA批準上(shang)(shang)(shang)市(shi)的(de)(de)(de)(de)(de)(de)(de)兩個納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)均為(wei)(wei)(wei)(wei)非(fei)注(zhu)(zhu)射(she)用(yong)制(zhi)劑(ji)(ji)(ji)，分(fen)(fen)(fen)別為(wei)(wei)(wei)(wei)Neoral（環(huan)(huan)孢素軟(ruan)膠囊，內容(rong)物為(wei)(wei)(wei)(wei)黃(huang)色至淡黃(huang)棕色的(de)(de)(de)(de)(de)(de)(de)澄(cheng)清液(ye)體(ti)）和Restasis（治療干眼癥的(de)(de)(de)(de)(de)(de)(de)0.05%環(huan)(huan)孢霉素眼用(yong)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)劑(ji)(ji)(ji)）。僅一種丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)注(zhu)(zhu)射(she)用(yong)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)（Microfol）處于(yu)臨床研究中，該處方(fang)中所使用(yong)的(de)(de)(de)(de)(de)(de)(de)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)是辛酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)鈉和泊(bo)(bo)(bo)(bo)洛(luo)(luo)沙姆188。丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)長(chang)鏈(lian)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)三酯(zhi)(zhi)(zhi)(zhi)(LCT)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)注(zhu)(zhu)射(she)劑(ji)(ji)(ji)Diprivan于(yu)1996年(nian)(nian)6月獲(huo)美國(guo)FDA批準上(shang)(shang)(shang)市(shi)，臨床應用(yong)時(shi)易引(yin)發高(gao)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)三酯(zhi)(zhi)(zhi)(zhi)血癥和胰腺炎等(deng)不(bu)良(liang)反應，長(chang)期(qi)輸注(zhu)(zhu)還(huan)可導致丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)輸注(zhu)(zhu)綜合(he)征。隨著(zhu)(zhu)(zhu)中/長(chang)鏈(lian)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)的(de)(de)(de)(de)(de)(de)(de)問世，開(kai)發了丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)中長(chang)鏈(lian)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)注(zhu)(zhu)射(she)液(ye)Propofol-Lipuro，能(neng)更(geng)快地(di)(di)(di)(di)提供(gong)能(neng)量，并具有良(liang)好的(de)(de)(de)(de)(de)(de)(de)肝臟耐(nai)(nai)受性、更(geng)快的(de)(de)(de)(de)(de)(de)(de)甘(gan)(gan)(gan)油(you)(you)(you)(you)(you)(you)(you)(you)(you)三酯(zhi)(zhi)(zhi)(zhi)清除率和減輕LCT脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)肪(fang)(fang)(fang)(fang)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)帶來的(de)(de)(de)(de)(de)(de)(de)注(zhu)(zhu)射(she)疼痛(tong)(tong)等(deng)優點(dian)。2007年(nian)(nian)Daewon制(zhi)藥(yao)(yao)公司在韓國(guo)上(shang)(shang)(shang)市(shi)了丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)注(zhu)(zhu)射(she)液(ye)Aquafol，主(zhu)要(yao)的(de)(de)(de)(de)(de)(de)(de)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)為(wei)(wei)(wei)(wei)聚乙(yi)二(er)醇-15-羥(qian)基(ji)(ji)硬(ying)脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)酸(suan)(suan)(suan)(suan)(suan)(suan)(suan)酯(zhi)(zhi)(zhi)(zhi)（Solutol HS15）、助(zhu)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)化(hua)(hua)劑(ji)(ji)(ji)為(wei)(wei)(wei)(wei)四氫呋(fu)喃、聚乙(yi)二(er)醇醛和泊(bo)(bo)(bo)(bo)洛(luo)(luo)沙姆188。Aquafol利用(yong)常溫下為(wei)(wei)(wei)(wei)液(ye)態的(de)(de)(de)(de)(de)(de)(de)丙(bing)(bing)泊(bo)(bo)(bo)(bo)酚(fen)(fen)(fen)(fen)(fen)自身(shen)為(wei)(wei)(wei)(wei)油(you)(you)(you)(you)(you)(you)(you)(you)(you)相(xiang)，從而避免了脂(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)質的(de)(de)(de)(de)(de)(de)(de)使用(yong)，臨床研究表(biao)明該納(na)(na)米(mi)(mi)(mi)乳(ru)(ru)(ru)(ru)(ru)(ru)(ru)會(hui)(hui)產(chan)(chan)生顯著(zhu)(zhu)(zhu)的(de)(de)(de)(de)(de)(de)(de)注(zhu)(zhu)射(she)痛(tong)(tong)，此注(zhu)(zhu)射(she)疼痛(tong)(tong)由(you)較多(duo)的(de)(de)(de)(de)(de)(de)(de)游(you)離藥(yao)(yao)物引(yin)起(qi)而非(fei)輔(fu)料(liao)所致。

圖2丙泊酚脂(zhi)(zhi)肪(fang)乳3、脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)注射劑脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)（liposomes）是由磷(lin)脂(zhi)(zhi)和其他兩(liang)親(qin)性(xing)(xing)物(wu)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)分散于(yu)(yu)水(shui)中(zhong)(zhong)形(xing)成(cheng)(cheng)的(de)球(qiu)形(xing)封(feng)閉囊(nang)泡。脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)是通(tong)過混合特(te)定比例(li)的(de)兩(liang)親(qin)性(xing)(xing)物(wu)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)（如磷(lin)脂(zhi)(zhi)和膽固(gu)醇）形(xing)成(cheng)(cheng)的(de)，當它們在(zai)水(shui)溶(rong)液(ye)中(zhong)(zhong)水(shui)合時，會(hui)排列成(cheng)(cheng)一層或(huo)多(duo)(duo)(duo)(duo)層同心的(de)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)雙分子(zi)(zi)膜(mo)包封(feng)而(er)成(cheng)(cheng)的(de)超微型(xing)(xing)(xing)球(qiu)狀載(zai)體(ti)(ti)(ti)(ti)(ti)(ti)，可(ke)用(yong)于(yu)(yu)藥(yao)(yao)物(wu)包載(zai)。脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)的(de)概(gai)念(nian)在(zai)1965年(nian)(nian)由英國(guo)Bangham等(deng)提出，1974年(nian)(nian)Rahman等(deng)首先將脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)作為藥(yao)(yao)物(wu)的(de)載(zai)體(ti)(ti)(ti)(ti)(ti)(ti)應用(yong)。第一款脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)注射劑是由美(mei)(mei)國(guo)NeXstar公(gong)(gong)司（已被(bei)Gilead公(gong)(gong)司并購）開(kai)(kai)發(fa)(fa)的(de)兩(liang)性(xing)(xing)霉素B脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)Ambisome，能有效(xiao)降低兩(liang)性(xing)(xing)霉索B引起的(de)急性(xing)(xing)腎毒性(xing)(xing)。Ambisome于(yu)(yu)1990年(nian)(nian)在(zai)歐洲獲(huo)(huo)批(pi)上市(shi)，1997年(nian)(nian)在(zai)美(mei)(mei)國(guo)上市(shi)，用(yong)于(yu)(yu)念(nian)珠菌、曲霉菌、隱球(qiu)菌等(deng)造成(cheng)(cheng)的(de)深部(bu)真菌感(gan)染以及內(nei)臟利(li)什曼(man)病。第一款抗(kang)腫瘤藥(yao)(yao)物(wu)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)是由美(mei)(mei)國(guo)Sequus制藥(yao)(yao)公(gong)(gong)司開(kai)(kai)發(fa)(fa)的(de)阿霉素脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)Doxil，于(yu)(yu)1995年(nian)(nian)獲(huo)(huo)FDA批(pi)準上市(shi)用(yong)于(yu)(yu)治(zhi)療(liao)進展期及鉑類化療(liao)藥(yao)(yao)化療(liao)后復(fu)發(fa)(fa)的(de)卵(luan)巢癌患者。Doxil的(de)組成(cheng)(cheng)成(cheng)(cheng)分中(zhong)(zhong)含有兩(liang)親(qin)性(xing)(xing)磷(lin)脂(zhi)(zhi)-聚合物(wu)共軛物(wu)聚乙二醇-硬脂(zhi)(zhi)酰磷(lin)脂(zhi)(zhi)酰乙醇胺（DSPE-PEG2000），親(qin)水(shui)端(duan)的(de)存在(zai)使脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)免于(yu)(yu)被(bei)單核(he)吞(tun)噬系(xi)統（Mononuclear Phagocytic System，MPS）快速(su)清(qing)除(chu)而(er)延長血液(ye)循環時間，長循環特(te)性(xing)(xing)有利(li)于(yu)(yu)增加脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)在(zai)病變(bian)部(bu)位的(de)相對蓄積(ji)量。隨著(zhu)新型(xing)(xing)(xing)載(zai)體(ti)(ti)(ti)(ti)(ti)(ti)材料和表面修飾技術(shu)的(de)開(kai)(kai)發(fa)(fa)和應用(yong)，對脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)的(de)處方(fang)和工藝進行改進，相繼(ji)開(kai)(kai)發(fa)(fa)了環境響應型(xing)(xing)(xing)、主(zhu)動靶向(xiang)型(xing)(xing)(xing)、長效(xiao)緩釋型(xing)(xing)(xing)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)，例(li)如熱敏脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)、pH敏感(gan)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)、磁性(xing)(xing)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)、導向(xiang)肽偶聯(lian)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)、多(duo)(duo)(duo)(duo)肽陽離子(zi)(zi)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)、免疫脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)、多(duo)(duo)(duo)(duo)囊(nang)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)等(deng)。目前已有多(duo)(duo)(duo)(duo)種類型(xing)(xing)(xing)的(de)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)獲(huo)(huo)批(pi)上市(shi)或(huo)進入臨床研究階段，相信隨著(zhu)技術(shu)的(de)積(ji)累，更多(duo)(duo)(duo)(duo)優異的(de)脂(zhi)(zhi)質(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)(zhi)體(ti)(ti)(ti)(ti)(ti)(ti)將會(hui)被(bei)相繼(ji)開(kai)(kai)發(fa)(fa)。

圖3脂質體示意圖

表3已上(shang)市的(de)部分(fen)脂(zhi)質體(ti)

脂(zhi)質(zhi)(zhi)體(ti)(ti)(ti)具有良(liang)好(hao)的(de)組(zu)織相(xiang)容性(xing)、生物可降解性(xing)、安全(quan)性(xing)、靶(ba)向性(xing)、緩釋性(xing)、制(zhi)備條件溫和(he)等特點。但脂(zhi)質(zhi)(zhi)體(ti)(ti)(ti)也存在(zai)很多缺點嚴重制(zhi)約脂(zhi)質(zhi)(zhi)體(ti)(ti)(ti)產(chan)品(pin)的(de)開發(fa)和(he)應用(yong)(yong)，例如藥(yao)(yao)(yao)物包(bao)封(feng)率低、穩定性(xing)差和(he)易發(fa)生藥(yao)(yao)(yao)物泄(xie)漏、生產(chan)工藝復雜、技(ji)(ji)(ji)術要求高、質(zhi)(zhi)量控制(zhi)難(nan)以及需要高端輔料(liao)和(he)高精密設備等。新技(ji)(ji)(ji)術、新材料(liao)以及新載體(ti)(ti)(ti)的(de)成功應用(yong)(yong)將(jiang)極大促進脂(zhi)質(zhi)(zhi)體(ti)(ti)(ti)注射(she)給藥(yao)(yao)(yao)系統的(de)發(fa)展，與其他(ta)生物技(ji)(ji)(ji)術如基因工程(cheng)、蛋白質(zhi)(zhi)工程(cheng)等的(de)結合(he)將(jiang)使(shi)藥(yao)(yao)(yao)物治療更加個性(xing)化(hua)和(he)人性(xing)化(hua)，相(xiang)信這些會進一步擴(kuo)展脂(zhi)質(zhi)(zhi)體(ti)(ti)(ti)作為藥(yao)(yao)(yao)物遞送載體(ti)(ti)(ti)的(de)應用(yong)(yong)范圍。