陳積 趙小倩 胡姍姍 馬彥巧 劉燕 譚丹楓 陳澤慧 田應(yīng)彪
中圖分類號(hào) R283 文獻(xiàn)標(biāo)志碼 A 文章編號(hào) 1001-0408(2018)05-0615-06
DOI 10.6039/j.issn.1001-0408.2018.05.10
摘 要 目的:制備復(fù)方莪術(shù)油脂質(zhì)體(ZTOC-LPS)并對(duì)其質(zhì)量進(jìn)行評(píng)價(jià)。方法:以復(fù)方莪術(shù)油中莪術(shù)油(以吉馬酮表征)和維A酸的包封率及載藥量等為考察指標(biāo),篩選ZTOC-LPS的制備方法及處方中大豆卵磷脂(SPC)的加入量、脂質(zhì)中SPC-膽固醇(CH)質(zhì)量比、莪術(shù)油-脂質(zhì)質(zhì)量比、維A酸-脂質(zhì)質(zhì)量比、水浴溫度;并對(duì)最優(yōu)處方制備工藝所制脂質(zhì)體進(jìn)行質(zhì)量評(píng)價(jià)和初步穩(wěn)定性考察。結(jié)果:優(yōu)選的制備方法為乙醇注入法;最優(yōu)處方制備工藝為每1 mL脂質(zhì)體中SPC 4 mg、SPC-CH質(zhì)量比3 ∶ 1、莪術(shù)油-脂質(zhì)質(zhì)量比1 ∶ 9、維A酸-脂質(zhì)質(zhì)量比1 ∶ 70、水浴溫度55 ℃。所制3批脂質(zhì)體中莪術(shù)油和維A酸的平均包封率分別為(64.63±1.00)%和(90.33±0.72)%,載藥量分別為(9.09±0.14)%和(1.43±0.02)%,粒徑為(257.41±7.58) nm,Zeta電位為(-38.77±0.81) mV,多分散系數(shù)為 0.10±0.04;離心加速試驗(yàn)結(jié)果顯示脂質(zhì)體具有良好的物理穩(wěn)定性;脂質(zhì)體樣品在(4±2) ℃條件下放置 1 個(gè)月時(shí)各項(xiàng)考察指標(biāo)均未發(fā)生明顯變化。結(jié)論:建立的制備方法簡(jiǎn)單可行,所制脂質(zhì)體質(zhì)量符合要求,可為后續(xù)復(fù)方莪術(shù)油新劑型的研究提供參考。
關(guān)鍵詞 莪術(shù)油;維A酸;脂質(zhì)體;包封率;載藥量;制備工藝;質(zhì)量評(píng)價(jià)
ABSTRACT OBJECTIVE: To prepare zedoary turmeric oil compound liposomes (ZTOC-LPS) and evaluate its quality. METHODS: The preparation method of liposome, the addition amount of soybean phosphatidylcholine (SPC), ratio of SPC to cholesterol (CH) in lipid, drug-lipid ratio of zedoary turmeric oil (ZTO), drug-lipid ratio of tretinoin in formulation, and water bath temperature were screened using encapsulation efficiency and drug-loading amount of ZTO (represented by germacrone) and tretinoin as investigation indexes. Quality evaluation and primary stability investigation were conducted for liposomes prepared by optimal preparation technology. RESULTS: The optimal preparation method was ethanol injection method; The optimal preparation technology were SPC 4 mg in 1 mL lipid, the mass ratio of SPC to CH 3 ∶ 1, the ratio of ZTO to lipid 1 ∶ 9 , the ratio of tretinoin to lipid 1 ∶ 70, water bath temperature of 55 ℃. Encapsulation efficiencies of ZTO and tretinoin were (64.63±1.00)% and (90.33±0.72)% in 3 batches of ZTOC-LPS, respectively. Drug-loading amount of ZTO and tretinoin were (9.09±0.14)% and (1.43±0.02)%, respectively. Particle size was (257.41±7.58) nm, Zeta potential was (-38.77±0.81) mV, PDI was 0.10±0.04; the results of centrifugal acceleration test showed that the liposomes had good physical stability. No obvious change was found in each investigation index of ZTOC-LPS that stored at (4±2) ℃ for 1 month. CONCLUSIONS: Established preparation technology is simple and feasible, the quality of the prepared ZTOC-LPS conforms to the requirements, and it can provide reference for the following research of ZTOC-LPS.
KEYWORDS Zedoary turmeric oil; Tretinoin; Liposomes; Encapsulation efficiency; Drug-loading amount; Preparation technology; Quality evaluation
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