陳積 趙小倩 胡姍姍 馬彥巧 劉燕 譚丹楓 陳澤慧 田應彪
中圖分類號 R283 文獻標志碼 A 文章編號 1001-0408(2018)05-0615-06
DOI 10.6039/j.issn.1001-0408.2018.05.10
摘 要 目的:制備復方莪術油脂質體(ZTOC-LPS)并對其質量進行評價。方法:以復方莪術油中莪術油(以吉馬酮表征)和維A酸的包封率及載藥量等為考察指標,篩選ZTOC-LPS的制備方法及處方中大豆卵磷脂(SPC)的加入量、脂質中SPC-膽固醇(CH)質量比、莪術油-脂質質量比、維A酸-脂質質量比、水浴溫度;并對最優處方制備工藝所制脂質體進行質量評價和初步穩定性考察。結果:優選的制備方法為乙醇注入法;最優處方制備工藝為每1 mL脂質體中SPC 4 mg、SPC-CH質量比3 ∶ 1、莪術油-脂質質量比1 ∶ 9、維A酸-脂質質量比1 ∶ 70、水浴溫度55 ℃。所制3批脂質體中莪術油和維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,多分散系數為 0.10±0.04;離心加速試驗結果顯示脂質體具有良好的物理穩定性;脂質體樣品在(4±2) ℃條件下放置 1 個月時各項考察指標均未發生明顯變化。結論:建立的制備方法簡單可行,所制脂質體質量符合要求,可為后續復方莪術油新劑型的研究提供參考。
關鍵詞 莪術油;維A酸;脂質體;包封率;載藥量;制備工藝;質量評價
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
銀屑病是一種常見的慢性炎癥皮膚疾病,已經影響了全球2%~3%的人口[1-2],外用藥物治療是其主要的治療方法之一。銀屑病的傳統治療主要有免疫抑制劑、類固醇激素、物理療法等方法,有如毒副作用及不良反應較多等缺點,故不易被患者接受。中醫藥治療銀屑病具有療效較好、副作用較少、復發率低等特點,在治療上具有一定的優勢[3]。……