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題 名 | 白蘝與蜜紅葡萄及其成分之製劑製備暨其抗光老化及抗光致癌性機制之探討=The Investigation on Preparations of Ampelopsis Japonica, Vitis vinifera x-Vitis labrus Cal. and Their Active Constituents and Their Mchanisms for Anti-photoaging and Anti-photocarcinogenesis |
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作 者 | 溫國慶; | 書刊名 | 中醫藥年報 |
卷 期 | 3 2014.12[民103.12] |
頁 次 | 頁(14)1-(14)75 |
分類號 | 414.34 |
關鍵詞 | 楊梅黃酮; 槲皮素; 白蘝; 蜜紅葡萄; 固態脂質奈米粒; Myricetin; Quercetin; Ampelopsis japonica; Vitis vinifera x Vitis labrus Cal.; Solid lipid nanoparticle; |
語 文 | 中文(Chinese) |
中文摘要 | 研究目的:本篇研究目的在於以白蘝及蜜紅葡萄之三指標成分 Myricetin、Quercetin 與 Resveratrol作標的,進行其抑制 MMPs 活性之上游調控機制之探討,亦將上述標的物製備為固態脂質奈米微粒、奈米結構脂質載體和乳劑三種劑型,探討其藥物載體物化性質及經皮吸收效果比較,以開發載藥率高、經皮吸收佳、且安定性佳的新劑型。 研究方法:將 Myricetin、Quercetin 與 Resveratrol進行處方設計,製備成適合包覆藥物的固態脂質奈米微粒 (solid lipid nanoparticles, SLN)、奈米結構脂質載體 (nanostructured lipid carriers, NLC)和乳劑 (emulsion, Em)三種劑型後,配合四種界面活性劑系統組成,共 12 種劑型,並測量載體的粒徑、粒子分散指標和表面電位。進行體外穿透、釋放實驗與藥物在皮膚內的含量,並以示差熱掃描分析儀、穿透式電子掃描顯微鏡觀測載體的性質與型態以評估藥物載體的安定性與應用性。 結果與討論:包覆 0.5% (w/v) 的藥物載體之平均粒徑與未含藥的空白處方無差異,其趨勢以 NLC < Em< SLN。以 NLC 系統粒徑最小介於 150~250 nm。經穿透皮膚實驗結果得知 Myricetin、Quercetin 的穿透速度以 NLC 系統最高,但 Myricetin穿透速度低於 0.04 (μg/cm2/h)而 Quercetin 為 0.431 (μg/cm2/h),但 Resveatrol 則以 Em系統最好為 1.52 (μg/cm2/h)。三化合物的穿透皮膚的能力以 Resveratrol > Quercetin > Myricetin。 皮內含量實驗結果發現 Myricetin 在 NLC系統中最好; Quercetin 在 Em系統中最好是控制組的 12.09 倍。而 Resveratrol 則在 NLC系統中最高平均值為175.97 (μg/g)。在釋放實驗中探討化合物從製劑中釋放到皮膚表面的能力,結果發現 Myricetin釋放速度是 NLC高於 SLN,而 Quercetin 釋放速度趨勢為 Em > NLC > SLN,結果與 Resveratrol一致。 從示差熱掃描分析與穿透式電子掃描顯微鏡結果影像圖得知固態脂質雖然屬於非穩定的 α脂質晶型結構,但為邊緣明顯圓形的表面型態,且經三週內驗證粒子顆粒、分散指標以及表面電位穩定,因此為安定的藥物載體。Myricetin 可抑制 UV所誘發之纖維母細胞 MMP-1及 3之表現,而此活性係透過抑制 p-JNK及 p-ERK,及抑制 Smad7、c-Jun、c-fos 之表現。 |
英文摘要 | AIM: This study aimed to investigate the percutaneous absorption of the traditional emulsion (Em), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) of myricetin and quercetin which are the constituents of Ampelopsis japonica and Vitis vinifera x-Vitis labrus. A high drug load, percutaneous absorption and stable dose form was developed for these compounds. In addition the anti-photoaging activity and mechanisms of myricetin was studied. METHOD: Three dosage forms-traditional emulsion, SLN, NLC-A and NLC-O/F/W-and four surfactants consisted twelve formulations for myricetin and quercetin. The particle size, particle dispersion index and zeta potential of the particles were determined. The particle aws applied in percutaneous absorption study, release and skin deposit study. The characterics and type of particle was assayed by DSC and TEM for evaluating the stability and application of the particles. RESULTS & DISCUSSION: 1. The particle size of 0.5% (w/v) compounds was similar to compound free particle and the particle size ranges from 150 to 250 nm. 2. The results indicated that the highest percutaneous rate of myricetin and quercetin was NLC and that of resveratrol was Em. The percutaneous rate of myricetin was 0.04 μg/cm2/h, quercetin was 0.431 μg/cm2/h and resveratrol was 1.52 μg/cm2/h. The subsequence of percutaneous rate was resveratrol > quercetin > myricetin. The results of skin deposit assay indicated the highest of myrecetin and resveratrol were NLC and that of quercetion was Em. The skin deposit of quercetin/Em is 12.09 times of control and that of resveratrol/NLC is 175.97 μg/g. The results of release study indicated that the release rate of myricetin/NLC was higher than myricetin/SLN, and the subsequence of quercetin and resveratrol were Em > NLC > SLN. The results of DSC and TEM indicated that SLN was an unstable α lipid crystal with round edge. The particle size, particle dispersion index and zeta potential were stable after three weeks. Myricetin inhibited UV-induced MMP-1 and 3 expression in fibroblast via inhibiting p-JNK, p-ERK, Smad7, c-Jun and c-fos expression. |
本系統中英文摘要資訊取自各篇刊載內容。