【摘要】：柔性脂質(zhì)體(flexible nano-liposomes,FL)是一種優(yōu)良的給藥載體,但液體狀態(tài)下的藥物泄漏已嚴(yán)重阻礙了其進(jìn)一步廣泛應(yīng)用,因此,抑制藥物泄漏已成為亟待解決的行業(yè)共性技術(shù)問(wèn)題。本文將5種常見(jiàn)揮發(fā)油如艾葉油(Folium Artemisiae Argyi oil,FA)、桉葉油(Folium Eucalypti oil,FE)、茉莉油(Arabian Jasmine oil,AJ)、丁香油(Syzygium Aromaticum oil,SA)和連翹油(Fructus Forsythiae oil,FF)分別包埋于鹽酸巴馬汀納米柔性脂質(zhì)體(palmatine chloride loaded flexible nano-liposomes,PFL)的脂質(zhì)雙分子層內(nèi),通過(guò)體外泄漏曲線評(píng)價(jià)篩選能夠降低PFL藥物泄漏的最佳揮發(fā)油及其用量水平;考察包埋揮發(fā)油后對(duì)PFL包封率、粒徑、電位、變形性與結(jié)構(gòu)的影響,并通過(guò)白兔陰道給藥考察其對(duì)黏膜的刺激性;最后,采用水平雙室擴(kuò)散池評(píng)價(jià)揮發(fā)油對(duì)PFL體外透皮透黏膜給藥行為的影響。結(jié)果顯示,5種揮發(fā)油均能不同程度地抑制PFL內(nèi)水相中藥物的泄漏,但艾葉油抑制泄漏的程度顯著優(yōu)于其他4種揮發(fā)油(P0.05),且艾葉油與脂質(zhì)質(zhì)量比為1∶6時(shí)具有最佳的抑制泄漏作用;包埋艾葉油的PFL與PFL在包封率、粒徑、電位與變形性等方面無(wú)顯著性差異(P0.05),且二者層狀囊泡結(jié)構(gòu)相似;包埋艾葉油后也進(jìn)一步增強(qiáng)了PFL促進(jìn)內(nèi)水相中藥物透皮透黏膜的吸收能力,而對(duì)白兔陰道黏膜無(wú)刺激性。綜上,在柔性脂質(zhì)體的磷脂膜中包埋合適的揮發(fā)油(如艾葉油)不僅可在一定程度上抑制內(nèi)水相中藥物的泄漏,且能夠增強(qiáng)柔性脂質(zhì)體促進(jìn)藥物透皮透黏膜的吸收。因此,本文為克服液體狀態(tài)下納米柔性脂質(zhì)體藥物泄漏提供了一種新方法和新思路。
[Abstract]:Flexible liposome (flexible nano-liposomes,FL) is an excellent drug delivery carrier, but drug leakage in liquid state has seriously hindered its wide application. Therefore, inhibiting drug leakage has become a common technical problem to be solved. Five common essential oils, such as (Folium Artemisiae Argyi oil,FA, (Folium Eucalypti oil,FE, (Arabian Jasmine oil,AJ, (Syzygium Aromaticum oil,SA and (Fructus Forsythiae oil, were used in this paper. FF) was embedded in the lipid bilayer of palmatine hydrochloride nano-flexible liposome (palmatine chloride loaded flexible nano-liposomes,PFL) respectively. The optimal volatile oil and its dosage level could be reduced by evaluating the leakage curve of PFL in vitro. The effects of entrapped essential oil on the entrapment efficiency, particle size, potential, deformation and structure of PFL were investigated. Finally, the effects of volatile oil on transdermal transmucosal delivery of PFL in vitro were evaluated by horizontal double chamber diffusion cell. The results showed that all of the five essential oils could inhibit the leakage of the drugs in the aqueous phase of PFL to some extent, but the oil of Artemisia argyi was significantly better than the other four kinds of essential oils (P0.05). When the ratio of oil to lipids was 1:6, it had the best effect on inhibiting leakage. There was no significant difference in encapsulation efficiency, particle size, potential and deformability between PFL and PFL (P0.05), and the structure of lamellar vesicles was similar between them. The embedding of Artemisia lanceolata oil further enhanced the ability of PFL to promote the transdermal and transmucosal absorption of drugs in the aqueous phase, but had no irritation to the vaginal mucosa of white rabbits. In conclusion, embedding suitable essential oil (such as Artemisia lanceolata oil) in the phospholipid membrane of flexible liposomes can not only inhibit the leakage of drugs in the internal water phase to some extent, but also enhance the flexible liposome to promote the transdermal absorption of drugs through the mucous membrane. Therefore, this paper provides a new method and new idea for overcoming drug leakage of nano-flexible liposomes in liquid state.
【作者單位】： 西安醫(yī)學(xué)院藥學(xué)院;
【基金】：國(guó)家自然科學(xué)基金資助項(xiàng)目(81303231) 陜西省自然科學(xué)基金面上項(xiàng)目(2015JM8442)
【分類號(hào)】：R943

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