中药挥发油对盐酸巴马汀纳米柔性脂质体药剂学性能的影响
发布时间：2018-12-24 09:33
【摘要】：柔性脂质体(flexible nano-liposomes,FL)是一种优良的给药载体,但液体状态下的药物泄漏已严重阻碍了其进一步广泛应用,因此,抑制药物泄漏已成为亟待解决的行业共性技术问题。本文将5种常见挥发油如艾叶油(Folium Artemisiae Argyi oil,FA)、桉叶油(Folium Eucalypti oil,FE)、茉莉油(Arabian Jasmine oil,AJ)、丁香油(Syzygium Aromaticum oil,SA)和连翘油(Fructus Forsythiae oil,FF)分别包埋于盐酸巴马汀纳米柔性脂质体(palmatine chloride loaded flexible nano-liposomes,PFL)的脂质双分子层内,通过体外泄漏曲线评价筛选能够降低PFL药物泄漏的最佳挥发油及其用量水平;考察包埋挥发油后对PFL包封率、粒径、电位、变形性与结构的影响,并通过白兔阴道给药考察其对黏膜的刺激性;最后,采用水平双室扩散池评价挥发油对PFL体外透皮透黏膜给药行为的影响。结果显示,5种挥发油均能不同程度地抑制PFL内水相中药物的泄漏,但艾叶油抑制泄漏的程度显著优于其他4种挥发油(P0.05),且艾叶油与脂质质量比为1∶6时具有最佳的抑制泄漏作用;包埋艾叶油的PFL与PFL在包封率、粒径、电位与变形性等方面无显著性差异(P0.05),且二者层状囊泡结构相似;包埋艾叶油后也进一步增强了PFL促进内水相中药物透皮透黏膜的吸收能力,而对白兔阴道黏膜无刺激性。综上,在柔性脂质体的磷脂膜中包埋合适的挥发油(如艾叶油)不仅可在一定程度上抑制内水相中药物的泄漏,且能够增强柔性脂质体促进药物透皮透黏膜的吸收。因此,本文为克服液体状态下纳米柔性脂质体药物泄漏提供了一种新方法和新思路。
[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.
【作者单位】： 西安医学院药学院;
【基金】：国家自然科学基金资助项目(81303231) 陕西省自然科学基金面上项目(2015JM8442)
【分类号】：R943
本文编号：2390464
[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.
【作者单位】： 西安医学院药学院;
【基金】：国家自然科学基金资助项目(81303231) 陕西省自然科学基金面上项目(2015JM8442)
【分类号】：R943
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