本文選題：聚乳酸 + 柚皮素��； 參考：《太原理工大學》2017年碩士論文

【摘要】：近些年來,以緩控釋給藥系統(tǒng)、靶向給藥系統(tǒng)、經(jīng)皮給藥系統(tǒng)為代表的藥物傳輸系統(tǒng)發(fā)展迅猛,為臨床治療提供了更多的選擇。其中,緩釋和控釋系統(tǒng)是發(fā)展最快的新型給藥系統(tǒng),具有許多優(yōu)越性:可緩釋藥物,從而延長藥物作用時間;可在保證療效的前提下,減少給藥劑量,減輕毒副反應;還可提高藥物的穩(wěn)定性。研究者們常將高分子聚合物作為藥物載體應用于藥物緩釋和控釋系統(tǒng),并將它們制備成粒徑為1~(-1)000 nm的粒子,這些納米粒子能穿透組織間隙并被細胞吸收,并通過人體最小的毛細血管。制備聚合物納米粒的載體材料以合成的可生物降解的聚合物體系和天然的大分子體系為主,其中聚乳酸(PLA)因為良好的生物相容性和生物可降解性被廣泛應用。柚皮素是一種具有抗菌、抗氧化、抗?jié)�、抑制肝臟的纖維化、抗腫瘤活性的黃酮衍生物。但是,它易氧化,在體內(nèi)代謝速度快,血藥濃度不易控制,存在肝腸循環(huán),口服生物利用度較低,嚴重制約了其在生物領(lǐng)域的應用。為克服其缺點,本論文采用可降解的聚乳酸為載體,將柚皮素制備成聚乳酸載柚皮素納米粒,期望能夠為今后柚皮素緩釋制劑的研究提供一些有價值的參考,促進柚皮素的臨床應用。本論文主要工作如下:1、本論文采用改良的溶劑揮發(fā)法制備了聚乳酸載柚皮素納米粒,采用單因素實驗分別考察了聚乳酸分子量、聚乳酸質(zhì)量濃度、油水相體積比、超聲時間、投藥比以及乳化劑質(zhì)量分數(shù)對納米粒粒徑、載藥量和包封率的影響,并篩選出了最佳制備工藝參數(shù);采用場發(fā)射掃描電子顯微鏡、傅立葉紅外光譜儀、x射線衍射儀、激光粒度儀、紫外可見分光光度計、酶標儀對納米粒的形貌、組成、粒徑、載藥性能、緩釋性能和抗菌性能等進行了表征測試。結(jié)果表明,最佳制備條件是聚乳酸分子量8萬,聚乳酸質(zhì)量濃度0.03g·ml~(-1),聚乙烯醇(pva)質(zhì)量分數(shù)1%,油水相體積比1:5,超聲時間1min,投藥比5:1。由最佳工藝制得的載藥納米粒呈圓整球形,平均粒徑為135.2nm,分散指數(shù)為0.073,載藥量為22.3%,包封率為64.7%,且在體外環(huán)境下釋藥時間在250h以上,具有良好的緩釋效果。然而其緩釋樣液在低濃度下(低于20μg·ml~(-1))甚至會促進金黃色葡萄球菌的生長。2、為了提高聚乳酸載柚皮素納米粒的抗菌性能,本論文將其與淀粉載銀納米顆粒進行復合,制備了聚乳酸包覆柚皮素及淀粉載銀復合納米材料。首先,在本實驗室前人工作的基礎(chǔ)上,采用液相化學還原法,以葡萄糖為還原劑,淀粉為保護劑制備了淀粉載銀納米顆粒;采用場發(fā)射掃描電子顯微鏡、透射電子顯微鏡、傅立葉紅外光譜儀、x射線衍射儀、激光粒度儀對淀粉載銀納米顆粒的形貌、組成、粒徑等進行了表征;然后采用改良的溶劑揮發(fā)法制備了聚乳酸復合納米粒,通過正交實驗篩選了最佳的制備工藝條件;采用場發(fā)射掃描電子顯微鏡、透射電子顯微鏡、X射線衍射儀、激光粒度儀、紫外可見分光光度計、酶標儀對復合納米粒的形貌、組成、粒徑、載藥、緩釋和抗菌性能等進行了表征測試。結(jié)果顯示,淀粉載銀納米顆粒呈球形,平均粒徑為10.1 nm,分散指數(shù)為0.112。制備的聚乳酸復合納米粒的最佳條件是PLA質(zhì)量濃度0.03 g·m L~(-1),淀粉載銀0.02 g,乳化劑質(zhì)量分數(shù)1%,油水比1:5。該條件下制得的聚乳酸復合納米粒呈圓整球形,平均粒徑為379 nm,分散指數(shù)為0.132,載藥量為20.8%,包封率為53.8%,其具有良好的抗菌效果,并且柚皮素的緩釋效果沒有受到影響。
[Abstract]:In recent years, the drug delivery system, targeting drug delivery system, targeted drug delivery system and transdermal drug delivery system, has developed rapidly and provided more options for clinical treatment. The slow release and controlled release system is the fastest developing new drug delivery system, with many advantages: the drug delivery system can be extended to prolong the drug action time; On the premise of ensuring the curative effect, it can reduce the dosage, reduce the side effects, and improve the stability of the drug. The researchers often use polymer as drug carrier in drug release and controlled release system, and prepare particles with a particle size of 1~ (-1) 000 nm, which can penetrate the interstitial space and be absorbed by the cells. A biodegradable polymer system and a natural macromolecular system are synthesized through the preparation of the carrier material of polymer nanoparticles, in which polylactic acid (PLA) is widely used because of its good biocompatibility and biodegradability. Naringenin is an antiseptic, antioxidation, anti ulcer, and inhibiting liver. However, it is easy to oxidize, it is easy to oxidize, it has fast metabolism in the body, the concentration of blood drug is not easy to control, the liver intestine circulation is not easy to be controlled, the oral bioavailability is low, which seriously restricts its application in biological field. In order to overcome its shortcomings, this paper uses degradable polylactic acid as the carrier to prepare naringenin. The lactate naringin nanoparticles are expected to provide some valuable reference for the study of naringin sustained-release preparation in the future. The main work of this thesis is as follows: 1. The paper uses the modified solvent evaporation method to prepare the polylactic naringin nanoparticles, and the single factor experiment is used to investigate the polylactic acid fraction respectively. The effects of the weight, the mass concentration of the polylactic acid, the volume ratio of the oil and water, the time of the ultrasonic, the ratio of the dosage and the mass fraction of the emulsifier on the size of the nanoparticles, the amount of drug loading and the encapsulation efficiency, and the optimum processing parameters were selected. The field emission scanning electron microscope, the Fu Liye infrared spectrometer, the X ray diffractometer, the laser particle size instrument, and the UV visible fraction were used. The morphology, composition, particle size, particle size, drug loading performance, sustained release and antibacterial properties of nanoparticles were characterized by photometer. The results showed that the optimum preparation conditions were 80 thousand of the molecular weight of polylactic acid, 0.03g. Ml~ (-1) of polylactic acid, 1% of polyvinyl alcohol (PVA), 1:5 of oil water phase volume ratio, 1min of ultrasonic time, and dosage of 5:1 The drug loaded nanoparticles obtained by the best process are round and round, with an average particle size of 135.2nm, a dispersion index of 0.073, a drug loading of 22.3%, a encapsulation rate of 64.7%, and a release time of more than 250h in an in vitro environment, with a good release effect. However, the slow-release sample may even promote the golden yellow grape under low concentration (below 20 mu g. Ml~ (-1)). The growth of.2, in order to improve the antibacterial properties of pomelomingin nanoparticles, was combined with starch containing silver nanoparticles to prepare poly (lactic acid) coated naringenin and starch containing silver composite nanomaterials. First, on the basis of previous work in our laboratory, liquid chemical reduction was used as a reducing agent with glucose. Starch loaded silver nanoparticles were prepared as a protector, and the morphology, composition and particle size of the starch loaded silver nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, Fu Liye infrared spectrometer, X ray diffractometer, and laser particle size analyzer, and then the modified solvent evaporation method was used to prepare the polylactic acid composite. The best preparation conditions were screened by orthogonal experiment. The morphology, composition, particle size, particle size, drug loading, release and antibacterial properties of the composite nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, X ray diffractometer, laser particle size analyzer, UV visible spectrophotometer and enzyme labeling instrument. The starch carrying silver nanoparticles are spherical, the average particle size is 10.1 nm. The optimum conditions for the poly lactic acid composite nanoparticles prepared by the dispersion index of 0.112. are the PLA mass concentration 0.03 G. M L~ (-1), the starch containing silver 0.02 g, the emulsifier mass fraction 1%, the oil and water ratio of the poly lactic acid composite nanoparticles are round and round, and the average particle size is 37. 9 nm, dispersibility index 0.132, drug loading 20.8%, encapsulation rate 53.8%, it has good antibacterial effect, and naringenin sustained-release effect has not been affected.

【學位授予單位】：太原理工大學
【學位級別】：碩士
【學位授予年份】：2017
【分類號】：TB383.1;TQ460.1

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