標題：山萘酚靶向脂質(zhì)體的制備與評價

文獻鏈接：https://xueshu.baidu.com/usercenter/paper/show?paperid=1g680vn0jq2m08y05w0v02a0ha417808&site=xueshu_se

作者：劉祖浩，雷玉杰，宋浩穎，常聰

摘要：

目的制備山萘酚靶向脂質(zhì)體(cRGD-LP-KAE)并考察初步穩(wěn)定性.方法 以L-α-磷脂酰膽堿(PC),膽固醇(CHO),二硬脂�；�磷脂酰乙醇胺-聚乙二醇-環(huán)精氨酰甘氨酰天冬氨酸(DSPE-PEG-cRGD),山萘酚(KAE)為材料,采用薄膜分散法結(jié)合微孔濾膜法制備cRGD-LP-KAE;以粒徑,包封率等指標篩選膽脂比,藥脂比,聚脂比與凍干保護劑,確定脂質(zhì)體的最優(yōu)處方工藝;用透射電鏡觀察脂質(zhì)體形貌,粒度電位儀檢測脂質(zhì)體粒徑及其分布,zeta電位,紫外分光光度法檢測脂質(zhì)體載藥量與包封率;以脂質(zhì)體復溶后粒徑,包封率的變化為指標考察初步穩(wěn)定性.結(jié)果 最優(yōu)處方工藝是CHO,KAE,DSPE-PEG-cRGD和PC的摩爾比為15 ︰ 6 ︰ 4 ︰ 120,蔗糖作為凍干保護劑,其與PC的質(zhì)量比是4 ︰ 1.根據(jù)該處方工藝制備的脂質(zhì)體呈類球形結(jié)構(gòu),粒徑和zeta電位分別是(148.60±0.20)nm和(-21.97±0.15)mV,包封率和載藥量分別是(98.97±0.27)%和(1.12±0.06)%,在低溫存儲15天時粒徑增加2.76%,包封率降低2.71%.結(jié)論cRGD-LP-KAE粒徑小且分布均勻,包封率高,在低溫存儲時穩(wěn)定性良好。

譯文：

Objective to prepare kaempferol targeted liposomes (crgd LP KAE) and investigate its preliminary stability Methods using L - α - phosphatidylcholine (PC), cholesterol (CHO), distearoyl phosphatidylethanolamine polyethylene glycol cycloarginyl glycyl aspartic acid (DSPE peg crgd), kaempferol (KAE) as materials, crgd LP KAE was prepared by membrane dispersion method combined with microporous filtration membrane method; The optimal formulation and technology of liposomes were determined by selecting the bile lipid ratio, drug lipid ratio, polyester ratio and freeze-drying protectants according to particle size, entrapment efficiency and other indicators; The morphology of liposomes was observed by transmission electron microscope, the particle size and distribution of liposomes were detected by particle size potential meter, the zeta potential, and the drug loading and entrapment efficiency of liposomes were detected by UV spectrophotometry; The initial stability of liposomes was evaluated by the changes of particle size and entrapment efficiency after re dissolution Results the optimal formulation process was that the molar ratio of CHO, KAE, DSPE peg crgd and PC was 15 ∶ 6 ∶ 4 ∶ 120, and the mass ratio of sucrose to PC was 4 ∶ 1. The liposomes prepared according to the formulation process were spherical like structure, with particle size and zeta potential of (148.60 ± 0.20) nm and (-21.97 ± 0.15) MV, respectively. The entrapment efficiency and drug loading were (98.97 ± 0.27)% and (1.12 ± 0.06)% respectively. When stored at low temperature for 15 days, the particle size increased by 2.76%, and the entrapment efficiency decreased by 2.71%.It is necessary to Conclusion crgd LP KAE has small particle size, uniform distribution, high encapsulation efficiency and good stability in low temperature storage.

DOI：10.3969/j.issn.1008-987x.2021.03.09

研究背景

山萘酚（α-mangostin）是一種來源于山竹果皮的天然產(chǎn)物，具有一定的*氧化、*微生物等生物活性。由于其水溶性差、生物利用度低、在體分布不均等問題，其直接應用受到限制。脂質(zhì)體作為一種包載性強、生物相容性良好的載藥系統(tǒng)，在改善山萘酚藥代行為方面具有潛力。

此外，為提升山萘酚在特定細胞或組織中的富集效率，可將脂質(zhì)體進一步修飾以實現(xiàn)主動靶向。例如，通過引入小分子配體（如RGD、多肽、糖類）、抗體片段或其他識別結(jié)構(gòu)，可增強其細胞識別性和轉(zhuǎn)運能力。

山萘酚脂質(zhì)體系統(tǒng)結(jié)合了納米遞送平臺與天然活性分子的優(yōu)勢，具備一定的開發(fā)前景。通過PEG修飾可以顯著延長脂質(zhì)體在體內(nèi)的循環(huán)時間，而引入RGD、葉酸或其他配體實現(xiàn)主動靶向，可增強在疾病部位的聚集與攝取能力。

本體系的后續(xù)優(yōu)化方向可包括：

• 不同PEG鏈長與密度對靶向效果的影響；

• 多肽序列選擇與排列對親和力的調(diào)節(jié)；

• 與其他天然藥物（如姜黃素、白藜蘆醇）組合遞送的協(xié)同效果；

• 體內(nèi)藥動學、組織分布及安全性評估。

西安pg電子官方生物提供相關(guān)產(chǎn)品：

Peptides PEG DSPE

RGD-PEG-DSPE

cRGD-PEG-Hyd-DSPE

cRGD(c[RGDfc])-PEG-DSPE

cRGD(c[RGDfK])-PEG-DSPE

cRGD(c[RGDyK])-PEG-DSPE

iRGD-PEG-DSPE

TAT-PEG-DSPE

Cy3-iRGD-PEG-DSPE

FITC-iRGD-PEG-DSPE

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