Alerta

CATIONIC LIPIDS FOR USE IN LIPID NANOPARTICLES

Resumen de: EP4678164A2

Compounds are provided having the following structure:or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein a, b, c, d, G¹, G², L¹, L², R^1a, R^1b, R^2a, R^2b, R^3a, R^3b, R^4a, R^4b, R⁵, R⁶, R⁷, R⁸ and X are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, nanoparticles comprising the compounds and methods for their use and preparation are also provided.

NOVEL IONIZABLE CATIONIC LIPIDS CONTAINING THIOETHER LINKAGE

Resumen de: WO2025109504A1

The invention relates to novel ionizable amine lipids incorporating one or more sulphur atoms in the tail section. These lipids can be used in combination with other components to form lipid nanoparticles with oligonucleotides. The invention describes the synthesis of the lipids of formula (I), formation and characterization of nanoparticles and biological experiments demonstrating that the lipid nanoparticles prepared with these novel lipids can efficiently deliver their cargo (e.g. RNA, DNA, mRNA, siRNA, miRNA, pDNA, circular DNA, dsRNA, small biologically active molecules) into the cells.

BIOSENSORS COMPRISING CHARGED BIOPOLYMERS AND USE THEREOF

Resumen de: CN120769984A

A biosensor for detecting the presence or amount of a charged analyte in a sample is provided. The biosensor may include a core component and a charged biopolymer component, the charged biopolymer component including one or more layers of a charged biopolymer. An outermost layer of the charged biopolymer component is oppositely charged relative to the charged analyte and is capable of binding to the charged analyte. The biosensor may comprise two or more alternating layers of oppositely charged biopolymers, each layer being oppositely charged relative to an adjacent layer. Also provided are devices coupled to the biosensor for quantifying a signal resulting from binding of the biosensor to the charged analyte, and methods of using the biosensor to detect the presence or amount of a charged analyte in a sample.

NOVEL LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS

Resumen de: MX2025010536A

The present invention provides novel ionizable lipids and novel lipid nanoparticles comprising messenger RNA (mRNA) useful for the delivery of nucleic acids, related pharmaceutical compositions or vaccines as defined herein for use in human or veterinary medicine, in particular for use in the treatment and/or prophylaxis of cancer diseases.

IONIZABLE LIPID MOLECULE, PREPARATION METHOD THEREFOR AND USE THEREOF

Resumen de: EP4678629A1

An ionizable lipid molecule, a preparation method therefor and a use thereof. Specifically, provided are a compound represented by formula I, and a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug or solvate thereof. The definition of each group in the formula is as described in the description. Also provided is a lipid nanoparticle, containing the ionizable lipid compound represented by formula (I). Further provided are a composition and a related use. The compound of formula I can be used to prepare the lipid nanoparticle for delivering a nucleic acid therapeutic agent or an active agent in vivo and in vitro.

NANOPARTICLE FORMULATIONS FOR A NON-OPIOID DRUG

Resumen de: AU2024234362A1

This disclosure is directed to a nanoparticle formulation for N,N-Diethyl-2-(N-(2-(4-hydroxyphenylamino)-2-oxoethyl)sulfamoyl)benzamide (SRP-3D (DA)), an active pharmaceutical ingredient that is insoluble in water and cannot be dissolved in any injection-safe vehicle to a sufficient concentration for dosing. Also encompassed by the disclosure are nanoparticulate suspension comprising a nanoparticulate SRP-3D (DA) (or SRP-3D (DA) nanoparticles), a wetting agent and a cryoprotectant. The nanoparticulate compositions comprise SRP-3D (DA) particles having an average particle size of less than about 500 nm or less than about 300 nm.

MUNS FUSION PROTEIN CAPABLE OF FORMING MICROSPHERES AND USES THEREOF

Resumen de: EP4678653A1

The invention relates to a fusion protein encoding a polypeptide based on the minimal region of the Orthoreovirus muNS protein capable of forming microspheres and/or nanospheres, modified to permit the addition of polypeptides at the C-terminal.

靶向治疗溃疡性结肠炎的固体脂质纳米粒-菊粉凝胶复合物及其制备方法

Resumen de: CN121313547A

本发明公开了一种靶向治疗溃疡性结肠炎的固体脂质纳米粒‑菊粉凝胶复合物及其制备方法，属于医药技术领域，该复合物包括菊粉凝胶以及分散在菊粉凝胶中的固体脂质纳米粒；所述的固体脂质纳米粒包括甘油酯外壳及其包被的油酸、具有抗炎和抗氧化作用的药物、以及阳离子脂质；油酸、具有抗炎和抗氧化作用的药物和阳离子脂质的质量比为1：1‑1.5：2.5‑3；所述的固体脂质纳米粒中的载药量为1wt％‑10wt％。该复合物以菊粉凝胶作为递释系统，内搭载功能固体脂质纳米粒，可以降低肠道铁死亡，清除活性氧，具有促进肠道屏障修复、减轻炎症反应等功效，在溃疡性结肠炎的治疗方面具有良好的应用前景。

一种粘膜上皮细胞靶向的口服ROS响应型纳米酶及其制备方法和应用

Resumen de: CN121313671A

本发明公开了一种粘膜上皮细胞靶向的口服ROS响应型纳米酶及其制备方法和应用，涉及生物医药技术领域。该口服ROS响应型纳米酶包括Ce‑CCDs碳点和甜菜碱聚合物，该甜菜碱聚合物包覆于该Ce‑CCDs碳点表面，形成纳米颗粒；该Ce‑CCDs碳点是以金属铈源与绿原酸为原料，通过热解法制备得到。本发明通过结构创新与功能整合，使制备的纳米酶在催化活性、靶向递送、协同治疗及产业化应用等方面均展现出突出优势，为炎症性肠病的高效、安全治疗提供了新的技术方案，具有显著的技术创新性与临床应用价值。

一种可电离脂质及其制备方法和应用、药物组合物

Resumen de: CN121318767A

本发明提供了一种可电离脂质及其制备方法和应用、药物组合物，属于药物递送技术领域。本发明提供了一种可电离脂质，在无需引入靶向配体修饰的情况下，能够实现核酸药物在脾脏的特异性表达，有效避免肝脏等非靶器官的脱靶表达。该类化合物无佐剂活性，不引起抗原提呈细胞的活化，递送编码自身抗原的mRNA，可重建机体对自身抗原的特异性免疫耐受，从而达到从根本上治疗自身免疫病的目的，在自身免疫病疫苗开发及免疫治疗等领域具有广阔应用前景。

一种可电离脂质分子及其制备方法和应用、脂质纳米颗粒及其应用

Resumen de: CN121318763A

本发明提供了一种可电离脂质分子及其制备方法和应用、脂质纳米颗粒及其应用，属于药物化学技术领域。本发明提供了一种可电离脂质分子，是一种新型可电离脂质分子，与非阳离子脂质、固醇和聚乙二醇脂质制得的LNP能提高负载物核酸药物的递送效率，且毒性小。实施例的数据表明，在体外和体内的递送中，具有优良的递送核酸至细胞中的能力，并显著优于USFDA批准的阳性对照(SM‑102)氨基脂质。

一种自组装多肽复合物及其应用

Resumen de: CN121313785A

本发明涉及生物医药技术领域，具体涉及一种自组装多肽复合物及其应用，所述自组装多肽复合物由氟化修饰的阳离子高分子多肽递送载体与母乳来源多肽自组装而成，所述母乳来源多肽的氨基酸序列为VTQPLAPVHNPISV。本发明通过采用氟化修饰的阳离子高分子多肽递送载体(PF)结合母乳来源多肽(MAMP‑1)，能够有效减轻NEC小鼠脑、肺、肠损伤，且PF结合MAMP‑1后比单独用MAMP‑1效果更显著，保护作用更有效。通过改造，有望开发出更高效、更安全的用于预防或治疗NEC的药物、保健品或食品添加物，推动从基础研究向临床应用转化。

细胞外囊泡组合物和制备

Resumen de: AU2024269259A1

In various aspects and embodiments provided are compositions containing extracellular vesicles (including modified extracellular vesicles), methods of making preparations of extracellular vesicles, methods of modifying extracellular vesicles and methods of using modified and/or unmodified extracellular vesicles.

一种基于蔷薇果细胞外囊泡的新型靶向药物递送系统

Resumen de: CN121313557A

本发明涉及生物医学工程及药物递送技术领域，具体公开了一种基于蔷薇果细胞外囊泡的新型靶向药物递送系统，包括：制备蔷薇果来源细胞外囊泡；制备载药囊泡；制备靶向修饰载药囊泡；本发明通过蔷薇果成分特异性下调干性相关通路，同时利用阿霉素杀伤常规肿瘤细胞，形成互补的治疗机制，从根本上降低肿瘤复发风险。利用DSPE‑PEG‑PBA的苯硼酸基团特异性识别肿瘤细胞表面过表达的唾液酸，显著提高药物在肿瘤组织的富集，同时减少对正常组织的分布。借助RHNVs天然的生物相容性和低免疫原性，结合PEG链的长循环特性，在保证递送效率的同时最大限度地降低全身毒性，特别是减轻阿霉素的心脏毒性和骨髓抑制。

一种缓解母猪便秘及炎症的功能性饲料添加剂及其制备方法和应用

Resumen de: CN121312745A

本发明提供了一种缓解母猪便秘及炎症的功能性饲料添加剂及其制备方法和应用，所述缓解母猪便秘及炎症的功能性饲料添加剂以重量份数计包括植物提取物10‑30份、水翁花多酚‑介孔二氧化硅纳米颗粒0.5‑2份和植物多糖0.1‑1份。本发明提供的功能性饲料添加剂可通过调控母猪肠道中潜在生物活性代谢物、碳水化合物活性酶的相对含量和血清中代谢物的相对含量，从而减轻机体炎症，缓解便秘，显著降低了母猪便秘发生率，改善了母猪机体健康，提高了母猪的生产性能。

一种基于牦牛骨肽活性提取物的骨密度增强剂制备方法及应用

Resumen de: CN121312834A

本发明涉及骨密度增强剂技术领域，且公开了一种基于牦牛骨肽活性提取物的骨密度增强剂制备方法及应用，包括以下质量份原料：钙化合物20‑25份、氨基葡萄糖硫酸钾盐33‑42份、硫酸软骨素24‑28份、胶原蛋白肽15‑20份、双磷酸盐15‑18份、牦牛骨肽活性提取物基核壳颗粒10‑15份。牦牛骨肽活性提取物基核壳颗粒能够避免牦牛骨肽活性提取物中的肽链被胃酸和消化酶降解，导致成骨活性降低，进而促进成骨细胞的增殖和分化，提高骨密度。

氟化可吸入/口服脂质体纳米颗粒药物递送平台及其制备和应用

Resumen de: CN121313611A

本发明公开了一种氟化可吸入/口服脂质体纳米颗粒药物递送平台及其制备方法和应用。氟化可吸入/口服脂质体纳米颗粒药物递送平台具有核壳结构，核壳结构包括脂质核心层和响应型交联壳层；脂质核心层包括含叔胺基的可电离脂质、接枝碳碳双键结构片段的DSPE衍生物、固醇和PEG化脂质且包裹药物；响应型交联壳层由包含PFA和ROS响应型交联剂在内的物料与脂质核心层中DSPE衍生物通过碳碳双键聚合形成。本发明通过在LNPs外层修饰氟化聚合物壳层扩展其给药途径，解决LNPs难以高效口服递送的问题。

一种巨噬细胞膜包被的自组装纳米制剂及其制备方法与应用

Resumen de: CN121313599A

本发明属于生物医药技术领域，具体公开了一种巨噬细胞膜包被的自组装纳米制剂及其制备方法与应用。所述纳米制剂以表没食子儿茶素没食子酸酯（EGCG）、氯化铁（FeCl3）和依达拉奉（EDV）自组装形成的纳米颗粒为核心，外层包被巨噬细胞膜。其制备方法为“一锅法”，即将EGCG、FeCl3和EDV在磷酸盐缓冲液中混合自组装，离心纯化后，再与巨噬细胞膜通过超声融合。该纳米制剂粒径均一，具有优异的自由基清除能力和抗氧化活性，并能够有效穿越血脑屏障，靶向脑缺血再灌注损伤区域，在制备治疗缺血性脑卒中的药物中表现出显著效果。

一种长效干粉微球吸入剂及制备方法和应用

Resumen de: CN121313612A

本发明属于药物制剂领域，公开了一种长效干粉微球吸入剂及制备方法和应用。吸入剂以磷脂制备的多囊囊泡与干粉辅料混合物作为药物载体，包载治疗肺部疾病的活性成分，通过喷雾干燥技术制备的一种长效干粉微球吸入剂。该长效干粉微球吸入剂与传统单囊脂质体制备的干粉微球吸入剂相比有更长时间的缓释效果。该制剂采用先制备多囊囊泡再喷雾干燥的独特工艺，所得微球具有1‑5μm的空气动力学粒径，能有效沉积于肺部，并展现显著的长效缓释特性，体外释放48h累积释放率达64%左右。与传统单囊脂质体吸入剂相比，本发明有效延长了药物作用时间，减少给药频率，提高了患者依从性。本发明为肺部给药系统的研究提供了新思路，具有广阔的临床应用前景。

一种碳酸钙纳米药物的制备方法及其应用

Resumen de: CN121313827A

本发明公开了一种碳酸钙纳米药物的制备方法和应用，本发明以碳酸钙纳米颗粒为载体，成本低廉、制备简单可量产，且能在肿瘤弱酸性微环境中分解，消耗H⁺以提高肿瘤微环境pH值，同时避免体内积累，无额外毒副作用；采用透明质酸（HA）修饰载体，可与肿瘤细胞CD44受体特异性结合，结合纳米颗粒的高通透性和滞留效应（EPR），增强靶向性，提升光敏剂在肿瘤部位的富集量；另外，通过装载光敏剂竹红菌素（HB），有效改善光敏剂疏水性与聚集体问题，提升PDT效率；并且联合高压氧疗法，同步改善肿瘤低氧微环境，破解PDT因缺氧导致的疗效瓶颈，形成“靶向递送‑微环境调节‑高效PDT”的协同作用。

一种负载雷公藤红素的纳米颗粒及其制备方法与应用

Resumen de: CN121313604A

本发明属于药物技术领域，具体涉及一种负载雷公藤红素的纳米颗粒及其制备方法与应用，所述负载雷公藤红素的纳米颗粒（Cel‑GDNPs），包括生姜外泌体（GDNPs）和包封于所述生姜外泌体内部的雷公藤红素（Cel）。本发明将Cel作为治疗药物的同时，采用的载体GDNPs本身具有抗炎活性，在治疗结肠炎等炎症性疾病时，Cel与GDNPs可发挥多组分协同治疗效应，相较于单独使用Cel或GDNPs，能够更有效地抑制促炎因子（如TNF‑α,IL‑1β,IL‑6）的表达，从而实现协同增效的治疗效果，为开发新型天然复方制剂提供了新策略。

用于递送生物活性剂的可电离阳离子脂质化合物

Resumen de: WO2025002399A1

The present disclosure relates to novel lipid compounds for delivering one or more biologically active molecules to a subject. The present application also relates to a composition or a nanoparticle comprising said lipid compounds, methods of preparing said lipid compounds, method of using said lipid compounds and use of said lipid compounds.

用于调节纤溶酶原激活物抑制剂-1(PAI-1)的方法和组合物

Resumen de: AU2024280598A1

A siRNA molecule for inhibiting expression of plasminogen activator inhibitor-1 (PAI-1) is disclosed and may have a sense strand and an antisense strand. The sense strand may have at least 80% sequence identity to any one of SEQ ID NOs: 3, 5, 7, and 9. In some embodiments, the antisense strand may have at least 80% sequence identity to any one of SEQ ID NOs: 4, 6, 8, and 10. The sense strand and/or the antisense strand may comprise one or more modified nucleotides. The sense strand and/or the antisense strand may comprise of a ligand. A lipid nanoparticle comprising the siRNA molecule is also disclosed. Methods of using the siRNA molecule or the lipid nanoparticle comprising the siRNA molecule to treat a subject who suffers from at least one PAI-1-associated condition, disease or disorder are also disclosed.

用于靶向树突细胞的纳米递送的方法和组合物

Resumen de: TW202506200A

The present disclosure relates to novel compounds, methods, and cell-targeting formulations, e.g., a lipid nanoparticle (LNP) for targeted delivery to a tissue or a cell type. The compound and formulation provided herein are designed to have a targeting moiety configured to provide selective delivery features for the formulation and a lipid tail for being incorporated into the bilayer membrane of the formed lipid nanoparticle.

一种使用玉米醇溶蛋白和黄芪多糖提高甘草酸稳定性的方法及在制备护肝药物中的应用

Nº publicación: CN121313603A 13/01/2026

Solicitante:

合肥工业大学

Resumen de: CN121313603A

一种使用玉米醇溶蛋白和黄芪多糖提高甘草酸稳定性的方法及在制备护肝药物中的应用，包括：(1)原料溶解；(2)原料混合；(3)纳米粒子制备与冻干。本发明制备的玉米醇溶蛋白/黄芪多糖/甘草酸纳米颗粒，在体外模拟消化实验中，其生物可及性达到72.84％，相比游离甘草酸(30.70％)显著提高。该纳米复合物自由基清除率在66.23％～73.34％之间，并在储存两天后仍能保持40％以上活性，表现出良好的pH、离子强度、温度和存储稳定性。细胞实验表明，在100μg/mL浓度下，该纳米复合物可将AML‑12细胞存活率提高至95.50％，显著优于游离甘草酸(20μg/mL时为83.77％)，具有更强的稳定性和细胞保护作用。