CN115501184B - 基于peg-plga聚合物胶束的重症哮喘治疗用探针 - Google Patents

基于peg-plga聚合物胶束的重症哮喘治疗用探针 Download PDF

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CN115501184B
CN115501184B CN202211382766.1A CN202211382766A CN115501184B CN 115501184 B CN115501184 B CN 115501184B CN 202211382766 A CN202211382766 A CN 202211382766A CN 115501184 B CN115501184 B CN 115501184B
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周林福
王建国
陈子
徐双兰
马陈惠
史东生
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Jiangsu Province Hospital First Affiliated Hospital Of Nanjing Medical University
Xuzhou Huaihai Life Science Industry Research Institute Co ltd
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Abstract

本发明的基于PEG‑PLGA聚合物胶束的重症哮喘治疗用探针,属于哮喘治疗技术领域,包括聚合物胶束和治疗剂,治疗剂表面包覆聚合胶束,治疗剂包括近红外光染料IR780荧光探针和沙美特罗,采用雾化吸入的方式进入肺部,治疗的疾病为重症哮喘,可以直接到达病灶,治疗效果好,提高利用率。

Description

基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针
技术领域
本发明属于重症哮喘治疗技术领域,更具体来说,涉及一种基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针。
背景技术
支气管哮喘(bronchial asthma)是由多种细胞(如嗜酸性粒细胞、肥大细胞、T淋巴细胞、中性粒细胞、气道上皮细胞等)和细胞组分参与的气道慢性炎症为特征的异质性疾病,这种慢性炎症与气道高反应性相关,通常出现广泛而多变的可逆性呼气气流受限,导致反复发作的喘息、气促、胸闷和(或)咳嗽等症状,强度随时间变化。多在夜间和(或)清晨发作、加剧,多数患者可自行缓解或经治疗缓解。支气管哮喘如诊治不及时,随病程的延长可产生气道不可逆性缩窄和气道重塑。
发明内容
1.发明要解决的技术问题
本发明的目的在于解决现有重症哮喘的治疗问题。
2.技术方案
为达到上述目的,本发明提供的技术方案为:
本发明的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,包括聚合物胶束和治疗剂,治疗剂表面包覆聚合胶束,治疗剂包括近红外光染料IR780荧光探针和沙美特罗。
优选的,聚合物胶束基于PEG-PLGA,聚合物胶束表面带有Siglec-9抗体。
优选的,聚合物胶束具有油溶性。
优选的,聚合物胶束为纳米结构。
优选的,Siglec-9抗体均匀分布在聚合物胶束的表面。
3.有益效果
采用本发明提供的技术方案,与现有技术相比,具有如下有益效果:
(1)本发明的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,包括聚合物胶束和治疗剂,治疗剂表面包覆聚合胶束,治疗剂包括近红外光染料IR780荧光探针和沙美特罗,采用雾化吸入的方式进入肺部,治疗的疾病为重症哮喘,可以直接到达病灶,治疗效果好,提高利用率。
附图说明
图1为本发明的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针的结构示意图;
图2为本发明的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针的治疗流程示意图。
示意图中的标号说明:
100、聚合物胶束;
200、IR780荧光探针
300、沙美特罗;
400、Siglec-9抗体。
具体实施方式
为了便于理解本发明,下面将参照相关附图对本发明进行更全面的描述,附图中给出了本发明的若干实施例,但是,本发明可以以许多不同的形式来实现,并不限于本文所描述的实施例,相反地,提供这些实施例的目的是使对本发明的公开内容更加透彻全面。
需要说明的是,当元件被称为“固设于”另一个元件,它可以直接在另一个元件上或者也可以存在居中的元件;当一个元件被认为是“连接”另一个元件,它可以是直接连接到另一个元件或者可能同时存在居中元件;本文所使用的术语“垂直的”、“水平的”、“左”、“右”以及类似的表述只是为了说明的目的。
除非另有定义,本文所使用的所有的技术和科学术语与属于本发明的技术领域的技术人员通常理解的含义相同;本文中在本发明的说明书中所使用的术语只是为了描述具体的实施例的目的,不是旨在于限制本发明;本文所使用的术语“及/或”包括一个或多个相关的所列项目的任意的和所有的组合。
实施例1
参照附图1-图2所示,本实施例的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,包括聚合物胶束100和治疗剂,治疗剂表面包覆聚合胶束100,治疗剂包括近红外光染料IR780荧光探针200和沙美特罗300,采用雾化吸入的方式进入肺部,治疗的疾病为重症哮喘,可以直接到达病灶,治疗效果好,提高利用率。
本实施例的聚合物胶束100基于PEG-PLGA,聚合物胶束100表面带有Siglec-9抗体400。
本实施例的聚合物胶束100具有油溶性。
本实施例的聚合物胶束100为纳米结构。
本实施例的Siglec-9抗体400均匀分布在聚合物胶束100的表面。
PLGA-PEG的聚合物胶束100表面带有羧基可以修饰Siglec-9抗体400,帮助纳米粒子靶向到重症哮喘病灶区域起到靶向治疗的作用。
该纳米探针采用雾化吸入的方式进入肺部,治疗的疾病为重症哮喘,可以直接到达病灶,沙美特罗300和Siglec-9抗体400都能起到治疗作用,IR780荧光探针200可以起到指示剂的作用,证明纳米探针到达肺部。
1、载IR780荧光探针的PLGA-PEG-COOH胶囊制备(50mg)
取500μL PLGA10K-mPEG5K(100mg/mL),50μL IR780(10mg/mL),450μL三氯甲烷混合均匀,加入到6mL 1%的PVA和TPGS的混合液(外水相,PVA:TPGS为1:5)中,在冰浴情况下用探头超声超声5分钟(80W)形成油-水复乳。最后将混合液加入到30mL 0.3%的PVA中(分散相),搅拌过夜,使氯仿挥发,使PLGA球表面固化。以100KD的超滤管进行超滤浓缩清洗,最后用纯水定容至5mL,将样品收集于4度保存。取适量样本烘干称重计算浓度及固含量。
2、载沙美特罗及IR780荧光探针的PLGA-PEG-COOH胶囊制备(50mg)
取500μL PLGA10K-mPEG5K(100mg/mL),50μL IR780(10mg/mL),100μL沙美特罗(20mg/mL),350μL三氯甲烷混合均匀,加入到6mL 1%的PVA和TPGS的混合液(外水相,PVA:TPGS为1:5)中,在冰浴情况下用探头超声超声5分钟(80W)形成油-水复乳。最后将混合液加入到30mL 0.3%的PVA中(分散相),搅拌过夜,使氯仿挥发,使PLGA球表面固化。以100KD的超滤管进行超滤浓缩清洗,最后用纯水定容至5mL,将样品收集于4度保存。取适量样本烘干称重计算浓度及固含量。
3、载药PLGA-PEG-COOH胶束偶联Siglec-9抗体
取1mL载药PLGA-PEG-COOH胶束(10mg/mL)离心后,更换溶液,分散于0.5mL MES中(100mM,pH 4.8),加入抗体(300μg)于37℃吸附1h。称取EDC用100mM MES配成240mg/mL溶液,加入80μL,37℃偶联过夜,离心用纯水纯化,最后保存在水中。
以上所述实施例仅表达了本发明的某种实施方式,其描述较为具体和详细,但并不能因此而理解为对本发明专利范围的限制;应当指出的是,对于本领域的普通技术人员来说,在不脱离本发明构思的前提下,还可以做出若干变形和改进,这些都属于本发明的保护范围;因此,本发明专利的保护范围应以所附权利要求为准。

Claims (5)

1.基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,其特征在于:包括聚合物胶束(100)和治疗剂,所述治疗剂表面包覆聚合胶束(100),所述治疗剂包括近红外光染料IR780荧光探针(200)和沙美特罗(300)。
2.根据权利要求1所述的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,其特征在于:所述聚合物胶束(100)基于PEG-PLGA,所述聚合物胶束(100)表面带有Siglec-9抗体(400)。
3.根据权利要求1所述的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,其特征在于:所述聚合物胶束(100)具有油溶性。
4.根据权利要求1所述的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,其特征在于:所述聚合物胶束(100)为纳米结构。
5.根据权利要求1所述的基于PEG-PLGA聚合物胶束的重症哮喘治疗用探针,其特征在于:所述Siglec-9抗体(400)均匀分布在聚合物胶束(100)的表面。
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