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Merck
  • Hyaluronic acid-decorated PLGA-PEG nanoparticles for targeted delivery of SN-38 to ovarian cancer.

Hyaluronic acid-decorated PLGA-PEG nanoparticles for targeted delivery of SN-38 to ovarian cancer.

Anticancer research (2013-06-12)
Kiran Kumar Vangara, Jingbo Louise Liu, Srinath Palakurthi
摘要

Extreme hydrophobicity and poor stability of SN-38, a highly potent topoisomerase I inhibitor, has prevented its clinical use. Its encapsulation into nanoparticles may be a way to overcome these problems. Here we report the use of SN-38-loaded hyaluronic acid (HA)-decorated poly(lactic-co-glycolic acid)-polyethylene glycol (PLGA-PEG) nanoparticles (NPs) for targeted ovarian cancer therapy. PLGA-PEG nanoparticles loaded with SN-38 were prepared by single- emulsion (O/W) solvent evaporation method. HA was decorated onto the nanoparticles by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) coupling and the extent of HA conjugation was quantified by hexadecyltrimmethylammonium bromide (CTAB) assay. Cancer cell specificity of the NPs was determined by flow cytometry and cytotoxicity of the NPs was tested by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium (MTT) bromide assay. Mean size, zeta potential and encapsulation efficiency of PLGA-PEG-HA NPs were 265.6 ± 3.8 nm, -30.4 ± 0.1 mV and 75.8 ± 4.1%, respectively. Cellular uptake of PLGA-PEG-HA NPs was 8- and 16-fold higher in CD44-positive cell lines, SKOV-3 and OVCAR-8, as compared to CD44-negative cells (CHO). Cytotoxicity of the targeted NPs was significantly higher as compared to non-targeted NPs for the above cell lines. These results suggest that PLGA-PEG-HA NPs could be an efficient delivery system for SN-38 for targeted therapy of ovarian cancer.

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Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, bacterial glycosaminoglycan polysaccharide
Sigma-Aldrich
RESOMER® RG 502 H,聚(d,L-丙交酯--乙交酯), acid terminated, viscosity 0.16-0.24 dL/g 
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聚(D,L-丙交酯-co-乙交酯), lactide:glycolide (50:50), mol wt 30,000-60,000
Sigma-Aldrich
透明质酸 钠盐 来源于公鸡鸡冠, avian glycosaminoglycan polysaccharide
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聚(D,L-丙交酯-co-乙交酯), lactide:glycolide (75:25), mol wt 66,000-107,000
Sigma-Aldrich
(S)-(+)-喜树碱, ≥90% (HPLC), powder
Sigma-Aldrich
Resomer® RG 504 H,聚(D,L-丙交酯-co-乙交酯), acid terminated, lactide:glycolide 50:50, Mw 38,000-54,000
Sigma-Aldrich
Resomer® RG 503 H,聚(D,L-丙交酯--乙交酯), acid terminated, lactide:glycolide 50:50, Mw 24,000-38,000
Sigma-Aldrich
Resomer® RG 752 H,聚(D,L-丙交酯-co-乙交酯), acid terminated, lactide:glycolide 75:25, Mw 4,000-15,000
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透明质酸 钠盐 来源于牛玻璃体液
Sigma-Aldrich
Resomer® RG 502,聚(D,L-丙交酯-co-乙交酯), lactide:glycolide 50:50, ester terminated, Mw 7,000-17,000
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透明质酸 钠盐 来源于马链球菌, mol wt 8,000-15,000
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7-乙基-10-羟基喜树脂, ≥98% (HPLC), powder
Sigma-Aldrich
伊立替康 盐酸盐, topoisomerase inhibitor
Sigma-Aldrich
聚(D,L-丙交酯-co-乙交酯), lactide:glycolide 65:35, Mw 40,000-75,000
Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, mol wt 1,000,000-1,250,000
Sigma-Aldrich
聚(D,L-丙交酯-co-乙交酯), ester terminated, Mw 50,000-75,000
Sigma-Aldrich
透明质酸 钠盐 来源于兽疫链球菌, bacterial glycosaminoglycan polysaccharide
Sigma-Aldrich
Resomer® RG 505,聚(D,L-丙交酯-co-乙交酯), ester terminated, Mw 54,000-69,000
Sigma-Aldrich
Resomer® RG 504,聚(D,L-丙交酯-co-乙交酯), lactide:glycolide 50:50, ester terminated, Mw 38,000-54,000
Sigma-Aldrich
Resomer® RG 756 S,聚(D,L-丙交酯-co-乙交酯), ester terminated, lactide:glycolide 75:25, Mw 76,000-115,000
Sigma-Aldrich
Resomer® RG 503,聚(D,L-丙交酯-co-乙交酯), lactide:glycolide 50:50, ester terminated, Mw 24,000-38,000
Sigma-Aldrich
共聚物 ®RG 653 H,聚(D,L-丙交酯-co-乙交酯), acid terminated, Mw 24,000-38,000
Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, mol wt 300,000-500,000
Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, mol wt 1,500,000-1,750,000
Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, mol wt 30,000-50,000
Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, mol wt 2,000,000-2,400,000
Sigma-Aldrich
Resomer® RG 858 S,聚(D,L-丙交酯--乙交酯), ester terminated, lactide:glycolide 85:15, Mw 190,000-240,000
Sigma-Aldrich
透明质酸 钠盐 来源于马链球菌, mol wt 1,200
透明质酸钠, BRP, European Pharmacopoeia (EP) Reference Standard