Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles

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• 作者：Bong-Seok Kang^a ; ¹ ; Jin-Seok Choi^a ; ¹ ; Sang-Eun Lee^a ; Joon-Kyung Lee^a ; Tae-Hyeon Kim^a ; Woo Suk Jang^a ; Amolnat Tunsirikongkon^b ; Jin-Ki Kim^c ; ^{jinkikim@hanyang.ac.kr} ; Jeong-Sook Park^a ; ^{eicosa@cnu.ac.kr}
• 关键词：ABZ ; albendazole ; CS ; chitosan ; PLGA ; poly-dl-lactic-co-glycolic acid ; SEM ; scanning electric microscopy ; FT-IR ; fourier-transform infrared ; DSC ; differential scanning calorimetry ; XRD ; x-ray powder diffraction ; P188 ; poloxamer 188 ; P407 ; poloxamer 407 ; DMSO ; dimethylsulfoxide ; MTT ; 3-(4 ; 5-dimethylthiazol-2-yl)-2 ; 5-diphenytetrazolium bromide ; DMEM ; dulbecco&rsquo ; s modified eagle&rsquo ; s medium ; FBS ; fetal bovine serum ; HPLC ; high-performance liquid chromatography ; PDI ; polydispersity index ; HLB
• 刊名：Carbohydrate Polymers
• 出版年：2017
• 出版时间：1 March 2017
• 年：2017
• 卷：159
• 期：Complete
• 页码：39-47
• 全文大小：1199 K
• 卷排序：159

文摘

To improve the solubility and anticancer activity of albendazole (ABZ), chitosan (CS)-coated poly-dl-lactic-co-glycolic acid (PLGA) nanoparticles were developed. CS was used to coat ABZ-loaded PLGA nanoparticles to enhance both mucoadhesiveness and colloidal stability. CS-coated PLGA nanoparticles were prepared by suspending the nanoparticles in CS solution after solvent diffusion. The CS-coated PLGA nanoparticles were characterized, and ABZ release was studied in vitro from various formulations. The mucoadhesive properties and in vitro anticancer activities of CS-coated PLGA nanoparticles were investigated by measurement of zeta potentials and the MTT assay, respectively. Spherical nanoparticles below 500 nm in diameter were successfully prepared; the particle size distribution was narrow. Complete encapsulation of ABZ in CS-coated PLGA nanoparticles was confirmed by SEM, FTIR, DSC, and XRD. The particle sizes of CS-coated PLGA nanoparticles were in the range of 260–480 nm; the encapsulation efficiency was 43.4–54.6%; and the yield 58.5–67.8%. The zeta potential of CS-coated nanoparticles was above +27 mV and stability was maintained for 4 weeks. At pH 7.4, the in vitro release of ABZ from nanoparticles (P188-5) was 200-fold higher than that from untreated ABZ; this persisted for 12 h. Moreover, ABZ release from CS-coated PLGA nanoparticles (P188-CS0.5) was 1.5-fold higher than that from untreated ABZ at pH 1.2. Additionally, the ABZ-loaded CS-coated nanoparticles exhibited superior mucoadhesion and improved cytotoxicity. The results show that CS coating of PLGA nanoparticles may improve the anticancer effect and the mucoadhesive properties of ABZ-loaded nanoparticles.