title: Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles.
abstract: 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 500nm 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 260-480nm; the encapsulation efficiency was 43.4-54.6%; and the yield 58.5-67.8%. The zeta potential of CS-coated nanoparticles was above +27mV 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 12h. 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.
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
authors.forename: Bong-Seok
authors.initials: BS
authors.lastname: Kang
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
authors.forename: Jin-Seok
authors.initials: JS
authors.lastname: Choi
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
authors.forename: Sang-Eun
authors.initials: SE
authors.lastname: Lee
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
authors.forename: Joon-Kyung
authors.initials: JK
authors.lastname: Lee
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
authors.forename: Tae-Hyeon
authors.initials: TH
authors.lastname: Kim
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea.
authors.forename: Woo Suk
authors.initials: WS
authors.lastname: Jang
authors.affiliation: Division of Pharmaceutical Sciences, Faculty of Pharmacy, Thammasat University, Rangsit Center, Pathumthani 12120, Thailand.
authors.forename: Amolnat
authors.initials: A
authors.lastname: Tunsirikongkon
authors.affiliation: College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-Ro, Sangnok-Gu, Ansan 15588, Republic of Korea. Electronic address: jinkikim@hanyang.ac.kr.
authors.forename: Jin-Ki
authors.initials: JK
authors.lastname: Kim
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-Ro, Yuseong-Gu, Daejeon 34134, Republic of Korea. Electronic address: eicosa@cnu.ac.kr.
authors.forename: Jeong-Sook
authors.initials: JS
authors.lastname: Park
mesh_terms: D015766:Albendazole / Q000737:chemistry / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D004337:Drug Carriers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D048271:Chitosan; D015766:Albendazole
keywords: Albendazole; Anticancer activity; Chitosan; Mucoadhesion; PLGA Nanoparticle