title: Immune activity and biodistribution of polypeptide K237 and folic acid conjugated amphiphilic PEG-PLGA copolymer nanoparticles radiolabeled with 99mTc.
abstract: In a previous study, amphiphilic copolymer, polypeptide K237 (HTMYYHHYQHHL) and folic acid (FA) modified poly(ethylene glycol)-poly(lactic-co-glycolic acid) (K237/FA-PEG-PLGA) nanoparticles were developed and studied as a drug carrier. To further promote the clinical application of K237/FA-PEG-PLGA nanoparticles and provide guidance for future research, we need to examine their specific biodistribution in vivo. In this study, K237/FA-PEG-PLGA nanoparticles were effectively labeled by a direct method with Technetium-99m (99mTc) using stannous chloride as a reducing agent. The optimal stability of the labeled nanoparticles was determined by evaluating their radiochemical purity in serum, physiological saline, diethylenetriaminepentaacetic acid (DTPA) and cysteine solutions. The affinity of ligands and receptors was elicited by cell binding and blocking experiments in KDR/folate receptor high expressing SKOV-3 ovarian cancer cells. The nanoparticles biodistribution was studied after intravenous administration in healthy mice xenografted with SKOV-3 cells. A higher percent injected dose per gram of tissue (% ID/g) was observed in liver, kidney, spleen, blood and tumor at 3 and 9 h post-injection. Scintigraphic images revealed that the radioactivity was mainly concentrated in tumor, liver, kidney and bladder; and in the heart, lung, and muscle was significantly lower at 3 h. The radioactivity distribution in the images is consistent with the in vivo biodistribution data. Our works demonstrated that K237/FA-PEG-PLGA nanoparticles have great potential as biodegradable drug carriers, especially for tumors expressing the folate and KDr receptor.
authors: The Second Affiliated Hospital & Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.|The First Affiliated Hospital of Bengbu Medical College, Bengbu, China.
authors: Zelai
authors: Z
authors: He
authors: Department of Pathology, Jining No.1 Peoples' Hospital, Jining, China.
authors: Xiangyu
authors: X
authors: Zhang
authors: The Second Affiliated Hospital & Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.|The First Affiliated Hospital of Bengbu Medical College, Bengbu, China.
authors: Jingwen
authors: J
authors: Huang
authors: Department of Internal Medicine, Affiliated Cancer Hospital of Zhengzhou University, Henan Cancer Hospital, Zhengzhou, China.
authors: Yufeng
authors: Y
authors: Wu
authors: The Second Affiliated Hospital & Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.
authors: Xuanzhang
authors: X
authors: Huang
authors: The Second Affiliated Hospital & Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.
authors: Jie
authors: J
authors: Chen
authors: Department of Nuclear Medicine, The Affiliated Provincial Hospital of Anhui Medical University, Hefei, China.
authors: Junyong
authors: J
authors: Xia
authors: The First Affiliated Hospital of Bengbu Medical College, Bengbu, China.
authors: Hao
authors: H
authors: Jiang
authors: Ultrasonic Department, Shanghai Songjiang Center Hospital, Shanghai, China.
authors: Jing
authors: J
authors: Ma
authors: The Second Affiliated Hospital & Yuying Children's Hospital of Wenzhou Medical University, Wenzhou, China.
authors: Jian
authors: J
authors: Wu
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D004195:Disease Models, Animal; D005492:Folic Acid / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D006801:Humans; D007553:Isotope Labeling; D008297:Male; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry / Q000648:ultrastructure; D009369:Neoplasms / Q000000981:diagnostic imaging / Q000188:drug therapy / Q000473:pathology; D009842:Oligopeptides / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D015609:Organotechnetium Compounds; D011092:Polyethylene Glycols / Q000737:chemistry; D011098:Polyglactin 910 / Q000737:chemistry; D014018:Tissue Distribution; D023041:Xenograft Model Antitumor Assays
chemical_list: C000604146:K237 peptide; D009842:Oligopeptides; D015609:Organotechnetium Compounds; C102418:poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer; D011098:Polyglactin 910; D011092:Polyethylene Glycols; D005492:Folic Acid
keywords: K237; PEG-PLGA; biodistribution; nanoparticles; folate