title: A novel gastroretentive porous microparticle for anti-Helicobacter pylori therapy: preparation, in vitro and in vivo evaluation.
abstract: Gastroretentive drug delivery system is a promising option for the treatment of Helicobacter pylori infection, which can prolong gastric residence time and supply high drug concentration in the stomach. In the present study, a low density system of metronidazole-loaded porous Eudragit® RS microparticle with high drug loading capacity (>25%) was fabricated via electrospray method. The porous structure and size distribution of microparticles were affected by polymer concentration and flow rate of solution. FTIR and XRD analyses indicated that drug has been entrapped into the porous microparticles. In addition, sustained release profiles and slight cytotoxicity in vitro were detected. Gamma scintigraphy study in vivo demonstrated that ¹³¹I-labeled microparticles retained in stomach for over 8h, and about 65.50% radioactive counts were finally detected in the region of interest. The biodistribution study confirmed that hotspot of radioactivity was remaining in the stomach. Furthermore, metronidazole-loaded porous microparticles can eradicate H. pylori completely with lower dose and administration frequency of antibiotic compared with pure drug, which were also more helpful for the healing of mucosal damages. These results suggest that prepared porous microparticle has the potential to provide better treatment for H. pylori infection.
authors.affiliation: Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.
authors.forename: Shilei
authors.initials: S
authors.lastname: Hao
authors.affiliation: Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.
authors.forename: Yazhou
authors.initials: Y
authors.lastname: Wang
authors.affiliation: Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China. Electronic address: wangbc2000@126.com.
authors.forename: Bochu
authors.initials: B
authors.lastname: Wang
authors.affiliation: Department of Clinical Microbiology and Clinical Immunology, Third Military Medical University, Chongqing 400038, China.
authors.forename: Quanming
authors.initials: Q
authors.lastname: Zou
authors.affiliation: Department of Clinical Microbiology and Clinical Immunology, Third Military Medical University, Chongqing 400038, China.
authors.forename: Hao
authors.initials: H
authors.lastname: Zeng
authors.affiliation: Department of Nuclear Medicine, Chongqing Cancer Institution, Chongqing 400030, China.
authors.forename: Xiaoliang
authors.initials: X
authors.lastname: Chen
authors.affiliation: Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.
authors.forename: Xi
authors.initials: X
authors.lastname: Liu
authors.affiliation: Key Laboratory of Biorheological Science and Technology, Ministry of Education, College of Bioengineering, Chongqing University, Chongqing 400030, China.
authors.forename: Junyu
authors.initials: J
authors.lastname: Liu
authors.affiliation: Department of Nuclear Medicine, Chongqing Cancer Institution, Chongqing 400030, China.
authors.forename: Songke
authors.initials: S
authors.lastname: Yu
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D015169:Colony Count, Microbial; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005260:Female; D016481:Helicobacter Infections / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D016480:Helicobacter pylori / Q000187:drug effects / Q000254:growth & development; D006801:Humans; D008795:Metronidazole / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics / Q000627:therapeutic use; D051379:Mice; D008810:Mice, Inbred C57BL; D016062:Porosity; D013270:Stomach / Q000187:drug effects / Q000382:microbiology / Q000473:pathology
chemical_list: D000180:Acrylic Resins; D000890:Anti-Infective Agents; D008795:Metronidazole; C050528:Eudragit RS
keywords: Electrospray; Eudragit RS (PubChem CID: 104931); Helicobacter pylori; Iodine-131 (PubChem CID: 24855); Local delivery; Metronidazole (PubChem CID: 4173); Porous microparticles; SPECT/CT tomography