title: Lectin-Conjugated Clarithromycin and Acetohydroxamic Acid-Loaded PLGA Nanoparticles: a Novel Approach for Effective Treatment of H. pylori.
abstract: Helicobacter pylori infection remains challenging as it mainly colonized beneath the deep gastric mucosa and adheres to epithelial cells of the stomach. Concanavalin-A (Con-A)-conjugated gastro-retentive poly (lactic-co-glycolic acid) (PLGA) nanoparticles of acetohydroxamic acid (AHA) and clarithromycin (CLR) were prepared and evaluated under in vitro conditions. Solvent evaporation method was employed for preparation of nanoparticles and characterized for particle size distribution, surface morphology, percent drug entrapment, and in vitro drug release in simulated gastric fluid. Optimized nanoparticles were conjugated with Con-A and further characterized for Con-A conjugation efficiency and mucoadhesion and tested for in vitro anti-H. pylori activity. The conjugation with Con-A further sustained the drug release over a period of 8 h when compared to non-conjugated nanoparticles of AHA and CLR. In vitro anti H. pylori study confirmed that Con-A-conjugated nanoparticles containing both drugs, i.e., CLR and AHA, had shown maximum zone of inhibition compared to other formulations. In a nut shell, results suggest that the developed systems could be used for better therapeutic activity against H. pylori infection.
authors.affiliation: Department of Pharmaceutics, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, C.G., 495 009, India. suniljain25in@yahoo.com.
authors.forename: Sunil K
authors.initials: SK
authors.lastname: Jain
authors.affiliation: Department of Pharmaceutics, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, C.G., 495 009, India.
authors.forename: Tanweer
authors.initials: T
authors.lastname: Haider
authors.affiliation: Department of Pharmaceutics, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, C.G., 495 009, India.
authors.forename: Amrish
authors.initials: A
authors.lastname: Kumar
authors.affiliation: Department of Pharmaceutics, Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, C.G., 495 009, India.
authors.forename: Akhlesh
authors.initials: A
authors.lastname: Jain
mesh_terms: D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D017291:Clarithromycin / Q000008:administration & dosage / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005753:Gastric Mucosa / Q000382:microbiology; D016481:Helicobacter Infections / Q000188:drug therapy; D016480:Helicobacter pylori / Q000187:drug effects*; D006877:Hydroxamic Acids / Q000008:administration & dosage / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D037102:Lectins / Q000737:chemistry*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D013270:Stomach / Q000382:microbiology
chemical_list: D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D006877:Hydroxamic Acids; D037102:Lectins; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C006358:acetohydroxamic acid; D017291:Clarithromycin
keywords: H. pylori; acetohydroxamic acid; carbodiimide technique; clarithromycin; concanavalin-A