title: Positively charged polymeric nanoparticles: application in improving therapeutic efficacy of meloxicam after oral administration.
abstract: The potential of positively charged polymeric nanoparticles in improving therapeutic efficacy of meloxicam (MLX), a poorly water-soluble anti-inflammatory agent was evaluated. MLX loaded positively charged nanoparticles were prepared by using poly-epsilon-caprolactone (PCL) as a biodegradable polymer and didodecyldimethylammonium bromide (DDAB) as a cationic surfactant. The MLX nanoparticles were characterized for particle size and encapsulation efficiency. MLX loaded PCL nanoparticles and MLX suspension were evaluated for their in vivo anti-inflammatory activity and ulcerogenic potential. MLX loaded PCL nanoparticles had particle sizes of approximately 300 nm and the encapsulation efficiency of MLX was approximately 90%. The polymeric nanoparticles significantly improved the anti-inflammatory activity of MLX (P< 0.01) as compared to that of MLX suspension. The higher anti-inflammatory effect was maintained for a longer duration (6 h). The polymeric nanoparticles also resulted in less ulcerogenicity as compared to that of MLX suspension.
authors.affiliation: Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz (East), Mumbai, India.
authors.forename: P
authors.initials: P
authors.lastname: Khachane
authors.forename: A A
authors.initials: AA
authors.lastname: Date
authors.forename: M S
authors.initials: MS
authors.lastname: Nagarsenker
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D002208:Caproates; D002351:Carrageenan; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy / Q000473:pathology; D005528:Foot / Q000473:pathology; D005612:Freeze Drying; D007783:Lactones; D008297:Male; D000077239:Meloxicam; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced; D013501:Surface-Active Agents / Q000737:chemistry; D013535:Suspensions; D013843:Thiazines / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*; D013844:Thiazoles / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002208:Caproates; D007783:Lactones; D011108:Polymers; D000644:Quaternary Ammonium Compounds; D013501:Surface-Active Agents; D013535:Suspensions; D013843:Thiazines; D013844:Thiazoles; C046112:didodecyldimethylammonium; C121056:caprolactone; D002351:Carrageenan; D000077239:Meloxicam