title: Lyophilized mucoadhesive-dendrimer enclosed matrix tablet for extended oral delivery of albendazole.
abstract: Dendrimers are multifunctional carriers widely employed for delivering drugs in a variety of disease conditions including HIV/AIDS and cancer. Albendazole (ABZ) is a commonly used anthelmintic drug in human as well as veterinary medicine. In this investigation, ABZ was formulated as a "muco-dendrimer" based sustained released tablet. The mucoadhesive complex was synthesized by anchoring chitosan to fifth generation PPI dendrimer (Muco-PPI) and characterized by UV, FTIR, (1)H NMR spectroscopy and electron microscopy. ABZ was entrapped inside Muco-PPI followed by lyophilization and tableting as matrix tablet. A half-life (t1/2) of 8.06±0.15, 8.17±0.47, 11.04±0.73, 11.49±0.92, 12.52±1.04 and 16.9±1.18h was noted for ABZ (free drug), conventional ABZ tablet (F1), conventional ABZ matrix tablet (F2), PPI-ABZ complex, PPI-ABZ matrix tablet (F3) and Muco-PPI-ABZ matrix tablet (F4), respectively. Thus the novel mucoadhesive-PPI based formulation of ABZ (F4) increased the t1/2 of ABZ significantly by almost twofold as compared to the administration of free drug. The in vivo drug release data showed that the Muco-PPI based formulations have a significantly higher Cmax (2.40±0.02μg/mL) compared with orally administered free ABZ (0.19±0.07μg/mL) as well as conventional tablet (0.20±0.05μg/mL). In addition, the Muco-PPI-ABZ matrix tablet displayed increased mean residence time (MRT) and is therefore a potential candidate to appreciably improve the pharmacokinetic profile of ABZ.
authors.affiliation: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar (M.P.) 470003, India.
authors.forename: Shakir
authors.initials: S
authors.lastname: Mansuri
authors.affiliation: Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, United States.
authors.forename: Prashant
authors.initials: P
authors.lastname: Kesharwani
authors.affiliation: International Medical University, School of Pharmacy, Department of Pharmaceutical Technology, Jalan Jalil Perkasa 19, 57000 Kuala Lumpur, Malaysia. Electronic address: rakeshkumar@imu.edu.my.
authors.forename: Rakesh Kumar
authors.initials: RK
authors.lastname: Tekade
authors.affiliation: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar (M.P.) 470003, India.
authors.forename: Narendra Kumar
authors.initials: NK
authors.lastname: Jain
mesh_terms: D000269:Adhesives / Q000008:administration & dosage / Q000737:chemistry*; D000284:Administration, Oral; D015766:Albendazole / Q000008:administration & dosage / Q000737:chemistry*; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000737:chemistry; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D048271:Chitosan / Q000737:chemistry; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000737:chemistry*; D050091:Dendrimers / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005612:Freeze Drying; D006207:Half-Life; D008297:Male; D009092:Mucous Membrane / Q000378:metabolism*; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D013607:Tablets / Q000008:administration & dosage / Q000737:chemistry*
chemical_list: D000269:Adhesives; D000871:Anthelmintics; D003692:Delayed-Action Preparations; D050091:Dendrimers; D004337:Drug Carriers; D013607:Tablets; D048271:Chitosan; D015766:Albendazole
keywords: Albendazole; MRT; Matrix tablet; Muco-PPI; Mucoadhesion