title: Antihypertensive nano-ceuticales based on chitosan biopolymer: Physico-chemical evaluation and release kinetics.
abstract: Prime risk factor behind cardiovascular associated mortality and morbidity is hypertension. The main challenge with antihypertensive (AHT) drug therapy is their extreme hydrophobic nature and very low oral bio-availability; which result into higher dosage/frequency and associated side effects of drugs. The main objective of this study was to fabricate AHT nano-ceuticals in hydrophilic carriers of natural origin to improve drugs' solubility, protection and sustained release. AHT nano-carrier systems (NCS) encapsulating captopril, amlodipine and valsartan were fabricated using chitosan (CS) polymer by ionic gelation assisted ultra-sonication method. Drug encapsulation efficiencies of 92±1.6%, 91±0.9% and 87±0.5% were observed for captopril, valsartan and amlodipine respectively. Scanning electron microscopy (SEM) based analysis had revealed that captopril loaded polymeric NCS were regular, smooth and without any agglomeration. FTIR analyses of drug loaded and empty NCS demonstrated that drugs were molecularly dispersed inside the nanoparticles via week hydrogen bonding. Captopril and valsartan have demonstrated grafting reaction with N-H group of chitosan. Zeta sizer results had confirmed that average size of chitosan nanoparticles was below 100 nm. Encapsulation of captopril had reduced the surface charge value from +52.6±4.8 to +46.5±5.2 mV. Controlled release evaluation of highly encapsulated drug captopril had revealed a slow release in vitro from NCS in physiological buffer. Thus, here reported innovative AHT nano-ceuticals of polymeric origin can improve the oral administration of currently available hydrophobic drugs while providing the extended-release function.
authors.affiliation: Department of Biosciences, COMSATS Institute of Information Technology, Park road, Islamabad, Pakistan.
authors.forename: Taskeen
authors.initials: T
authors.lastname: Niaz
authors.affiliation: Department of Materials Science and Engineering, Institute of Space Technology, Islamabad 44000, Pakistan.
authors.forename: Saima
authors.initials: S
authors.lastname: Shabbir
authors.affiliation: Department of Physics, COMSATS Institute of Information Technology, Park road, Islamabad, Pakistan.
authors.forename: Shahid
authors.initials: S
authors.lastname: Manzoor
authors.affiliation: Industrial Biotechnology Division, National Institute of Biotechnology and Genetic Engineering (NIBGE), Faisalabad, Pakistan.
authors.forename: Asma
authors.initials: A
authors.lastname: Rehman
authors.affiliation: Atta-ur-Rehman School of Applied Biosciences (ASAB), National University of Sciences and Technology (NUST), Islamabad, Pakistan.
authors.forename: Abdur
authors.initials: A
authors.lastname: Rahman
authors.affiliation: School of Chemical and Materials Engineering (SCME), National University of Sciences and Technology (NUST), Islamabad, Pakistan.
authors.forename: Habib
authors.initials: H
authors.lastname: Nasir
authors.affiliation: Department of Biosciences, COMSATS Institute of Information Technology, Park road, Islamabad, Pakistan. Electronic address: m.imran@comsats.edu.pk.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Imran
mesh_terms: D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000737:chemistry; D002216:Captopril / Q000008:administration & dosage* / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D065546:Drug Liberation; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D012995:Solubility
chemical_list: D000959:Antihypertensive Agents; D003692:Delayed-Action Preparations; D048271:Chitosan; D002216:Captopril
keywords: ACEI; Antihypertensive drugs; Chitosan; Extended release; Nanoparticles