Preparation, Optimization, and Evaluation of Methoxy Poly(ethylene glycol)-co-Poly(ε-caprolactone) Nanoparticles Loaded by Rivastigmine for Brain Delivery. 2020

Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
Department of Pharmaceutical Nanotechnology, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.

The objective of this study was to formulate and investigate the neuropharmacokinetics and pharmacodynamics of rivastigmine (Riv) loaded methoxy poly(ethylene glycol)-co-poly(ε-caprolactone) (MPEG-PCL) nanoparticles (Riv-NPs) in rats after IV administration. The MPEG-PCL was synthesized via ring-opening polymerization of ε-caprolactone by MPEG and used to prepare Riv-NPs by the nanoprecipitation method. Response surface D-optimal design was applied to optimize Riv-NPs drug delivery system. The optimized formulation showed a particle size (PS) of 98.5 ± 2.1 nm, drug loading (DL) of 19.2 ± 1.1%, and sustained release behavior of the drug. Moreover, the optimized Riv-NPs were characterized by AFM and DSC analyses. A simple and sensitive HPLC-DAD method for bioanalysis was developed and successfully applied to the pharmacokinetic study. The neuropharmacokinetic study in rats indicated that the integration plot was linear, and the brain uptake clearance of the drug-loaded in MPEG-PCL NPs was significantly higher than the free drug. Furthermore, results of pharmacodynamic studies using the Morris water maze test demonstrated faster regain of memory loss with Riv-NPs when compared to the free drug solution. The results revealed that the mentioned biodegradable nanoparticle holds promise as a suitable drug carrier for brain drug delivery.

UI MeSH Term Description Entries
D010316 Particle Size Relating to the size of solids. Particle Sizes,Size, Particle,Sizes, Particle
D011091 Polyesters Polymers of organic acids and alcohols, with ester linkages--usually polyethylene terephthalate; can be cured into hard plastic, films or tapes, or fibers which can be woven into fabrics, meshes or velours. Polyester
D011092 Polyethylene Glycols Polymers of ETHYLENE OXIDE and water, and their ethers. They vary in consistency from liquid to solid depending on the molecular weight indicated by a number following the name. They are used as SURFACTANTS, dispersing agents, solvents, ointment and suppository bases, vehicles, and tablet excipients. Some specific groups are NONOXYNOLS, OCTOXYNOLS, and POLOXAMERS. Macrogols,Polyoxyethylenes,Carbowax,Macrogol,Polyethylene Glycol,Polyethylene Oxide,Polyethyleneoxide,Polyglycol,Glycol, Polyethylene,Glycols, Polyethylene,Oxide, Polyethylene,Oxides, Polyethylene,Polyethylene Oxides,Polyethyleneoxides,Polyglycols,Polyoxyethylene
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D000068836 Rivastigmine A carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE. (S)-N-Ethyl-3-((1-dimethyl-amino)ethyl)-N-methylphenylcarbamate,ENA 713,ENA-713,Exelon,Rivastigmine Hydrogen Tartrate,RivastigmineTartrate,SDZ ENA 713,713, ENA,713, SDZ ENA,ENA 713, SDZ,ENA713,Hydrogen Tartrate, Rivastigmine,Tartrate, Rivastigmine Hydrogen
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D016503 Drug Delivery Systems Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity. Drug Targeting,Delivery System, Drug,Delivery Systems, Drug,Drug Delivery System,Drug Targetings,System, Drug Delivery,Systems, Drug Delivery,Targeting, Drug,Targetings, Drug
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D053758 Nanoparticles Nanometer-sized particles that are nanoscale in three dimensions. They include nanocrystaline materials; NANOCAPSULES; METAL NANOPARTICLES; DENDRIMERS, and QUANTUM DOTS. The uses of nanoparticles include DRUG DELIVERY SYSTEMS and cancer targeting and imaging. Nanocrystalline Materials,Nanocrystals,Material, Nanocrystalline,Materials, Nanocrystalline,Nanocrystal,Nanocrystalline Material,Nanoparticle

Related Publications

Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
April 2014, The Journal of pharmacy and pharmacology,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
December 2017, Research in pharmaceutical sciences,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
June 2011, Biomaterials,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
February 2012, Biomaterials,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
June 2015, Scientific reports,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
October 2018, Journal of biomaterials science. Polymer edition,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
April 2014, Journal of biomedical nanotechnology,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
April 2017, Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
May 2012, Nanoscale research letters,
Hamed Mohamadpour, and Amir Azadi, and Kobra Rostamizadeh, and Sina Andalib, and Mohammad Reza Saghatchi Zanjani, and Mehrdad Hamidi
March 2023, Journal of colloid and interface science,
Copied contents to your clipboard!