Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer’s disease

Rompicherla, Sampath Kumar L.; Karthik, A.; Bojja, Sree Lalitha; Kumar, Nitesh; Rao, C. Mallikarjuna

doi:10.1007/s00210-021-02096-0

Cited by 37 publications

(21 citation statements)

References 31 publications

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“…In this method, lipophilic drugs can be dissolved in an organic solvent together with phospholipids, whereas hydrophilic molecules can be dissolved in an aqueous solution and then incorporated into liposomes during the hydration process. The disadvantages of this method are its low entrapment efficiency, difficult removal of organic solvents, and small-scale production [ 56 ].…”

Section: Liposomes: Classification Preparation Characterization and P...mentioning

confidence: 99%

“…For example, IN liposomes showed better rivastigmine distribution in the hippocampus and cortex than IN and IV-free drugs [ 93 ]. Pharmacodynamic studies have been performed to evaluate the efficacy of IN liposomes using different animal models depending on the disease [ 56 , 90 , 94 ].…”

Section: Liposomes: Classification Preparation Characterization and P...mentioning

confidence: 99%

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Recent Advances in Intranasal Liposomes for Drug, Gene, and Vaccine Delivery

2023

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Liposomes are safe, biocompatible, and biodegradable spherical nanosized vesicles produced from cholesterol and phospholipids. Recently, liposomes have been widely administered intranasally for systemic and brain delivery. From the nasal cavity, liposome-encapsulated drugs and genes enter the systemic circulation primarily via absorption in the respiratory region, whereas they can be directly transported to the brain via the olfactory pathway. Liposomes can protect drugs and genes from enzymatic degradation, increase drug absorption across the nasal epithelium, and prolong the residence time in the nasal cavity. Intranasal liposomes are also a potential approach for vaccine delivery. Liposomes can be used as a platform to load antigens and as vaccine adjuvants to induce a robust immune response. With the recent interest in intranasal liposome formulations, this review discusses various aspects of liposomes that make them suitable for intranasal administration. We have summarized the latest advancements and applications of liposomes and evaluated their performance in the systemic and brain delivery of drugs and genes administered intranasally. We have also reviewed recent advances in intranasal liposome vaccine development and proposed perspectives on the future of intranasal liposomes.

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Section: Liposomes: Classification Preparation Characterization and P...mentioning

confidence: 99%

Section: Liposomes: Classification Preparation Characterization and P...mentioning

confidence: 99%

Recent Advances in Intranasal Liposomes for Drug, Gene, and Vaccine Delivery

2023

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“…Intranasal administration of rivastigmine [ 165 ] or galantamine liposomes [ 166 ] was already established to be a practical and effective method of increasing medication bioavailability in the brain. Intranasal administration of liposomes containing quercetin, an antioxidant, was also found to be a viable method of delivery [ 167 ].…”

Section: Advances In Drug Delivery Across the Blood–brain Barriermentioning

confidence: 99%

Current Strategies to Enhance Delivery of Drugs across the Blood–Brain Barrier

et al. 2022

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The blood–brain barrier (BBB) has shown to be a significant obstacle to brain medication delivery. The BBB in a healthy brain is a diffusion barrier that prevents most substances from passing from the blood to the brain; only tiny molecules can pass across the BBB. The BBB is disturbed in specific pathological illnesses such as stroke, diabetes, seizures, multiple sclerosis, Parkinson’s disease, and Alzheimer’s disease. The goal of this study is to offer a general overview of current brain medication delivery techniques and associated topics from the last five years. It is anticipated that this review will stimulate readers to look into new ways to deliver medications to the brain. Following an introduction of the construction and function of the BBB in both healthy and pathological conditions, this review revisits certain contested questions, such as whether nanoparticles may cross the BBB on their own and if medications are selectively delivered to the brain by deliberately targeted nanoparticles. Current non-nanoparticle options are also discussed, including drug delivery via the permeable BBB under pathological circumstances and the use of non-invasive approaches to improve brain medication absorption.

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“…RT was separated from the plasma and tissue samples using a modi ed liquid-liquid extraction method [11]. Rat plasma or tissue homogenate (100µl) was mixed with 20µl of 1M sodium hydroxide solution and vortexed for 120 seconds.…”

Section: Extraction Of Rt From Biological Samplesmentioning

confidence: 99%

“…Estimation of acetylcholinesterase (AChE) was conducted in male Wistar rats 24 h after the last pharmacodynamic test [11]. The animals were killed by decapitation and the brains were removed and then homogenized with ice-cold 150 mM KCl.…”

Section: Estimation Of Brain Acetylcholinesterasementioning

confidence: 99%

Rivastigmine Loaded PEG-PLGA Nanoparticles for Enhanced Delivery to the Brain: In-Vitro and In-Vivo Studies for Alzheimer’s disease

Prakash¹,

Prakash²,

Prasad³

et al. 2022

Preprint

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Purpose Rivastigmine Tartrate (RT) is a reversible cholinesterase inhibitor used for the treatment of Alzheimer's disease and CNS disorder. The entry of the drug to the brain is restricted is due to the presence of the Blood-Brain Barrier (BBB). In this work, we have developed amphiphilic copolymer, poly (ethylene glycol)-poly (lactide-coglycolide (PEG-PLGA) loaded RT nanoparticles to enhance brain delivery. Methods Rivastigmine-loaded PEG-PLGA nanoparticles were prepared using the nanoprecipitation technique. Pegylated polyethylene glycol (polymer) and Pluronic F68 (Surfactant) were selected as preparation of Polymeric Nanoparticle. Characterization studies on the formulation such as DSC, Zeta potential, SEM, and Drug Entrapment were conducted. In-vitro drug release, Pharmacokinetic, and Pharmacodynamics studies were performed. Results The prepared nanoparticles are spherical and the size ranges from a minimum of 125.93 ± 0.55 to a maximum of 179.60 ± 1.06 nm. In vitro release studies in PBS pH 7.4 showed a biphasic release pattern of the drug from the nanoparticles. Pharmacokinetic studies in male Wistar rats showed an increase in the Cmax of RT when administered as PEG- PLGA nanoparticles than RT administered as a solution in PBS and a notable 3.5fold increase in the T1/2 also was observed. Tissue distribution studies also showed a 4fold increase in the amount of RT as nanoparticles that have entered the brain when compared to RT in PBS. Conclusion The Smaller size of the nanoparticles along with the presence of hydrophilic PEG group has assisted in enhancing the concentration of Rivastigmine in the brain which has consequently even improved the memory learning skills of the animals

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Pharmacokinetic and pharmacodynamic evaluation of nasal liposome and nanoparticle based rivastigmine formulations in acute and chronic models of Alzheimer’s disease

Cited by 37 publications

References 31 publications

Recent Advances in Intranasal Liposomes for Drug, Gene, and Vaccine Delivery

Recent Advances in Intranasal Liposomes for Drug, Gene, and Vaccine Delivery

Current Strategies to Enhance Delivery of Drugs across the Blood–Brain Barrier

Rivastigmine Loaded PEG-PLGA Nanoparticles for Enhanced Delivery to the Brain: In-Vitro and In-Vivo Studies for Alzheimer’s disease

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