Effects of physicochemical properties and other factors on systemic nasal drug delivery

Behl, Christian; Pimplaskar, H.K; Sileno, Anthony; deMeireles, J.C; Romeo, V. D.

doi:10.1016/s0169-409x(97)00063-x

Cited by 254 publications

(109 citation statements)

References 138 publications

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“…It could produce beneficial effect with very much low dose. Based on the previous findings, the decrease effective dose might be associated with many factors including the increase opportunity to transfer directly from the olfactory mucosa along the olfactory pathway to the central nervous system (Cho et al, 2006) via bypassing the Blood-Brain Barrier (BBB), which prevented some CNS-active drugs from reaching the brain (Behl et al, 1998). In addition, it could also decrease the influence of the first pass metabolism (Krauze, 2006).…”

Section: Discussionmentioning

confidence: 99%

Neuroprotective Effect of Quercetin Encapsulated Liposomes: A Novel Therapeutic Strategy against Alzheimer's Disease

Phachonpai¹

2010

American Journal of Applied Sciences

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Problem statement:The prevalence of Alzheimer's disease is increasing but the efficacy of treatment is still very limited due to various factors including the blood brain barrier. Recent findings demonstrated the crucial role of oxidative stress on the pathophysiology of disease. In addition the burden of blood brain barrier can be overcome by nasal administration and vesicle-carrier mediated delivery system. Based on the potent antioxidant effect of quercetin and the burden of blood brain barrier, we hypothesized that the nasal administration of quercetin liposomes could protect against neurodegeneration in Alzheimer's disease. Approach: This study was designed to evaluate the effect and possible action of nasal administration of quercetin liposomes on neurodegeneration in animal model of Alzheimer's disease. Male Wistar rats were pretreated with quercetin liposomes, containing 0.5 mg of quercetin in 20 μL via intranasal route once daily continually for 2 weeks before and 1 week after AF64A administration. After the quercetin liposomes treatment, the density of neurons and cholinergic neurons in hippocampus were assessed using histochemical and immunohistochemical techniques whereas the activities of Superoxide Dismutase (SOD), Catalase (CAT), Glutathione Peroxidase (GPx) and Malondialdehide (MDA), a lipid peroxidation product, were determined using biochemical assays. Results: Quercetin liposomes attenuated the degeneration of neurons and cholinergic neurons in hippocampus. The elevation of SOD, CAT and GPx activities and the reduction of MDA in hippocampus were also observed. Therefore, the neuroprotective of quercetin liposomes occurred partly via the reduction of oxidative stress. Conclusion: Our studies suggested that nasal administration of quercetin liposomes may be the potential novel therapeutic strategy against Alzheimer's disease. However, further researches are still essential.

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Section: Discussionmentioning

confidence: 99%

Neuroprotective Effect of Quercetin Encapsulated Liposomes: A Novel Therapeutic Strategy against Alzheimer's Disease

Phachonpai¹

2010

American Journal of Applied Sciences

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“…It was noticeable that the dose of quercetin required via nasal administration was very much low dose and also produced the rapid onset of cognitive enhancing effect. Based on the previous findings, the decrease effective dose might be associated with many factors including the increase opportunity to transfer directly from the olfactory mucosa along the olfactory pathway to the Central Nervous System (CNS) (Cho et al, 2006) via bypassing BBB, which prevented some CNS-active drugs from reaching the brain (Behl et al, 1998). In addition, it could also decrease the influence of the first pass metabolism (Krauze, 2006).…”

Section: Discussionmentioning

confidence: 99%

Effects of Quercetin Encapsulated Liposomes via Nasal Administration: A Novel Cognitive Enhancer

Tong-Un¹,

Muchimapura²,

Phachonpai³

2010

American Journal of Applied Sciences

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Problem statement: Demand for cognitive-enhancing drugs is growing. Numerous medicinal plants possessing antioxidant activity have received much attention as food supplement to improve cognitive function. Quercetin is a potent free radical scavenger and antioxidant. However, the limitations of quercetin: Rapidly metabolized is an obstacle to its use for a cognitive enhancer. In addition, the burden of blood brain barrier can be overcome by nasal administration and liposomes. In the present study, we investigated whether nasal administration of quercetin liposomes could improve spatial memory in healthy adult rats. Approach: Male Wistar rats were pretreated with quercetin liposomes, containing 0.5 mg of quercetin in 20 µL (dose = 20 µg), via right nasal cavity once daily continually for 4 weeks. Evaluation of rodent learning and memory was assessed by Morris water maze test and then all rats were sacrificed for determining the survival and cholinergic neurons densities in hippocampus. Results: Quercetin liposomes via nasal route treated rats exhibited a significant improvement in cognitive performance. In addition, nasal administration of quercetin liposomes also resulted in induced the densities of survival and cholinergic neurons in hippocampus. However, further researches about the precise underlying mechanism are still required. Conclusion: Our studies demonstrate that quercetin liposomes via nasal administration may have a candidate for cognitive enhancer in the future.

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“…Nasal absorption can be affected by the physicochemical characteristics of the administered drug such as Mw, solubility, dissolution rate, partition coefficient, charge, pKa, particle size and polymorphism [10]. The physicochemical properties of a drug can be altered by the presence of some enhancers in the formulation by modifying drug solubility, partition coefficient, or ionic interactions with the drug [4].…”

Section: Limitations Of Nasal Deliverymentioning

confidence: 99%

“…Nasal bioadhesive dosage forms can be classified as bioadhesive powders [31,32], micro and nanoparticulate systems [33], hydrogels [34][35][36] and inserts . Among nasal inserts, bioadhesive solid dosage forms are promising for prolonged drug delivery that allow easy dosing with high potential for systemic administration.…”

Section: Nasal Insertsmentioning

confidence: 99%

Nasal Inserts for Drug Delivery: An Overview

Algin-Yapar¹

2014

Trop. J. Pharm Res

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Effects of physicochemical properties and other factors on systemic nasal drug delivery

Cited by 254 publications

References 138 publications

Neuroprotective Effect of Quercetin Encapsulated Liposomes: A Novel Therapeutic Strategy against Alzheimer's Disease

Neuroprotective Effect of Quercetin Encapsulated Liposomes: A Novel Therapeutic Strategy against Alzheimer's Disease

Effects of Quercetin Encapsulated Liposomes via Nasal Administration: A Novel Cognitive Enhancer

Nasal Inserts for Drug Delivery: An Overview

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