Nose-to-brain delivery of lamotrigine-loaded PLGA nanoparticles

Nigam, Kuldeep; Kaur, Atinderpal; Tyagi, Amit; Nematullah,; Khan, Farah; Gabrani, Reema; Dang, Shweta

doi:10.1007/s13346-019-00622-5

Cited by 71 publications

(23 citation statements)

References 39 publications

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“…122 Thus, various novel drug delivery strategies are under investigation which coverup such limitations and improves the efficiency of the intranasal route. Nigam et al (2019) utilized PLGA nanoparticle for direct nose-to-brain delivery of lamotrigine. The study shows the intranasal PLGA-nanoparticle significantly improved the pharmacokinetic behavior of the drug and also the brain targeting efficiency.…”

Section: Quantum Dotsmentioning

confidence: 99%

“…The study shows the intranasal PLGA-nanoparticle significantly improved the pharmacokinetic behavior of the drug and also the brain targeting efficiency. 126 Similarly, Musumeci et al (2018) formulated oxcarbazepine loaded PLGA nanoparticle to treat epileptic seizure and deliver it through the intranasal route. The strategy demonstrated improved brain targeting and higher drug concentration of drug in the brain.…”

Section: Quantum Dotsmentioning

confidence: 99%

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<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

Alexander¹,

Agrawal²,

Uddin³

et al. 2019

IJN

118

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The treatment of central nervous system (CNS) disorders always remains a challenge for the researchers. The presence of various physiological barriers, primarily the blood–brain barrier (BBB) limits the accessibility of the brain and hinders the efficacy of various drug therapies. Hence, drug targeting to the brain, particularly to the diseased cells by circumventing the physiological barriers is essential to develop a promising therapy for the treatment of brain disorders. Presently, the investigations emphasize the role of different nanocarrier systems or surface modified target specific novel carrier system to improve the efficiency and reduce the side effects of the brain therapeutics. Such approaches supposed to circumvent the BBB or have the ability to cross the barrier function and thus increases the drug concentration in the brain. Although the efficacy of novel carrier system depends upon various physiological factors like active efflux transport, protein corona of the brain, stability, and toxicity of the nanocarrier, physicochemical properties, patient-related factors and many more. Hence, to develop a promising carrier system, it is essential to understand the physiology of the brain and BBB and also the other associated factors. Along with this, some alternative route like direct nose-to-brain drug delivery can also offer a better means to access the brain without exposure of the BBB. In this review, we have discussed the role of various physiological barriers including the BBB and blood-cerebrospinal fluid barrier (BCSFB) on the drug therapy and the mechanism of drug transport across the BBB. Further, we discussed different novel strategies for brain targeting of drug including, polymeric nanoparticles, lipidic nanoparticles, inorganic nanoparticles, liposomes, nanogels, nanoemulsions, dendrimers, quantum dots, etc. along with the intranasal drug delivery to the brain. We have also illustrated various factors affecting the drug targeting efficiency of the developed novel carrier system.

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Section: Quantum Dotsmentioning

confidence: 99%

Section: Quantum Dotsmentioning

confidence: 99%

<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

Alexander¹,

Agrawal²,

Uddin³

et al. 2019

IJN

118

View full text Add to dashboard Cite

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“…PLGA nanoparticles exhibit rapid uptake by the brain, sustained delivery of drug, biodegradability, biocompatibility, and less toxicity making them promising carriers for delivering drugs directly into the brain [21][22][23]. Nigam et al [23] developed LTG-loaded PLGA nanoparticles whereas Lalani et al [24] formulated LTG-loaded PLGA nanoparticles functionalized with Transferrin and Lactoferrin. These results from these studies show that such nanoparticles delivered intranasally provided better biodistribution of the therapeutic drug in the brain and improved pharmacodynamics as well as provide better management of neuropathic pain.…”

Section: Introductionmentioning

confidence: 99%

Lamotrigine loaded PLGA nanoparticles intended for direct nose to brain delivery in epilepsy: pharmacokinetic, pharmacodynamic and scintigraphy study

Shah

Dubey

Vyas

et al. 2021

Artificial Cells, Nanomedicine, and Biotechnology

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The present study aimed to investigate the brain targeting efficacy of Lamotrigine (LTG) loaded PLGA nanoparticles (LTG-PNPs) upon intranasal administration. LTG-PNPs were fabricated through the emulsification-solvent evaporation technique and evaluated for % Entrapment efficiency, particle size, in-vitro release, surface morphology, crystallinity, ex-vivo permeation & thermal behaviour. Biodistribution, gamma scintigraphy, and pharmacodynamic studies were performed in BALB/c mice, New Zealand rabbits, and Wistar rats respectively. LTG-PNPs exhibited % EE 71%; particle size 170.0 nm; Polydispersity index 0.191; zeta potential À16.60 mV. LTG-PNPs exhibited a biphasic release pattern. Biodistribution and gamma scintigraphy studies proved a greater amount of LTG in the brain following intranasal delivery of LTG-PNPs in comparison to LTG-SOL. Pharmacodynamic studies demonstrated delayed seizure onset time with LTG-PNPs in comparison to LTG-SOL. Intranasal administration of LTG-PNPs provided prolonged release, higher bioavailability, and better brain targeting bypassing the BBB. The developed formulation could be administered as a once-a-day formulation that would reduce the dosing frequency; dose; dose-related side effects; cost of the therapy and would be beneficial in the management of epilepsy as compared to the LTG-SOL. However, the proof of concept generated through these studies needs to be further validated in higher animals and human volunteers.

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“…For quicker onset of action lamotrigine orally disintegrating tablet has been formulated by Patil et al 9 Though, several crystal products of LT has been reported over past years for the improvement of solubility and dissolution rate, however an optimized crystalline product of LT with citric acid (CA) is yet to be reported. [10][11][12] The present work aimed for the development and characterization of a novel crystalline product of LT with CA to improve its dissolution rate and oral absorption for enhanced clinical outcome. The study involved characterization of the LT-CA crystal products by different analytical techniques along with in vitro dissolution studies to report the optimized crystal product for future in vivo studies.…”

Section: Introductionmentioning

confidence: 99%

Crystal products of lamotrigine-citric acid for improvement of in vitro drug release in simulated gastric fluid

Satapathy

Patel

Sahoo

et al. 2021

JSCS

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Crystal engineering is an integral part of the drug development research. Crystal forms can modify the physicochemical properties of the parent drug molecule. The present work was aimed at the synthesis and characterization of crystalline product of lamotrigine (LT), a FDA approved anti-epileptic drug, with citric acid (CA) to improve its release in gastric region and oral absorption. The crystalline products of LT-CA were developed by solvent evaporation method using ethanol-water as the solvent system. Appearance of new charac-teristic peaks in the FTIR spectra for the crystal products indicated formation of new crystal state. In DSC thermogram, melting point of the experimental crystal products was different than that of the pure drug. Further, formation of new crystalline phase was confirmed from XRD data through the identification of new sharp peaks for the selected crystal products. A higher cumulative percen-tage of drug release was observed for the crystal products than the free drug within 60 min of drug release in simulated gastric fluid. However, in vivo studies are warranted for the future technology transfer of the product at industrial scale.

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Nose-to-brain delivery of lamotrigine-loaded PLGA nanoparticles

Cited by 71 publications

References 39 publications

<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

Lamotrigine loaded PLGA nanoparticles intended for direct nose to brain delivery in epilepsy: pharmacokinetic, pharmacodynamic and scintigraphy study

Crystal products of lamotrigine-citric acid for improvement of in vitro drug release in simulated gastric fluid

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