Nose-to-brain delivery of teriflunomide-loaded lipid-based carbopol-gellan gum nanogel for glioma: Pharmacological and in vitro cytotoxicity studies

Gadhave, Dnyandev; Rasal, Nishant K.; Sonawane, Ravindra S.; Sekar, Mahendran; Kokare, Chandrakant

doi:10.1016/j.ijbiomac.2020.11.047

Cited by 63 publications

(28 citation statements)

References 63 publications

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“…Drug accumulation in the brain can be observed using gamma scintigraphy images after labeling the drug, SLNs, or NLCs with 99m Tc [ 66 , 72 ]. This technique is also used in PK studies to quantify drug accumulation in blood and the brain [ 73 , 74 , 75 ]. Fluorescence imaging is also used for the DiR DiIC18-labeled CS-NLCs [ 76 ].…”

Section: In Vivo Evaluation Of Intranasal Formulations For Nose-to-br...mentioning

confidence: 99%

“…In a recent study, 99m Tc radiolabeled teriflunomide was loaded into NLC gellan gum-carbopol 974P gel [ 74 ]. In mice, the brain:blood concentration ratios of the NLC gel (IN) were approximately 2–3- and 8–10-fold higher than those of the NLC dispersion (IN and IV, respectively).…”

Section: In Vivo Evaluations Of Sln and Nlc-based Formulations For No...mentioning

confidence: 99%

“…Most of these studies compared SLN and NLC gels (IN) with the free drug (IN and IV). In some studies, SLN and NLC gels (IN) were compared with SLN and NLC suspensions (IV) [ 26 , 74 ], which did not enable proper comparison of the efficacies of gelling systems over plain SLNs and NLCs.…”

Section: Effects Of Gelling Systems and Surface Modifications Of Slns...mentioning

confidence: 99%

“…ratios (2-3-and 8-10-fold vs. IN and IV NLCs, respectively); safety (histopathological examination and biochemical markers)[74] TPGS, D-α-Tocopherol polyethylene glycol 1000 succinate; TMC, N,N,N-trimethyl chitosan.…”

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confidence: 99%

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Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery

Nguyen

Maeng

2022

Pharmaceutics

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Nose-to-brain drug delivery has been of great interest for the treatment of many central nervous system (CNS) diseases and psychiatric disorders over past decades. Several nasally administered formulations have been developed to circumvent the blood-brain barrier and directly deliver drugs to the CNS through the olfactory and trigeminal pathways. However, the nasal mucosa’s drug absorption is insufficient and the volume of the nasal cavity is small, which, in combination, make nose-to-brain drug delivery challenging. These problems could be minimized using formulations based on solid lipid nanoparticles (SLNs) or nanostructured lipid carriers (NLCs), which are effective nose-to-brain drug delivery systems that improve drug bioavailability by increasing drug solubility and permeation, extending drug action, and reducing enzymatic degradation. Various research groups have reported in vivo pharmacokinetics and pharmacodynamics of SLNs and NLCs nose-to-brain delivery systems. This review was undertaken to provide an overview of these studies and highlight research performed on SLN and NLC-based formulations aimed at improving the treatment of CNS diseases such neurodegenerative diseases, epilepsy, and schizophrenia. We discuss the efficacies and brain targeting efficiencies of these formulations based on considerations of their pharmacokinetic parameters and toxicities, point out some gaps in current knowledge, and propose future developmental targets.

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Section: In Vivo Evaluation Of Intranasal Formulations For Nose-to-br...mentioning

confidence: 99%

Section: In Vivo Evaluations Of Sln and Nlc-based Formulations For No...mentioning

confidence: 99%

Section: Effects Of Gelling Systems and Surface Modifications Of Slns...mentioning

confidence: 99%

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confidence: 99%

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Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery

Nguyen

Maeng

2022

Pharmaceutics

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“…Gadhave et al [ 79 ] developed a carbopol-gellan gum in situ gel containing teriflunomide-loaded NLC for the treatment of gliomas. Gellan gum is a natural anionic polysaccharide capable of forming a hydrogel in the presence of cations in the nasal cavity.…”

Section: Solid Lipid Nanoparticles (Sln) and Nanostructured Lipid Carriers (Nlc) For Nasal Deliverymentioning

confidence: 99%

In Vitro Studies on Nasal Formulations of Nanostructured Lipid Carriers (NLC) and Solid Lipid Nanoparticles (SLN)

et al. 2021

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The nasal route has been used for many years for the local treatment of nasal diseases. More recently, this route has been gaining momentum, due to the possibility of targeting the central nervous system (CNS) from the nasal cavity, avoiding the blood−brain barrier (BBB). In this area, the use of lipid nanoparticles, such as nanostructured lipid carriers (NLC) and solid lipid nanoparticles (SLN), in nasal formulations has shown promising outcomes on a wide array of indications such as brain diseases, including epilepsy, multiple sclerosis, Alzheimer’s disease, Parkinson’s disease and gliomas. Herein, the state of the art of the most recent literature available on in vitro studies with nasal formulations of lipid nanoparticles is discussed. Specific in vitro cell culture models are needed to assess the cytotoxicity of nasal formulations and to explore the underlying mechanism(s) of drug transport and absorption across the nasal mucosa. In addition, different studies with 3D nasal casts are reported, showing their ability to predict the drug deposition in the nasal cavity and evaluating the factors that interfere in this process, such as nasal cavity area, type of administration device and angle of application, inspiratory flow, presence of mucoadhesive agents, among others. Notwithstanding, they do not preclude the use of confirmatory in vivo studies, a significant impact on the 3R (replacement, reduction and refinement) principle within the scope of animal experiments is expected. The use of 3D nasal casts to test nasal formulations of lipid nanoparticles is still totally unexplored, to the authors best knowledge, thus constituting a wide open field of research.

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Nanoparticle Formulations

Singh,

Parikh,

Sethi

et al. 2024

Nanocarrier Vaccines

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Nose-to-brain delivery of teriflunomide-loaded lipid-based carbopol-gellan gum nanogel for glioma: Pharmacological and in vitro cytotoxicity studies

Cited by 63 publications

References 63 publications

Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery

Pharmacokinetics and Pharmacodynamics of Intranasal Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Nose-to-Brain Delivery

In Vitro Studies on Nasal Formulations of Nanostructured Lipid Carriers (NLC) and Solid Lipid Nanoparticles (SLN)

Nanoparticle Formulations

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