Intranasal teriflunomide microemulsion: An improved chemotherapeutic approach in glioblastoma

Gadhave, Dnyandev; Gorain, Bapi; Tagalpallewar, Amol; Kokare, Chandrakant

doi:10.1016/j.jddst.2019.02.013

Cited by 54 publications

(26 citation statements)

References 31 publications

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“…The decrease in PDI corresponding to an increase in Smix% might be due to the fact of successful coating of smaller oil droplets using increased concentration of Smix and whereas insufficient Smix concentration may result in coalescence of the droplet and lead to an increase in PDI [ 26 , 44 ]. These findings are in agreement with the previous findings by other researchers [ 41 , 42 , 45 ].…”

Section: Resultssupporting

confidence: 94%

Development and Optimization of Naringenin-Loaded Chitosan-Coated Nanoemulsion for Topical Therapy in Wound Healing

et al. 2020

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The potential role of naringenin (NAR), a natural flavonoid, in the treatment of chronic wound has prompted the present research to deliver the drug in nanoemulsion (NE) form, where synergistic role of chitosan was achieved through development of chitosan-coated NAR NE (CNNE). The NE consisted of Capryol 90, Tween 20 and Transcutol P, which was fabricated by low-energy emulsification method to encapsulate NAR within the oil core. The optimization of the formulated NEs was performed using Box–Behnken statistical design to obtain crucial variable parameters that influence globule size, size distribution and surface charge. Finally, the optimized formulation was coated with different concentrations of chitosan and subsequently characterized in vitro. The size of the CNNE was found to be increased when the drug-loaded formulation was coated with chitosan. Controlled release characteristics depicted 67–81% release of NAR from the CNNE, compared to 89% from the NE formulation. Cytotoxicity study of the formulation was performed in vitro using fibroblast cell line (NIH-3T3), where no inhibition in proliferation of the cells was observed with CNNE. Finally, the wound healing potential of the CNNE was evaluated in an abrasion-created wound model in experimental animals where the animals were treated and compared histologically at 0 and 14 days. Significant improvement in construction of the abrasion wound was observed when the animals were treated with formulated CNNE, whereas stimulation of skin regeneration was depicted in the histological examination. Therefore, it could be summarized that the chitosan coating of the developed NAR NE is a potential platform to accelerate healing of wounds.

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Section: Resultssupporting

confidence: 94%

Development and Optimization of Naringenin-Loaded Chitosan-Coated Nanoemulsion for Topical Therapy in Wound Healing

et al. 2020

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“…On a similar note, Gadhave and his team worked on ME and mucoadhesive hydrogel (MME) for the intranasal delivery of teriflunomide (TFM) with the aim of increasing the brain delivery of TFM [118]. TFM is a selective and reversible inhibitor of the mitochondrial enzyme dihydroorotate dehydrogenase that is necessary for the de novo synthesis of pyrimidine nucleotides [149].…”

Section: Drug Delivery Systems For Nose-to-brain Delivery In Gliobmentioning

confidence: 99%

Nasal Drug Delivery of Anticancer Drugs for the Treatment of Glioblastoma: Preclinical and Clinical Trials

et al. 2019

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Glioblastoma (GBM) is the most lethal form of brain tumor, being characterized by the rapid growth and invasion of the surrounding tissue. The current standard treatment for glioblastoma is surgery, followed by radiotherapy and concurrent chemotherapy, typically with temozolomide. Although extensive research has been carried out over the past years to develop a more effective therapeutic strategy for the treatment of GBM, efforts have not provided major improvements in terms of the overall survival of patients. Consequently, new therapeutic approaches are urgently needed. Overcoming the blood–brain barrier (BBB) is a major challenge in the development of therapies for central nervous system (CNS) disorders. In this context, the intranasal route of drug administration has been proposed as a non-invasive alternative route for directly targeting the CNS. This route of drug administration bypasses the BBB and reduces the systemic side effects. Recently, several formulations have been developed for further enhancing nose-to-brain transport, mainly with the use of nano-sized and nanostructured drug delivery systems. The focus of this review is to provide an overview of the strategies that have been developed for delivering anticancer compounds for the treatment of GBM while using nasal administration. In particular, the specific properties of nanomedicines proposed for nose-to-brain delivery will be critically evaluated. The preclinical and clinical data considered supporting the idea that nasal delivery of anticancer drugs may represent a breakthrough advancement in the fight against GBM.

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“…Recently, several researchers have proposed the inclusion of nanoformulations within mucoadhesive gelling systems for nasal administration in order to enhance the nasal residence time and reduce the mucociliary clearance [146,147]. On a similar note, Gadhave and his team worked on microemulsion (ME) and mucoadhesive hydrogel (MME) for intranasal delivery of teriflunomide (TFM) with the aim to increase the brain delivery TFM [118]. TFM is a selective and reversible inhibitor of the mitochondrial enzyme dihydroorotate dehydrogenase necessary for the de novo synthesis of pyrimidine nucleotides [148].…”

Section: Drug Delivery Systems For Nose-to-brain Delivery In Glioblasmentioning

confidence: 99%

“…However, has been reported that oral administration of TFM should be performed with caution because of the high risk of severe liver injury [149]. Recent studies have demonstrated its action as an antitumor agent in breast cancer [150], glioblastoma [118], prostate cancer [151] and lung cancer [152]. Anti-EPHA3 functionalized nanoparticles increased the median animal survival by 1.37-fold compared to non-targeted nanoparticles.…”

Section: Drug Delivery Systems For Nose-to-brain Delivery In Glioblasmentioning

confidence: 99%

“…TFM-MME formulation did not reflect any changes in liver or kidney biomarkers, hematology, and histopathological examination at low and medium doses. Although these formulations demonstrated to be safe for nasal administration, the study needs more robust in vitro and in vivo investigations to demonstrate the efficacy of the TFM-ME and TFM-MME to treatment of GBM[118].One strategy to improve brain tumor accumulation of drug delivery systems is the functionalization of the surface of nanocarriers with targeting moieties. Ephrin type-A receptor 3 (EPHA3) is a membrane-associated receptor overexpressed in the stroma and vasculature of gliomas[153].…”

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Nasal Drug Delivery of Anticancer Drugs for the Treatment of Glioblastoma: Preclinical and Clinical Trials

Bruinsmann¹,

Vaz²,

Alves³

et al. 2019

Preprint

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Glioblastoma (GBM) is the most lethal form of brain tumor, characterized by rapid growth and surrounding tissue invasion. The current standard treatment is surgery followed by radiotherapy, and concurrent chemotherapy, typically with temozolomide. Although extensive research has been performed over the past years to develop an effective therapeutic strategy for the treatment of GBM, efforts have not provided major improvements in the overall survival of patients with GBM. Thus, new therapeutic approaches are urgently needed. A major challenge in the development of therapies for central nervous system (CNS) disorders is overcoming the blood–brain barrier (BBB). In this context, the intranasal (IN) route of drug administration has been proposed as a non-invasive alternative route to directly targeting the CNS. In fact, this route of drug administration may bypass the blood-brain barrier and reduce systemic side effects. Recently, formulations have been developed to further enhance nose-to-brain transport, mainly with the use of nano-sized and nanostructured drug delivery systems. The focus of this review will be on the strategies developed to deliver a number of anticancer compounds for the treatment of GBM using the nasal administration. In particular, the specific properties of nanomedicines proposed for the nose-to-brain delivery will be critically evaluated. The number of preclinical and clinical data reviewed support the idea that nasal delivery of anticancer drugs might represent a breakthrough advancement in the fight against GBM.

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Intranasal teriflunomide microemulsion: An improved chemotherapeutic approach in glioblastoma

Cited by 54 publications

References 31 publications

Development and Optimization of Naringenin-Loaded Chitosan-Coated Nanoemulsion for Topical Therapy in Wound Healing

Development and Optimization of Naringenin-Loaded Chitosan-Coated Nanoemulsion for Topical Therapy in Wound Healing

Nasal Drug Delivery of Anticancer Drugs for the Treatment of Glioblastoma: Preclinical and Clinical Trials

Nasal Drug Delivery of Anticancer Drugs for the Treatment of Glioblastoma: Preclinical and Clinical Trials

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