Rethinking carbamazepine oral delivery using polymer-lipid hybrid nanoparticles

Ana, Raquel da; Mendes, Maria; Sousa, João; Pais, Alberto A. C. C.; Falcão, Amı́lcar

doi:10.1016/j.ijpharm.2018.11.028

Cited by 50 publications

(20 citation statements)

References 44 publications

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“…The stability of formulations was evaluated through analytical centrifugation, using the LUMiFuge (L.U.M. GmbH, Germany) stability analyzer, which measures the intensity of transmitted near infrared (NIR) light during the centrifugation of the sample [22]. The analytical centrifugation provides an early assessment of possible instability phenomena.…”

Section: Stability Studiesmentioning

confidence: 99%

QbD-driven development of intranasal lipid nanoparticles for depression treatment

Vitorino

Silva

Gouveia

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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Depression is a life-threatening psychiatric disorder and a multifactorial global public health concern. Current pharmacological treatments present limited efficacy, and are associated with several harmful side effects and development of pharmacoresistance mechanisms. Developing more effective therapeutic options is therefore a priority. This work aims at efficiently designing an antidepressant therapeutic surrogate relying on a dual strategy supported on lipid nanoparticles and intranasal delivery. For that purpose, the formulation was comprehensively optimized following a quality by design perspective. Critical quality attributes (CQAs) ranged from physicochemical to intranasal performance features. The optimized formulation was administered to mice in order to assess the antidepressive and anxiolytic effects by applying the forced swimming and marble-burying tests, respectively. A cross-analysis of the predictive models established for the set of 12 CQAs elicited the formulation containing similar proportion of solid and liquid lipids and lower surfactant concentration as the optimal one. Despite increasing the liquid lipid amount yielded smaller and more homogeneous particle size, and higher release rate, nanostructured lipid carriers (NLCs) provided an earlier and superior pig nasal mucosa permeability than nanoemulsions, along with better stability and cytotoxic profiles. Importantly, the intranasal delivery of the optimal lipid nanoparticle formulation reduced both depressive and anxiety-like behaviors, which positions these intranasal nanosystems in line with the hypothesis of provisioning timely and better acting antidepressant therapies. 1. Introduction Depression is a life-threatening mental disorder and a major public health concern, affecting more than 300 million people of all ages worldwide [1]. It leads to disability, noteworthy health-related costs and decreased quality of life, being considered a prominent risk factor for many other diseases, including neuropsychiatric, cardiovascular, and metabolic conditions [2,3]. Conventional pharmacological treatments for depression are considered relatively well defined. Antidepressant standard-of-care comprises oral selective serotonin reuptake inhibitors (SSRIs, e.g. fluoxetine) and serotonin-norepinephrine reuptake inhibitors (SNRIs, e.g.

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Section: Stability Studiesmentioning

confidence: 99%

QbD-driven development of intranasal lipid nanoparticles for depression treatment

Vitorino

Silva

Gouveia

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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“…LPH are archetype of nanocarriers composed of an internal polymeric core enclosed by an outer lipid bioactive shell composed of one or more layers or components [20,21]. By virtue of their unique structure, LPH have versatile competence to encapsulate different types of payloads such as hydrophilic, hydrophobic drugs or nucleic acids, highlighting promising in vivo therapeutic outcomes [22][23][24][25]. The concomitance of both polymer and lipid imparts the LPH structural integrity, serum stability, sustained drug release (from the polymer core) and high biocompatibility (from the lipid shell) [21].…”

Section: Introductionmentioning

confidence: 99%

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

et al. 2020

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A platform capable of specifically delivering an antiviral drug to the liver infected with hepatitis B is a major concern in hepatology. Vaccination has had a major effect on decreasing the emerging numbers of new cases of infection. However, the total elimination of the hepatitis B virus from the body requires prolonged therapy. In this work, we aimed to target the liver macrophages with lipid polymer hybrid nanoparticles (LPH), combining the merit of polymeric nanoparticles and lipid vesicles. The hydrophilic antiviral drug, entecavir (E), loaded LPH nanoparticles were optimized and physicochemically characterized. A modulated lipidic corona, as well as, an additional coat with vitamin E were used to extend the drug release enhance the macrophage uptake. The selected vitamin E coated LPH nanoparticles enriched with lecithin-glyceryl monostearate lipid shell exhibited high entrapment for E (80.47%), a size � 200 nm for liver passive targeting, extended release over one week, proven serum stability, retained stability after refrigeration storage for 6 months. Upon macrophage uptake in vitro assessment, the presented formulation displayed promising traits, enhancing the cellular retention in J774 macrophages cells. In vivo and antiviral activity futuristic studies would help in the potential application of the ELPH in hepatitis B control.

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“…Epilepsy is a serious neurological disorder characterized by the recurrent, periodic, and unpredictable occurrence of epileptic seizures which might be due to imbalance in excitatory and inhibitory pathways within the central nervous system (CNS) (Ana et al . ). Epilepsy has emerged as a serious health concern affecting 50–70 million people globally accounting 0.75% of global health burden (Trinka et al .…”

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confidence: 97%

High mobility group box 1 (HMGB1) as a novel frontier in epileptogenesis: from pathogenesis to therapeutic approaches

Paudel

Semple

Jones

et al. 2019

Journal of Neurochemistry

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Epilepsy is a serious neurological condition exhibiting complex pathology and deserving of more serious attention. More than 30% of people with epilepsy are not responsive to more than 20 anti‐epileptic drugs currently available, reflecting an unmet clinical need for novel therapeutic strategies. Not much is known about the pathogenesis of epilepsy, but evidence indicates that neuroinflammation might contribute to the onset and progression of epilepsy following acquired brain insults. However, the molecular mechanisms underlying these pathophysiological processes are yet to be fully understood. The emerging research suggests that high‐mobility group box protein 1 (HMGB1), a DNA‐binding protein that is both actively secreted by inflammatory cells and released by necrotic cells, might contribute to the pathogenesis of epilepsy. HMGB1 as an initiator and amplifier of neuroinflammation, and its activation is implicated in the propagation of seizures in animal models. The current review will highlight the potential role of HMGB1 in the pathogenesis of epilepsy, and implications of HMGB1‐targeted therapies against epilepsy. HMGB1 in this context is an emerging concept deserving further exploration. Increased understanding of HMGB1 in seizures and epilepsy will pave the way in designing novel and innovative therapeutic strategies that could modify the disease course or prevent its development.

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Rethinking carbamazepine oral delivery using polymer-lipid hybrid nanoparticles

Cited by 50 publications

References 44 publications

QbD-driven development of intranasal lipid nanoparticles for depression treatment

QbD-driven development of intranasal lipid nanoparticles for depression treatment

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

High mobility group box 1 (HMGB1) as a novel frontier in epileptogenesis: from pathogenesis to therapeutic approaches

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