Definition and validation of the Design Space for co-milled nasal powder containing nanosized lamotrigine

Gieszinger, Péter; Tomuță, Ioan; Casian, Tibor; Bartos, Cs.; Szabó‐Révész, Piroska; Ambrus, Rita

doi:10.1080/03639045.2018.1483388

Cited by 12 publications

(12 citation statements)

References 34 publications

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“…antiepileptic drug and only available on the market in tablet form [3]. Since the beginning a nanosized LAM containing nasal powder has been produced, the process of sample preparation has been optimized and the samples were tested in vivo [4].…”

Section: Op-19mentioning

confidence: 99%

Nasal formulation of active ingredients to induce systemic and central nervous systemic effects

Gieszinger

Ambrus

Szabó‐Révész

2019

I. Symposium of Young Researchers on Pharmaceutical Technology, Biotechnology and Regulatory Science

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Section: Op-19mentioning

confidence: 99%

Nasal formulation of active ingredients to induce systemic and central nervous systemic effects

Gieszinger

Ambrus

Szabó‐Révész

2019

I. Symposium of Young Researchers on Pharmaceutical Technology, Biotechnology and Regulatory Science

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“…By applying powder formulations, higher administration dose and better adhesion to the nasal mucosa can be achieved, that may cause better absorption through the barrier [32,33]. In our previous studies, nanosized lamotrigine (LAM) containing nasal powder was produced and developed by the Quality by Design method [34,35].…”

Section: Introductionmentioning

confidence: 99%

“…Previously, a nanosized LAM containing nasal powder was produced, optimized and its preparation method was well established. As a continuation of our previous studies [34,35], the aim of this work was to determine the physicochemical properties, the in vitro characteristics and the in vivo absorption profile of a possible novel, nasal powder dosage form of LAM and compare it to the physical mixture as a reference with the hypothesis that smaller particle size results in higher absorption.…”

Section: Introductionmentioning

confidence: 99%

Investigation of the Absorption of Nanosized lamotrigine Containing Nasal Powder via the Nasal Cavity

et al. 2020

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Nasal drug delivery has become a popular research field in the last years. This is not surprising since the nose possesses unique anatomical and physical properties. Via the nasal mucosa local, systemic, and directly central nerve systemic (CNS) effect is achievable. Powders have favorable physicochemical properties over liquid formulations. Lamotrigine (LAM) is an antiepileptic agent with a relatively mild side effect spectrum, but only available in tablet form on market. Reducing the particle size to the nano range can affect the bioavailability of pharmaceutical products. The aim of this article was to continue the work started, compare the in vitro properties of a nanonized lamotrigine containing nasal powder (nanoLAMpowder) and its physical mixture (PM) that were prepared by dry milling. Moreover, to study their trans-epithelial absorption to reach the blood and target the brain by axonal transport. Due to the dry milling technique, the particle size of LAM, their surface and also their structure changed that led to higher in vitro dissolution and permeability rate. The results of the in vivo tests showed that the axonal transport of the drug was assumable by both intranasal formulations because the drug was present in the brain within a really short time, but the LAM from the nanoLAMpowder liberated even faster.

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“…Our research group has made successful efforts to develop nasal powder form of LAM with a top-down method [49,50]. As the nose is a great alternative administration route to allocate APIs directly into the CNS and provides great possibilty to take advantage of NCs, we envisage that a novel, NC formulation made with a bottom-up method could improve the interaction between the drug and the nasal epithelium.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of lamotrigine containing nanocapsules for nasal administration

Gieszinger

Csaba

García-Fuentes

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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Nanocapsules (NCs) have become one of the most researched nanostructured drug delivery systems due to their advantageous properties and versatility. NCs can enhance the bioavailabiliy of hydrophobic drugs by impoving their solubility and permeability. Also, they can protect these active pharmaceutical agents (APIs) from the physiological environment with preventing e.g. the enzymatic degradation. NCs can be used for many administration routes: e.g. oral, dermal, nasal and ocular formulations are exisiting in liquid and solid forms. The nose is one of the most interesting alternative drug administration route, because local, systemic and direct central nervous system (CNS) delivery can be achived; this could be utilized in the therapy of CNS diseases. Therefore, the goal of this study was to design, prepare and investigate a novel, lamotrigin containing NC formulation for nasal administration. The determination of micrometric parameters (particle size, polydispersity index, surface charge), in vitro (drug loading capacity, release and permeability investigations) and in vivo characterization of the formulations were performed in the study. The results indicate that the formulation could be a promising alternative of lamotrigine (LAM) as the NCs were around 305 nm size with high encapsulation efficiency (58.44%). Moreover, the LAM showed rapid and high release from the NCs in vitro and considerable penetration to the brain tissues was observed during the in vivo study.

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Definition and validation of the Design Space for co-milled nasal powder containing nanosized lamotrigine

Abstract: From the DS generated by the software, an optimal formulation was obtained and the results validated the experimental design. The QbD approach was a useful and effective tool of understanding the parameters that affect the quality of the desired product.

Cited by 12 publications

References 34 publications

Nasal formulation of active ingredients to induce systemic and central nervous systemic effects

Nasal formulation of active ingredients to induce systemic and central nervous systemic effects

Investigation of the Absorption of Nanosized lamotrigine Containing Nasal Powder via the Nasal Cavity

Preparation and characterization of lamotrigine containing nanocapsules for nasal administration

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