Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

Bastiat, Guillaume; Plourde, François; Motulsky, Aude; Fürtös, Alexandra; Dumont, Yvan; Quirion, Rémi; Fuhrmann, Gregor; Leroux, Jean‐Christophe

doi:10.1016/j.biomaterials.2010.04.009

Cited by 75 publications

(54 citation statements)

References 46 publications

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“…Rivastigmine Acetylcholinesterase Inhibitor in Alzheimer's disease [53] Gelatin containing microemulsion based gel Isopropyl myristate and Tween 85…”

Section: Safflower Oilmentioning

confidence: 99%

Oleogel: A promising base for transdermal formulations

Balasubramanian¹,

Damodar²,

Sughir³

2012

Asian J Pharm

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S ince last two decades the work on oleogels is being exploited in pharmaceutical, cosmetics, and nutraceutical industries for their desired rheological, physical, and chemical stabilities in semisolid formulations. Recently, we had developed a stable and efficacious oleogel containing diclofenac diethylamine for topical application. The present review article deals with the literature of oleogels including its application in various fields from last few decades till date. The literature reveals that the oleogels have simplicity in manufacturing, high physical, chemical, and mechanical stability and better invivo efficacy, which make them appropriate to employ as bases for topical formulations.

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“…Rivastigmine Acetylcholinesterase Inhibitor in Alzheimer's disease [53] Gelatin containing microemulsion based gel Isopropyl myristate and Tween 85…”

Section: Safflower Oilmentioning

confidence: 99%

Oleogel: A promising base for transdermal formulations

Balasubramanian¹,

Damodar²,

Sughir³

2012

Asian J Pharm

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“…It is currently marketed as oral solution, capsules, and a transdermal patch. The existing formulations require daily dosing of rivastigmine [4]. However, limitations with its oral therapy include restricted entry into the brain due to its hydrophilicity, necessitating frequent dosing and cholinergic side effects like severe bradycardia, nausea, dyspepsia, vomiting, and anorexia [5, 6].…”

Section: Introductionmentioning

confidence: 99%

Rivastigmine Loaded L-Lactide-Depsipeptide Polymeric Nanoparticles: Decisive Formulation Variables Optimization

Pagar

Vavia²

2013

Sci. Pharm.

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The main aim of the investigation was to explore a novel L-lactide-depsipeptide copolymer for the development of rivastigmine-loaded polymeric nanoparticles. L-lactide-depsipeptide synthesis was based on the ring opening polymerization reaction of L-lactide with the cyclodepsipeptide, cyclo(Glc-Leu), using tin 2-ethyl hexanoate as an initiator. Rivastigmine-loaded nanoparticles were prepared by the single emulsion-solvent evaporation technique. The influence of various critical formulation variables like sonication time, amount of polymer, amount of drug, stabilizer concentration, drug-to-polymer ratio, and organic-to-aqueous phase ratio on particle size and entrapment efficiency was studied. The optimized formulation having a particle size of 142.2 ± 21.3 nm with an entrapment efficiency of 60.72 ± 3.72% was obtained. Increased rivastigmine entrapment within the polymer matrix was obtained with a relatively low organic-to-aqueous phase ratio and high drug-to-polymer ratio. A decrease in the average size of the nanoparticles was observed with a decrease in the amount of polymer added and an increase in the sonication time. Prolonged sonication time, however, decreased rivastigmine entrapment. From the different lyoprotectant tested, only trehalose was found to prevent nanoparticle aggregation upon application of the freeze-thaw cycle. Drug incorporation into the polymeric matrix was confirmed by the DSC and XRD study. The spherical nature of the nanoparticles was confirmed by the SEM study. The in vitro drug release study showed the sustained release of more than 90% of the drug up to 72 h. Thus, L-lactide-depsipeptide can be used as an efficient carrier for the nanoparticle preparation of rivastigmine.

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“…Results (Figure 7) indicated that the organogel formulation behaved like a semi-solid drug depot, which could extend the release of drug from 36 h to almost 15 d. Specially, the release of CC from the control oily solution reached almost 87.0% in the first 24 h, which was only 28.2% for CC-loaded organogel. However, there still existed initial burst of drug to some extent, which was a ubiquitous phenomenon for this in situ drug delivery system due to the lag time between the injection of formulation solution and the formation of semi-solid implant (Bastiat et al, 2010). The percent prediction values of Y 24h and Y 15d were 27.6% and 92.9%, respectively, which were 28.2% and 92.4% as actual, suggesting a good prediction ability of the model equation.…”

Section: In Vitro Release Evaluationmentioning

confidence: 90%

Self-assembled drug delivery system based on low-molecular-weight bis-amide organogelator: synthesis, properties and in vivo evaluation

Cao

et al. 2016

Drug Delivery

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(2016) Self-assembled drug delivery system based on low-molecular-weight bisamide organogelator: synthesis, properties and invivo evaluation, Drug Delivery, 23:8, 3168-3178, DOI: 10.3109/10717544.2016 RESEARCH ARTICLESelf-assembled drug delivery system based on low-molecular-weight bis-amide organogelator: synthesis, properties and in vivo evaluation Zhen Li, Jinxu Cao, Heran Li, Hongzhuo Liu, Fei Han, Zhenyun Liu, Chao Tong, and Sanming Li School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, P.R. China Abstract Context: Orgnaogels based on amino acid derivatives have been widely used in the area of drug delivery. Objective: An organogel system based on L-lysine derivatives was designed and prepared to induce a thermal sensitive implant with higher transition temperature, better mechanical strength, and shorter gelation time. Materials and methods: The organogel was prepared by injectable soybean oil and methyl (S)-2,5-ditetradecanamidopentanoate (MDP), which was synthesized for the first time. Candesartan cilexetil (CC) was chosen as model drug. Different formulations were designed and optimized by response surface method. Thermal, rheology properties, and gelation kinetics of the optimized formulation had been characterized. The release behaviors in vitro, as well as in vivo were evaluated in comparison with the oily solution of drugs. Finally, the local inflammation response of in situ organogel was assessed by histological analysis. Results and discussion: Results showed that the synthesized gelator, MDP, had a good gelation ability and the organogels obtained via the self-assembly of gelators in vegetable oils exhibited great thermal and rheology properties, which guaranteed their state in body. In vivo pharmacokinetic demonstrated that the organogel formulation could extend the drug release and maintain a therapeutically effective plasma concentration at least 10 d. In addition, this implant showed acceptable moderate inflammation. Conclusion: The in situ forming L-lysine-derivative-based organogel could be a promising matrix for sustained drug delivery of the drugs with low solubility. KeywordsBiocompatibility, gelator, in situ implant system, in vivo release, organogel History

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Tyrosine-based rivastigmine-loaded organogels in the treatment of Alzheimer’s disease

Cited by 75 publications

References 46 publications

Oleogel: A promising base for transdermal formulations

Oleogel: A promising base for transdermal formulations

Rivastigmine Loaded L-Lactide-Depsipeptide Polymeric Nanoparticles: Decisive Formulation Variables Optimization

Self-assembled drug delivery system based on low-molecular-weight bis-amide organogelator: synthesis, properties and in vivo evaluation

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