Enhanced oral bioavailability of an antipsychotic drug through nanostructured lipid carriers

Jawahar, N; Hingarh, Prashant Kumar; Radhakrishnan, Arun; Selvaraj, Jubie; Anbarasan, Arigo; Sathianarayanan, S.; Nagaraju, G.

doi:10.1016/j.ijbiomac.2018.01.121

Cited by 60 publications

(23 citation statements)

References 22 publications

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“…NLCs are a new generation of lipid nanoparticles that have been developed through the combination of advantages from different nanocarriers. This kind of carrier seems to be a suitable delivery system intended for topical, oral, pulmonary, ocular and parenteral administration of drugs [33–35]. We based our study on the successful effect of IVM against PSCs from previous studies.…”

Section: Discussionmentioning

confidence: 99%

Nanostructured lipid carriers of ivermectin as a novel drug delivery system in hydatidosis

et al. 2019

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BackgroundThe larval stage of the tapeworm Echinococcus granulosus is the causative agent of hydatid disease in humans. This zoonotic parasitic infection remains a major health problem in certain areas of the world where is still endemic. In view of the ineffectiveness of some drug treatments, the surgical removal of cysts remains the preferred treatment option together with the administration of albendazole and mebendazole. However, severe side effects of these drugs have been reported which demands developing new scolicidal agents that confer suitable efficacy and fewer side effects during surgery.MethodsTo that purpose, in the present work we assessed the effectiveness of ivermectin (IVM), a macrocyclic lactone endectocide that has shown to be an effective nematocidal drug against other important parasitic infections. To overcome the limitations observed in some drug formulations and resistance, we used nano lipid carriers (NLCs) as a targeted and sustained drug delivery system for IVM. We evaluated the in vitro cestocidal and apoptotic effects of NLCs-loaded IVM versus IVM by quantifying the expression of caspase-3 mRNA.ResultsWe found that after 60 and 120 min of administration, 800 μg/ml and 400 μg/ml NLCs-loaded IVM induced 100% mortality, respectively. On the other hand, the 800 μg/ml of IVM induced 100% mortality rate 150 min after administration. Additionally, we found that NLCs-loaded IVM induced higher mRNA caspase-3 expression suggesting a more potent apoptotic effect on the parasite.ConclusionsThese data suggest that NLCs-loaded IVM may be a promising alternative to current treatments although in vivo studies are needed.

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Section: Discussionmentioning

confidence: 99%

Nanostructured lipid carriers of ivermectin as a novel drug delivery system in hydatidosis

et al. 2019

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“…Olanzapine is a BCS class II drug, meaning that it has high permeability across the walls of the gastrointestinal tract but low aqueous solubility which can limit the absorbable dose. 34 The dissolution performance of forms I and IV were compared in vitro ( Figure 6), and the dissolution rate of form IV was found to be far faster than form I, with dissolution of the former complete within 15 minutes compared to 90 minutes for the latter. The crystals of the two forms were sieved to ensure that a similar particle size was used for each form, and hence the difference in dissolution rate can be attributed solely to the physical form of the drug.…”

Section: Extraction Of Form IV and Further Characterizationmentioning

confidence: 99%

Olanzapine Form IV: Discovery of a New Polymorphic Form Enabled by Computed Crystal Energy Landscapes

Askin¹,

Cockcroft²,

Price³

et al. 2019

Crystal Growth & Design

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Olanzapine is a polymorphic drug molecule that has been extensively studied, with over 60 structures reported in the Cambridge Structural Database. All anhydrous and solvated forms of olanzapine known to date contain the SC0 dimer packing motif. In this study, a new screening approach was adopted involving heat-induced forced crystallization from a polymer-based molecular dispersion of olanzapine. Simultaneous differential scanning calorimetry-powder X-ray diffraction (DSC-PXRD) was used to heat the amorphous dispersion and to identify a novel physical form from diffraction and heat flow data. Comparison of the diffraction data with those from a computed crystal energy landscape allowed the crystal structure to be determined. The result was the discovery of a new polymorph, form IV, which does not use the SC0 motif. Hence, while dimer formation is the dominant process that defines crystal packing for olanzapine formed from solution, it seems that molecularly dispersing the drug in a polymeric matrix permits crystallization of alternative motifs. Having identified form IV, it proved possible to scale up the synthesis and demonstrate its enhanced dissolution properties over form I.

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“…It has poor bioavailability due to hepatic first-pass metabolism and low permeability into the brain due to efflux by P-glycoproteins [133]. Due to its low oral bioavailability, researchers have created various container preparations [134]. Joseph et al 2017 conducted research on glyceryl monostearate nanoparticles with olanzapine [133].…”

Section: Drug Delivery For Schizophrenia and Bipolar Disordersmentioning

confidence: 99%

“…Pervaiz and colleagues described the release of olanzapine loaded in PNA (poly(N-isopropylacrylamide-co-acrylic acid)) microgels for 72 h [135]. In vitro bioaccessibility research of Jawahar and colleagues indicated 5 1 2 -fold increase in oral bioavailability for nano structured lipid carriers with olanzapine [134]. Cyclodextrins containers were also used for this neuroleptic [136].…”

Section: Drug Delivery For Schizophrenia and Bipolar Disordersmentioning

confidence: 99%

Nano Carrier Drug Delivery Systems for the Treatment of Neuropsychiatric Disorders: Advantages and Limitations

et al. 2020

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Neuropsychiatric diseases are one of the main causes of disability, affecting millions of people. Various drugs are used for its treatment, although no effective therapy has been found yet. The blood brain barrier (BBB) significantly complicates drugs delivery to the target cells in the brain tissues. One of the problem-solving methods is the usage of nanocontainer systems. In this review we summarized the data about nanoparticles drug delivery systems and their application for the treatment of neuropsychiatric disorders. Firstly, we described and characterized types of nanocarriers: inorganic nanoparticles, polymeric and lipid nanocarriers, their advantages and disadvantages. We discussed ways to interact with nerve tissue and methods of BBB penetration. We provided a summary of nanotechnology-based pharmacotherapy of schizophrenia, bipolar disorder, depression, anxiety disorder and Alzheimer’s disease, where development of nanocontainer drugs derives the most active. We described various experimental drugs for the treatment of Alzheimer’s disease that include vector nanocontainers targeted on β-amyloid or tau-protein. Integrally, nanoparticles can substantially improve the drug delivery as its implication can increase BBB permeability, the pharmacodynamics and bioavailability of applied drugs. Thus, nanotechnology is anticipated to overcome the limitations of existing pharmacotherapy of psychiatric disorders and to effectively combine various treatment modalities in that direction.

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Enhanced oral bioavailability of an antipsychotic drug through nanostructured lipid carriers

Cited by 60 publications

References 22 publications

Nanostructured lipid carriers of ivermectin as a novel drug delivery system in hydatidosis

Nanostructured lipid carriers of ivermectin as a novel drug delivery system in hydatidosis

Olanzapine Form IV: Discovery of a New Polymorphic Form Enabled by Computed Crystal Energy Landscapes

Nano Carrier Drug Delivery Systems for the Treatment of Neuropsychiatric Disorders: Advantages and Limitations

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