Beyond liposomes: Recent advances on lipid based nanostructures for poorly soluble/poorly permeable drug delivery

Teixeira, M.C.; Carbone, Claudia; Souto, Eliana B.

doi:10.1016/j.plipres.2017.07.001

Cited by 174 publications

(99 citation statements)

References 68 publications

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“…Drug delivery system has received significant attention due to the potential to improve the therapeutic efficiency of drug candidates by increasing their aqueous solubility, bioavailability, and stability. 24 One of the common drug delivery vehicles is liposomes, which is composed of several lipid bilayers enclosing aqueous compartments and are able to encapsulate both hydrophilic and hydrophobic agents. 25 The size, surface charge and moieties, lipid constituents, and cholesterol contents of liposomes can be manipulated to produce liposomal drug formulations with various physicochemical properties and thus dramatically improve the bioavailability and toxicity of drug candidates.…”

Section: Introductionmentioning

confidence: 99%

<p>Development of Nanosome-Encapsulated Honokiol for Intravenous Therapy Against Experimental Autoimmune Encephalomyelitis</p>

Hsiao¹,

Chen²,

Liang³

et al. 2020

IJN

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Background: Honokiol has been reported to possess anti-inflammatory and neuroprotective activities. However, the poor aqueous solubility of honokiol limits its clinical application for systemic administration. Purpose: This study aims to develop a novel formulation of nanosome-encapsulated honokiol (NHNK) for intravenous therapy against mouse experimental autoimmune encephalomyelitis (EAE) that mimics human multiple sclerosis. Methods: Nanosomes and NHNK were prepared by using an ultra-high pressure homogenization (UHPH) method. Mice were treated with NHNK or empty nanosomes during the peak phase of EAE symptoms. Symptoms of EAE were monitored and samples of the spinal cord were obtained for histopathological examinations. Results: The stock of NHNK containing honokiol in the nanosome formulation, which showed the structure of single phospholipid bilayer membranes, was well formulated with the particle size of 48.0 ± 0.1 nm and the encapsulation efficiency 58.1 ± 4.2%. Intravenous administration of NHNK ameliorated the severity of EAE accompanied by a significant reduction of demyelination and inflammation in the spinal cord. Furthermore, NHNK decreased the number of IL-6 + , Iba-1 + TNF + , Iba-1 + IL-12 p40 + , and CD3 + IFN-γ + cells infiltrating the spinal cord. Conclusion: The UHPH method simplified the preparation of NHNK with uniformly distributed nanosize and high encapsulation efficiency. Intravenous administration of NHNK ameliorated the severity of EAE by suppressing the infiltration of activated microglia and Th1 cells into the spinal cord. Collectively, these results suggest that the formulation of NHNK is a prospective therapeutic approach for inflammatory CNS diseases, such as multiple sclerosis.

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Section: Introductionmentioning

confidence: 99%

<p>Development of Nanosome-Encapsulated Honokiol for Intravenous Therapy Against Experimental Autoimmune Encephalomyelitis</p>

Hsiao¹,

Chen²,

Liang³

et al. 2020

IJN

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“…Research has demonstrated that raising the amount of stearic acid associated with the hydrophilic polymer promotes matrix solubilization increases the matrix porosity and promotes a faster drug release [60]. Due to the lipophilic character of SLN, these particles act as absorption enhancers upon oral administration, contributing to improving the bioavailability of the loaded active ingredients [61][62][63][64]. SLN also show great potential for the oral delivery of nutraceutics [47,[65][66][67], which is a research area that is receiving growing attention both from academia and industry [68][69][70][71].…”

Section: Resultsmentioning

confidence: 99%

Quantification of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles by a Validated Reverse-Phase HPLC Photodiode Array

Rigon

Fachinetti

Severino³

et al. 2019

Applied Sciences

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A new method based on reverse-phase HPLC combined with photodiode array (PDA) was developed to quantify the release of trans-resveratrol (tRES) from solid lipid nanoparticles (SLN). The mobile phase was composed of 75:0:25 (V/V) water/methanol/acetonitrile at 0–3.5 min, 32.5:30.0:37.5 (V/V) water/methanol/acetonitrile at 3.6–5.8 min, and 75:0:25 (V/V) water/methanol/acetonitrile at 5.9–10 min. The flow rate was set at 1.0 mL/min, and tRES was detected at the wavelength of 306.6 nm. A concentration range of 1–100 µg/mL was used to obtain the linear calibration curve. SLN were produced by ultrasound technique to load 0.1% (wt/wt) of tRES, and the in vitro release of the drug was run in modified Franz diffusion cells. The mean recovery of tRES was found to be 96.84 ± 0.32%. The intra-assay and inter-assay coefficients of variation were less than 5%. The proposed method was applied to in vitro permeability studies, and the Weibull model was found to be the one that best fits the tRES release, which is characterized by a simultaneous lipid chain relaxation and erosion during drug release.

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“…This section details the most commonly used methods for the production of each type of nanoparticles illustrated in Figure 4. Lipid nanoparticles can be of different types (e.g., liposomes [13][14][15][16], nanoemulsions [14,17,18], solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) [19][20][21][22][23][24]), each produced from very different lipids (e.g., phospholipids, synthetic oils, essential oils from plants, fatty acids, di-, mono-, and triglycerides, cholesterol), commonly resembling those existing in the human body and also in food. Due to their lipid composition, these particles are usually referred to as biocompatible, biodegradable and are generally recognized as safe [25][26][27].…”

Section: Production Methods Of Clinically Compliant Nanopharmaceuticsmentioning

confidence: 99%

Nanopharmaceutics: Part II—Production Scales and Clinically Compliant Production Methods

et al. 2020

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Due the implementation of nanotechnologies in the pharmaceutical industry over the last few decades, new type of cutting-edge formulations-nanopharmaceutics-have been proposed. These comprise pharmaceutical products at the nanoscale, developed from different types of materials with the purpose to, e.g., overcome solubility problems of poorly water-soluble drugs, the pharmacokinetic and pharmacodynamic profiles of known drugs but also of new biomolecules, to modify the release profile of loaded compounds, or to decrease the risk of toxicity by providing site-specific delivery reducing the systemic distribution and thus adverse side effects. To succeed with the development of a nanopharmaceutical formulation, it is first necessary to analyze the type of drug which is to be encapsulated, select the type matrix to load it (e.g., polymers, lipids, polysaccharides, proteins, metals), followed by the production procedure. Together these elements have to be compatible with the administration route. To be launched onto the market, the selected production method has to be scaled-up, and quality assurance implemented for the product to reach clinical trials, during which in vivo performance is evaluated. Regulatory issues concerning nanopharmaceutics still require expertise for harmonizing legislation and a clear understanding of clinically compliant production methods. The first part of this study addressing "Nanopharmaceutics: Part I-Clinical trials legislation and Good Manufacturing Practices (GMP) of nanotherapeutics in the EU" has been published in Pharmaceutics. This second part complements the study with the discussion about the production scales and clinically compliant production methods of nanopharmaceutics.Nanomaterials 2020, 10, 455 2 of 16 funding opportunities within Member States, Associated Countries and Third Countries. The strategic plan for the next Horizon Europe framework programme has clearly set nanomedicines and advanced therapies as priorities. To succeed, the nanoproduct needs to be manufacturable at large scale and its quality assured in order to reach clinical trials. The topic is indeed of high scientific interest considering the number of scientific papers dealing with clinical trials and nanoparticles over the last twenty years (Figure 1). Nanomaterials 2020, 10, x FOR PEER REVIEW 2 of 17European Commission aims to lead innovation towards the development of these nanopharmaceutics by launching several funding opportunities within Member States, Associated Countries and Third Countries. The strategic plan for the next Horizon Europe framework programme has clearly set nanomedicines and advanced therapies as priorities. To succeed, the nanoproduct needs to be manufacturable at large scale and its quality assured in order to reach clinical trials. The topic is indeed of high scientific interest considering the number of scientific papers dealing with clinical trials and nanoparticles over the last twenty years (Figure 1).

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Beyond liposomes: Recent advances on lipid based nanostructures for poorly soluble/poorly permeable drug delivery

Cited by 174 publications

References 68 publications

<p>Development of Nanosome-Encapsulated Honokiol for Intravenous Therapy Against Experimental Autoimmune Encephalomyelitis</p>

<p>Development of Nanosome-Encapsulated Honokiol for Intravenous Therapy Against Experimental Autoimmune Encephalomyelitis</p>

Quantification of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles by a Validated Reverse-Phase HPLC Photodiode Array

Nanopharmaceutics: Part II—Production Scales and Clinically Compliant Production Methods

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