scholarly journals Sorafenib Repurposing for Ophthalmic Delivery by Lipid Nanoparticles: A Preliminary Study

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1956
Author(s):  
Angela Bonaccorso ◽  
Veronica Pepe ◽  
Cristina Zappulla ◽  
Cinzia Cimino ◽  
Angelo Pricoco ◽  
...  

Uveal melanoma is the second most common melanoma and the most common intraocular malignant tumour of the eye. Among various treatments currently studied, Sorafenib was also proposed as a promising drug, often administered with other compounds in order to avoid resistance mechanisms. Despite its promising cellular activities, the use of Sorafenib by oral administration is limited by its severe side effects and the difficulty to reach the target. The encapsulation into drug delivery systems represents an interesting strategy to overcome these limits. In this study, different lipid nanoparticulate formulations were prepared and compared in order to select the most suitable for the encapsulation of Sorafenib. In particular, two solid lipids (Softisan or Suppocire) at different concentrations were used to produce solid lipid nanoparticles, demonstrating that higher amounts were able to achieve smaller particle sizes, higher homogeneity, and longer physical stability. The selected formulations, which demonstrated to be biocompatible on Statens Seruminstitut Rabbit Cornea cells, were modified to improve their mucoadhesion, evaluating the effect of two monovalent cationic lipids with two lipophilic chains. Sorafenib encapsulation allowed obtaining a sustained and prolonged drug release, thus confirming the potential use of the developed strategy to topically administer Sorafenib in the treatment of uveal melanoma.

Author(s):  
Vipul Ajit Sansare ◽  
Abhijeet Mohan Kanavaje

Acne is a disfiguring disorder of the skin with significant cosmetic morbidity that may lead to serious psychological and social dysfunction. The skin disease comes in two forms. The most well-known form is Acne vulgaris (referred to as acne), which mostly manifests in teens but may continue into the early 20s. The second form is called Acne rosacea (referred to as rosacea) and mostly affects 30- to 60-year-olds. The two forms, despite sharing a common prefix, are quite unrelated in their respective pathophysiology, have different approaches to treatment and hence are considered two separate conditions. The conventional drug delivery system is efficient in the management of acne but poor patient compliance and adverse effects limit its efficacy. Lipid nanoparticles are novel nano lipid carriers made from biocompatible lipid which reduces toxicity; improve physical stability, skin hydration, and film formation. Furthermore, lipid nanoparticles protect the encapsulated drug from degradation. Thus current review focused on the potential use of lipid nanoparticles for the management of acne.


Micron ◽  
2010 ◽  
Vol 41 (1) ◽  
pp. 51-58 ◽  
Author(s):  
Nispa Seetapan ◽  
Piyawan Bejrapha ◽  
Wanwisa Srinuanchai ◽  
Uracha Rungsardthong Ruktanonchai

2004 ◽  
Vol 183 (1) ◽  
pp. 123-126 ◽  
Author(s):  
Steven J. Michel ◽  
Andrew M. Fried ◽  
Shamyshree Sinha ◽  
John Willson ◽  
Eric Bensadoun ◽  
...  

2020 ◽  
Vol 21 (9) ◽  
pp. 3084 ◽  
Author(s):  
Vanessa Desantis ◽  
Ilaria Saltarella ◽  
Aurelia Lamanuzzi ◽  
Assunta Melaccio ◽  
Antonio Giovanni Solimando ◽  
...  

MicroRNAs (miRNAs, or miRs) are single-strand short non-coding RNAs with a pivotal role in the regulation of physiological- or disease-associated cellular processes. They bind to target miRs modulating gene expression at post-transcriptional levels. Here, we present an overview of miRs deregulation in the pathogenesis of multiple myeloma (MM), and discuss the potential use of miRs/nanocarriers association in clinic. Since miRs can act as oncogenes or tumor suppressors, strategies based on their inhibition and/or replacement represent the new opportunities in cancer therapy. The miRs delivery systems include liposomes, polymers, and exosomes that increase their physical stability and prevent nuclease degradation. Phase I/II clinical trials support the importance of miRs as an innovative therapeutic approach in nanomedicine to prevent cancer progression and drug resistance. Results in clinical practice are promising.


2019 ◽  
Vol 9 (20) ◽  
pp. 4438 ◽  
Author(s):  
Amélia Silva ◽  
Carlos Martins-Gomes ◽  
Tiago Coutinho ◽  
Joana Fangueiro ◽  
Elena Sanchez-Lopez ◽  
...  

The surface properties of nanoparticles have decisive influence on their interaction with biological barriers (i.e., living cells), being the concentration and type of surfactant factors to have into account. As a result of different molecular structure, charge, and degree of lipophilicity, different surfactants may interact differently with the cell membrane exhibiting different degrees of cytotoxicity. In this work, the cytotoxicity of two cationic solid lipid nanoparticles (SLNs), differing in the cationic lipids used as surfactants CTAB (cetyltrimethylammonium bromide) or DDAB (dimethyldioctadecylammonium bromide), referred as CTAB-SLNs and DDAB-SLNs, respectively, was assessed against five different human cell lines (Caco-2, HepG2, MCF-7, SV-80, and Y-79). Results showed that the cationic lipids used in SLN production highly influenced the cytotoxic profile of the particles, with CTAB-SLNs being highly cytotoxic even at low concentrations (IC50 < 10 µg/mL, expressed as CTAB amount). DDAB-SLNs produced much lower cytotoxicity, even at longer exposure time (IC50 from 284.06 ± 17.01 µg/mL (SV-80) to 869.88 ± 62.45 µg/mL (MCF-7), at 48 h). To the best of our knowledge, this is the first report that compares the cytotoxic profile of CTAB-SLNs and DDAB-SLNs based on the concentration and time of exposure, using different cell lines. In conclusion, the choice of the right surfactant for biological applications influences the biocompatibility of the nanoparticles. Regardless the type of drug delivery system, not only the cytotoxicity of the drug-loaded nanoparticles should be assessed, but also the blank (non-loaded) nanoparticles as their surface properties play a decisive role both in vitro and in vivo.


2014 ◽  
Vol 24 (3) ◽  
pp. 171-181 ◽  
Author(s):  
Fengzhen Wang ◽  
Li Chen ◽  
Sunmin Jiang ◽  
Jun He ◽  
Xiumei Zhang ◽  
...  

2014 ◽  
Vol 1688 ◽  
Author(s):  
Min S. Wang ◽  
Amol Chaudhari ◽  
Yuanjie Pan ◽  
Stephen Young ◽  
Nitin Nitin

ABSTRACTThe goal of this study was to determine the potential use of starch Pickering emulsion as a vehicle to deliver a natural phenolic compound, curcumin in the oral cavity. To this end, an oil-in-water (o/w) emulsion was prepared using starch molecules as the stabilizer/emulsifier. The physical stability, oxygen permeability and release of curcumin from the starch Pickering emulsion in simulated saliva fluid (SSF) were determined. The results of this study showed that the starch stabilized o/w emulsions were stable for up to 2 weeks. The starch Pickering emulsion also provided better protection against oxidation than a surfactant-stabilized emulsion, and the digestion of the starch Pickering emulsion using amylase led to the complete disruption and phase separation of the emulsion.


2021 ◽  
Vol 12 ◽  
Author(s):  
Arindam K. Dey ◽  
Adrien Nougarède ◽  
Flora Clément ◽  
Carole Fournier ◽  
Evelyne Jouvin-Marche ◽  
...  

Nonviral systems, such as lipid nanoparticles, have emerged as reliable methods to enable nucleic acid intracellular delivery. The use of cationic lipids in various formulations of lipid nanoparticles enables the formation of complexes with nucleic acid cargo and facilitates their uptake by target cells. However, due to their small size and highly charged nature, these nanocarrier systems can interact in vivo with antigen-presenting cells (APCs), such as dendritic cells (DCs) and macrophages. As this might prove to be a safety concern for developing therapies based on lipid nanocarriers, we sought to understand how they could affect the physiology of APCs. In the present study, we investigate the cellular and metabolic response of primary macrophages or DCs exposed to the neutral or cationic variant of the same lipid nanoparticle formulation. We demonstrate that macrophages are the cells affected most significantly and that the cationic nanocarrier has a substantial impact on their physiology, depending on the positive surface charge. Our study provides a first model explaining the impact of charged lipid materials on immune cells and demonstrates that the primary adverse effects observed can be prevented by fine-tuning the load of nucleic acid cargo. Finally, we bring rationale to calibrate the nucleic acid load of cationic lipid nanocarriers depending on whether immunostimulation is desirable with the intended therapeutic application, for instance, gene delivery or messenger RNA vaccines.


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