Developing Actively Targeted Nanoparticles to Fight Cancer: Focus on Italian Research

Active targeting is a valuable and promising approach with which to enhance the therapeutic efficacy of nanodelivery systems, and the development of tumor-targeted nanoparticles has therefore attracted much research attention. In this field, the research carried out in Italian Pharmaceutical Technology academic groups has been focused on the development of actively targeted nanosystems using a multidisciplinary approach. To highlight these efforts, this review reports a thorough description of the last 10 years of Italian research results on the development of actively targeted nanoparticles to direct drugs towards different receptors that are overexpressed on cancer cells or in the tumor microenvironment. In particular, the review discusses polymeric nanocarriers, liposomes, lipoplexes, niosomes, solid lipid nanoparticles, squalene nanoassemblies and nanobubbles. For each nanocarrier, the main ligands, conjugation strategies and target receptors are described. The literature indicates that polymeric nanoparticles and liposomes stand out as key tools for improving specific drug delivery to the site of action. In addition, solid lipid nanoparticles, squalene nanoparticles and nanobubbles have also been successfully proposed. Taken together, these strategies all offer many platforms for the design of nanocarriers that are suitable for future clinical translation.

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Factorial Design Studies and Biopharmaceutical Evaluation of Simvastatin Loaded Solid Lipid Nanoparticles for Improving the Oral Bioavailability

ISRN Nanotechnology ◽

10.1155/2014/951016 ◽

2014 ◽

Vol 2014 ◽

pp. 1-8 ◽

Cited By ~ 10

Author(s):

Kovoru Krishnam Raju ◽

Beeravelli Sudhakar ◽

Kolapalli Venkata Ramana Murthy

Keyword(s):

Solid Lipid Nanoparticles ◽

Oral Bioavailability ◽

Competitive Inhibition ◽

Polymeric Nanoparticles ◽

Analytical Techniques ◽

Lipid Nanoparticles ◽

Lymphatic Transport ◽

Solid Lipid ◽

Reductase Inhibitors ◽

Coa Reductase

Statins are HMG-CoA reductase inhibitors, which lower the cholesterol level through reversible and competitive inhibition; they are involved in the biosynthesis of cholesterol and other sterols. Simvastatin exhibits poor oral bioavailability (<5%) and undergoes extensive microsomal metabolism by CYP enzymes. CYP3A4 is the major metabolizing enzyme that metabolizes lactone form of simvastatin and significantly lowers intestinal uptake. The hydrophobic properties of simvastatin prevent complete dissolution of the drug in the intestinal fluid which also contributes to its lower bioavailability. SLNs are alternative carrier system to polymeric nanoparticles. SLNs are in submicron size range (1–1000 nm). To overcome the hepatic first pass metabolism and to enhance the bioavailability, intestinal lymphatic transport of drugs can be exploited. In the present study, attempt has been made to prepare solid lipid nanoparticles of simvastatin to improve the bioavailability. SLNs of simvastatin were prepared with Trimyristin by hot homogenization followed by ultrasonication method. The SLNs were characterized for various physicochemical properties and analytical techniques like PXRD, DSC to study thermal nature and morphology of formulation and excipients. Promising results of the study indicated the applicability of simvastatin solid lipid nanoparticles as potential tools for improvement of bioavailability of poorly soluble drugs.

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Formulation of Nanostructured lipid particles

Asian Pacific Journal of Nursing and Health Sciences ◽

10.46811/apjnh/3.2.4 ◽

2020 ◽

Vol 3 (2) ◽

pp. 20-24

Author(s):

Kavita Rani ◽

Amit Kumar J. Raval ◽

Dinesh Kaushik ◽

Rajesh Khathuriya

Keyword(s):

Drug Delivery ◽

Solid Lipid Nanoparticles ◽

Second Generation ◽

Polymeric Nanoparticles ◽

Lipid Nanoparticles ◽

Therapeutic Approaches ◽

Solid Lipid ◽

Lipid Particles ◽

Lipid Nanocarriers ◽

Lipid Formulations

Lipid nanocarriers are developed as an alternative to polymeric nanoparticles, liposomes and emulsions. NLCs are the second generation lipid carriers developed to overcome problems associated with Solid Lipid Nanoparticles and are utilized in various therapeutic approaches. NLCs were used for the delivery of lipophilic drugs .Biocompatible nature of lipids is responsible for its development as a good drug delivery. It was found to be having excellent characteristics over other lipid formulations.

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Nanostructured lipid carriers, solid lipid nanoparticles, and polymeric nanoparticles: which kind of drug delivery system is better for glioblastoma chemotherapy?

Drug Delivery ◽

10.1080/10717544.2016.1189465 ◽

2016 ◽

Vol 23 (9) ◽

pp. 3408-3416 ◽

Cited By ~ 31

Author(s):

Jie Qu ◽

Liangqiao Zhang ◽

Zhihua Chen ◽

Guohua Mao ◽

Ziyun Gao ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Solid Lipid Nanoparticles ◽

Polymeric Nanoparticles ◽

Lipid Nanoparticles ◽

Nanostructured Lipid Carriers ◽

Solid Lipid

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Polysorbate 80 Coated Solid Lipid Nanoparticles for the Delivery of Temozolomide Into the Brain

The Open Pharmacology Journal ◽

10.2174/1874143601808010021 ◽

2018 ◽

Vol 8 (1) ◽

pp. 21-28

Author(s):

Pawan Yadav ◽

Goutam Rath ◽

Gazal Sharma ◽

Ranjit Singh ◽

Amit Kumar Goyal

Keyword(s):

Solid Lipid Nanoparticles ◽

Animal Studies ◽

Polymeric Nanoparticles ◽

Lipid Nanoparticles ◽

Polysorbate 80 ◽

Angiogenic Therapy ◽

Solid Lipid ◽

Apoptotic Activity ◽

The Brain ◽

Patient Survival Rate

Introduction:Anti-angiogenic therapy can produce transient regression in tumor in case of Glioblastoma (GBM); however, no prolongation of patient survival rate had so far been achieved.Methodology:To address this problem, an effort was made to design and characterize a temozolomide loaded nanosystem for targeting the tumor vasculature in the brain using polymeric nanoparticles. It included the formation of Temozolomide (TMZ) loaded Solid-Lipid Nanoparticles (SLNs) and their conjugation with polysorbate-80 (P-80) which enhanced the penetration of drug to blood-brain barrier resulting in the enhancement of pro-apoptotic activity.Results:Conjugating nanoparticles with a tumor-penetrating polymer (P-80) further enhanced the therapeutic efficacy of the drug.Conclusion:The animal studies indicated the enhanced potential of the developed system in the effective treatment of glioblastoma.

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Solid Lipid Nanoparticles: Emerging Colloidal Nano Drug Delivery Systems

Pharmaceutics ◽

10.3390/pharmaceutics10040191 ◽

2018 ◽

Vol 10 (4) ◽

pp. 191 ◽

Cited By ~ 71

Author(s):

Vijay Mishra ◽

Kuldeep Bansal ◽

Asit Verma ◽

Nishika Yadav ◽

Sourav Thakur ◽

...

Keyword(s):

Drug Delivery ◽

Solid Lipid Nanoparticles ◽

Drug Delivery Systems ◽

Polymeric Nanoparticles ◽

Lipid Nanoparticles ◽

Delivery Systems ◽

Routes Of Administration ◽

Size Dependent ◽

Solid Lipid ◽

Nano Drug Delivery

Solid lipid nanoparticles (SLNs) are nanocarriers developed as substitute colloidal drug delivery systems parallel to liposomes, lipid emulsions, polymeric nanoparticles, and so forth. Owing to their unique size dependent properties and ability to incorporate drugs, SLNs present an opportunity to build up new therapeutic prototypes for drug delivery and targeting. SLNs hold great potential for attaining the goal of targeted and controlled drug delivery, which currently draws the interest of researchers worldwide. The present review sheds light on different aspects of SLNs including fabrication and characterization techniques, formulation variables, routes of administration, surface modifications, toxicity, and biomedical applications.

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Evaluating Cytotoxicity of Hyaluronate Targeted Solid Lipid Nanoparticles of Etoposide on SK-OV-3 Cells

Journal of Drug Delivery ◽

10.1155/2014/746325 ◽

2014 ◽

Vol 2014 ◽

pp. 1-7 ◽

Cited By ~ 5

Author(s):

Parviz Mohammadi Ghalaei ◽

Jaleh Varshosaz ◽

Hojatollah Sadeghi Aliabadi

Keyword(s):

Ovarian Carcinoma ◽

Solid Lipid Nanoparticles ◽

Sodium Hyaluronate ◽

Lipid Nanoparticles ◽

Free Drug ◽

Epithelial Ovarian Carcinoma ◽

Assay Method ◽

Sodium Fluorescein ◽

Targeted Nanoparticles ◽

Solid Lipid

The epithelial ovarian carcinoma is one of the most fatal gynecological cancers. Etoposide is used in treating platinum-resistant ovarian cancer. Sodium hyaluronate is a substance that binds to the CD44 receptors overexpressed in SK-OV-3 cells of epithelial ovarian carcinoma. The aim of the present work was to study the cytotoxicity effect of hyaluronate targeted solid lipid nanoparticles (SLNs) of etoposide on SK-OV-3 cells. The cytotoxicity of the targeted and nontargeted SLNs of etoposide was compared to free drug on the SK-OV-3 cells by MTT assay method. The cellular uptake of the targeted and nontargeted nanoparticles containing sodium fluorescein was also studied. The difference of cell vitality between nontargeted nanoparticles and also targeted nanoparticles with free drug was significant. Targeted nanoparticles also caused more toxicity than nontargeted nanoparticles (P<0.05). After 4 hours of incubating, the fluorescence was remarkably higher in the cells treated by targeted SLNs rather than nontargeted ones, and there was no observable fluorescence in cells incubated with pure sodium fluorescein. Hyaluronate targeted SLNs containing etoposide increased the cytotoxicity of etoposide on SK-OV-3 cells which may be a worthwhile potential method for reducing the prescribed dose and systemic side effects of this drug in epithelial ovarian carcinoma.

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