Preparation and Physicochemical Characterization of Biodegradable mPEG-PCL Core-Shell Micelles for Delivery of Artemisinin

Manjili, Hamid Reza Kheiri; Malvandi, Hojjat; Mosavi, M.; Danafar, Hossein

doi:10.15171/ps.2016.37

Cited by 24 publications

(10 citation statements)

References 27 publications

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“…Numerous drug delivery systems including PCL-PEG-PCL micelles (17), biodegradable mPEG-PCL core-shell micelles (18), nanoliposomes (19), chitosan, gelatin, and alginate nanocapsules (20), pegylated nanoliposome (21), and ordered mesoporous SBA-15 particles (22), have been so far studied and evaluated to improve solubility, bioavailability or stability of ART for its parenteral delivery into cancer cells. Nevertheless, none of these delivery systems is designed to selectively promote ART transport and its delivery to the brain tumors via blood brain barrier.…”

Section: Introductionmentioning

confidence: 99%

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

2018

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In the present study, a transferrin-conjugated nanostructured lipid carrier (TF-NLCs) for brain delivery of artemisinin (ART) was developed. ART-loaded NLCs (ART-NLCs) were prepared using solvent evaporation method and the impact of various formulation or process variables on the responses were assessed using a Taguchi design. Optimized ART-NLC was then coupled with transferrin as targeting ligand and its in vitro cytotoxicity was investigated against U-87MG brain cancer cell line. As a result, the following values are suggested by the software to prepare the optimized formulation: 20 mg Compritol®, 0.25% Tween 80, 5 mg oleic acid, 2.5 mL dichloromethane and 4 min sonication. Mean particle size (PS), zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), mean release time (MRT) of adopted formulation were confirmed to be 145 ± 12.5 nm, 24.3 ± 1.5 mV, 0.513 ± 0.021, 82.3 ± 7.3 % and 24.0 ± 1.1 h, respectively. Following conjugation of optimized ART-NLCs with TF, PS and MRT were increased, while ZP, and EE were decreased significantly. TF-ART-NLCs showed higher cytotoxic activity compared to non-targeted NLCs and free drug. These results indicated that the TF-ART-NLCs could potentially be exploited as a delivery system for anticancer and antimalarial drug ART in brain tumors and malaria.

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Section: Introductionmentioning

confidence: 99%

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

2018

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“…Impressively, the prepared AHZ nanoprodrug showed a significantly increased drug loading capacity (69.6 wt %, nearly reaching the limit calculated from the molecular structure) compared to the conventional ART encapsulated nanodrugs (usually less than 40 wt %, Table S2). − ,− …”

Section: Resultsmentioning

confidence: 99%

Bioinspired Microenvironment Responsive Nanoprodrug as an Efficient Hydrophobic Drug Self-Delivery System for Cancer Therapy

et al. 2021

ACS Appl. Mater. Interfaces

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Artemisinin compounds have shown satisfactory safety records in anti-malarial clinical practice over decades and have revealed value as inexpensive anti-tumor adjuvant chemotherapeutic drugs. However, the rational design and precise preparation of nanomedicines based on the artemisinin drugs are still limited due to their non-aromatic and fragile chemical structure. Herein, a bioinspired coordination-driven self-assembly strategy was developed to manufacture the artemisinin-based nanoprodrug with a significantly increased drug loading efficacy (∼70 wt %) and decreased preparation complexity compared to conventional nanodrugs. The nanoprodrug has suitable size distribution and robust colloidal stability for cancer targeting in vivo. The nanoprodrug was able to quickly disassemble in the tumor microenvironment with weak acidity and a high glutathione concentration, which guarantees a better tumor inhibitory effect than direct administration and fewer side effects on normal tissues in vivo. This work highlights a new strategy to harness a robust, simplified, organic solvent-free, and highly repeatable route for nanoprodrug manufacturing, which may offer opportunities to develop cost-effective, safe, and clinically available nanomedicines.

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“…Diblock copolymers composed of hydrophilic and hydrophobic blocks with variable lengths can encapsulate hydrophobic drugs in the core of the nanomicelle and/or attach hydrophilic drugs on the surface in the aqueous medium (25). Some common polymers used in the composition of nanomicelles are poly(ethylene glycol) (PEG) (26), N-(2-hydroxypropyl) methacrylamide (HPMA) (27), poly(l-lactic acid) (PLA) (28), poly(lactic-co-glycolic acid) (PLGA) (29), polycaprolactone (PCL) (30), and chi-tosan (31,32). Most polymeric nanomicelles investigated for drug delivery applications have been used successfully in cancer.…”

Section: Contextmentioning

confidence: 99%

A Brief Review on Advantages of Nano-based Drug Delivery Systems

Hami

2021

Ann Mil Health Sci Res

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Context: During the past two decades, the development of drug delivery systems based on nanomaterials has yielded nanocarriers for smart application in nanomedicine to treat diseases. Evidence Acquisition: The current review presents a summary of some advances in the development and application of nano-delivery systems for improving the efficacy of conventional drugs and reducing their adverse effects through the production of smart delivery carriers with targeting moieties and controlled release strategies used in therapy. The searches were conducted in ScienceDirect, Scopus, Google Scholar, and PubMed databases for relevant studies. Results: As reviewed in the present paper, the investigated targeted drug delivery systems have proven to be more effective than free drugs by enhancing efficacy and reducing the systemic toxicity of therapy. In addition, many studies have shown remarkable advantages of nanoscale drug delivery carriers regarding the possibility to improve properties such as solubility, stability, absorption, diffusivity, bioavailability, targeting, and controlled release of drugs. Conclusions: Despite many advantages of nanoscale drug delivery systems reported in the medical literature, deeper research about the composition, synthesis, characteristics, and clinical applications in this area is needed.

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Preparation and Physicochemical Characterization of Biodegradable mPEG-PCL Core-Shell Micelles for Delivery of Artemisinin

Cited by 24 publications

References 27 publications

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

Targeted Nanostructured Lipid Carrier for Brain Delivery of Artemisinin: Design, Preparation, Characterization, Optimization and Cell Toxicity

Bioinspired Microenvironment Responsive Nanoprodrug as an Efficient Hydrophobic Drug Self-Delivery System for Cancer Therapy

A Brief Review on Advantages of Nano-based Drug Delivery Systems

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