Magnetic Solid Lipid Nanoparticles Research Articles

Development of a Radiolabeled Folate-Mediated Drug Delivery System for Effective Delivery of Docetaxel.

Many preclinical studies are carried out with the aim of developing new formulations for the effective delivery of taxane class drugs, one of the most important anticancer drugs used clinically today. In this study, a radiolabeled folate-mediated solid lipid magnetic nanoparticle (SLMNP) system was developed by loading superparamagnetic iron oxide nanoparticles (MNP) and docetaxel (DTX) into the solid lipid nanoparticles as a drug delivery system that will function both in cancer treatment and diagnosis. For this purpose, first, SLMNP was synthesized by the hot homogenization method, and the surface of the particles was modified with a folate derivative to carry the particles to tissues with folate receptors. The synthesized magnetic solid lipid nanoparticles were loaded with DTX, and then radiolabeling was carried out with technetium-99 m (99mTc-DTX-SLMNP). Structural characteristics of these nanoparticles were determined by characterization methods. According to the TEM images of MNPs, SLN, and SLMNPs, MNPs were observed between 25and 35 nm, SLNs between 400 and 500 nm, and SLMNPs between 350 and 450 nm. The drug entrapment efficiency of SLMNPs loaded with DTX was found to be 19%, and the percentage efficiency of radiolabeling was found to be 98.0 ± 2.0%. The biological behavior of this radiolabeled system was investigated in vitro and in vivo. Folate receptor-positive SKOV-3 and folate receptor-negative A549 cancer cell lines were studied. The IC50 values of DTX-SLMNP in SKOV-3 and A549 cells were 50.21 and 172.27 μM at 48 h, respectively. Gamma camera imaging studies of 99mTc-DTX-SLMNP and magnetically applied 99mTc-DTX-SLMNP compounds were performed on tumor-bearing CD-1 nude mice. The uptake in the folate receptor-positive tumor region was higher than that in the folate receptor negative tumor region. We proposed that the drug delivery system we prepared in this study be evaluated for preclinical studies of new drug carrier formulations of the taxane class of anticancer drugs.

Synthesis, radiolabeling and in vitro evaluation of azathioprine loaded magnetic solid lipid nanoparticles

Synthesis, radiolabeling and in vitro evaluation of azathioprine loaded magnetic solid lipid nanoparticles

Magnetic Solid Nanoparticles and Their Counterparts: Recent Advances towards Cancer Theranostics.

Cancer is currently a leading cause of death worldwide. The World Health Organization estimates an increase of 60% in the global cancer incidence in the next two decades. The inefficiency of the currently available therapies has prompted an urgent effort to develop new strategies that enable early diagnosis and improve response to treatment. Nanomedicine formulations can improve the pharmacokinetics and pharmacodynamics of conventional therapies and result in optimized cancer treatments. In particular, theranostic formulations aim at addressing the high heterogeneity of tumors and metastases by integrating imaging properties that enable a non-invasive and quantitative assessment of tumor targeting efficiency, drug delivery, and eventually the monitoring of the response to treatment. However, in order to exploit their full potential, the promising results observed in preclinical stages need to achieve clinical translation. Despite the significant number of available functionalization strategies, targeting efficiency is currently one of the major limitations of advanced nanomedicines in the oncology area, highlighting the need for more efficient nanoformulation designs that provide them with selectivity for precise cancer types and tumoral tissue. Under this current need, this review provides an overview of the strategies currently applied in the cancer theranostics field using magnetic nanoparticles (MNPs) and solid lipid nanoparticles (SLNs), where both nanocarriers have recently entered the clinical trials stage. The integration of these formulations into magnetic solid lipid nanoparticles—with different composition and phenotypic activity—constitutes a new generation of theranostic nanomedicines with great potential for the selective, controlled, and safe delivery of chemotherapy.

Preparation and Characterization of Magnetic Solid Lipid Nanoparticles as a Targeted Drug Delivery System for Doxorubicin.

Purpose: In the present study, we investigated the magnetic solid lipid nanoparticles (mSLNs) for targeted delivery of doxorubicin (DOX) into breast cancer cells. Methods: The synthesis of iron oxide nanoparticles was carried out by co-precipitation of a ferrous and ferric aqueous solution with the addition of a base; moreover, during precipitation process, the magnetite nanoparticles should be coated with stearic acid (SA) and tripalmitin (TPG). An emulsification dispersion-ultrasonic method was employed to prepare DOX loaded mSLNs. Fourier transforms infrared spectroscopy, vibrating sample magnetometer, and photon correlation spectroscopy (PCS) were used to characterize the subsequently prepared nanoparticles. In addition, the antitumor efficacy of particles was evaluated on MCF-7 cancer cell lines. Results: The findings showed that entrapment efficiency values for solid lipid and magnetic SLNs were 87±4.5% and 53.7±3.5%, respectively. PCS investigations showed that particle size increased with magnetic loading in the prepared NPs. In vitro drug release of DOX-loaded SLN and DOX-loaded mSLN in phosphate buffer saline (pH=7.4) showed that the amount of drug released approached 60% and 80%, respectively after 96 h of incubation. The electrostatic interactions between magnetite and drug had little effect on the release characteristics of the drug. The higher toxicity of DOX as nanoparticles compared to free drug was inferred from in vitro cytotoxicity. Conclusion: DOX encapsulated magnetic SLNs can act as a suitable and promising candidate for controlled and targeted therapy for cancer.

Formulation and Evaluation of Leflunomide Loaded Magnetic Solid-Lipid Nanoparticles for The Targeted Therapy of Breast Cancer

Formulation and Evaluation of Leflunomide Loaded Magnetic Solid-Lipid Nanoparticles for The Targeted Therapy of Breast Cancer

Chitosan-coated magnetic solid lipid nanoparticles for controlled release of letrozole

In present study, magnetic solid lipid nanoparticles (MSLNs) with chitosan (CHI) coating were defined, and the rapid delivery of Letrozole (LTZ) to cancer cells by both active and passive targeting were evaluated. LTZ loaded MSLNs were fabricated using the modified solvent evaporation-ultrasonic combination method. The physicochemical parameters were optimized to achieve a suitable drug delivery system. Afterward Fourier transform infrared spectroscopy (FTIR), differential scanning calorimeter (DSC) and X-ray diffraction (XRD) used as characteristic analyses. DPPH free radical scavenging test was carried out to evaluate the antioxidant capacities of LEC (Lecithin), MSLNs, LTZ, LTZ + MSLNs, and BHT (Butylated hydroxytoluene). DPPH test indicated similar antioxidant activities for LTZ + MSLNs and BHT. For the determining of anti-breast cancer potentials of LEC, MNPs, LTZ, and LTZ + MSLNs, MTT assay was used on the normal cell line (HUVEC), breast adenocarcinoma (MCF7), breast carcinoma (Hs 578Bst), infiltrating ductal cell carcinoma (Hs 319.T), infiltrating lobular carcinoma of breast (UACC-3133), inflammatory carcinoma of the breast (UACC-732), and metastatic carcinoma (MDA-MB-453) cell lines. The desired and favorable particle size and surface charge nanocarrier for targeting cancer cells was obtained. The effect of LFPMF on drug release of the drug delivery system distinctly demonstrated. The findings showed that MSLN loaded with LTZ increased chemotherapy efficiency. LTZ encapsulated MSLN can act as a suitable and promising candidate for targeted and controlled therapy for cancer.

Nutlin-loaded magnetic solid lipid nanoparticles for targeted glioblastoma treatment.

AimGlioblastoma multiforme is one of the deadliest forms of cancer, and current treatments are limited to palliative cares. The present study proposes a nanotechnology-based solution able to improve both drug efficacy and its delivery efficiency.Materials & methodsNutlin-3a and superparamagnetic nanoparticles were encapsulated in solid lipid nanoparticles, and the obtained nanovectors (nutlin-loaded magnetic solid lipid nanoparticle [Nut-Mag-SLNs]) were characterized by analyzing both their physicochemical properties and their effects on U-87 MG glioblastoma cells.ResultsNut-Mag-SLNs showed good colloidal stability, the ability to cross an in vitro blood–brain barrier model, and a superior pro-apoptotic activity toward glioblastoma cells with respect to the free drug.ConclusionNut-Mag-SLNs represent a promising multifunctional nanoplatform for the treatment of glioblastoma multiforme.

Triggered release of paclitaxel from magnetic solid lipid nanoparticles by magnetic hyperthermia

We developed a magnetic solid lipid nanoparticles formulation of paclitaxel (PTX-loaded MSLNs) via emulsification-diffusion method. The physicochemical characterization of PTX-loaded MSLNs was performed by AFM, DLS, determination of entrapment efficiency (EE) and drug loading (DL), DSC, VSM, and physical stability. The in vitro effect of temperature and pulsed magnetic hyperthermia on drug release were studied. PTX-loaded MSLNs had a particle diameter around 250 nm with a narrow size distribution, spherical morphology, EE of 67.3 ± 1.2% and a DL of 17.1 ± 0.4 μg/mg. A decrease of the melting point of the lipid was observed following the preparation of the MSLNs. A threefold increase in the in vitro drug release rate was seen when temperature was raised from 25 to 43 °C. The lipid coating of MPs confer a temperature-dependent drug release and magnetic hyperthermia was used to trigger controlled PTX release from MSLNs.

Magnetic solid lipid nanoparticles co-loaded with albendazole as an anti-parasitic drug: Sonochemical preparation, characterization, and in vitro drug release

The magnetic nanoparticles (MNPs) are applied as carriers for the efficient delivery of albendazole (ABZ) following its full characterization in terms of structure, morphology, size, and surface characteristics. The best composition and tunable properties for the achievement of more drug loading, controlled drug release, and delivery were optimized. A potential platform for anti-parasitic drug delivery was observed by uniform magnetic solid lipid NPs (MSLNPs) core/shell structure multifunctional mesoporous nano-capsules, which was composed of inorganic (Fe3O4) NPs as the core and stearic acid as the shell. This solid lipid NPs (SLNPs) and MSLNPs were identified and recognized by energy dispersive X-ray spectroscopy (EDX), X-ray diffraction (XRD), field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), vibrating sample magnetometer (VSM), Fourier-transform infrared spectroscopy (FTIR), and Dynamic light scattering (DLS) analyzer, which accordingly denote spherical particle morphology. The average particle sizes of SLNPs and MSLNPs were between 20 and 120 nm, depending on ultrasound irradiation, reagents concentration, and their order of addition. The ultrasound-prepared MSLNPs were homogeneously distributed with spherical shape and little agglomeration on SLNPs surface. Our in vitro release study demonstrated that 84.0% of ABZ was gradually released within 36 h. Moreover, in comparison to other strategies, the synthesis procedure presented here is more rapid and environment friendly and possesses high efficiency for ABZ delivery.

Magnetic solid lipid nanoparticles in hyperthermia against colon cancer

A reproducible double emulsion/solvent evaporation procedure is developed to formulate magnetic solid lipid nanoparticles (average size≈180nm) made of iron oxide cores embedded within a glyceryl trimyristate solid matrix. The physicochemical characterization of the nanocomposites ascertained the efficacy of the preparation conditions in their production, i.e. surface properties (electrokinetic and thermodynamic data) were almost indistinguishable from those of the solid lipid nanomatrix, while electron microscopy characterizations and X-ray diffraction patterns confirmed the satisfactory coverage of the magnetite nuclei. Hemocompatibility of the particles was established in vitro. Hysteresis cycle determinations defined the appropriate magnetic responsiveness of the nanocomposites, and their heating characteristics were investigated in a high frequency alternating gradient of magnetic field: a constant maximum temperature of 46°C was obtained within 40min. Finally, in vitro tests performed on human HT29 colon adenocarcinoma cells demonstrated a promising decrease in cell viability after treatment with the nanocomposites and exposure to that alternating electromagnetic field. To the best of our knowledge, this is the first time that such type of nanoformulation with very promising hyperthermia characteristics has been developed for therapeutic aims.

Drug Targeting: Active Targeting of Sorafenib: Preparation, Characterization, and In Vitro Testing of Drug‐Loaded Magnetic Solid Lipid Nanoparticles (Adv. Healthcare Mater. 11/2015)

Drug Targeting: Active Targeting of Sorafenib: Preparation, Characterization, and In Vitro Testing of Drug‐Loaded Magnetic Solid Lipid Nanoparticles (Adv. Healthcare Mater. 11/2015)

Active Targeting of Sorafenib: Preparation, Characterization, and In Vitro Testing of Drug-Loaded Magnetic Solid Lipid Nanoparticles.

Sorafenib is an anticancer drug approved by the Food and Drug Administration for the treatment of hepatocellular and advanced renal carcinoma. The clinical application of sorafenib is promising, yet limited by its severe toxic side effects. The aim of this study is to develop sorafenib-loaded magnetic nanovectors able to enhance the drug delivery to the disease site with the help of a remote magnetic field, thus enabling cancer treatment while limiting negative effects on healthy tissues. Sorafenib and superparamagnetic iron oxide nanoparticles are encapsulated in solid lipid nanoparticles by a hot homogenization technique using cetyl palmitate as lipid matrix. The obtained nanoparticles (Sor-Mag-SLNs) have a sorafenib loading efficiency of about 90% and are found to be very stable in an aqueous environment. Plain Mag-SLNs exhibit good cytocompatibility, whereas an antiproliferative effect against tumor cells (human hepatocarcinoma HepG2) is observed for drug-loaded Sor-Mag-SLNs. The obtained results show that it is possible to prepare stable Sor-Mag-SLNs able to inhibit cancer cell proliferation through the sorafenib cytotoxic action, and to enhance/localize this effect in a desired area thanks to a magnetically driven accumulation of the drug. Moreover, the relaxivity properties observed in water suspensions hold promise for Sor-Mag-SLN tracking through clinical magnetic resonance imaging.

Preparation and characterization of cisplatin magnetic solid lipid nanoparticles (MSLNs): effects of loading procedures of Fe3O4 nanoparticles.

In order to improve formulation of targeting chemotherapy, cisplatin-loaded magnetic solid lipid nanoparticles (MSLNs) were prepared. In present study, the deliberate loading of Fe3O4 magnetic nanoparticles (MNs) into cisplatin SLNs was developed. SLNs were produced by film scattering ultrasonic technique. The effects of two different loading procedures of MNs on the microstructure and physicochemical properties of MSLNs were investigated by transmission electron microscopy (TEM), zetasizer, infrared spectroscopy (IR), and fluorescence spectroscopy. In vitro drug release and cytotoxicity against human cervical carcinoma SiHa cells, in vivo tumor cell uptake and target tissue distribution of MSLNs under external magnetic field were investigated. The encapsulation efficiency of cisplatin and the content of MNs in procedure I SLNs were 69.20 ± 4.5% and 2.16 ± 0.53 mg/mL, respectively, which were higher than those of procedure II MSLNs. In procedure I, the MNs, which were combined with lipids during film formation, distributed in the middle of the lipid layer in SLNs. Differently, in procedure II, the MNs and cisplatin were contained in an interior compartment in SLNs, resulting from mixing with drugs during hydration of lipid film. The procedure I MSLNs had higher cytotoxicity than procedure II MSLNs or free cisplatin. With in vivo intratumoral administration, cisplatin concentration in the tumor tissue was maintained at higher level for MSLNs than that for free cisplatin, especially under external magnetic field. Procedure I, the developed deliberate MNs loading method, was superior over procedure II in cisplatin encapsulation efficiency, MNs content and cell cytotoxicity.

Synthesis of Ibuprofen Loaded Magnetic Solid Lipid Nanoparticles

Ibuprofen loaded magnetic solid lipid nanoparticles (Ib-MSLNs) were successfully fabricated using a two-step method: 1)preparation of a warm O/W microemulsion (aqueous surfactant solution with a lipid phase, containing Ibuprofen, stearic acid, 1-octadecanol and lecithin) in which modified lipophilic magnetite (Fe <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">3</sub> O <sub xmlns:mml="http://www.w3.org/1998/Math/MathML" xmlns:xlink="http://www.w3.org/1999/xlink">4</sub> ) nanoparticles were incorporated, and 2)formation of MSLNs by dispersing the warm microemulsion in cold water under mechanical stirring. The Ib-MSLNs were characterized by transmission electron microscopy, X-ray powder diffraction (XRD), and superconducting quantum interference device (SQUID) magnetometer. TEM and XRD results showed that SLN nanoparticles embedded with magnetic nanoparticles was successfully formed. SQUID measurements indicated that Ib-MSLN exhibited superparamagnetic behavior with a blocking temperature of 98 K. The encapsulation efficiency was measured by high pressure liquid chromatography (HPLC). The magnetite-loaded solid lipid nanoparticles can be potentially used in drug targeting and controlled releasing.