Physicochemical characterization techniques for solid lipid nanoparticles: principles and limitations

Kathe, Niranjan; Henriksen, Brian; Chauhan, Harsh

doi:10.3109/03639045.2014.909840

Cited by 103 publications

(56 citation statements)

References 116 publications

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“…1990'lı yıllarda mevcut kolloidal taşıyıcı sistemlere (emülsiyonlar, lipozomlar, polimerik nanopartiküller) alternatif bir taşıyıcı sistem olarak ortaya çıkan katı lipit nanopartiküller, fizyolojik lipitlerden oluştuğu için oldukça yüksek biyouyumluluk ve biyobozunurluk buna karşılık düşük sistemik toksisite ve düşük sitotoksisite gösterirler. Organik çözücü kalıntısı içermemesi, geniş ölçekte üretimlerinin mümkün olması, kolay hazırlanma süreci, fiziksel kararlılığı, kararsız ilaçları kimyasal degradasyona karşı koruması ve ilacın kontrollü olarak salınması gibi avantajlara sahip olduğu için KLN'lere olan ilgi gün geçtikçe artmaktadır (Rai et al, 2008;Andreozzi et al, 2011;Kathe et al, 2014). Bu sistemlerin radyofarmasi alanına taşınması ise yeni teşhis ve tedavi yöntemlerinin geliştirilmesinde umut verici bir ışık olarak görünmektedir.…”

Section: şEkil 1 Kurkuminin Kimyasal Yapısıunclassified

The Role of Curcumin-Loaded Solid Lipid Nanoparticles Labeled with Tc-99m in the Liver-Spleen Scintigraphy

Yenilmez¹,

Ayan²,

Gündoğdu³

et al. 2016

jist

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ÖZET: Son zamanlarda, hastalıkların tanı ve tavisini kolaylaştırmak amacıyla, nanoteknoloji ve moleküler görüntüleme alanları, çok fonksiyonlu nanopartiküllerin oluşturulması ile birleştirilmiştir. Nanopartiküllerden oluşturulan yeni nesil görüntüleme ajanlarının sahip olduğu çok yönlü ve eşsiz özelliklerinden faydalanan alanlardan biriside nükleer tıp alanıdır. Yapılan bu çalışmada; kurkumin yüklü katı lipit nanopartiküllerin (K-KLN) karaciğer ve dalak sintigrafisinde kullanılabilirliliği araştırıldı. Öncelikle, kurkumin yüklü katı lipit nanopartiküller (K-KLN) mikroemülsiyon ve düşük-sıcaklıkda katılaştırma yöntemiyle hazırlandı. Lazer kırınımı (LD) analizi ile partikül boyutu belirlendi. Termogravimetrik analizi (TGA) ile K-KLN'lerin sıcaklığa karşı stabil olduğu gözlemlendi. Daha sonra K-KLN'ler Teknesyum-99m ( 99m Tc) ile radyoaktif olarak işaretlendi. İnce katman kromatografi yöntemi ile radyoaktif işaretleme etkinliği %95'den daha fazla olarak bulundu. ABSTRACT:Recently, nanotechnology and molecular imaging fields are integrated to facilitate the diagnosis and the treatment of diseases with create multi-functional nanoparticles. Nuclear medicine is one of the fields that benefit from the multi-faceted and unique characteristics of new generation imaging agents that are made of nanoparticles. This study investigated the feasibility of using curcumin-loaded SLNs in liver and spleen scintigraphy. Initially, the curcumin-loaded solid lipid nanoparticles (C-SLN) were prepared using microemulsion and solidification at low temperatures. The size of the C-SLN particle is measured by Laser diffraction (LD) method. Moreover, by applying thermogravimetric analysis (TGA) it is observed that C-SLN particles are stable with temperature variation. Then, they are radiolabeled with Technetium-99m ( 99m Tc). Using the thin-layer chromatography method, the radiolabeling efficiency was found to be higher than 95%. Tc-C-SLNs were injected to the rabbit intravenously (i.v.) and using a gamma camera, dynamic images were recorded. Liver and spleen were clearly displayed in these dynamic images. In addition to scintigraphic findings, the presence of 99m Tc-C-SLNs in the liver and the spleen was observed in the ex vivo biodistribution studies and the analyses performed under the fluorescence microscope.

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Section: şEkil 1 Kurkuminin Kimyasal Yapısıunclassified

The Role of Curcumin-Loaded Solid Lipid Nanoparticles Labeled with Tc-99m in the Liver-Spleen Scintigraphy

Yenilmez¹,

Ayan²,

Gündoğdu³

et al. 2016

jist

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“…The results showed that blank SLNs exhibited no significant toxicity up to 50 µM of equivalent doses of EA. That is why SLNs are introduced as a biocompatible drug delivery carrier (20).…”

Section: Cytotoxic Effects Of Ea and Ea-loaded Slnsmentioning

confidence: 99%

Enhanced Anti-Cancer Capability of Ellagic Acid Using Solid Lipid Nanoparticles (SLNs)

et al. 2018

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Background: Ellagic acid (EA) is a polyphenol, whose anti-cancer properties have been demonstrated in several cancer studies, but the poor water solubility and low bioavailability have limited its therapeutic potential. Objectives: The present study proposed to develop solid lipid nanoparticles (SLNs) as a delivery system for improving the anticancer capability of EA on prostate cancer cell line. Methods: EA-loaded SLNs were prepared by hot homogenization technique and characterized by different techniques. Cytotoxicity of EA and EA-loaded SLNs on prostate cancer cell line (PC3) was evaluated by 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay, and nucleus condensation, or chromatin fragmentation (the signs of apoptosis) were studied by 4'-6-diamidino-2-phenylindole (DAPI) staining. The expression of B-cell lymphoma 2 (Bcl-2) and Bcl-2-associated X protein (Bax), which are involved in apoptosis, were evaluated by quantitative reverse transcription polymerase chain reaction (qRT-PCR). Results:The nanoparticles with appropriate characteristics (particle size of 96 nm and Encapsulation Efficiency of 88%) were prepared. The in vitro drug release profile showed a burst release in the first hours and followed by a sustained EA release until 72 hours. EA-loaded SLNs displayed a good stability for 4 weeks of storage at 4 -8°C. Cytotoxicity evaluations demonstrated that EA-loaded SLNs prevented prostate cancer cells growth in a low IC50 value compared to the EA. The results of qRT-PCR demonstrated that EA causes up-regulation of Bax and this regulation intensified when EA was loaded into SLNs, but there was no punctual correlation between the EA and EA-loaded SLNs in down-regulation of Bcl-2. Conclusions:The results strengthen our hope that loading EA into SLNs could possibly overcome the therapeutic limitations of EA and make it more effective in prostate cancer therapy.

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“…Furthermore, solid lipid nanoparticles have low drug encapsulation and sophisticated techniques are required for their preparation. 10 Hence, other drug delivery systems are required to ameliorate these obstacles and to improve the anticancer efficacy of AE.…”

Section: Introductionmentioning

confidence: 99%

Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies

Freag¹,

Elnaggar²,

Abdelmonsif³

et al. 2016

IJN

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Recently, research has progressively highlighted on clues from conventional use of herbal medicines to introduce new anticancer drugs. Aloe-emodin (AE) is a herbal drug with promising anticancer activity. Nevertheless, its clinical utility is handicapped by its low solubility. For the first time, this study aims to the fabrication of surface-functionalized polyethylene glycol liquid crystalline nanoparticles (PEG-LCNPs) of AE to enhance its water solubility and enable its anticancer use. Developed AE-PEG-LCNPs were optimized via particle size and zeta potential measurements. Phase behavior, solid state characteristics, hemocompatibility, and serum stability of LCNPs were assessed. Sterile formulations were developed using various sterilization technologies. Furthermore, the potential of the formulations was investigated using cell culture, pharmacokinetics, biodistribution, and toxicity studies. AE-PEG-LCNPs showed particle size of 190 nm and zeta potential of −49.9, and PEGylation approach reduced the monoolein hemolytic tendency to 3% and increased the serum stability of the nanoparticles. Sterilization of liquid and lyophilized AE-PEG-LCNPs via autoclaving and γ-radiations, respectively, insignificantly affected the physicochemical properties of the nanoparticles. Half maximal inhibitory concentration of AE-PEG-LCNPs was 3.6-fold lower than free AE after 48 hours and their cellular uptake was threefold higher than free AE after 24-hour incubation. AE-PEG-LCNPs presented 5.4-fold increase in t 1/2 compared with free AE. Biodistribution and toxicity studies showed reduced AE-PEG-LCNP uptake by reticuloendothelial system organs and good safety profile. PEGylated LCNPs could serve as a promising nanocarrier for efficient delivery of AE to cancerous cells.

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Physicochemical characterization techniques for solid lipid nanoparticles: principles and limitations

Cited by 103 publications

References 116 publications

The Role of Curcumin-Loaded Solid Lipid Nanoparticles Labeled with Tc-99m in the Liver-Spleen Scintigraphy

The Role of Curcumin-Loaded Solid Lipid Nanoparticles Labeled with Tc-99m in the Liver-Spleen Scintigraphy

Enhanced Anti-Cancer Capability of Ellagic Acid Using Solid Lipid Nanoparticles (SLNs)

Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies

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