Influence of natural organic matter (NOM) coatings on nanoparticle adsorption onto supported lipid bilayers

Bo, Zhang,Avsar, Saziye Yorulmaz,Corliss, Michael K.,Chung, Minsub,Cho, Nam-Joon Elsevier 2017 Journal of hazardous materials Vol.339 No.-

<P><B>Abstract</B></P> <P>As the worldwide usage of nanoparticles in commercial products continues to increase, there is growing concern about the environmental risks that nanoparticles pose to biological systems, including potential damage to cellular membranes. A detailed understanding of how different types of nanoparticles behave in environmentally relevant conditions is imperative for predicting and mitigating potential membrane-associated toxicities. Herein, we investigated the adsorption of two popular nanoparticles (silver and buckminsterfullerene) onto biomimetic supported lipid bilayers of varying membrane charge (positive and negative). The quartz crystal microbalance-dissipation (QCM-D) measurement technique was employed to track the adsorption kinetics. Particular attention was focused on understanding how natural organic matter (NOM) coatings affect nanoparticle-bilayer interactions. Both types of nanoparticles preferentially adsorbed onto the positively charged bilayers, although NOM coatings on the nanoparticle and lipid bilayer surfaces could either inhibit or promote adsorption in certain electrolyte conditions. While past findings showed that NOM coatings inhibit membrane adhesion, our findings demonstrate that the effects of NOM coatings are more nuanced depending on the type of nanoparticle and electrolyte condition. Taken together, the results demonstrate that NOM coatings can modulate the lipid membrane interactions of various nanoparticles, suggesting a possible way to improve the environmental safety of nanoparticles.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Interaction of Ag and C<SUB>60</SUB> nanoparticles with charged lipid membranes was studied. </LI> <LI> Quartz crystal microbalance experiments measured the adsorption kinetics. </LI> <LI> Natural organic matter (NOM) either inhibited or promoted nanoparticle adsorption. </LI> <LI> Adsorption profile depended on nanoparticle type, electrolyte condition, and NOM. </LI> </UL> </P>

Observation of chitosan coated lipid nanoparticles with different lipid compositions under simulated <i>in vitro</i> digestion system

Shin, Gye Hwa,Kim, Jun Tae IRL Press 2018 Food hydrocolloids Vol.84 No.-

<P><B>Abstract</B></P> <P>The effects of lipid composition and chitosan coating on lipid digestion ability were investigated using a simulated <I>in vitro</I> digestion system, including oral, gastric, and small intestine stages. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were prepared with only palm oil and the mixture of palm oil and medium-chain triglyceride (MCT) oil, respectively. Chitosan-coated SLNs (CS-SLNs) and NLCs (CS-NLCs) were prepared with a drop-wise method. CS-NLCs were more completely digested than the NLCs, while the NLCs showed higher free fatty acid release than SLNs. Chitosan coating increased the particle size of both SLNs and NLCs from 100.0 to 104.9 nm to 130.0 and 146.5 nm, respectively. Chitosan coating also increased the initial digestion rate of NLCs by modulating lipid droplet aggregation. But, chitosan coating showed little impact on the digestion of SLNs because SLNs did not strongly impact the lipid droplet aggregation state. These results have important implications for the fabrication of functional foods and beverages to achieve control of lipid digestion in the gastrointestinal tract.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Four lipid nanoparticles were prepared to compare the lipid digestion. </LI> <LI> The particles were subjected to an <I>in vitro</I> simulated digestive system and compared. </LI> <LI> NLC showed more rapid digestion than SLN due to the liquid lipid. </LI> <LI> Free fatty acid release profile of CS-SLN was almost same to that of SLN. </LI> <LI> CS-NLC showed greater free fatty acid release than NLC. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>

Recent advancements in lipid–mRNA nanoparticles as a treatment option for cancer immunotherapy

Karmacharya Prajeena,Patil Basavaraj Rudragouda,김종오 한국약제학회 2022 Journal of Pharmaceutical Investigation Vol.52 No.4

Background Cancer remains a serious health concern worldwide, and different approaches are being developed for its treatment. The strategy to use the immune system as an approach for treating cancer has recently gained momentum. Messenger RNA (mRNA) has been assessed as an up-and-coming resource for the evolution of advanced cancer immunotherapies over the past decades. However, degradation in extracellular compartments and during endosomal escape remain obstacles for efficient mRNA delivery and limit the therapeutic applications of this approach. Area covered Lipid-based nanocarriers are gaining significant attention as non-viral mRNA vectors. Various lipid-based nanocarrier types have been developed to enhance the stability of mRNA molecules, facilitate their transfection, and ensure delivery to an intracellular compartment suitable for further processing. This review discusses the development of novel mRNA delivery systems using lipids for effective cancer immunotherapy. Expert opinion mRNAs are superior to other biomolecules for developing therapeutic drugs and vaccines with multiple medical applications that are currently being explored by researchers in various biomedical fields. Lipid-based mRNA nanoparticles can improve the potency of the mRNA by enhancing its stability, enabling its cellular uptake, and facilitating its endosomal escape. Targetability of these therapeutics can be increased by conjugating their surface with the desired ligands or targeting agents. Lipid–mRNA nanoparticles are increasingly being incorporated in cancer immunotherapy applications, including vaccines, monoclonal antibodies, and chimeric antigen receptor T-cell treatment, and several such nanoparticles are being assessed in clinical trials. Further research that assesses key variables for transfection efficiency of lipid–mRNA nanoparticles will expedite the development of improved therapeutics.

Effect of lipid on physicochemical properties of solid lipid nanoparticle of paclitaxel

Jong-Suep Baek,Sang Chul Shin,조정원 한국약제학회 2012 Journal of Pharmaceutical Investigation Vol.42 No.5

The aim of this study was to compare physicochemical properties of solid lipid nanoparticles (SLN) made from different lipids. To make small, stable, uniform and highly encapsulated SLNs, many factors such as the components (lipid, stabilizer) and preparation condition (sonication time, power) can be considered. Out of those, we selected solid lipid as lipid matrix to investigate an effect on SLNs. The SLNs were characterized by particle size, zeta potential, solubility and in vitro release study. In this study,SLNs showed different physicochemical properties and release profiles according to used solid lipid. In case of particle size, M-SLN showed biggest particle size (412.5 ± 29.4 nm) and highest encapsulation efficiency (61.2 ± 4.8 %). And, B-SLN showed highest cumulative drug percentage (85.0 ± 1.7 %, 24 h) in release study. These results suggest that lipids type affect physicochemical properties and release profile of SLN.

In vitro Anticancer Activity of Paclitaxel Incorporated in Low-melting Solid Lipid Nanoparticles

Lee, Mi-Kyung,Yang, Jae-Heon The Korean Society of Pharmaceutical Sciences and 2009 Journal of Pharmaceutical Investigation Vol.39 No.3

Triglyceride solid lipid with medium chain fatty acid, tricaprin (TC), was used as a core matrix of lipid nanoparticles (LN) to solubilize water-insoluble paclitaxel and enhance the stability of nanoparticles by immobilization of incorporated drug in the solid core during storage at low temperature. In the present study, TC-LN containing paclitaxel was prepared by hot melt homogenization method using TC as a core lipid and phospholipids as stabilizers. The particle size of TC-LN containing paclitaxel was less than 200 nm and its zeta potential was around -40 mV. Calorimetric analysis showed TC core could be solidified by freezing and thawing in the manufacturing process in which the hot dispersion should be prepared at elevated temperature and subsequently cooled to obtain solid lipid nanoparticles. The melting transition of TC core was observed at $27.5^{\circ}C$, which was lower than melting point of TC bulk. The particle size of TC-LN remained unchanged when kept at $4^{\circ}C$. Paclitaxel containing TC-LN showed comparable anticancer activity to the Cremophore ELbased paclitaxel formulation against human ovarian (OVCAR-3) and breast (MCF-7) cancer cell lines. Thus, lipid nanoparticles with medium chain solid lipid may have a potential as alternative delivery system for parenteral administration of paclitaxel.

A Simple Evaporation Method for Large-Scale Production of Liquid Crystalline Lipid Nanoparticles with Various Internal Structures

Kim, Do-Hoon,Lim, Sora,Shim, Jongwon,Song, Ji Eun,Chang, Jong Soo,Jin, Kyeong Sik,Cho, Eun Chul American Chemical Society 2015 ACS APPLIED MATERIALS & INTERFACES Vol.7 No.36

<P>We present a simple and industrially accessible method of producing liquid crystalline lipid nanoparticles with various internal structures based on phytantriol, Pluronic F127, and vitamin E acetate. Bilayer vesicles were produced when an ethanolic solution dissolving the lipid components was mixed with deionized water. After the evaporation of ethanol from the aqueous mixture, vesicles were transformed into lipid-filled liquid crystalline nanoparticles with well-defined internal structures such as hexagonal lattices (mostly inverted cubic <I>Pn</I>3<I>m</I>), lined or coiled pattern (inverted hexagonal H<SUB>2</SUB>), and disordered structure (inverse microemulsion, L<SUB>2</SUB>), depending on the compositions. Further studies suggested that their internal structures were also affected by temperature. The internal structures were characterized from cryo-TEM and small-angle X-ray scattering results. Microcalorimetry studies were performed to investigate the degree of molecular ordering/crystallinity of lipid components within the nanostructures. From the comparative studies, we demonstrated the present method could produce the lipid nanoparticles with similar characteristics to those made from a conventional method. More importantly, the production only requires simple tools for mixing and ethanol evaporation and it is possible to produce 10 kg or so per batch of aqueous lipid nanoparticles dispersions, enabling the large-scale production of the liquid crystalline nanoparticles for various biomedical applications.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/aamick/2015/aamick.2015.7.issue-36/acsami.5b06413/production/images/medium/am-2015-06413p_0008.gif'></P>

Silica-coated solid lipid nanoparticles enhance antioxidant and antiradical effects of meloxicam

Jessy Shaji,Dhanila Varkey 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.5

Oxidative stress and decreased antioxidant status are the hallmarks in patients suffering from rheumatoid arthritis. A targeted nanocarrier can enhance the therapeutic efficacy of meloxicam, a preferential cyclooxygenase-2 inhibitor with potential suppressive effects on free-radical mediated damage. Silica-coated solid lipid nanoparticles of meloxicam were fabricated by melt emulsification ultrasound homogenization technique and characterized for formation, morphology, morphometrical properties, drug entrapment, drug release pattern and storage stability. The in vitro antioxidant potential of lipid nanoparticles was evaluated by various antiradical and antioxidant assays including 1,1-diphenyl-2-picryl-hydrazil free radical scavenging, nitric oxide radical inhibition, lipid peroxidation, hydroxyl radical scavenging and superoxide anion radical scavenging activity. Lipid nanoparticles were successfully characterized for morphometrical parameters by photon correlation spectroscopy measurements. Transmission electron microscopy and atomic force microscopy studies confirmed the production of lipid nanoparticles. Meloxicam was successfully encapsulated within the lipid matrix as indicated by high drug entrapment efficiency,Fourier transform infrared spectroscopy and powder X-ray diffraction studies. The drug release from lipid nanoparticles exhibited a biphasic release pattern with good storage stability. Free radical scavenging activity of silica-coated meloxicam loaded solid lipid nanoparticles in all assays was higher than the free drug and was found to increase in a dose dependent manner. A nanocarrier based delivery system of meloxicam potentiates its free radical suppression effects and can further enhance its therapeutic efficacy in the management of rheumatoid arthritis.

Paromomycin Loaded Solid Lipid Nanoparticles: Characterization of Production Parameters

Maryam Ghadiri,Alireza Vatanara,Delaram Doroud,A. Roholamini Najafabadi 한국생물공학회 2011 Biotechnology and Bioprocess Engineering Vol.16 No.3

Paromomycin has been shown to have antileishmaniasis activity; however, its clinical use is restricted to some content owing to its poor skin penetration. To identify innovative methods of dermal administration of paromomycin and controlling the release delivery system,paromomycin was loaded into the solid lipid media as nanoparticles. Type of the method; microemulsion or solvent diffusion, the type of lipid; cetyl palmitate or stearic acid, were comparatively investigated on the average diameter,size distribution and entrapment efficiency of the lipid nanoparticles to maximize entrapment efficiency, reduce the particle size and its distribution. Three quantitative factors, paromomycin content, weight fraction of Tween 80and drug to lipid ratio, were also investigated at two levels for Solid Lipid Nanoparticles (SLNs) formulation in a fractional factorial design. The results indicated that microemulsion was the most efficient method and stearic acid was the preferred lipid for SLNs formulation. The average size of the particles was reduced to 299.08 nm and the entrapment efficiency was enhanced from immediate release to 24 h.

Lipid-based surface engineering of PLGA nanoparticles for drug and gene delivery applications

Rajendran JC Bose,이수홍,박한수 한국생체재료학회 2016 생체재료학회지 Vol.20 No.4

The use of poly(lactic-co-glycolic acid) (PLGA)-based nanocarriers presents several major challenges, including their synthetic hydrophobic surface, low transfection efficiency, short circulation half-life, and nonspecific tissue distribution. Numerous engineering strategies have been employed to overcome these problems, with lipid-based surface functionalization of PLGA nanoparticles (NPs) showing promising results in the development of PLGA-based clinical nanomedicines. Surface engineering with different lipids enhances the target specificity of the carrier and improves its physicochemical properties as well as NP-cell associations, such as cellular membrane permeability, immune responses, and long circulation half-life in vivo. This review focuses on recent advances in the lipid-based surface engineering of PLGA NPs for drug and gene delivery applications.

Cationic lipid nanoparticles for nucleic acid delivery: microfluidics versus thin film hydration

Park Hyeseon,Lee Jaeseong,Jeon-Woong Kang,Min Ji-Young,Lee Jeongmin,Hong Jiwoo,Shim Gayong 한국약제학회 2026 Journal of Pharmaceutical Investigation Vol.56 No.2

Purpose Lipid-based nanoparticles, designed to mimic cell membrane structures, are extensively employed in drug delivery systems due to their bioavailability and versatility. The monodispersity of these carriers in terms of size is crucial for safe and effective drug or nucleic acid delivery. This study investigated a microfluidic chip-based methodology for the monodisperse fabrication of size-controllable nanoparticles, comparing its performance with conventional methods. Methods Variations in flow rates and lipid concentrations resulted in significant differences in the physical properties of lipid nanoparticles (LNPs), including nanoparticle diameter and polydispersity index. Optimal flow rates and lipid concentrations were identified, resulting in nanoparticles of the desired size and with low polydispersity index values. Using these parameters, nucleic acid-loaded LNPs were prepared and compared to liposomes produced via the conventional thin film hydration method, with identical lipid and nucleic acid compositions. Results The microfluidic approach enabled the production of monodisperse LNPs that were smaller in size compared to conventional methods. Higher nucleic acid loading was observed in the LNPs, and they exhibited enhanced protection against external enzymatic degradation. In vitro studies involved the transfection of Hela cells with both types of nanoparticles to assess nucleic acid delivery efficiency via RNA interference. The results demonstrated comparable nucleic acid delivery efficiency using LNPs compared to liposomes. Additionally, the biodistribution results demonstrated that LNPs exhibit delayed excretion, suggesting prolonged retention within the body after nanoparticle administration in mice. These findings suggest the potential for long-term in vivo persistence of LNPs, characterized by their high loading capacity. Conclusion These results highlight the advantages of using microfluidic-based processes for producing LNPs designed for nucleic acid delivery, particularly in the context of drug development and manufacturing.