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Showing papers on "Solid lipid nanoparticle published in 2018"


Journal ArticleDOI
TL;DR: This review highlights the significance of size and PDI in the successful design, formulation and development of nanosystems for pharmaceutical, nutraceutical and other applications.
Abstract: Lipid-based drug delivery systems, or lipidic carriers, are being extensively employed to enhance the bioavailability of poorly-soluble drugs. They have the ability to incorporate both lipophilic and hydrophilic molecules and protecting them against degradation in vitro and in vivo. There is a number of physical attributes of lipid-based nanocarriers that determine their safety, stability, efficacy, as well as their in vitro and in vivo behaviour. These include average particle size/diameter and the polydispersity index (PDI), which is an indication of their quality with respect to the size distribution. The suitability of nanocarrier formulations for a particular route of drug administration depends on their average diameter, PDI and size stability, among other parameters. Controlling and validating these parameters are of key importance for the effective clinical applications of nanocarrier formulations. This review highlights the significance of size and PDI in the successful design, formulation and development of nanosystems for pharmaceutical, nutraceutical and other applications. Liposomes, nanoliposomes, vesicular phospholipid gels, solid lipid nanoparticles, transfersomes and tocosomes are presented as frequently-used lipidic drug carriers. The advantages and limitations of a range of available analytical techniques used to characterize lipidic nanocarrier formulations are also covered.

1,891 citations


Journal ArticleDOI
TL;DR: The aim of this article is to review the advantages and limitations of these delivery systems based on the route of administration and to emphasis the effectiveness of such formulations.
Abstract: During the recent years, more attentions have been focused on lipid base drug delivery system to overcome some limitations of conventional formulations. Among these delivery systems solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are promising delivery systems due to the ease of manufacturing processes, scale up capability, biocompatibility, and also biodegradability of formulation constituents and many other advantages which could be related to specific route of administration or nature of the materials are to be loaded to these delivery systems. The aim of this article is to review the advantages and limitations of these delivery systems based on the route of administration and to emphasis the effectiveness of such formulations.

396 citations


Journal ArticleDOI
TL;DR: Light is shed on different aspects of SLNs including fabrication and characterization techniques, formulation variables, routes of administration, surface modifications, toxicity, and biomedical applications.
Abstract: 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.

339 citations


Journal ArticleDOI
TL;DR: This review highlights the NLC with focus on the structure, the various fabrication techniques used and the characterization techniques which are critical in the development of a suitable and stable formulation.

293 citations


Journal ArticleDOI
TL;DR: A critical assessment of the characteristics of colloidal particles that impact the effectiveness of protein delivery systems, such as particle composition, size, permeability, interfacial properties, and stability are provided.

262 citations


Journal ArticleDOI
TL;DR: The importance of obtaining a detailed knowledge of the structure of the lipid nanoparticles is highlighted, which is useful for the rational design of this type of nanocarriers and propose solutions to the challenges involved in their formulation.

261 citations


Journal ArticleDOI
TL;DR: An overview of lipid based nanocarriers developed with the aim to enhance dermal and transdermal drug delivery and recent applications of lipid-based nanoccarriers for the management of skin diseases and other illnesses are highlighted.

251 citations


Journal ArticleDOI
TL;DR: Despite the cutaneous use of SLN and NLC has been proposed for both local and transdermal delivery, the reported studies show promising results only for local application, so more research is required to better understanding the interaction mechanisms of lipid nanoparticles with skin lipids.

237 citations


Journal ArticleDOI
TL;DR: This review paper presents an overview of different preparation methods of polymeric and novel lipid-based (niosome and solid lipid) nanoparticles.
Abstract: A wide number of drug nanocarriers have emerged to improve medical therapies, and in particular to achieve controlled delivery of drugs, genes or gene expression-modifying compounds, or vaccine antigens to a specific target site. Of the nanocarriers, lipid-based and polymeric nanoparticles are the most widely used. Lipid-based systems like niosomes and liposomes are non-toxic self-assembly vesicles with an unilamellar or multilamellar structure, which can encapsulate hydrophobic/hydrophilic therapeutic agents. Polymeric nanoparticles, usually applied as micelles, are colloidal carriers composed of biodegradable polymers. Characteristics such as loading capacity, drug release rate, physical and chemical stability, and vesicle size are highly dependent on experimental conditions, and material and method choices at the time of preparation. To be able to develop effective methods for large scale production and to meet the regulatory requirements for eventual clinical implementation of nanocarriers, on...

132 citations


Journal ArticleDOI
TL;DR: Results of sensory analysis indicated that nanoencapsulation could obviate the poor solubility and tomato after taste of lycopene, and nanocarrier’s potential for food fortification.
Abstract: In this study, lycopene, was loaded on nanostructured lipid carrier and solid lipid nanoparticles using combination of high shear homogenization and ultrasonication method. Effect of applied lipids types, nanocarrier’s type and lycopene loading on physicochemical properties of developed nanocarriers were studied. Particle sizes of developed nanocarriers were between 74.93 and 183.40 nm. Encapsulation efficiency of nanostructured lipid carrier was significantly higher than solid lipid nanoparticles. Morphological study of developed nanocarriers using scanning electron microscopy showed spherical nanoparticles with smooth surface. Lycopene was entrapped in nanocarriers without any chemical interaction with coating material according to Fourier transform infrared spectroscopy spectrum and differential scanning calorimetry thermogram. Glycerol monostearate containing nanoparticles showed phase separation after 30 days in 6 and 25 °C, whereas this event was not observed in nanosuspensions that produced by glycerol distearate. Lycopene release in gastrointestinal condition was studied by the dialysis bag method. To evaluate nanocarrier’s potential for food fortification, developed lycopene-loaded nanocarriers were added to orange drink. Results of sensory analysis indicated that nanoencapsulation could obviate the poor solubility and tomato after taste of lycopene. Fortified sample with lycopene nanocarriers didn’t show significant difference with blank orange drink sample except in orange odor.

123 citations


Journal ArticleDOI
TL;DR: This review focuses on different SLN and SMSLN systems that are useful for oral delivery of phyto-bioactive compounds to treat various chronic diseases.
Abstract: Solid lipid nanoparticle (SLN) delivery systems have a wide applicability in the delivery of phyto-bioactive compounds to treat various chronic diseases, including diabetes, cancer, obesity and neurodegenerative diseases. The multiple benefits of SLN delivery include improved stability, smaller particle size, leaching prevention and enhanced lymphatic uptake of the bioactive compounds through oral delivery. However, the burst release makes the SLN delivery systems inadequate for the oral delivery of various phyto-bioactive compounds that can treat such chronic diseases. Recently, the surface-modified SLN (SMSLN) was observed to overcome this limitation for oral delivery of phyto-bioactive compounds, and there is growing evidence of an enhanced uptake of curcumin delivered orally via SMSLNs in the brain. This review focuses on different SLN and SMSLN systems that are useful for oral delivery of phyto-bioactive compounds to treat various chronic diseases.

Journal ArticleDOI
TL;DR: Findings of the study suggest that the developed FLZ loaded SLNs topical gels have superior significant fast therapeutic index in treatment of PV over commercially available Candistan® cream.
Abstract: Solid lipid nanoparticles (SLNs) are very potential formulations for topical delivery of antifungal drugs. Hence, the purpose of this research was to formulate the well-known antifungal agent Fluconazole (FLZ)-loaded SLNs topical gel to improve its efficiency for treatment of Pityriasis Versicolor (PV). FLZ-SLNs were prepared by modified high shear homogenization and ultrasonication method using different concentration of solid lipid (Compritol 888 ATO, Precirol ATO5) and surfactant (Cremophor RH40, Poloxamer 407). The physicochemical properties and the in vitro release study for all FLZ-SLNs were investigated. Furthermore, the optimized FLZ-SLN formula was incorporated into gel using Carpobol 934. A randomized controlled clinical trial (RCT) of potential batches was carried out on 30 well diagnosed PV patients comparing to market product Candistan® 1% cream. Follow up was done for 4 weeks by clinical and KOH examinations. The results showed that FlZ-SLNs were almost spherical shape having colloid...

Journal ArticleDOI
TL;DR: The results suggested that Cur-SLNs could be a potential useful chemotherapeutic formulation for breast cancer therapy.
Abstract: Curcumin (Cur) has been widely used in medicine, due to its antibacterial, anti-inflammatory, antioxidant, and antitumor effects. However, its clinic application is limited by its instability and poor solubility. In the present wok, curcumin was loaded into solid lipid nanoparticles (SLNs), in order to improve the therapeutic efficacy for breast cancer. The results measured using transmission electron microscopy (TEM) indicated that Cur-SLNs have a well-defined spherical shape; the size was about 40 nm with a negative surface charge. The drug loading and encapsulation efficiency in SLNs reached 23.38% and 72.47%, respectively. The Cur-SLNs showed a stronger cytotoxicity against SKBR3 cells. In vitro cellular uptake study demonstrated a high uptake efficiency of the Cur-SLNs by SKBR3 cells. Moreover, Cur-SLNs induced higher apoptosis in SKBR3 cells, compared to cells treated by free drug. In addition, Western blot analysis revealed that Cur-SLNs could promote the ratio of Bax/Bcl-2, but decreased the expression of cyclin D1 and CDK4. These results suggested that Cur-SLNs could be a potential useful chemotherapeutic formulation for breast cancer therapy.

Journal ArticleDOI
TL;DR: The preclinical findings demonstrated the positive impact of the coated SLN on the delivery of paclitaxel by inhalation and demonstrated that FR was involved in these improvements, especially in M109-HiFR cells.
Abstract: Inhaled chemotherapy for the treatment of lung tumors requires that drug delivery systems improve selectivity for cancer cells and tumor penetration and allow sufficient lung residence. To this end, we developed solid lipid nanoparticles (SLN) with modified surface properties. We successfully synthesized a new folate-grafted copolymer of polyethylene glycol (PEG) and chitosan, F-PEG-HTCC, with a PEG-graft ratio of 7% and a molecular weight range of 211–250 kDa. F-PEG-HTCC-coated, paclitaxel-loaded SLN were prepared with an encapsulation efficiency, mean diameter, and zeta potential of about 100%, 250 nm, and +32 mV, respectively. The coated SLN entered folate receptor (FR)-expressing HeLa and M109-HiFR cells in vitro and M109 tumors in vivo after pulmonary delivery. The coated SLN significantly decreased the in vitro half-maximum inhibitory concentrations of paclitaxel in M109-HiFR cells (60 vs 340 nM, respectively). We demonstrated that FR was involved in these improvements, especially in M109-HiFR cells...

Journal ArticleDOI
Yining Xu1, Yaxian Zheng1, Lei Wu1, Xi Zhu1, Zhirong Zhang1, Yuan Huang1 
TL;DR: It was shown that INS HA2-O-SLNs effectively facilitated the escape of the loaded insulin from the acidic endosomes, which preserved the biological activity of insulin to a greater extent during the intracellular transport.
Abstract: Although nanoparticles (NPs) have been demonstrated as promising tools for improving oral absorption of biotherapeutics, most of them still have very limited oral bioavailability. Lyso–endosomal degradation in epithelial cells is one of the important but often-neglected physiological barriers, limiting the transport of cargoes across the intestinal epithelium. We herein reported a solid lipid nanoparticle (SLN) platform with a unique feature of endosomal escape for oral protein drug delivery. The SLNs consisted of a solid-lipid shell, which contained an endosomal escape agent (GLFEAIEGFIENGWEGMIDGWYG, HA2), and an aqueous core that is loaded with insulin (INS HA2-O-SLNs). SLNs without and with the HA2 peptide in the aqueous core (INS SLNs and INS HA2-W-SLNs, respectively) were used as the control groups. Our study showed that INS HA2-O-SLNs effectively facilitated the escape of the loaded insulin from the acidic endosomes, which preserved the biological activity of insulin to a greater extent during the i...

Journal ArticleDOI
TL;DR: In vitro results proved that nanoparticles improved permeability of AG compared to free AG, and fluorescent SLN were detected in brain parenchyma outside the vascular bed, confirming their ability to overcome the blood-brain barrier.

Journal ArticleDOI
TL;DR: C-SLNs show higher in vitro muchoadesive properties and a higher permeability in alveolar epithelial cells A549 than uncoated SLNs, indicating that the developed C- SLNs can be used as a promising carrier for sasfer and efficient management of TB.

Journal ArticleDOI
TL;DR: The results demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.
Abstract: Triamcinolone acetonide (TA), an intermediate acting corticosteroid, is used in the treatment of posterior ocular diseases, such as inflammation, posterior uveitis, and diabetic macular edema. The objective of this investigation was to prepare TA-loaded solid lipid nanoparticles (TA-SLNs) and in situ gel (TA-SLN-IG) formulations for delivery into the deeper ocular tissues through the topical route. TA-SLNs were prepared by hot homogenization and ultrasonication method using glyceryl monostearate and Compritol® 888ATO as solid lipids and Tween®80 and Pluronic® F-68 as surfactants. TA-SLNs were optimized and converted to TA-SLN-IG by the inclusion of gellan gum and evaluated for their rheological properties. In vitro transcorneal permeability and in vivo ocular distribution of the TA-SLNs and TA-SLN-IG were studied using isolated rabbit corneas and New Zealand albino rabbits, respectively, and compared with TA suspension, used as control (TA-C). Particle size, PDI, zeta potential, assay, and entrapment efficiency of TA-SLNs were in the range of 200–350 nm, 0.3–0.45, −52.31 to −64.35 mV, 70–98%, and 97–99%, respectively. TA-SLN-IG with 0.3% gellan gum exhibited better rheological properties. The transcorneal permeability of TA-SLN and TA-SLN-IG was 10.2 and 9.3-folds higher compared to TA-C. TA-SLN-IG showed maximum tear concentration at 2 h, indicating an improved pre-corneal residence time, as well as higher concentrations in aqueous humor, vitreous humor and cornea at 6 h, suggesting sustained delivery of the drug into the anterior and posterior segment ocular tissues, when compared to TA-SLN and TA-C. The results, therefore, demonstrate that the lipid based nanoparticulate system combined with the in situ gelling agents can be a promising drug delivery platform for the deeper ocular tissues.

Journal ArticleDOI
TL;DR: This review focuses on the two drug delivery systems and derivatives of β-elemene for cancer therapy, and a number of highly active anticancer β-Elemene derivatives have been obtained through modification of the structure ofβ- elemene.
Abstract: β-elemene is a noncytotoxic Class II antitumor drug extracted from the traditional Chinese medicine Curcuma wenyujin Y. H. Chen et C. Ling. β-elemene exerts its effects by inhibiting cell proliferation, arresting the cell cycle, inducing cell apoptosis, exerting antiangiogenesis and antimetastasis effects, reversing multiple-drug resistance (MDR), and enhancing the immune system. Elemene injection and oral emulsion have been used to treat various tumors, including cancer of the lung, liver, brain, breast, ovary, gastric, prostate, and other tissues, for >20 years. The safety of both elemene injection and oral emulsion in the clinic has been discussed. Recently, the secondary development of β-elemene has attracted the attention of researchers and made great progress. On the one hand, studies have been carried out on liposome-based systems (including solid lipid nanoparticles [SLNs], nanostructured lipid carriers [NLCs], long-circulating liposomes, active targeting liposomes, and multidrug-loaded liposomes) and emulsion systems (including microemulsions, self-emulsion drug delivery systems [SEDDSs], and active targeting microemulsion) to solve the issues of poor solubility in water, low bioavailability, and severe phlebitis, as well as to improve antitumor efficacy. The pharmacokinetics of different drug delivery systems of β-elemene are also summarized. On the other hand, a number of highly active anticancer β-elemene derivatives have been obtained through modification of the structure of β-elemene. This review focuses on the two drug delivery systems and derivatives of β-elemene for cancer therapy.

Journal ArticleDOI
TL;DR: Citral-loaded solid lipid nanoparticles (citral-SLNs) were prepared via a high-pressure homogenization method, using glyceryl monostearate as the solid lipid and a mixture of Tween 80 and Span 80 at a weight ratio of 1:1 as the surfactant to enhance its stability in acidic surroundings.

Journal ArticleDOI
TL;DR: Both excipients and fabrication methods are crucial for the function and size of nanoparticles and should be considered simultaneously in designing particles to obtain the optimal drug absorption and efficacy, especially for local treatments.
Abstract: Introduction: Solid lipid nanoparticles are promising drug carriers for systemic circulations as well as local applications. One of the major challenges for drug delivery is designing nanocarriers ...

Journal ArticleDOI
TL;DR: Drug loaded SLNs with small particle size and narrow size distribution with good solid loading, encapsulation efficiency and drug loading percentage could be prepared using the optimised conditions and cytotoxicity results showed that the prepared SLNs are non-toxic to Raw cell line.

Journal ArticleDOI
TL;DR: The aim of this study was to improve the physicochemical stability of β-carotene by encapsulating into solid lipid nanoparticles (SLNPs) containing palmitic acid and corn oil, stabilized using whey protein isolate (WPI).

Journal ArticleDOI
TL;DR: Results revealed rapid ALM brain delivery of the optimized formula, and toxicological results confirmed the safety of NF for nasal administration, encouraging for further clinical trials of the developed system in humans in future research.

Journal ArticleDOI
TL;DR: Solid lipid nanoparticles containing Eugenia caryophyllata essential oil were prepared by high‐shear homogenization and ultrasound methods, and used to eradicate pathogens, highlighting the effectiveness of SLN formulations against human pathogens.
Abstract: In this study, solid lipid nanoparticles containing Eugenia caryophyllata essential oil (SLN-EO) were prepared by high-shear homogenization and ultrasound methods, and used to eradicate pathogens. SLN formulations were evaluated for their size, zeta potential and encapsulation efficacy (EE). The morphological and thermal properties of the formulations were analysed by transmission electron microscopy (TEM) and differential scanning calorimetry methods. The lead formulations were chosen and tested with minimum inhibitory concentration (MIC), MBC and time-kill methods to investigate the antimicrobial activity against Salmonella typhi, Pseudomonas aeruginosa, Staphylococcus aureus and Candida albicans. The particle size of three final formulations were 397 ± 10·1, 786·9 ± 11 and 506·4 ± 22 nm respectively. The zeta potential of all formulations was negative values. The size of the formulations was slightly increased during 3 months storage at 25°C. The TEM imaging showed that formulation had spherical shape. The EE of EO was estimated approximately 70%. MIC and MCC values of SLN-EO were lower than those of the oil alone. The time-kill studies showed that SLN-EO was either equivalent to or better than EO (P-value <0·05). The results of this study highlighted the effectiveness of SLN formulations against human pathogens. SIGNIFICANCE AND IMPACT OF THE STUDY Microbial resistance to antibiotics is a major problem in the treatment of diseases. Therefore, overcoming antimicrobial resistance is an urgent need. Drug delivery via nanoparticles and applying natural products are promising approaches to reduce microbial resistance. This study is designed to evaluate the antimicrobial activity of solid lipid nanoparticles (SLN) containing Eugenia caryophyllata essential oil (EO) against human pathogens. The results indicated that the antimicrobial activity of EO was remarkably enhanced when encapsulated in SLN.

Journal ArticleDOI
Jingyi Xue1, Taoran Wang1, Qiaobin Hu1, Mingyon Zhou1, Yangchao Luo1 
TL;DR: In this paper, four loading methods were tested for their efficacy to encapsulate curcumin into solid lipid nanoparticles (SLNs) and four different loading methods varied in the use of organic solvent, and the order of critical steps including addition of curcurumin and solid lipids, deprotonation of NaCas at pH 12, and pectin adsorption at pH 4.

Journal ArticleDOI
TL;DR: A strong negative correlation between particle size and concentration is revealed in diluted samples, which should be adopted to monitor nanocolloidal stability, especially in drug delivery.
Abstract: Elucidation of the structural properties of colloids is paramount for a successful formulation. However, the intrinsic dynamism of colloidal systems makes their characterization a difficult task and, in particular, there is a lack of physicochemical techniques that can be correlated to their biological performance. Nanoparticle tracking analysis (NTA) allows measurements of size distribution and nanoparticle concentration in real time. Its analysis over time also enables the early detection of physical instability in the systems not assessed by subtle changes in size distribution. Nanoparticle concentration is a parameter with the potential to bridge the gap between in vitro characterization and biological performance of colloids, and therefore should be monitored in stability studies of formulations. To demonstrate this, we have followed two systems: extruded liposomes exposed to increasing CHCl3 concentrations, and solid lipid nanoparticles prepared with decreasing amounts of poloxamer 188. NTA and dynamic light scattering (DLS) were used to monitor changes in nanoparticle number and size, and to estimate the number of lipid components per particle. The results revealed a strong negative correlation between particle size (determined by DLS) and concentration (assessed by NTA) in diluted samples, which should be adopted to monitor nanocolloidal stability, especially in drug delivery.

Journal ArticleDOI
TL;DR: Recent advances in epidermal and dermal drug deposition enhancement approaches, biopharmaceutical challenges with Dermal drug delivery, issues in formulation development, and regulatory aspects of nanosystem are covered.
Abstract: Skin is the largest and easily accessible organ of the body. Increases in incidences of dermatological disorders, demand for drug targeting, and patient compliance have increased the popularity of topical drug delivery amongst the people. However, drug delivery across the skin is still a challenge for researchers because permeation of maximum drugs is hindered by the upper layer of the epidermis (stratum corneum). Several approaches like use of chemical permeation enhancers and physical methods such as sonophoresis, iontophoresis, electroporation, microneedles, etc., have been used to deliver the drugs topically. These methods of topical drug delivery have some limitations and drawbacks. Therefore new techniques based on nano drug delivery system such as ultradeformable liposomes, nanostructured lipid carriers, nanoemulsions, solid lipid nanoparticles, lipospheres, nanoparticles, and ethosomes have been exploited for enhancing epidermal and dermal drug deposition. Development of these nanosytems requires a good understanding of mechanism of drug permeation, physicochemical properties of drug and carriers, and technological advancements in methodology. Therefore, this article covers recent advances in epidermal and dermal drug deposition enhancement approaches, biopharmaceutical challenges with dermal drug delivery, issues in formulation development, and regulatory aspects of nanosystem. This review article also discusses the concern of topical drug delivery in immunization, gene delivery, and cosmeceuticals.

Journal ArticleDOI
TL;DR: Delivery by design (DbD) as discussed by the authors is a more rational approach to create colloidal delivery systems with properties suitable for commercial applications, which has been shown to be effective in many cases.
Abstract: The development of colloidal delivery systems (CDS) to encapsulate, protect, and release bioactive agents has exploded in recent years, as seen by the large increase in papers published in this area. These delivery systems include micelles, microemulsions, nanoemulsions, emulsions, multiple emulsions, solid lipid nanoparticles, protein nanoparticles, and biopolymer microgels. Despite this fact, it is unclear how many of these delivery systems are actually being adapted by industry, or if they are even suitable for commercial applications. Many of the CDS described in scientific manuscripts are prepared from ingredients that are not legally acceptable in foods, are fabricated using processing operations that are uneconomic or cannot be scaled up, or have properties incompatible with the intended final application. This article describes the principle of `delivery by design’ (DbD) as a more rational approach to create CDS with properties suitable for commercial applications.

Journal ArticleDOI
TL;DR: Different techniques used to produce SLN and NLC with potential or effective peptide encapsulation are outlined and basic principles of covalent and non-covalent lipidization are described and discussed as a prerequisite to improve hydrophilic peptides encapsulation in lipid-based nanosuspensions.