Use Of Solid Lipid Nanoparticles Research Articles

Emphasis on Nanostructured Lipid Carriers in the Ocular Delivery of Antibiotics.

Drug distribution to the eye is still tricky because of the eye's intricate structure. Systemic delivery, as opposed to more traditional methods like eye drops and ointments, is more effective but higher doses can be harmful. The use of solid lipid nanoparticles (SLNPs) as a method of drug delivery has been the subject of research since the 1990s. Since SLNPs are derived from naturally occurring lipids, they pose no health risks to the user. To raise the eye's absorption of hydrophilic and lipophilic drugs, SLNs can promote corneal absorption and improve the ocular bioavailability of SLNPs. To address problems related to ocular drug delivery, many forms of nano formulation were developed. Some of the methods developed are, emulsification and ultra-sonication, high-speed stirring and ultra-sonication, thin layer hydration, adapted melt-emulsification, and ultrasonication techniques, hot o/w micro-emulsion techniques, etc. Results: Nanostructured lipid carriers are described in this review in terms of their ocular penetration mechanism, structural characteristic, manufacturing process, characterization, and advantages over other nanocarriers. Recent developments in ocular formulations with nanostructured bases, such as surfacemodified attempts have been made to increase ocular bioavailability in both the anterior and posterior chambers by incorporating cationic chemicals into a wide variety of polymeric systems.

Dacarbazine-encapsulated solid lipid nanoparticles for skin cancer: physical characterization, stability, in-vivo activity, histopathology, and immunohistochemistry.

This study examined the use of solid lipid nanoparticles (SLNs) to administer Dacarbazine (DTIC) to skin melanoma cells with minimal adverse effects. Melanoma is a tricky skin cancer to cure, and standard chemotherapy has many negative effects. Encapsulating DTIC in SLNs may allow the drug to target melanoma cells without harming healthy cells. The study developed and tested DTIC-loaded SLNs for skin melanoma treatment. This study encapsulated Dacarbazine (DTIC) in solid lipid nanoparticles (SLNs). SLNs with reversed micelles were produced utilizing specified ratios of the surfactant Kolliphor® P188 and phosphatidylcholine. To track SLN drug localisation, gold nanoparticles were conjugated to the DTIC. Nanoparticle size and form were examined using DLS and TEM. These approaches ensured SLNs had the correct size and shape for drug delivery. In the study, various parameters of the developed solid lipid nanoparticles (SLNs) were evaluated, including particle size, zeta potential, polydispersity index (PDI), entrapment efficacy, and cumulative drug permeation. The values for these parameters varied across the different formulations, with particle size ranging from 146 ± 4.71 nm to 715 ± 7.36 nm, zeta potential from -12.45 ± 2.78 mV to -30.78 ± 2.83 mV, PDI from 0.17 ± 0.013 to 0.51 ± 0.023, entrapment efficacy from 37.78 ± 2.78% to 87.45 ± 4.78%, and cumulative drug permeation from 117 ± 4.77 μg/cm2 to 275 ± 5.67 μg/cm2. To determine the optimal anti-cancer formulation, the DTIC-SLNs-8 nanoparticles were mixed with an optimized concentration of Gellan gum (0.01% w/v) and applied to DMBA-induced skin tumors in rats for six weeks, twice daily. Histopathology demonstrated that DTIC-SLNs-8-treated rats had less keratosis, inflammatory responses, and angiogenesis than free DTIC-treated rats. The development of SLNs may be a promising approach for melanoma treatment due to their improved drug retention over the skin. The optimised anti-cancer formulation DTIC-SLNs-8 showed improved efficacy with minimal side effects as compared to free DTIC.

Tocilizumab-coated solid lipid nanoparticles loaded with cannabidiol as a novel drug delivery strategy for treating COVID-19: A review.

Commonly used clinical strategies against coronavirus disease 19 (COVID-19), including the potential role of monoclonal antibodies for site-specific targeted drug delivery, are discussed here. Solid lipid nanoparticles (SLN) tailored with tocilizumab (TCZ) and loading cannabidiol (CBD) are proposed for the treatment of COVID-19 by oral route. TCZ, as a humanized IgG1 monoclonal antibody and an interleukin-6 (IL-6) receptor agonist, can attenuate cytokine storm in patients infected with SARS-CoV-2. CBD (an anti-inflammatory cannabinoid and TCZ agonist) alleviates anxiety, schizophrenia, and depression. CBD, obtained from Cannabis sativa L., is known to modulate gene expression and inflammation and also shows anti-cancer and anti-inflammatory properties. It has also been recognized to modulate angiotensin-converting enzyme II (ACE2) expression in SARS-CoV-2 target tissues. It has already been proven that immunosuppressive drugs targeting the IL-6 receptor may ameliorate lethal inflammatory responses in COVID-19 patients. TCZ, as an immunosuppressive drug, is mainly used to treat rheumatoid arthritis, although several attempts have been made to use it in the active hyperinflammatory phase of COVID-19, with promising outcomes. TCZ is currently administered intravenously. It this review, we discuss the potential advances on the use of SLN for oral administration of TCZ-tailored CBD-loaded SLN, as an innovative platform for managing SARS-CoV-2 and related infections.

Solid Lipid Nanoparticles: Multitasking Nano-Carriers for Cancer Treatment.

Despite all the advances seen in recent years, the severe adverse effects and low specificity of conventional chemotherapy are still challenging problems regarding cancer treatment. Nanotechnology has helped to address these questions, making important contributions in the oncological field. The use of nanoparticles has allowed the improvement of the therapeutic index of several conventional drugs and facilitates the tumoral accumulation and intracellular delivery of complex biomolecules, such as genetic material. Among the wide range of nanotechnology-based drug delivery systems (nanoDDS), solid lipid nanoparticles (SLNs) have emerged as promising systems for delivering different types of cargo. Their solid lipid core, at room and body temperature, provides SLNs with higher stability than other formulations. Moreover, SLNs offer other important features, namely the possibility to perform active targeting, sustained and controlled release, and multifunctional therapy. Furthermore, with the possibility to use biocompatible and physiologic materials and easy scale-up and low-cost production methods, SLNs meet the principal requirements of an ideal nanoDDS. The present work aims to summarize the main aspects related to SLNs, including composition, production methods, and administration routes, as well as to show the most recent studies about the use of SLNs for cancer treatment.

Use of the quantum dot-labeled solid lipid nanoparticles for delivery of streptomycin and hydroxychloroquine: A new therapeutic approach for treatment of intracellular Brucella abortus infection

Brucellosis is considered one of the most important infectious diseases affecting any tissue and organ in the human body. Due to the intracellular pathogenesis of Brucella species, the use of conventional antibiotics for managing chronic brucellosis has several limitations. Therefore, the study focused on the use of solid lipid nanoparticles (SLN) to deliver streptomycin (STR) for intracellular infection, with or without the combination of hydroxychloroquine (HCQ) to evaluate if there might be a boost in the antibiotic effect when using the STR or STR-NPs alone. We used the double emulsion technique to synthesize Nano drug carriers; afterward, the physicochemical characteristics of synthesized Nano drug carriers were determined. The in vitro antibacterial activity of free drugs and Nano drug carriers were evaluated using well diffusion, broth microdilution assays (BMD), and murine macrophage-like cells cell line J774A.1. Additionally, acute and chronic phases of brucellosis were inducted into Wistar rats, and healing capacity of Nano drug carriers on liver and spleen tissues was compared with free drugs. The zeta potential of nanoparticles, means of size, Polydispersity Index (PDI), drugs loading, and encapsulation efficiency were 15.2 mV, 312.5 ± 26 nm, 0.433 ± 0.09, 16.6% and 89.5%, respectively. Well diffusion and BMD methods did not show a significantly differ between free drugs and nano drug carriers. However, the Nano drug carriers remarkably decreased the number of bacteria in the cell line compared to the free drugs. STR/HCQ-SLN enhanced the healing processes of the liver and spleen after brucellosis induction. STR/HCQ-SLN showed better inhibitory effects against the chronic phase of B. abortus infection in comparison to the STR-SLN, but this difference was not statistically significant. Using nanoplatforms to enhance conventional anti-brucellosis agents is promising, green and safe. Due to the continuous release of drugs, drugs increase their accumulation at the site of infection, causing a more significant effect on the chronic and acute phases of brucellosis.

A SHORT-TERM REVIEW ON SOLID LIPID NANOPARTICLES

In recent years, Solid lipid nanoparticles (SLNs) have been given a lot of attention as a potential drug distribution alternative to existing colloidal dispersion technologies. The use of SLNs as a pharmaceutical carrier has gotten a lot of focus in recent years. Nanostructure lipid carriers and SLNs are non-toxic since they are biodegradable. SLNs have various distinct properties in terms of therapeutic uses. SLNs are lipid-based nanocarriers with sizes ranging between 10 to 1000 nanometers. Decomposition of the drug can be protected by the drug entrapped in a lipid, physical stability; controlled drug release and remarkable acceptability are all benefits of SLNs over traditional drug carriers. The capacity to incorporate pharmaceuticals into nanocarriers opens up a new paradigm in drug delivery that could hold enormous promise in terms of improving bioavailability while also allowing for controlled and site-specific drug delivery. This article covers the manufacture and characterization of SLNs, as well as the administration and medicinal uses.

Perspectives and Prospective on Solid Lipid Nanoparticles as Drug Delivery Systems.

Combating multiple drug resistance necessitates the delivery of drug molecules at the cellular level. Novel drug delivery formulations have made it possible to improve the therapeutic effects of drugs and have opened up new possibilities for research. Solid lipid nanoparticles (SLNs), a class of colloidal drug carriers made of lipids, have emerged as potentially effective drug delivery systems. The use of SLNs is associated with numerous advantages such as low toxicity, high bioavailability of drugs, versatility in the incorporation of hydrophilic and lipophilic drugs, and the potential for production of large quantities of the carrier systems. The SLNs and nanostructured lipid carriers (NLCs) are the two most frequently used types of nanoparticles. These types of nanoparticles can be adjusted to deliver medications in specific dosages to specific tissues, while minimizing leakage and binding to non-target tissues.

Calorimetric Evaluation of Glycyrrhetic Acid (GA)- and Stearyl Glycyrrhetinate (SG)-Loaded Solid Lipid Nanoparticle Interactions with a Model Biomembrane.

Glycyrrhetic acid (GA) and stearyl glycyrrhetinate (SG) are two interesting compounds from Glycyrrhiza glabra, showing numerous biological properties widely applied in the pharmaceutical and cosmetic fields. Despite these appreciable benefits, their potential therapeutic properties are strongly compromised due to unfavourable physical-chemical features. The strategy exploited in the present work was to develop solid lipid nanoparticles (SLNs) as carrier systems for GA and SG delivery. Both formulations loaded with GA and SG (GA-SLNs and SG-SLNs, respectively) were prepared by the high shear homogenization coupled to ultrasound (HSH-US) method, and we obtained good technological parameters. DSC was used to evaluate their thermotropic behaviour and ability to act as carriers for GA and SG. The study was conducted by means of a biomembrane model (multilamellar vesicles; MLVs) that simulated the interaction of the carriers with the cellular membrane. Unloaded and loaded SLNs were incubated with the biomembranes, and their interactions were evaluated over time through variations in their calorimetric curves. The results of these studies indicated that GA and SG interact differently with MLVs and SLNs; the interactions of SG-SLNs and GA-SLNs with the biomembrane model showed different variations of the MLVs calorimetric curve and suggest the potential use of SLNs as delivery systems for GA.

Antitumor Activities of Co-loading Gemcitabine and Oxaliplatin into Oleic Acid-Based Solid Lipid Nanoparticle against Non-Small Cell Lung Cancer Cells

Lung cancer is a main global health problem with high incidence and case-fatality rates. The use of solid lipid nanoparticles (SLN) as a nanocarrier for chemotherapeutic agents has been suggested as an effective therapeutic approach. The current work objective was to investigate the antineoplastic activity of gemcitabine (GM) and oxaliplatin (OXA) co-loaded into oleic acid-based solid lipid nanoparticle (OA-SLN) in A549 non-small cell lung cancer cells. OA-SLN was synthesized using homogenization and physically characterized using the dynamic light scattering techniques. The anticancer properties of the combination of GM and OXA encapsulated in OA-SLN were evaluated using a series of cellular assays, such as cell viability using crystal violate, apoptosis using caspase-3 assay kit, and autophagy using human autophagy-related protein LC3-B ELISA kit. The z-average diameter of (GM+OXA) OA-SLN was (63.10 ± 1.53 nm). The (GM+OXA) OA-SLN formulation had significantly reduced cell growth in a dose-dependent manner on the A549 cells within 24 hours. The combination (GM+OXA) OA-SLN had more pronounced effects on autophagy (326.38 ± 4.21 pg/ml) than the untreated control cells (206.2 ± 6.69 pg/ml). Our findings indicate that co-encapsulation of GM and OXA into OA-SLN significantly improved their therapeutic efficacy against A549 cells.

Increased Therapeutic Efficacy of SLN Containing Etofenamate and Ibuprofen in Topical Treatment of Inflammation.

Innovative formulations, including solid lipid nanoparticles (SLNs), have been sought to improve skin permeation of non-steroidal anti-inflammatory drugs (NSAIDs). The present study explores the use of SLNs, prepared using a fusion-emulsification method, to increase skin permeation and in vivo activity of two relevant NSAIDs: A liquid molecule (etofenamate) and a solid one (ibuprofen), formulated in a 2% hydroxypropyl methylcellulose gel through the gelation of SLN suspensions. Compritol® 888 ATO and Tween® 80 were used as a solid lipid and a surfactant, respectively. All production steps were up scalable, resulting in SLNs with high encapsulation efficiency (>90%), a mean particle size of <250 nm, a polydispersity index <0.2, and that were stable for 12 months. In vitro permeation, using human skin in Franz diffusion cells, showed increased permeation and similar cell viability in Df and HaCaT cell lines for SLN formulations when compared to commercial formulations of etofenamate (Reumon® Gel 5%) and ibuprofen (Ozonol® 5%). In vivo activity in the rat paw edema inflammation model showed that SLN hydrogels containing lower doses of etofenamate (8.3 times lower) and ibuprofen (16.6 times lower) produced similar effects compared to the commercial formulations, while decreasing edema and inflammatory cell infiltration, and causing no histological changes in the epidermis. These studies demonstrate that encapsulation in SLNs associated to a suitable hydrogel is a promising technological approach to NSAIDs dermal application.

Toxicity studies of highly bioavailable isoniazid loaded solid lipid nanoparticles as per Organisation for Economic Co-operation and Development (OECD) guidelines

Solid lipid nanoparticles (SLNs) are presently being promoted to improve bioavailability of encapsulated drugs. These are well tolerated in living systems, as they are made from biocompatible material. Despite finding extensive applicability, these systems have not been sufficiently investigated for the toxicity so far. We have reported use of SLNs to improve plasma bioavailability of isoniazid (INH), a hepatotoxic, antitubercular drug. Presently we evaluate acute and repeated (28-day) oral dose toxicity, with satellite group, of developed INH loaded COMBI-SLN. In addition to high bioavailability, the COMBI-SLN exhibited 3 times higher LD50 (2000 mg/kg BW) versus 650 mg/kg BW for free INH. Results were complemented with histopathological evidence in brain, sciatic nerve and liver tissue all of which indicated enhanced safety of INH upon incorporation into SLNs. In the repeated dose study at doses selected as per Organisation for Economic Co-operation and Development (OECD) guidelines, a series of behavioural and haematological tests, clinical biochemistry (kidney and liver function, lipid profile) and histopathological studies were performed to evaluate the effect of low (250 mg/kg BW), medium (500 mg/kg BW) and high oral dose (1000 mg/kg BW). Absence of adverse effects like hepatotoxicity and peripheral neuropathy observed in rats at an oral intake level of 500 and 1000 mg/kg BW of COMBI-SLN, that is 20–40 folds above the anticipated human intake levels (after normalizing the surface area correction for rats), supports the conclusion that SLN are an intrinsically safe nanocarrier system that improves both the efficacy and the safety of INH.

Preparation of cetyl palmitate-based PEGylated solid lipid nanoparticles by microfluidic technique

In recent years, several studies have shown that the use of solid lipid nanoparticles (SLN) as a colloidal drug delivery system was more advantageous than lipid emulsions, liposomes and polymeric nanoparticles. SLNs have numerous advantages of different nanosystems and rule out many of their drawbacks. Despite the numerous advantages of SLNs, translation from the preclinical formulation to the industrial scale-up is limited. In order to provide a reproducible and reliable method of producing nanoparticles, and thus, obtain an industrial scale-up, several methods of synthesis of nanoparticles by microfluidic have been developed. Microfluidic technique allows a good control and a continuous online synthesis of nanosystems compared to synthesis in bulk, leading to a narrow size distribution, high batch-to-batch reproducibility, as well as to the industrial scale-up feasibility. This work described the optimization process to produce SLNs by microfluidics. The SLNs produced by microfluidics were characterized by complementary optical and morphological techniques and compared with those produced by bulk method. SLNs were loaded with paclitaxel and sorafenib, used as model drugs. The anti-cancer efficiency of the SLNs formulation was estimated with 2D and 3D tumour models of two different cell lines, and the cellular uptake was also studied with fluorescence-assisted measurements.

Use of Solid Lipid Nanoparticles for the Treatment of Acute Acoustic Stress-Induced Cochlea Damage.

To study the effects of drug delivery using solid lipid nanoparticles in the treatment of acute noise exposure-induced cochlea damage. The solid lipid nanoparticles (SLNs) were used as carriers to effectively encapsulate the drug clozapine, improve drug stability in the carrier system, and increase drug bioavailability in vivo. Solid lipid nanoparticles carrying clozapine were produced by ultrasonic technology. The clozapine solution or sulphate SLN was administered though intratympanic or intravenous injection on the first day of noise exposure Guinea pigs were exposed to 110 dB sound pressure level (SPL) noise (2 h per day with center frequencies of 0.25-4.0 kHz for 4 days). After noise exposure, the guinea pigs were subjected to auditory brainstem response (ABR) threshold measurements. Reactive oxygen species (ROS) levels were detected in the cochlea by electron spin resonance (ESR), and outer hair cell counts (OHCs) were obtained using silver nitrate (AgNO₃). SLN particles carrying clozapine exhibited protective effects on the cochlea. The threshold shift and ROS production in treated animals, especially in animals treated with clozapine SLN through intraperitoneal injection, were significantly lower than those in untreated animals.

A new agent for the treatment of lung cancer: B13 loaded solid lipid nanoparticles

Lung cancer is the leading cause of cancer-related deaths in humans. Recently, the effects of nano-carriers as chemotherapeutic agents on the treatment of lung cancer are in the main focus of cancer research. The use of solid lipid nanoparticles (SLNs) promises high hopes in treatment with the advantages of providing drug localisation in terms of action by both passive and active targeting based on their unique properties, including hydrophilic or hydrophobic loads. SLNs open new limits for long-term and side-specific drug delivery. In this study, a novel SLN of the ceramidase inhibitor, B13 (D-NMAPPD), with modified targeting property was designed, synthesised, and evaluated as potential anticancer agent on human lung cancer cells. Our results implied the efficiency of newly synthesised SLNs on lung cancer in the manner of anti-cancer activity with high cytotoxicity on cancer cells.

Solid Lipid Nanoparticles for Oral Drug Delivery: A Review

Background: The high molecular weight and increasing lipophilicity of drug face many problems starting from the drug development to formulation and conduction of pharmacological, toxicological and pharmacokinetic studies to its biological application. To overcome this problem, nano-sized formulations are in trend recently. The use of Solid lipid nanoparticles (SLNs) offers new insight into the formulation of the poor soluble and low bioavailable drug. Objective: The study aimed to investigate the literature concerning the development of SLNs for oral drug delivery of poorly soluble drugs, with a view survey the various methods of manufacturing and evaluation of formulation of SLNs and future prospects of SLNs and application of SLNs in oral delivery systems. Conclusion: Oral drug delivery is looking ahead progressively into newer directions due to the realization of various poor performance limiting factors such as reduced drug solubility or absorption, rapid metabolism, high actuation in plasma level of drug and variability caused due to food effect. These play a vital role in disappointing in vivo results, which leads in the failure of the conventional delivery system. Since the last decade, oral drug delivery has taken a new dimension with the increasing application of SLNs as a carrier for the delivery of poorly water-soluble or lipophilic drugs. The site-specific and sustained release effect of the drug is better achieved by using SLNs. This review highlights the various pros and cons, manufacturing techniques, characterization, and future prospects of SLNs in oral drug delivery systems.

Novel approach for overcoming the stability challenges of lipid-based excipients. Part 3: Application of polyglycerol esters of fatty acids for the next generation of solid lipid nanoparticles

Solid lipid nanoparticles (SLN) are an advantageous carrier system for the delivery of lipophilic active pharmaceutical ingredients (APIs). The use of SLN has been limited due to stability issues attributed to the unstable solid state of the lipid matrix. A novel approach for overcoming this problem is the application of polyglycerol esters of fatty acids (PGFAs) as lipid matrices with stable solid state. PG2-C18 full, a PGFA molecule, was used to develop SLN loaded with dexamethasone as a model API. Dexamethasone-loaded SLN were manufactured via melt-emulsification and high pressure homogenization in the dosage form of a lipid nanosuspension. SLN with median particle size of 242.1 ± 12.4 nm, zeta potential of −28.5 ± 7.8 mV, entrapment efficiency of 90.2 ± 0.7% and API released after 24 h of 81.7 ± 0.7%, were produced. Differential Scanning Calorimetry (DSC) and Small and Wide Angle X-Ray Scattering (SWAXS) analysis of the lipid nanosuspension evidenced the crystallization of PG2-C18 full in a monophasic system in α-form and absence of polymorphism and crystallite growth up to 6 months storage at room temperature. This resulted in stable performance of the SLN after storage: absence of particle agglomeration, no API expulsion, and stable release profile. The potential pulmonary administration of SLN was tested by the nebulization capacity of the lipid nanosuspension. Cellular exposures to SLN did not induce cytotoxicity or immune effect on pulmonary cells. The application of PGFAs as safe and stable lipid matrices provide a promising approach for the development of the next generation of SLN.

Brain uptake and accumulation of new levofloxacin-doxycycline combination through the use of solid lipid nanoparticles: Formulation; Optimization and in-vivo evaluation

The objective of this study is to investigate the feasibility of delivery of novel levofloxacin/ doxycycline (LEVO/DOX) combination to the brain by intranasal route to achieve a significant local concentration in the brain and a direct nose-to-brain pathway. Solid lipid nanoparticles (SLN) were selected as a drug carrier and employed Box–Behnken design for optimizing LEVO/DOX-SLN to achieve minimum particle size and maximum apparent entrapment efficiency (EE). SLNs were prepared by hot emulsification and characterized. In vitro release of optimized formulations showed prolonged drug release from the optimized formulation. The results of pharmacokinetic study of the optimized SLN-HPMC gel in plasma and brain revealed significant increase in the brain peak concentration (420, 315 ng/g), the AUC 0–360 min (57130 and 48693.13 ng. min/g) in comparison to intranasal LEVO/DOX free solution with the values of (160, 120) ng/g, (36850, 27637.5 ng⋅min/g) for LEVO and DOX, respectively. The optimized LD-SLN-HPMC gel gave a drug-targeting efficiency (DTE %) of 149.815 and 161.969 for LEVO and DOX, respectively, in comparison to the intravenous route. Moreover, the optimized formulation had a direct transport percentage (DTP %) of 33.285 and 40.236 for LEVO and DOX, respectively, which indicates a significant contribution of direct nose-to-brain pathway in brain drug delivery.

The use of new quinazolinone derivative and doxorubicin loaded solid lipid nanoparticles in reversing drug resistance in experimental cancer cell lines: A systematic study

The aim of this research is to study the feasibility of using carnauba wax as a new carrier for anticancer agents to deliver doxorubicin (DOX) as a model drug and a novel quinazolinone derivative (QZO-DER) to different types of normal and resistant cancer cell lines. A Box-Behnken design was implemented to investigate the influence of high melting point carnauba wax stabilized with cell membrane lipid (lecithin) and non-ionic biocompatible surfactant (span 60) in different concentration on particle size, entrapment efficiency of each drug and percent drug release. The solid lipid nanoparticles (SLNPs) were produced via the hot-melting homogenization technique. SLNPS particle size was from 16.58 ± 4 to 72.45 ± 1.21 nm and from 7.93 ± 1.67 to 174.31 ± 4.86 nm for DOX and QZO-DER respectively. Entrapment efficiency was from 51.78 ± 1.68% to 92.52 ± 2.47% and from 50.21 ± 1.8 to 82.95 ± 3.56% for DOX and QZO-DER respectively. While the percentage of release after 36 h was from 29.28 ± 3.89% to 78.08 ± 3.78% and from 37.5 ± 1.09 to 100 ± 1.25% for DOX and QZO-DER respectively. Selected formulations for DOX (OFX1 and OFX4) and QZO-DER (OFR4 and OFR6) were generated after validation of design. The in vitro anticancer activity was tested against both a panel of wild type and DOX-resistant human cancer cell lines. Cancer cell lines included colorectal cancer (HCT-116), breast cancer (MCF-7 and MDA-231), and lung adenocarcinoma (A549). Most of the tested SLNPs improved the efficacy of QZO-DER and DOX against the different cancer cell lines and have extended the spectrum to cover those accruing resistance during chemotherapy. QZO-DER loaded SLNPs exhibited the highest ability to reverse the drug resistance of MDA-231 cells compared to MDA-231/ADR cells was 19.7-fold, while DOX loaded SLNPs that showed reversal power was 1.8 fold for the same cells. Additionally, SLNPs showed a broad safety margin in normal cells. This study presented the use of SLNPs with carnauba wax as a potential therapeutic strategy to improve anticancer activity and overcome cancer resistance for clinical use.

SOLID LIPID NANOPARTICLES (SLNs) AS NANO DRUG DELIVERY CARRIERS: PREPARATION, CHARACTERIZATION AND APPLICATION

Over the last few years, there has been a significant consideration of solid lipid nanoparticles (SLNs) as an alternative method to other colloidal dispersion methods for drug delivery. Special consideration has been given to the use of SLNs as a drug carrier in recent years. SLNs are aqueous dispersions in which the colloidal particles consist of solid lipids that are biodegradable. As a result of their physical stability, the protection of the entrapped drug from decomposition, the provision of controlled drug release, and the exceptional acceptability, SLNs have several advantages over other drug carriers. This article focuses on the techniques of SLNs preparation and characterization, the effect of formulation variables on SLNs properties, the routes of administration, and the pharmaceutical applications. The data used for this review was collected by searching on Google Scholar and PubMed using the following keywords during the period from 2010 to date.

Solid Lipid Nanoparticles and Nanostructured Lipid Carriers: A Review of the Effect of Physicochemical Formulation Factors in the Optimization Process, Different Preparation Technique, Characterization, and Toxicity

Background:The high molecular weight and increasing lipophilicity drug face many problems starting from the drug development to formulation and conduction of pharmacological, toxicological and pharmacokinetic studies to its biological application. To overcome this problem, a different formulation of nano-sized drugs was developed recently. The use of Solid lipid nanoparticles (SLNs) and Nanostructured lipid carriers (NLCs) offers new insight into the formulation of the poorly soluble drug.Objective:The study aimed to investigate the literature with regard to the development of SLNs and NLCs for lipid-based nano drug delivery of poorly soluble drugs, with a view to identifying the factors influencing the optimization of the formulation of SLNs and NLCs and strategies to decrease the use of organic solvent during the preparation.Results:This review highlights the simple and easily scaled-up novel lipid nanoparticles (SLNs and NLCs) and their factors to be considered in the formulation for the proper selection of excipients. Also, this review summarizes the research findings reported by the different researchers regarding the principle formulation components, different preparation techniques, characterization, and toxicology of lipid nanoparticles.Conclusion:The SLNs/NLCs make this drug delivery system as one of the promising delivery systems, and safe colloidal lipid carriers for the delivery of poorly soluble drug and will be a solution to the formulation scientist for the solubility and permeability problem associated with the drugs to assure its good bioavailability.