Solid Lipid Nanoparticles Formulations Research Articles

Are Nanostructured Lipid Carriers (NLC) better than Solid Lipid Nanoparticles (SLN) for delivering abiraterone acetate through the gastrointestinal tract?

Abiraterone acetate (AbA) is a progesterone derivative indicated for the treatment of metastatic prostate cancer. This BCS (Biopharmaceutics Classification System) Class IV molecule has an extremely poor oral bioavailability (<10 %), notably due to its very low water solubility and intestinal permeability. Among the few existing galenic strategies to improve AbA’s oral bioavailability, lipid nanoparticles such as Solid Lipid Nanoparticles (SLN) and Nanostructured Lipid Carriers (NLC) are relevant nanovectors. The objective of this study is to develop and compare SLN and NLC for oral delivery of abiraterone acetate. Both SLN and NLC are biocompatible, biodegradable and produced by high pressure homogenization (HPH), an ecological-friendly manufacturing process, organic solvent-free and easily scalable. The HPH process allowed the formation of AbA-loaded SLN and NLC with particle size lower than 160 nm and high encapsulation efficiencies. The addition of a liquid lipid significantly reduced the mean diameter of the nanoparticles, reflecting the greater benefit of the NLC formulation compared to SLN. Both SLN and NLC formulations offered an important protection of AbA in intestinal media, with a better stability for NLC. When encapsulated in SLN or NLC, the AbA is strongly retained by the nanoparticles, whatever the dissolution medium, which means that both formulas are able to protect and retain the drug in the intestinal tract, right up to its delivery to the enterocytes surface. High concentrations of nanoparticles were administered without cytotoxicity, especially for the NLC, which provides a real added value in terms of biocompatibility with Caco-2 cells. Finally, the nanoparticles were able to penetrate into enterocytes by the transcellular route, demonstrating an intense cellular internalization.

“Formulation and Evaluation of Solid Lipid Nanoparticles by using High-Pressure Homogenization Technique for the Treatment of Cancer”

“Formulation and Evaluation of Solid Lipid Nanoparticles by using High-Pressure Homogenization Technique for the Treatment of Cancer”

Epigallocatechin-3-gallate Synergistically Inhibits the Proliferation of Lung Cancer Cells with Gemcitabine by Induction of Apoptosis Mediated by ROS Generation.

The present study focused on the formulation, characterization, and evaluation of solid lipid nanoparticles (SLNs) loaded with gemcitabine (GEM) and epigallocatechin-3-gallate (EGCG) for lung cancer treatment. A 2-level, 3-factor factorial design was used to optimize various process parameters in the preparation of SLNs. The average particle size and polydispersity index (PDI) of GEM-EGCG SLNs were found to be 122.8 ± 8.02 and 0.1738 ± 0.02, respectively. Drug loading and release studies indicated a sustained release behavior for GEM-EGCG SLNs, with release kinetics confirmed by the Higuchi model. Cell viability and anticancer activities were assessed using the MTT assay, which determined an IC50 value of 12.5 μg/mL for GEM-EGCG SLNs against A549 cell lines (lung carcinoma epithelial cells). The SLNs were able to internalize into the nuclei of cells, likely due to their small particle size, and were effective in killing cancer cells. Additionally, a study of ROS production-mediated apoptosis of A549 cells was performed through FACS. GEM-EGCG SLNs were found to be stable for 3 months. In vivo studies revealed better drug distribution in the lungs and improved pharmacokinetic profile compared with pure drugs. Overall, the results suggest that combining GEM and EGCG in biocompatible SLNs has resulted in synergistic antitumor potential and improved bioavailability for both drugs, making it a promising anticancer therapeutic regimen against lung cancer.

Hyaluronic acid-solid lipid nano transporter serum preparation for enhancing topical tretinoin delivery: skin safety study and visual assessment of skin.

The use of nanosized particles is becoming more popular for the topical treatment of skin conditions. In this research work, we created and investigated the effects of solid lipid nanoparticles (SLN) containing hyaluronic acid and tretinoin. Solvent emulsification diffusion method was used to prepare the SLN formulation and characterized for their physicochemical properties. Fourier transform infrared spectroscopy was used to confirm that hyaluronic acid and tretinoin were incorporated in the SLN. Furthermore, X-ray diffractogram, thermal analysis including DSC and TGA and in vitro dissolution, permeation tests were also performed along with microbial assessment. Clinical studies in human were performed to evaluate the effect of the SLN on skin wrinkles. The SLN was 750 ± 31.29nm in size, with a zeta potential of 13.07 ± 0.75mV and a narrow polydispersity index of 0.24 ± 0.12. The entrapment efficiency of tretinoin was found to be 90.07 4.79%. Clinical studies in healthy human volunteers demonstrated that 90% of the tested individuals had improved skin conditions (reduction in wrinkles), by at least one grade after 4weeks of treatment. Regarding the development on SLN, it was found that the internal phase concentration did not considerably affect the physicochemical and microbiological properties. Therefore, Hyaluronic acid has potential for the development of SLN applicable to cosmetic formulations, especially for skin. These findings show that the developed SLN have potential for use as cosmetics in the future.

Design and Optimization of Solid Lipid Nanoparticles for Enhanced Therapeutic Activity of Linagliptin.

To augment oral bioavailability, linagliptin (LGP) loaded solid lipid nanoparticles (SLNs) have been formed using the solvent evaporation technique of emulsification. Utilizing the Box Behken design (BBD), examining the relation between independent and dependent variables was possible. Particle size (PS), entrapment efficiency (EE), and in-vitro drug release (DR) studies were considered response factors, whereas the various concentrations of lipid carrier, surfactant, and co-surfactant were considered process variables for optimization. The design expert program was used to obtain the optimized batch. At 24 hours, it was discovered that the optimized batch expected responses for PS, %EE, and %DR were 105.83 nm, 81.19, and 96.69%, respectively. The observed PS, %EE, and %DR responses of the optimized batch at 24 hours were determined to be 101.36 nm, 80.56, and 96.31%, respectively. There is no interaction seen in the basic physical mixing of drug and polymer, according to the FTIR spectra of pure drugs, polymers, and drug and polymer mixtures. The optimized formulation’s average size was found to be 138 nm by the particle size analysis. Similarly, a value of 0.255 was found by the polydispersity index (PDI). This suggests that the SLN in the formulation has a homogeneous size dispersion. With a zeta value of -32.8 mV, stability is indicated. Linagliptin was effectively developed as a drug with a 24-hour sustained release. Wistar rats were used in the in-vivo evaluation of linagliptin SLN formulations. The drug bioavailability increased five times (a highly significant fivefold increase) in LGP-loaded SLNs (AUC0-t ≈ 134.5 μg*h/mL) compared to raw LGP (AUC0-t = 27.23 μg*h/mL).

Chondroitin Sulfate for Cartilage Regeneration, Administered Topically Using a Nanostructured Formulation.

In the pharmaceutical sector, solid lipid nanoparticles (SLN) are vital for drug delivery incorporating a lipid core. Chondroitin sulfate (CHON) is crucial for cartilage health. It is often used in osteoarthritis (OA) treatment. Due to conflicting results from clinical trials on CHON's efficacy in OA treatment, there has been a shift toward exploring effective topical systems utilizing nanotechnology. This study aimed to optimize a solid lipid nanoparticle formulation aiming to enhance CHON permeation for OA therapy. A 3 × 3 × 2 Design of these experiments determined the ideal parameters: a CHON concentration of 0.4 mg/mL, operating at 20,000 rpm speed, and processing for 10 min for SLN production. Transmission electron microscopy analysis confirmed the nanoparticles' spherical morphology, ensuring crucial uniformity for efficient drug delivery. Cell viability assessments showed no significant cytotoxicity within the tested parameters, indicating a safe profile for potential clinical application. The cell internalization assay indicates successful internalization at 1.5 h and 24 h post-treatment. Biopharmaceutical studies supported SLNs, indicating them to be effective CHON carriers through the skin, showcasing improved skin permeation and CHON retention compared to conventional methods. In summary, this study successfully optimized SLN formulation for efficient CHON transport through pig ear skin with no cellular toxicity, highlighting SLNs' potential as promising carriers to enhance CHON delivery in OA treatment and advance nanotechnology-based therapeutic strategies in pharmaceutical formulations.

The Science of Solid Lipid Nanoparticles: From Fundamentals to Applications.

Solid lipid nanoparticles (SLNs) play a crucial role in drug delivery, offering benefits such as enhanced bioavailability, targeted distribution, and reduced toxicity. This article provides a comprehensive overview of SLN formulation, development, and advancement in pharmaceutical research, examining their characteristics, classifications, and significance. The review also delves into the real-world applicability of various SLN formulations across different routes of administration, discussing their advantages, disadvantages, and challenges of scalability, along with strategies for efficient implementation. Furthermore, it explores the diverse applications of SLNs through various delivery methods, addressing the obstacles and potential solutions. By highlighting the critical role of SLNs in improving treatment outcomes, this review underscores their importance in modern drug delivery systems.

Development of formulation and evaluation of topical micro emulsion gel loaded with terbinafine HCL micro emulsion

Fungal infections, particularly in immunocompromised patients, present significant health challenges and are often difficult to treat with conventional topical therapies due to bioavailability issues. This study explores the development of a topical gel formulation using solid lipid nanoparticles (SLNs) loaded with Terbinafine, an antifungal agent, to improve drug delivery and efficacy. SLNs were prepared by a solvent diffusion method and optimized with stearic acid and poloxamer 188. The formulation with the highest entrapment efficiency (SLN F6) exhibited 92.13% ± 0.975. The optimized SLN formulation was incorporated into a gel base containing carbopol 934, resulting in SLN gel G3 with 1.5% carbopol showing the highest drug entrapment (91.39% ± 0.187). The gel was evaluated for physicochemical properties, including viscosity (369 cP), pH (6.12 ± 0.255), and spreadability (4.5). In vitro release studies indicated controlled drug release, fitting best with the Higuchi and Korsmeyer-Peppas models. FTIR analysis confirmed no significant interactions between the drug and excipients, supporting the formulation's purity and effectiveness. Scanning electron microscopy (SEM) confirmed the spherical shape and smooth surface of the nanoparticles. This study demonstrates that Terbinafine-loaded SLNs in a topical gel formulation provide a promising approach for sustained drug delivery in treating fungal infections.

IN VITRO EVALUATION OF THE ANTIBACTERIAL EFFECT OF CHITOSAN COATED TEICOPLANIN-LOADED LIPID NANOPARTICLES AGAINST STAPHYLOCOCCUS AUREUS

Objective: The aim of this research is to formulate teicoplanin-loaded solid lipid nanoparticles (SLN) coated with chitosan to sustain teicoplanin release for effective antibacterial therapy. Material and Method: “Double emulsion-solvent evaporation technique was used for the production of SLNs. The nanoparticles were characterised in terms of morphology, size, encapsulation efficacy, in-vitro drug release and antibacterial activity studies after optimization of process and formulation parameters. Result and Discussion: Transmission electron microscopy images confirmed the formation of spherical SLNs. With chitosan coating, the size increased (from 80 nm to 106 nm) and the negative value of zeta potential (- 11.29) changed to positive (+34.41). The in-vitro release data showed prolonged release of teicoplanin from optimized SLN and chitosan-coated SLN (c-SLN) formulations over 1 week. The antibacterial activity study (S. aureus and Methicillin-resistant S. aureus) showed the activity of the teicoplanin loaded SLN formulations. In conclusion, this study demonstrated the potential of c-SLN for effective delivery of teicoplanin.

PREPARATION OF LIPID-BASED FORMULATIONS USING LOCAL BEESWAX SOURCED FROM HONEYCOMBS

Solid lipids used in formulation of novel drug delivery systems in most developing countries are sourced from abroad and are quite expensive. Wax from honeycombs is readily available, and is even disposed as waste, but can be utilized as a solid lipid for the formulation of different lipid-based drug delivery systems. This study aims to formulate and compare the features of the solid lipid nanoparticle (SLNs) and nanostructured lipid carrier (NLCs) delivery systems of quinine hydrochloride made with local beeswax (that is beeswax from locally sources honeycomb waste) and other solid lipids sourced from abroad. Local beeswax was first purified by hot bath method. Solidified reverse micellar solutions (SRMS) were prepared by fusion method using Phospholipon®90H and either local beeswax, Softisan®154, foreign beeswax, or stearic acid, separately. SLNs and NLCs of quinine made with SRMS of each of these solid lipids were formulated using hot homogenization method. These SLNs and NLCs were characterized. The average particle size of SLNs and NLCs made with local beeswax was 93.60 ± 4.44 nm and 112.80 ± 3.89 nm, respectively, and was not significantly (p &gt; 0.05) different from the sizes of formulations made from other solid lipids (SLNs: 96.64 to 118.9 ± 4.13 nm and NLCs: 99.68 ± 6.75 to 117.30 ± 4.60 nm). The particles were monodispersed having PDI ranging from 0.281±0.054 to 0.308±0.055. Encapsulation efficiency and loading capacity were generally poor, especially among the SLN formulations. However, SLNs made with local beeswax and stearic acid were able to encapsulate quinine, whereas foreign beeswax and Softisan®154 had zero encapsulation. This study reveals that the features of the SLNs and NLCs made with local beeswax where highly comparable with those formulated with the imported solid lipids. Therefore, local beeswax can serve as a suitable affordable and available alternative to other imported solid lipids for formulating different lipid drug delivery systems.

Optimization of Solid Lipid Nanoparticle Formulation for Cosmetic Application Using Design of Experiments, PART II: Physical Characterization and In Vitro Skin Permeation for Sesamol Skin Delivery

Our research focuses on evaluating the preliminary stability of solid lipid nanoparticles (SLNs) in order to identify an optimal formulation for studying the skin penetration of SLNs loaded with sesamol, with a view to developing potential cosmetic applications. For this study, SLNs were prepared with varying lipid and surfactant compositions and produced through homogenization and ultrasonication. The particle size (PS), polydispersity index (PDI), zeta potential (ZP), and encapsulation efficiency (EE) were analyzed for the different formulations. We identified OP2Se as the optimal formulation for skin penetration assessment due to its stable PS, PDI, ZP, and EE over time, with a Turbiscan Stability Index (TSI) below 1 after a month, indicating favorable stability conditions. The in vitro skin permeation study compared sesamol-loaded SLNs with a control sesamol hydrogel, revealing controlled release characteristics ideal for localized skin effects without significant bloodstream penetration, attributed to the SLNs’ 200 nm particle size. Further exploration could enhance skin retention and targeting, potentially extending penetration studies and reducing particle size to improve accumulation in hair follicles. Exploring SLN applications beyond sesamol, such as incorporating mineral filters for suncare, offers promising avenues, underscoring SLNs’ versatility in cosmetic formulations and skincare applications.

A Quality by Design Approach for Optimizing Solid Lipid Nanoparticles of Bedaquiline for Improved Product Performance.

Bedaquiline (BQ) solid lipid nanoparticles (SLNs), which have previously been formulated for parenteral administration, have a risk of patient non-compliance in treating tuberculosis. This research presents a strategy to develop BQ SLNs for oral delivery to improve patient adherence, The upper and lower levels for the formulation excipients were generated from screening experiments. Using 4 input factors (BQ, lecithin, Tween 80, and PEG), a full factorial design from 3 × 2x2 × 2 experiments was randomly arranged to investigate 3 response variables: Particle size distribution (PSD), polydispersity index (PdI), and zeta potential (ZP). High shear homogenization was used to mix the solvent and aqueous phases, with 15% sucrose as a cryoprotectant. The response variables were assessed using a zeta sizer while TEM micrographs confirmed the PSD data. Solid-state assessments were conducted using powdered X-ray diffraction and scanning electron microscopy (SEM) imaging. A comparative invitro assessment was used to determine drug release from an equivalent dose of BQ free base powder and BQ-SLN, both packed in hard gelatin capsules. The sonicated formulations obtained significant effects for PSD, PdI, and ZP. The p-values (0.0001 for PdI, 0.0091 for PSD) for BQ as an independent variable in the sonicated formulation were notably higher than those in the unsonicated formulation (0.1336 for PdI, 0.0117 for PSD). The SEM images were between 100 - 400nm and delineated nanocrystals of BQ embedded in the lipid matrix. The SLN formulation provides higher drug levels over the drug's free base; a similarity factor (f2 = 18.3) was estimated from the dissolution profiles.

Microfluidic formulation of diazoxide-loaded solid lipid nanoparticles as a Novel approach for Friedreich's ataxia treatment

Friedreich ataxia (FRDA) is a hereditary autosomal recessive disorder characterized by frataxin deficiency, impacting mitochondrial function and causing oxidative damage. Diazoxide (DZX), a vasodilating drug used in the management of systemic hypertension, has shown promise in preclinical models but faces challenges in crossing the blood-brain barrier and potential toxicity at higher doses. This study aimed to create solid lipid nanoparticles (SLNs) loaded with DZX by microfluidic technique to improve blood-brain barrier (BBB) penetration and reduce side effects. Employing an in vitro BBB model, SLN-DZX demonstrated enhanced permeability compared to plain DZX. Cell viability assays carried out on FRDA fibroblast cells indicated enhanced viability with 1 μM SLN-DZX. Cellular uptake studies confirmed SLN internalization in FRDA fibroblasts, and subsequent treatment with SLN-DZX significantly reduced both total and mitochondrial ROS levels compared to control and empty SLN-treated cells. These findings suggest SLN-DZX as a potential therapeutic approach for FRDA, mitigating oxidative stress with improved BBB penetration and reduced toxicity.

In-vitro and In-silico Examinations on Baicalein-loaded Solid Lipid Nanoparticles for Neurodegeneration

Background:: In the current scenario, most of the population affected by neurogenera-tive disorders like Alzheimer's, Parkinson's, Huntington's, etc., exist among the 10% population 65 years of age group. Neurodegenerative diseases are characterised as chronic and progressive disorders that occur due to the degeneration of neurons. Baicalein is a flavonoid glycoside derived from the roots of Scutellaria baicalensis. Earlier research suggested that it could be used to treat neurodegenerative illnesses. Baicalein, which was selected for the current study, was designed in-to a solid lipid nanoparticle (SLN) formulation. The SLNs have low permeability across BBB and are delivered by the non-invasive route, i.e., through nasal delivery. The In-silico docking studies were performed to examine and compare the binding affinity of Baicalein to already established drugs on the two most viable targets of Alzheimer's disease, i.e., Beta- secretase and Acetylcho-linesterase. Objective:: The current work is to formulate and evaluate the Baicalein-loaded SLN for neuro-degenerative disorders via a non-invasive route. Methods:: Baicalein loaded SLN was developed by solvent emulsification diffusion method, and formulation is characterised by using different parameters such as particle size analysis, zeta po-tential, scanning electron microscope, transverse electron microscope, X-ray diffraction, Differen-tial scanning calorimetric, Fourier transforms -infrared radiations, drug entrapment, in-vitro drug release and in-silico docking studies. Results:: The particle size of Baicalein-loaded SLN was 755.2 ± 0.48 nm, the Polydispersity index was 0.06, and the zeta potential was -32.5 ± 0.36 mV. The drug entrapment and loading efficien-cy of the optimised formulation were found to be 94% ± 0.653 and 18.2% ± 0.553, respectively. Optimised formulation shows 84.6% ± 0.3% of drug release within 30 minutes, which demon-strates the sustained release of the drug. Conclusion:: Baicalein-loaded SLN is formulated and evaluated for the treatment of neurodegen-erative disorders. SLN is an approach to overcome the challenge of bypassing the BBB by admin-istering the drug via an intranasal route. Hence, when analysed together with the results of Bai-calein-loaded SLN and in-silico studies, it was correlated that Baicalein proved to have a targeted moiety for neurodegeneration.

Solid lipid nanoparticle: A potent vehicle of the kaempferol for brain delivery through the blood-brain barrier in the focal cerebral ischemic rat

Kaempferol is major flavonoid present in Convolvulus pluricaulis. This phytochemical protects the brain against oxidative stress, neuro-inflammation, neurotoxicity, neurodegeneration and cerebral ischemia induced neuronal destruction. Kaempferol is poorly water soluble. Our study proved that solid lipid nanoparticles (SLNs) were efficient carrier of kaempferol through blood-brain barrier (BBB). Kaempferol was incorporated into SLNs prepared from stearic acid with polysorbate 80 by the process of ultrasonication. Mean particle size and zeta potential of kaempferol loaded solid lipid nanoparticles (K-SLNs) were 451.2 nm and −15.0 mV. Atomic force microscopy showed that K-SLNs were spherical in shape. Fourier transformed infrared microscopy (FTIR) showed that both stearic acid and kaempferol were present in K-SLNs. X-ray diffraction (XRD) and differential scanning calorimetry (DSC) revealed that the matrices of K-SLNs were in untidy crystalline state. Entraptment efficiency of K-SLNs was 84.92%. In-vitro drug release percentage was 93.24%. Kaempferol loaded solid lipid nanoparticles (K-SLNs) showed controlled release profile. In-vitro uptake study showed significant efficiency of K-SLNs to cross blood-brain barrier (BBB). After oral administration into the focal cerebral ischemic rat, accumulation of fluorescent labeled K-SLNs was observed in the brain cortex which confirmed its penetrability into the brain. It significantly decreased the neurological deficit, infarct volume and level of reactive oxygen species (ROS) and decreased the level of pro-inflammatory mediators like NF-κB and p-STAT3. Damaged neurons and brain texture were improved. This study indicated increased bioavailability of kaempferol into the brain tissue through SLNs formulation.

The mechanistic insights of essential oil of Mentha piperita to control Botrytis cinerea and the prospection of lipid nanoparticles to its application

Botrytis cinerea is the phytopathogenic fungus responsible for the gray mold disease that affects crops worldwide. Essential oils (EOs) have emerged as a sustainable tool to reduce the adverse impact of synthetic fungicides. Nevertheless, the scarce information about the physiological mechanism action and the limitations to applying EOs has restricted its use. This study focused on elucidating the physiological action mechanisms and prospection of lipid nanoparticles to apply EO of Mentha piperita. The results showed that the EO of M. piperita at 500, 700, and 900 μL L−1 inhibited the mycelial growth at 100 %. The inhibition of spore germination of B. cinerea reached 31.43 % at 900 μL L−1. The EO of M. piperita decreased the dry weight and increased pH, electrical conductivity, and cellular material absorbing OD260 nm of cultures of B. cinerea. The fluorescence technique revealed that EO reduced hyphae width, mitochondrial activity, and viability, and increased ROS production. The formulation of EO of M. piperita loaded- solid lipid nanoparticles (SLN) at 500, 700, and 900 μL L−1 had particle size ∼ 200 nm, polydispersity index < 0.2, and stability. Also, the thermogravimetric analysis indicated that the EO of M. piperita-loaded SLN has great thermal stability at 50 °C. EO of M. piperita-loaded SLN reduced the mycelial growth of B. cinerea by 70 %, while SLN formulation (without EO) reached 42 % inhibition. These results supported that EO of M. piperita-loaded SLN is a sustainable tool for reducing the disease produced by B. cinerea.

Improving antifungal effect of peppermint essential oil

Nanoencapsulation of essential oils is a promising strategy for extending their antifungal activity and addressing evaporation and decomposition in unfavorable environmental conditions. This research aimed to synthesize and compare the physical properties of solid lipid nanoparticles (SLNs) containing peppermint essential oil (PE) during 12 months of storage at various temperatures (4°C, 25°C, 27°C with 60% relative humidity, 37°C, and 40°C with 75% relative humidity), and to investigate their antifungal activity compared to free PE. The SLN formulations were prepared using high-shear homogenization and ultrasound techniques and were analyzed using a particle size analyzer, differential scanning calorimetry, transmission electron microscopy, and microscopic images of fungal mycelium to assess encapsulation efficacy. The results showed that the PE-SLNs had a size of 164.2 ±5.8 nm, a PDI value of 0.176 ±0.01, a zeta potential value of –11.3 mV, and an encapsulation percentage of approximately 75 ±0.5%. Overall, the physical properties of the formulations showed a slight and acceptable increase over the 12-month storage period at all investigated temperatures. Furthermore, the in vitro inhibition percentage of free PE at a concentration of 2000 μL L–1 against Penicillium italicum and P. digitatum was 66.7% ±2.6 and 66.8% ±0.8, respectively, while for PE-SLNs it was 88.8% ±0.9 and 89.9% ±1.4. These results demonstrate the potential of SLNs as an effective carrier for sustained delivery of PE with improved antifungal activity during storage.

Examination of the effects of vitexin and vitexin-loaded solid lipid nanoparticles on neuropathic pain and possible mechanisms of action

This research aims to investigate the possible antiallodynic and antihyperalgesic effects of pure vitexin and vitexin-loaded solid lipid nanoparticles (SLN) on neuropathic pain and the pathways mediating these effects. Chronic constriction nerve injury was induced in female rats, and the effects of vitexin at the doses of 5, 10, 20, 40 mg/kg were evaluated. Ketanserin, ondansetron, WAY-100635, yohimbine and bicuculin, which are antagonists of receptors on pain pathways. were used to examine the mechanisms of the effects of vitexin. Pure vitexin exhibited antiallodynic activity at all administered doses, whereas antihyperalgesic activity was not observed at 5 mg/kg vitexin dose. SLN formulation was prepared with 5 mg/kg vitexin, the lowest dose. Vitexin-loaded formulation significantly increased antiallodynic and antihyperalgesic effects. Ondansetron, WAY-100635, yohimbine, and bicuculine antagonized the antiallodynic and antihyperalgesic effects of vitexin. So, it was concluded that serotonin (5-hydroxtryptamine, 5-HT) receptor subtypes 5-HT3 and 5-HT1A, alpha-2 adrenergic, and γ-Aminobutyric acid type A (GABA-A) receptors are involved in the antiallodynic and antihyperalgesic activity of vitexin. In conclusion, vitexin and vitexin-loaded formulation have the potential for clinical use in neuropathic pain management, and different pain pathways contributed to this effect. And also, it is thought that vitexin-loaded SLN formulation is more effective than pure vitexin, which will provide an advantage in treatment.

Dopamine- and Grape-Seed-Extract-Loaded Solid Lipid Nanoparticles: Interaction Studies between Particles and Differentiated SH-SY5Y Neuronal Cell Model of Parkinson's Disease.

Parkinson's disease (PD) is a prevalent neurodegenerative disorder, primarily associated with dopaminergic neuron depletion in the Substantia Nigra. Current treatment focuses on compensating for dopamine (DA) deficiency, but the blood-brain barrier (BBB) poses challenges for effective drug delivery. Using differentiated SH-SY5Y cells, we investigated the co-administration of DA and the antioxidant Grape Seed Extract (GSE) to study the cytobiocompability, the cytoprotection against the neurotoxin Rotenone, and their antioxidant effects. For this purpose, two solid lipid nanoparticle (SLN) formulations, DA-co-GSE-SLNs and GSE-ads-DA-SLNs, were synthesized. Such SLNs showed mean particle sizes in the range of 187-297 nm, zeta potential values in the range of -4.1--9.7 mV, and DA association efficiencies ranging from 35 to 82%, according to the formulation examined. The results showed that DA/GSE-SLNs did not alter cell viability and had a cytoprotective effect against Rotenone-induced toxicity and oxidative stress. In addition, this study also focused on the evaluation of Alpha-synuclein (aS) levels; SLNs showed the potential to modulate the Rotenone-mediated increase in aS levels. In conclusion, our study investigated the potential of SLNs as a delivery system for addressing PD, also representing a promising approach for enhanced delivery of pharmaceutical and antioxidant molecules across the BBB.

Antidiabetic Drug-loaded Solid Lipid Nanoparticle and Its Importance in Drug Delivery

The global health challenge of diabetes mellitus continues to escalate, affecting millions of people worldwide. Managing this chronic condition necessitates lifelong treatment to control hyperglycemia and prevent complications. The delivery of antidiabetic medications can be improved by solid lipid nanoparticles (SLNs). This review provides an overview of current research on antidiabetic-loaded SLNs, summarizing their efficacy, safety, and challenges. Various antidiabetic agents, including insulin, metformin, sulfonylureas, and GLP-1 agonists, have been successfully encapsulated into SLNs, offering improved pharmacokinetic profiles and therapeutic outcomes. Despite their potential, optimization of SLN formulations, scale-up challenges, and translation to clinical practice remain areas requiring further investigation. With ongoing advancements in nanotechnology and drug delivery, antidiabetic-loaded SLNs hold promise for revolutionizing diabetes therapy and improving patient care