Nanostructured Lipid Carriers Research Articles

Essential Oils as Dermocosmetic Agents, Their Mechanism of Action and Nanolipidic Formulations for Maximized Skincare

Essential oils (EOs) are known for their diverse bioactivities, including antioxidant, anti-inflammatory, antibacterial, antifungal, antiviral, skin-barrier repairing and anticancer, and therefore, hold profound potential to be used in cosmetic and skincare products. Owing to these properties, EOs have long been utilized to address a range of dermatological issues, from acne and inflammation to aging and dryness. However, problems associated with EOs beset their practical applications, which include high volatility, oxidation, hydrophobic nature, low bioavailability, skin irritation, chemical transformation and poor stability in air and light. A prospective of nanolipidic formulations, including the nanostructured lipid carriers (NLCs) and solid lipid nanoparticles (SLNs) system for improved skin delivery of these EOs highlights the possibility of their use in topical applications, which offer several advantages such as improved bioavailability and stability, lower toxicity and higher drug content. These nanoformulations protect the EOs from environmental degradation and improve their penetration into deeper skin layers, leading to prolonged therapeutic benefits. The delivery of bioactive agents using a conventional topical preparation exhibits low penetration, frequent applications, poor adherence and prolonged therapy duration, whereas the novel delivery system exhibits improved stability of the drug, enhanced skin penetration, enhanced retention and better therapeutic efficacy. This review provides a comprehensive compendium of information on EOs, which are widely used in skincare, along with their nanolipidic formulations for maximized skincare uses. The mechanism of action of EOs as skin bioactive agents, challenges associated with their use, advances in nanolipidic formulations and their market value as cosmetic skincare products are also explored.

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.

Transdermal delivery of Acheta domesticus protein hydrolysate using nanostructured lipid carriers and Derma Stamp ― Does the combination of lipid-based formulation and a physical technique add value for permeation and retention?

Acheta domesticus protein hydrolysate (PH) is a natural anti-skin aging compound, but its effectiveness is hindered by poor skin penetration due to its hydrophilicity and high molecular weight. This study aimed to compare the enhancement of PH skin delivery by increasing lipophilicity with nanostructured lipid carriers (NLCs) and bypassing the skin barrier using physical techniques, including Derma Stamp and dissolving microneedles (MNs). Fluorescein isothiocyanate (FITC)-tagged PH was prepared to track the transdermal transport, and complexed with dioctyl sodium sulfosuccinate (DSS) to be encapsulated into NLCs, prepared using a melt emulsification method. Skin delivery was evaluated in terms of skin permeation and skin retention using Franz diffusion cells. The FITC-PH loaded NLCs had a particle size of 238.9 ± 0.8 nm, a polydispersity index of 0.3 ± 0.0, a zeta potential of −23.6 ± 1.0 mV, and an encapsulation efficiency of 65.1 ± 2.1%. The MNs, prepared with polyvinylpyrrolidone K30 and polyvinyl alcohol (38:15 weight ratio), had uniform sharp needles and a high FITC-PH loading capacity of 97.2 ± 1.9%. PH permeation was most effectively enhanced through physical barrier bypassing, particularly with the Derma Stamp, followed by MNs and finally due to incorporation into NLCs. Notably, when utilizing the Derma Stamp, converting the aqueous solution of PH into an NLC formulation added positive benefits by significantly improving skin retention. In conclusion, it was suggested that while physical enhancement methods are crucial for permeation of the PH, optimizing formulation characteristics, such as incorporation into NLCs, further increased the overall effectiveness of skin delivery.

Nanostructured Lipid Carrier-Mediated Transdermal Delivery System of Glibenclamide for Gestational Diabetes: Pharmacokinetic and Pharmacodynamic Evaluation.

Gestational diabetes mellitus (GDM) poses significant risks during pregnancy for both mother and fetus. Adherence to oral antidiabetic medications, like glibenclamide (GB), can be challenging, necessitating novel drug delivery methods. Nanostructured lipid carriers (NLC) offer a promising approach by efficiently permeating the skin due to their small size and lipid-based composition. This study aimed to develop and evaluate transdermal patches loaded with glibenclamide NLCs to treat GDM. Glibenclamide NLCs were prepared using hot homogenization with ultrasonication and melt dispersion method. A central composite design was utilized to optimize the formulations. Transdermal patches containing optimized NLCs were developed using HPMC K 100 and Eudragit L polymers. The patches were evaluated for various parameters, and their pharmacokinetic and pharmacodynamic studies were carried out to assess their safety and efficacy. Optimized NLCs efficiently permeated rat skin. Cell viability studies indicated the nontoxicity of the formulations. NLC-loaded transdermal patches (F2 and F7) showed drug release of 1098 μg/cm2 and 1001.83 μg/cm2 in 24 h, with a 2.5-fold higher flux and permeation coefficient than the GB patch. Pharmacokinetic analysis revealed Tmax of 8 and 10 h and Cmax of 7127 ng/ml and 7960 ng/ml for F2 and F7, respectively, ensuring sustained drug action. AUC0-α was 625681 ng/ml·h and 363625 ng/ml·h for F2 and F7, respectively, indicating improved bioavailability. Transdermal patches incorporating NLCs hold promise for enhancing glibenclamide's therapeutic efficacy in GDM treatment. Improved skin permeation, sustained drug release, and enhanced bioavailability make NLC-based transdermal patches a potential alternative with better patient compliance.

Preparation and Characterization of Nanostructured Lipid Carriers (NLCs) Containing Glycyrrhiza glabra Extract for the Treatment of Skin Hyperpigmentation.

This study aimed to prepare, characterize, and in vitro and in vivo evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of Glycyrrhiza glabra L. (licorice) extract for the treatment of hyperpigmentation. Two fractions, one enriched with glabridin (FEG) and the other enriched with liquiritin (FEL), were obtained by partitioning the methanol (MeOH) extract of licorice roots with ethyl acetate (EtOAc) and partitioning the EtOAc fraction with butanol (n-BuOH) and water. The quantities of glabridin (Glab) and liquiritin (LQ) in the fractions were determined by high-performance liquid chromatography (HPLC). FEG and FEL were loaded in different NLC formulations, and surface characterization and long-term stability were studied using Dynamic Light Scattering (DLS). The best formulation was chosen for further surface characterization, including Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC), and Fouriertransform infrared (FTIR) spectroscopy. Moreover, entrapment efficiency percentage (EE%), in vitro drug release, in vivo skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti- tyrosinase activity were tested for the selected formulation. Based on HPLC results, FEG contained 34.501 mg/g of Glab, and FEL contained 31.714 mg/g of LQ. Among 20 different formulations, NLC 20 (LG-NLCs) showed desirable DLS results with a Z-average size of 185.3 ± 1.08 nm, polydispersity index (PDI) of 0.229 ± 0.35, and zeta potential of -16.2 ± 1.13 mV. It indicated good spherical shape, high EE% (79.01% for Glab and 69.27% for LQ), two-stage release pattern (an initial burst release followed by sustained release), efficient in vivo skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic. The LG-NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and in vivo penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation.

"Lipid Nanoparticles for Pulmonary Fibrosis: A Comprehensive Review".

Idiopathic pulmonary fibrosis (IPF) is a fatal progressive and irreversible ailment associated with the proliferation of fibroblast and accumulation of extracellular matrix (ECM) with gradual scarring of lung tissue. Despite several research studies, the treatments available are not efficient enough for the reversal of the disease and are constantly in progress. No drugs other than Pirfenidone and Nintedanib have been approved for the treatment of IPF, necessitating the exploration of novel therapeutic strategies. Recently, lipid-based nanoparticles (LNPs) have drawn more attention because of their potential to enhance the solubility of drugs, cross biological barriers of the lungs and specifically target lung fibrotic tissues, overcoming various challenges in treating IPF. LNPs offer a versatile platform to encapsulate a wide range of drugs, both hydrophilic and lipophilic, improving their bioavailability, allowing sustained release and reducing toxicity, which radiates their significant role in addressing the complexities of IPF. This review summarizes the pathogenesis and conventional treatment of idiopathic pulmonary fibrosis, along with their drawbacks. The review focuses on different types of lipid-based nanoparticles that have been tested in the treatment of idiopathic pulmonary fibrosis, including nanoemulsions, liposomes, solid lipid nanoparticles, nanostructured lipid carriers, niosomes and lipid-polymer hybrid nanoparticles. The review also highlights the future prospects that can offer a potential approach for developing novel strategies to treat idiopathic pulmonary fibrosis.

Optimization of nano-structured lipid carriers for enhanced salbutamol delivery via buccal mucoadhesive film

Salbutamol sulphate (SS) is a widely prescribed β2 agonist for different respiratory disorders. However, its short plasma half-life and poor oral bioavailability strongly limit its compliance. This study targeted formulating SS in nanostructured lipid carriers (SS-NLCs) embedded in a buccal mucoadhesive film to enhance bioavailability and sustain release through an easy route of administration aiming to improve patient compliance and reduce dose-related side effects. SS-NLCs were prepared using glycerol monostearate (GMS), Labrasol® oil, and poloxamer 407 utilizing a full 23 factorial design. Eight SS-loaded NLCs formulations were evaluated for particle size distribution, zeta potential, and entrapment efficiency. The optimum formula selected according to design expert® statistical analysis, was subsequently incorporated in a polymeric buccal mucoadhesive film and subjected to in vitro and in vivo characterization. The optimum SS-NLCs showed a mean particle size of 119.1 ± 1.28 nm, polydispersity index of 0.248 ± 0.023, zeta potential of - 40.9 ± 0.47 mV, and entrapment efficiency of 68.20 ± 2.05 % with apparent controlled release. Casting SS-NLCs in a mucoadhesive polymeric mixture resulted in a smooth strong film with a prolonged in vitro drug release duration reaching 10 h. In vivo, buccal application of the formulated film showed significantly higher Cmax (107.53 ± 5.20 ng/ml) and delayed Tmax to 4 h with improving the bioavailability of SS by 4.10 folds compared to oral SS solution. Consequently, the buccal polymeric mucoadhesive film of SS-NLCs holds promise as an alternative route for sustained release, enhancing bioavailability, and improving therapeutic efficacy in treating respiratory disorders.

The Use of Lipid-based Nanocarriers to Improve Ovarian Cancer Treatment: An Overview of Recent Developments.

Ovarian cancer poses a formidable health challenge for women globally, necessitating innovative therapeutic approaches. This review provides a succinct summary of the current research status on lipid-based nanocarriers in the context of ovarian cancer treatment. Lipid-based nanocarriers, including liposomes, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs), offer a promising solution for delivering anticancer drugs with enhanced therapeutic effectiveness and reduced adverse effects. Their versatility in transporting both hydrophobic and hydrophilic medications makes them well-suited for a diverse range of anticancer drugs. Active targeting techniques like ligand-conjugation and surface modifications have been used to reduce off-target effects and achieve tumour-specific medication delivery. The study explores formulation techniques and adjustments meant to enhance drug stability and encapsulation in these nanocarriers. Encouraging results from clinical trials and preclinical investigations underscore the promise of lipid-based nanocarriers in ovarian cancer treatment, providing optimism for improved patient outcomes. Notwithstanding these advancements, challenges related to clearance, long-term stability, and scalable manufacturing persist. Successfully translating lipidbased nanocarriers into clinical practice requires addressing these hurdles. To sum up, lipidbased nanocarriers are a viable strategy to improve the effectiveness of therapy for ovarian cancer. With their more focused medication administration and lower systemic toxicity, they may completely change the way ovarian cancer is treated and increase patient survival rates. Lipidbased nanocarriers need to be further researched and developed to become a therapeutically viable treatment for ovarian cancer.

Nanotechnology: Current Developments, Applications and Patents for Non-invasive Topical Cosmetics and Dermatological Therapeutic Delivery

: Nanotechnology exhibits the advancement in the field of invention, by improving the potency of the formulation through the delivery of inventive solutions. To resolve several limita-tions related to conventional formulations, nanotechnology applications are increasing in the cosmetics and dermatological area. Cosmetic and dermatological preparations are considered a thriving branch of the body care arena and their usage has increased dramatically through the past years. Scientists are designing innovative delivery mechanisms and emerging innovations that are presently being utilized in the development of cosmetics. Inventive nanocarriers such as nio-somes, liposomes, microemulsions, nanoemulsions, solid-lipid nanoparticles, nanospheres, and nanostructured (lipid) carriers have substituted the use of traditional drug delivery. These innova-tive nanocarriers have the convenience of better skin permeation, sustained and controlled drug delivery, precise location, higher stability, and greater incorporated capability. Since the usage of cosmetics has increased, the usual delivery system has been substituted by modern delivery ap-proaches. The introduction of newer advancements and novel drug delivery systems make cos-metics and cosmeceuticals more popular with increased market share. This review article on nan-otechnology employed in cosmetics and dermatology emphasizes the numerous innovative nanocarriers designed for cosmetic and dermatologic drug delivery, their negative and positive aspects, and their toxicity.

Modifications of biological membranes, fat globules and liposomes promoted by cavitation processes. Consequences and applications

Cavitation-based technologies, such as ultrasound (or acoustic cavitation, AC) and hydrodynamic cavitation (HC), are gaining interest among green processing technologies due to their cost effectiveness in operation, toxic solvent use reduction, and ability to obtain superior processed products, compared to conventional methods. Both AC and HC generate bubbles, but their effects may differ and it is difficult to make comparisons as both are based on different phenomena and are subject to different operational variables. AC is one of the most used techniques in extraction and homogenization processes at the laboratory level. However, upscaling to an industrial level is hard. On the other hand, HC is based on the passage of the liquid through a constriction (orifice plate, Venturi, throttling valve), which causes an increase in liquid velocity at the expense of local pressure, forcing the pressure around the contraction below the threshold pressure that induces the formation of cavities.Some applications of cavitation technologies, such as the production of liposomes or lipid nanoparticles (LNPs) allow the generation of delivery systems for biomedical applications.Many others (inactivation of pathogenic viruses, bacteria and algae for water purification, extraction procedures, third generation of biofuel production, green extractions) are based on the disruption of lipid membranes. There are also applications aimed at the modification of membranes (like the milk fat globule) for the development of innovative products. Process parameters, such as cavitation intensity, duration and temperature define the impact of the process on the physical, chemical, and biological characteristics of the membranes. Thus, the adequate implementation of cavitation processes requires understanding of interactions and synergistic mechanisms in complex systems and of their effects on membranes at the microscopic or molecular level. In the present work, the use of cavitation technologies for the generation of LNPs or nanostructured lipid carriers, and the effects of AC and HC treatments on several types of membrane systems (liposomes, solid lipid nanoparticles, milk fat globules, algae and bacterial membranes) are discussed, focusing on the structural and chemical modifications of lipidic structures under cavitation.

Advanced green chemistry, HPLC method development and validation: Integrating stability indicating, quality by design (QbD), in ferulic acid and its application in NLCs-based nanoformulation

The biopharmaceutical class IV classification of ferulic acid (FA) restricts its use. FA-loaded nanostructured lipid carriers (NLCs) were developed to overcome these issues. It is difficult to quantify the lowest concentration of the drug by another method. The proposed method can determine the lowest concentration in nanoformulation and biological fluids including urine, plasma, blood, and tissues. The proposed method utilizes a novel QbD-based approach, which reduces trial-and-error production costs and market recalls and maintains a risk-benefit ratio, due to the use of optimized inputs and outputs. The use of a green chemistry approach (Acetonitrile: water) can detect even small degradants. The degradant found under stress conditions ensures the safety, efficacy, quality, and stability of the formulations. The optimized method showed linearity with r2 0.9988 in a range of 10-60 µg/ml at a retention time of 3.690±0.01 at a run time of 8 minutes. The recovery rate of FA was found in a range of 95.28±0.54% to 97.98±0.48%. The obtained %RSD precision was (0.01-0.21%) for intra-day, whereas inter-day precision was (0.09-0.51%). The lowest concentrations to be detected and quantified were 2.4 and 7.3µg/ml. The AQbD approach built an optimized method providing significant output. The found stress degradation recovery was (6.2±0.98% to 33.46±0.22%), thus from the recovered degradant concentrations, further work for safety, efficacy, quality, and stability can proceed. Thus RP-HPLC adheres to ICH guidelines and is found to be straightforward, precise, and sensitive for routine quality control analysis of FA in bulk and nanoformulations, plasma, tissues, and other biological fluids.

Development of dihydrooxyresveratrol-loaded nanostructured lipid carriers for safe and effective treatment of hyperpigmentation

Hyperpigmentation, a dermatological concern caused by increased melanin production, affects many people worldwide. Traditional skin-brightening products target inhibition of cellular tyrosinase activity but often contain harmful toxicants. Oxyresveratrol (OXR) is a robust tyrosinase inhibitor, but its instability, poor water solubility, and low skin permeation limit its use. This study aimed to overcome these challenges by modifying OXR to dihydrooxyresverstrol (DHO) and encapsulating both compounds into nanostructured lipid carriers (NLCs). The developed NLCs loaded with OXR (OXR-NLC) and DHO (DHO-NLC) achieve desirable physicochemical properties, high percentages of entrapment efficiency, and stability for at least three months during 4–40 ℃ of storage. DHO itself and NLC formulation of OXR dramatically enhanced the photostability of OXR. Additionally, NLC formulations significantly promoted controlled release and facilitated penetration through the skin-like hydrophobic membrane of OXR and DHO. Importantly, these NLC formulations exhibited no cytotoxicity on human keratinocyte cells up to 500 µg/mL and effectively reduced melanogenesis in B16F10 cells. Our findings indicate that DHO-loaded NLC offers a promising strategy for developing cosmeceutical products to address hyperpigmentation and promote skin lightening.

Advances in Encapsulating Marine Bioactive Compounds Using Nanostructured Lipid Carriers (NLCs) and Solid Lipid Nanoparticles (SLNs) for Health Applications

As life expectancy rises and modern lifestyles improve, there is an increasing focus on health, disease prevention, and enhancing physical appearance. Consumers are more aware of the benefits of natural ingredients in healthcare products while also being mindful of sustainability challenges. Consequently, marine bioactive compounds have gained popularity as ingredients in cosmetics and food supplements due to their diverse beneficial properties. Nonetheless, the use of some of these compounds is restricted by their low stability and poor aqueous solubility, necessitating solutions to overcome these limitations. In this context, lipid nanoparticles, such as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), have been investigated for their potential to protect and improve the absorption of molecules through various routes, including oral and cutaneous. Numerous studies have shown that nanoencapsulating these compounds and incorporating them into cosmetics and food supplements can be effective. However, this application remains unregulated at the global level and is not currently addressed by existing legislation. Additional in vivo studies in both animals and humans are necessary to fully assess safety concerns.

Characteristics and Preparation of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers

Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have emerged as promising systems for delivering active ingredients. They are derived from physiological, biodegradable, and biocompatible lipids, offering benefits such as sustained release promotion and increased drug stability. These systems are apt for the efficient transport of therapeutic drugs to target tissues while also providing advantages such as facilitating large-scale industrial production, bioavailability, and protection against degradation. The preparation of these nanoparticles involves utilizing diverse types of lipids, surfactants, and solvents. Common lipid varieties encompass triglycerides, steroids, and fatty acids, selected based on the active ingredient for stabilization within the lipid matrix. Preparation methods can be categorized into high-energy and low-energy approaches. This study investigated the differences between the main methodologies used, comparing SLN and NLC systems, and scrutinizing their respective advantages, disadvantages, and applications.

Heme oxygenase 1 inhibitor discovery and formulation into nanostructured lipid carriers as potent and selective treatment against triple negative metastatic breast cancer

Heme oxygenase-1 (HO-1) has been identified as a potential new target in anticancer therapy, being overexpressed in different tumors and crucial for cell proliferation. Advances in the development of specific HO-1 inhibitors should support the understanding of controlling HO-1 activity as antitumoral strategies, opening the path for future therapeutic applications. In the present study, small series of new HO-1 inhibitors were synthesized by joining a butylimidazolic pharmacophore together with a hydrophobic moiety spaced by a 2-oxybenzamide central linker. The most active and selective HO-1 inhibitor, VP 21–04, 2-(4-(1H-imidazol-1-yl)butoxy)-N-benzyl-5-iodobenzamide (7b) was identified. This ligand showed strong cytotoxic activity against melanoma and breast cancer cell lines. Encapsulation of VP 21–04 in nanostructured lipid carriers (NLC 21–04) was performed to exploit its therapeutic potential by passive-targeting delivery ameliorating water-solubility and toxicity. Interestingly, NLC 21–04 showed a marked antiproliferative effect in both cancer cell lines, and an improved safety profile with a wider therapeutic window when compared to the free drug. Finally, NLC 21–04 showed a marked tumor growth reduction while being safe in an in ovo tumor model, highlighting the therapeutic potential of the developed nanoparticles against triple negative metastatic breast cancer.

Computational and experimental insights into glycyrrhizin-loaded nanostructured lipid carriers: docking, dynamics, design optimization, and anticancer efficacy in lung cancer cells

BackgroundLung cancer (LC) remains a predominant global health concern, especially with escalating tobacco-smoking rates. Present study provides computational screening, molecular dynamics, DFT and simulation analysis of phytoconstituents on EGFR receptors (2ITY and W2O), followed by selection of highest docking score phytoconstituents among 45 for further analysis. The formulation was optimized by Central composite design. Nanostructured-lipid carriers were prepared by high-speed homogenization, combining a 1:1 ratio of liquid lipid (Castor oil) and melted solid lipid (glyceryl monostearate) with 4% surfactant (tween 80) in a water phase containing Glycyrrhizin. The resulting mixture underwent high-speed homogenization at 8000 rpm for 40 min, followed by sonication for 15 min to achieve formulation development of GNLC. The anticancer potential of GNLC have been proved by experimental analysis through MTT assay using A549 Cell lines.ResultsGlycyrrhizin was found to possess maximum docking score − 8.863 and − 8.837 on both 2ITY and W2O respectively. The study unveils Glycyrrhizin’s interactions with EGFR pivotal in cancer progression and treatment. Molecular dynamics simulations highlighted the structural and dynamic interactions within a protein–ligand complex, indicating both stability and flexibility characteristics. DFT analysis of Glycyrrhizin revealed its molecular properties, suggesting stability and potential reactivity. Glycyrrhizin loaded nanostructured lipid carriers (GNLC) have been developed and analysed by various parameters like particle size and drug release zeta potential, SEM analysis, and solubility analysis reveals critical insights into their optimization for effective drug delivery. Both GNLC and Doxorubicin (0.78–50 µg/ml) were used for the activity. The anticancer potential at 12.50, 25 and 50 µg/ml pf GNLC was found to be statistically significant and was comparable with that of standard group Doxorubicin. The observed structural transformations in Glycyrrhizin into a lipid matrix indicate potential enhancements in its drug release.ConclusionsGNLC shows promising anti-cancer potential in lung cancer, further pre-clinical and clinical studies, is crucial to validate its efficacy, safety, and integration into standard therapeutic regimens.Graphical abstract

Improving oxidative stability of flaxseed oil by Zein-Basil seed gum electrospun nanofibers activated by thyme essential oil loaded nanostructured lipid carriers

In this research, zein/basil seed gum (BSG) electrospun active nanofibers (NFs) incorporated with thyme essential oil (TEO) were prepared to extend the oxidative stability of flaxseed oil. TEO was used in two forms free and encapsulated with nanostructured lipid carriers (NLCs). According to Field Scanning electron microscopy (FE-SEM), the NFs with a Zein/BSG ratio of 85:15 was a desirable sample with the best morphology and the lowest fiber diameter (569 nm). According to Fourier transform infrared (FT-IR), no new chemical interaction was confirmed during the electrospinning process. According to X-ray diffraction (XRD) analysis, the pure and active zein NFs didn't have a crystalline structure and were amorphous. The antioxidant activity of NFs estimated by DPPH scavenging analysis, was found to be in the range of 30–40 %. The fabricated NFs were placed in contact with flaxseed oil. Peroxide value (PV), DPPH scavenging activity, and oxidative stability index (OSI) were calculated over 45 days. The PV increased with increasing storage time (p < 0.05), but this change was lower in oil in contact with NFs. A significant increment in DPPH scavenging activity and OSI was observed during the storage of flaxseed oil by active NFs. The results of the study indicate that the zein/BSG NFs incorporated with TEO-loaded NLC has the potential to extend the shelf life of fatty food products such as flaxseed oil.

Tailoring cilnidipine nanostructured lipid carriers loaded transdermal patch for the treatment of hypertension: optimization, ex vivo and in vivo studies

The current investigation aimed to develop nanostructured lipid carriers (NLCs) as a potential transdermal drug delivery system for the improvement of cilnidipine (CIL) bioavailability. The high-pressure homogenization (HPH) method was utilized for the formulation of NLCs. Box-Behnken Design (BBD) was utilized to optimize CIL NLCs for entrapment efficiency, particle size and zeta potential. The resultant NLCs had a mean particle size of 98.2 ± 05.08 nm, a zeta potential of −16.1 ± 2.05 mV and an entrapment efficiency of 92.51 ± 4.18%. Transmission electron microscopy (TEM) revealed spherical or elongated particles for CIL-NLCs. The optimized NLCs were embedded in the transdermal patch and were formulated utilizing the solvent casting method and investigated for CIL content, physical characteristics, skin permeation and in vivo pharmacokinetics study. In vivo pharmacokinetics experiments with an NLCs-embedded transdermal patch show, an increase in C max and T max , 1305.66 ± 7.96 ng/mL and 4 h, respectively, when compared to the oral CIL dose. The flux values for ex vivo permeation studies for the CIL NLCs patch were determined to be 82.54 ± 4.80 µg/cm2/h. The bioavailability of CIL-loaded NLCs transdermal patch was found to be 2.9-fold greater than that of oral drug suspension, thus confirming the improvement of bioavailability of CIL by NLCs loaded transdermal patch.

Nanotechnological advancement for the treatment of neurodegenerative disorders

Neurodegenerative disorders are chronic and progressive conditions of the central nervous system. This review work focusses on some of the disorders like Alzheimer’s disease, Parkinson’s disease, Amyotrophic lateral sclerosis, and Huntington’s disease which are some of the most prevalent neurodegenerative disorders presenting a substantial challenge on the global health care system. These disorders are characterized by the loss of neurons and the formation of protein aggregates leading to cognitive and motor impairments. The treatment options are available but due to the complex pathophysiology of the disease and the intricate structure of the brain, effective concentrations of drugs are not delivered to brain. Here we discuss some of the recent strategies employed by scientists to enhance the drug delivery and drug targeting to the site of action that is brain for these disorders. Further, nanotechnology-based carrier systems have been discussed which are developed using different natural and synthetic polymers and lipid materials. Owing to many beneficial properties like nanometric size range, physicochemical properties and tunable surface-modifying features, nanocarriers serve as potential systems in the treatment of neurodegenerative diseases as they can easily cross the BBB and reach to the brain in effective concentration. This review article describes neurodegenerative disorders and the limitations associated with their conventional application. Different arrays of nanocarriers such as polymeric nanoparticles, liposomes, Solid Lipid Nanoparticles, Nanostructured Lipid Carriers, and Nanoemulsions have been extensively reviewed. To understand the nanomedicine market, the ongoing clinical trials for various nano-carriers employed to treat these disorders have been compiled and discussed.

Development of targeted lipid nanoparticles for the combined therapy of triple negative breast cancer: Can curcumin and 6-aminoflavone promote doxorubicin in vitro efficacy?

In the study of triple-negative breast cancer (TNBC) therapeutic approaches, researchers have recently focused on exploiting P-glycoprotein (P-gp) and hypoxia-inducible factor (HIF) inhibitors to enhance the effectiveness of chemotherapeutic agents, which are often limited by poor specificity and high toxicity. Additionally, herbal medicines have shown promising results as non-toxic P-gp and HIF inhibitors. However, the co-administration of chemotherapeutic agents with natural P-gp inhibitors, such as curcumin (CUR) or HIF-inhibitors like 6-aminoflavon (AF), remains challenging due to pharmacokinetic constraints. In the present work, solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are employed as drug delivery systems. CUR, AF, and a lipophilic doxorubicin (DOXO) ester (C12-DOXO) were individually loaded into both systems and subsequently used in combination. SLNs, both naked and hyaluronic acid (HA)-decorated, and NLCs were prepared and characterized. Given that NLCs have not yielded fully satisfactory results regarding drug entrapment and recovery, we have, for the time being, focused further characterization studies and cell line experiments exclusively on SLNs. SLNs were therefore tested on DOXO-sensitive and DOXO-resistant TNBC cell lines (MDA-MB-231 and MDA-MB-231/DX cells, respectively). HA-decorated SLNs showed effective C12-DOXO accumulation in P-gp-expressing cells, significantly reducing cell viability, including in DOXO-resistant cells. The combination of HA-decorated SLNs containing C12-DOXO (SLN-C12-DOXO-HA) with HA-decorated SLNs containing CUR (SLN-CUR-HA) or AF (SLN-AF-HA) demonstrated a significant reduction in cell viability across all concentrations, exceeding the cytotoxicity noted in the application of SLN-C12-DOXO-HA alone, especially at higher concentrations in both DOXO sensitive and resistant cell lines.