Nanostructured Lipid Carriers Research Articles

Paclitaxel loaded Capmul MCM and tristearin based nanostructured lipid carriers (NLCs) for glioblastoma treatment: screening of formulation components by quality by design (QbD) approach.

Paclitaxel (PTX), a naturally occurring diterpenoid isolated from Taxus brevifolia, is a first-line drug for the treatment of glioblastoma; however, it suffers from the disadvantages of poor water solubility and nonspecific biodistribution, which cause serious side effects in the human body. The marketed formulation suffers from serious side effects, such as allergic reactions, neutropenia, and neuropathy, which require safe and effective formulations of PTX. In the present study, PTX was entrapped in a solid-liquid lipid mixture with the aid of a surfactant using a modified solvent evaporation technique. Higher entrapment of the impressive stability of the formulation was achieved by employing quality design-based strategies. Optimized levels by employing a numerical optimization technique for each factor, that is, surfactant concentration (X1), lipid concentration (X2), and amount of organic solvent (X3) were 0.3%, 0.76% & 8.3 ml respectively. The resultant formulation exhibited a particle size of 121.44 nm, entrapment efficiency of 94.27%, and zeta potential of -20.21 mV with unimodal size distribution. A reduction in the % crystalline index from 48 to 3.4% ensured the amorphous form of the entrapped drug inside the formulation, which precludes the fear of leakage and instability of the formulation. Cell line studies conducted on U87MG Cell lines also suggested that the NLC of paclitaxel are more effective than those of pure PTX. In summary, PTXNLC seem to be a superior alternative carrier system for the formulation industry to obtain higher entrapment with excellent stability.

Nanostructured Lipid Carrier for Dermatological Application: A Comprehensive Review and Future Perspective

Abstract:: Dermatological disease states have psychological impacts that affect a patient’s life. In the management of such disorders, topical delivery has an important role. However, the conven-tional topical delivery systems suffer from various limitations, like skin irritation, a minute quan-tity of drugs reaching disease sites, and over and under medication, which leads to an adverse re-action and therapeutic failure, respectively. Therefore, researchers continuously search for an al-ternate delivery system for treating skin disease. In recent years, nanostructured lipid carriers (NLC) have emanated as promising carrier systems for topical delivery. The current review pro-vides an in-depth insight into topical administration for treating a variety of dermatological issues using NLCs as a carrier. This review highlights the suitability of NLCs as carriers for topical de-livery, their method of preparation, and their characterization. In the present review, the main emphasis has been given to the management of various dermatological problems by using NLCs as a carrier; a plethora of literature investigating NLC as the carrier for topical delivery has been included in this review. In this paper, an attempt has been made to provide a summary of the re-search carried out in this field that will encourage further research in this arena.

Improved Transdermal Delivery of Anti-hypertensive Drug Loaded Nanostructured Lipid Carriers: Statistical Design, Optimization, Depiction and Pharmacokinetic Assessment

Background: The vasoselective calcium-channel blocker lercanidipine hydrochloride (LCH) is poorly absorbed orally (only 10% bioavailability) owing to its low solubility and hepatic metabolism. Because of the LCH's poor solubility and permeability, bioavailability is low and very variable, stable aqueous liquid formulations are challenging to create, and a uniform distribution of the medication is almost impossible to produce. Objective: The purpose of this research was to see whether an approach involving the development of nanostructured lipid carriers (NLCs) might be used to create an effective, innovative oral formulation of LCH. The efficacy of several synthetic and natural liquid lipids was compared using a hot homogenization-ultrasonication strategy. Methods: Following initial improvements with hot homogenization and ultrasonication, the LCHloaded NLCs formulation was fine-tuned by Box-Behnken statistical analysis. The optimal LCHNLCs composition includes the lipid phase (2-4% w/v) of stearic acid and oleic acid, the surfactants poloxamer 188 (1%) and Tween 80(1%), and other ingredients. Results: The optimized NLCs formulation was found to have mean vesicle sizes of 128.72 ± 1.59 nm, polydispersity indices of 0.169 ± 0.06, zeta potentials of -36.81 ± 0.42 mV, and entrapment efficiencies of 79.84 ± 0.11%. The optimized NLCs formulation released much more LCH (88.74 ± 4.62) than the LCH-suspension (36.84 ± 0.37%) in in-vitro drug release experiments lasting up to 24 hours. Ex vivo studies on the ability of LCH-NLCs to pass through the gut showed that drug permeation was much better than it was with plain LCH-solution. The in vivo pharmacodynamic analysis demonstrated that, compared to conventional LCH-suspension, NLCs released LCH more slowly and steadily over a longer time period. Conclusion: These findings provide additional evidence that NLCs have great promise as a drug delivery technology for the treatment of hypertension, just as they show promise as a controlled release formulation for the treatment of LCH.

Encapsulation of Microalgae Tisochrysis lutea Extract in Nanostructured Lipid Carriers (NLCs) and Evaluation of Their Sunscreen, Wound Healing, and Skin Hydration Properties

Traditional sunscreens have relied on synthetic compounds to protect against harmful ultraviolet (UV) radiation. However, there is increasing interest in utilizing the natural photoprotective properties of microalgae extracts. This approach does not only aim to enhance the stability and efficacy of sun protection formulae but also seeks to reduce the reliance on synthetic sunscreens. This study investigates the encapsulation of Tisochrysis lutea extract (TL) in nanostructured lipid carriers (NLCs) to create a combination (NLC-TL) with enhanced physicochemical stability, antioxidant activity, SPF efficacy, wound healing capacity, and skin hydration. The particle size and ζ-potential were approximately 100 nm and −50 mV, respectively, and both formulations successfully passed the stability tests. The antioxidant activity, measured via DPPH assay, revealed that NLC-TL achieved the highest free radical scavenging activity across all tested concentrations, indicating a synergistic effect. The incorporation of TL in NLCs maintained the sun protection factor (SPF) of a 2% extract solution (1.53 ± 0.13). The wound healing assay indicated that NLC-TLs significantly enhanced wound closure compared to controls and TL alone. Additionally, skin hydration tests on healthy volunteers revealed that NLC-TLs provided superior and sustained hydration effects. These results highlight NLC-TLs’ potential as a multifunctional topical agent for cosmetic and therapeutic applications.

Silver nanoparticles in medicine and technology: Synthesis, functionality and future prospects

Nanomaterials, particularly nanoparticles (NPs), have emerged as forefront materials of the 21st century due to their unique properties and potential applications. Silver nanoparticles (AgNPs) are among the most attractive inorganic nanomaterials, widely used due to their significant antibacterial properties, broad-spectrum activity, and potential applications across various fields, including health, food storage, textiles, and environmental solutions. AgNPs exhibit a large surface-area-to-volume ratio, enabling enhanced interaction with bacterial cells, making them effective in medical and industrial applications. Despite concerns over their toxicity, AgNP-based products have been approved by multiple regulatory bodies. Nanoparticle synthesis methods are generally divided into physical, chemical, and biological approaches. Although physical and chemical methods are efficient, they involve toxic chemicals and energy-intensive processes. Biosynthesis, particularly plant-based, offers an eco-friendly alternative, reducing the environmental and health risks associated with chemical agents. The review also explores the therapeutic potential of AgNPs in drug delivery systems, especially in topical formulations like nanoemulsions, solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs). These nanocarriers enhance drug stability, skin penetration, and controlled release, making them ideal for dermal and transdermal delivery. Moreover, the use of AgNPs in dentistry is highlighted for their bactericidal properties, which help prevent infections and implant failure, with the potential for enhancing therapeutic outcomes without common drawbacks like tooth staining. Overall, AgNPs exhibit promising applications in biomedical, pharmaceutical, and dental fields, and their novel functionalities continue to advance the development of nanotechnology-driven solutions.

Current Nanotechnological Strategies for Delivery of Anti-Retroviral Drugs: Overview and Future Prospects

Abstract: Globally, over forty million people are living with Human Immunodeficiency Viral (HIV) infections. Highly Active Antiretroviral Therapy (HAART) consists of two or three Antiretroviral (ARV) drugs and has been used for more than a decade to prolong the life of AIDS-diagnosed patients. The persistent use of HAART is essential for effectively suppressing HIV replication. Frequent use of multiple medications at relatively high dosages is a major reason for patient noncompliance and an obstacle to achieving efficient pharmacological treatment. Despite strict compliance with the HAART regimen, the eradication of HIV from the host remains unattainable. Anatomical and Intracellular viral reservoirs are responsible for persistent infection. Elimination of the virus from these reservoirs is critical for successful long-term therapy. Therefore, innovative approaches are required to design safe and effective therapies. Nanotechnology has revolutionized HIV drug delivery by addressing key challenges, including improving drug solubility, targeting specific cells, extending drug release, protecting drugs from degradation, overcoming biological barriers, enabling combination therapy, and enhancing vaccine delivery. Several nanocarrier systems, such as dendrimers, nanoemulsions, liposomes, solid nanoparticles (SLNs), and nanostructured lipid carriers, have been proposed to treat HIV infection. Additionally, nanosuspensions of antiretroviral drugs offer promising strategies for improving treatment outcomes. While these advancements have significantly improved HIV management strategies, challenges remain, including unexpected toxicity, avoiding harmful biological interactions, and costs associated with the large-scale production of nanopharmaceuticals.

Protective Effects of Carotenoid-Loaded Nanostructured Lipid Carriers Against Ochratoxin-A-Induced Cytotoxicity

Ochratoxin A (OTA) is a mycotoxin produced by Aspergillus ochraceous and various Penicillium species, which are known for contaminating agricultural products and posing significant health risks, which include immunotoxicity. This study aims to evaluate the potential of nanostructured lipid carriers (NLCs) loaded with a carotenoid-enriched extract from pumpkin peel (Cucurbita maxima L.) in mitigating the toxic effects of OTA. To address the poor bioavailability and instability of carotenoids, nanoencapsulation techniques were employed to enhance their delivery and efficacy. NLCs were formulated using hydrogenated sunflower oil, pumpkin oil, and soy lecithin using hot high-pressure homogenization. The in vitro study involved co-digesting OTA-contaminated bread with an NLC formulation and assessing the impact of the encapsulated carotenoid on OTA bioaccessibility, bioavailability, and cellular toxicity using Caco-2 and Jurkat T cells. Even though no significant influence was observed on the bioaccessibility and bioavailability of OTA, carotenoid-loaded NLCs exhibited cytoprotective effects by improving cell viability and mitigating OTA-induced toxicity in both Caco-2 and Jurkat T cells. Particularly, the flow cytometry analysis highlighted the ability of carotenoids to mitigate OTA-induced cellular damage by decreasing ROS production and limiting mitochondrial mass changes. The study suggests that the encapsulation of carotenoids in NLCs represents a promising strategy to enhance their protective effects against OTA toxicity, potentially offering a novel approach to food safety and public health protection. The study underscores the potential of nanotechnology in improving the bioavailability and efficacy of natural antioxidants to mitigate mycotoxin-induced damage.

Bioactive compounds delivery and bioavailability in structured edible oils systems.

The health benefits of bioactive compounds are dependent on the amount of intake as well as on the amount of these compounds that become bioavailable and bioaccessible. Various systems have been developed to deliver and increase the bioaccessibility of bioactive compounds. This review explores the impact of gelled (oleogels, bigels, emulgels, emulsions, hydrogels, and hydrogel beads), micro-(gels, particles, spheres, capsules, emulsions, and solid lipid microparticles) and nanoencapsulated systems (nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, liposomes, and nanoliposomes) on the digestibility and bioavailability of lipophilic and hydrophilic bioactives. Structurant molecules, the oil type, antioxidants, emulsifiers, and coatings in delivery systems with promising potential in food applications are critically discussed. The release and bio-accessibility of bioactive compounds in gelled systems are influenced by various factors, such as the type and concentration of gelators, the gelator-to-oil ratio, the type of antioxidant, the network of the system, and its hydrophobicity. The stability, bioaccessibility, and controlled release of bioactives were improved in structured emulsions. Several variables, including wall material, oil/water ratios, encapsulation process, and pH conditions, can affect the bioactives release in microencapsulated systems. Factors like coating type and core-to-wall ratio impact the stability and release of core components. The encapsulating material, the encapsulation technology, and the nature of the nanomaterials all have an impact on the bioaccessibility of nanoencapsulated systems. Nanoliposomes provide enhanced stability and absorption. In general, all encapsulated systems have shown great potential in improving the distribution and availability of bioactive compounds.

Paroxetine Loaded Nanostructured Lipid Carriers Based In-situ Gel for Brain Delivery via Nasal Route for Enhanced Anti-Depressant Effect: In Vitro Prospect and In Vivo Efficacy.

This study focused on developing a thermosensitive gel with nanostructured lipid carriers (NLCs) loaded with paroxetine (PAR) to enhance the treatment and management of depression via nasal administration. Micro emulsion technique was utilized for the PAR-NLCs preparation. The acetyl alcohol and oleic acid were used in the ratio of 76:24. In the NLCs Tween 40, Span40 and Myrj 52 were used as a surfactant. The NLCs were then added into Poloxamer mixture to get thermosensitive NLCs based gel. Characterization, in vitro and in vivo studies were performed to check the efficiency of formulation in drug delivery. The entrapment efficiency of optimized PAR-NLCs was about 90%. The particle size, zeta potential and PDI were 155 ± 1.4nm, -25.9 ± 0.5mV, and 0.12 ± 0.01 respectively. The optimized gel showed a gelling temperature of 31.50 ± 0.50°C and a gelling time of 1 ± 0.12s with a pH of 6, suitable for nasal administration. The in vitro release assay of PAR-NLC-gel showed a cumulative release of about 59% in the first 6h after comparison with PAR-NLCs which showed almost 100%release. In vivo studies included forced swim test and tail suspension tests showed significant potential for treating depression when compared to PAR-NLCs. PAR-NLCs and NLCs based gel enhanced the tissue architecture and suppressed the expression of TNF-α in brain cortex from histological and immunohistochemical analysis. PAR- NLCs gel-based delivery system can prove to be an effective delivery system for brain targeting through nose for the better management of depression.

Demystifying the Potential of Embelin-Loaded Nanoformulations: a Comprehensive Review.

Phytoconstituent based therapies have the potential to reduce the adverse effects and enhance overall patient compliance for different diseased conditions. Embelin (EMB) is a natural compound extracted from Embelia ribes that has demonstrated high therapeutic potential, particularly as anti-inflammatory and anticancer therapeutic applications. However, its poor water solubility and low oral bioavailability limitations make it challenging to use in biomedical applications. Nanostructure-based novel formulations have shown the potential to improve physicochemical and biological characteristics of active pharmaceutical ingredients obtained from plants. Different nanoformulations that have been utilized to encapsulate/entrap EMB for various therapeutic applications are nanoliposomes, nanostructured lipid carriers, niosomes, polymeric nanoparticles, nanosuspensions, phytosomes, self nanoemulsifying drug delivery system, silver nanoparticles, microparticles, solid lipid nanoparticle, gold nanoparticles and nanomicelles. The common methods reported for the preparation of EMB nanoformulations are thin film hydration, nanoprecipitation, ethanol injection, emulsification followed by sonication. The size of nanoformulations ranged in between 50 and 345nm. In this review, the mentioned EMB loaded nanocarriers are methodically discussed for size, shape, drug entrapment, zeta potential, in vitro release & permeation and in vivo studies. Potential of EMB with other drugs (dual drug approach) incorporated in nanocarriers are also discussed (physicochemical and preclinical characteristics). Patents related to EMB nanoformulations are also presented which showed the clinical translation of this bioactive for future utilization in different indications.

Exploring Nanocarriers for Boosting Entacapone Bioavailability: A Journey through System Characterization and Assessment of Toxicity and Pharmacological and 2D Permeability Paybacks.

Catechol-O-methyltransferase inhibitors (iCOMT), such as entacapone, have been successfully employed to treat tremor-related symptoms of Parkinson's disease. However, iCOMT has been associated with a short half-life and poor oral bioavailability. Nanobased drug delivery systems have often been used to overcome this type of setbacks. Therefore, entacapone was encapsulated in PEGylated poly(lactic-co-glycolic acid) (PLGA)-based nanoparticles (NPs) via a nanoprecipitation process, as well as in PEGylated nanostructured lipid carriers (NLCs) using a solvent emulsification/evaporation method. Both nanoformulations presented sub-200 nm populations, with zeta-potential (ZP) values close to -30 mV, and showed stability at different pHs, while maintaining their physicochemical properties mostly intact, presenting only a change in their superficial charge (ZP values), indicating their interaction. Both nanoformulations presented interaction with mucins, which anticipates good permeation and bioavailability for oral and topical administration. No cytotoxic effects were observed for lyophilized PLGA NPs encapsulating entacapone, in which 2-hydroxypropyl-ß-cyclodextrin (HPβCD) was used as a cryoprotectant at 3% concentration (HP-PLGA@Ent), in human hepatocellular carcinoma (HepG2), human neuroblastoma (SH-SY5Y), or human epithelial colorectal adenocarcinoma (Caco-2) cell lines. Conversely, NLCs encapsulating entacapone (W-NLCs@Ent) presented cytotoxic effects on the HepG2 cell line, likely due to intracellular lipid accumulation or storage. Both nanoformulations maintained a COMT inhibition effect in HepG2 cells, using 3-BTD as the COMT probe. An increase of entacapone permeability in both monolayer and coculture models (Caco-2 and Caco-2/HT29-MTX, respectively) was observed for the developed nanoformulations. Overall, this work shows that encapsulated entacapone in different nanocarriers could be a stimulating alternative to solve entacapone setbacks, since they improve its physicochemical properties and permeability while still maintaining the COMT inhibitory activity.

Lymphatic targeting of cilnidipine by designing and developing a nanostructured lipid carrier drug delivery system

Objective The objective of current research is to design, develop, and optimize a cilnidipine (CLN) nanostructured lipid carrier (NLC)-based drug delivery system for the effective treatment of hypertension (HT). Significance Oral administration of CLN-loaded NLC (CLN NLC) containing glyceryl monostearate (GMS) as a solid and isopropyl myristate (IPM) as a liquid lipid may show remarkable lymphatic uptake through payer patches. Methods The emulsification probe sonication technique was used followed by optimization using 32 factorial designs. Results The optimized batch showed a mean particle size of 115.4 ± 0.22 nm with encapsulation efficiency of 98.32 ± 0.23%, polydispersity index (PDI) of 0.342 ± 0.03, and zeta potential (ZP, ζ) was −60.5 ± 0.24 which indicate excellent physical stability. In vitro studies showed a controlled release of CLN NLCs. Pharmacokinetics studies determined the C max of NLCs (373.47 ± 15.1) indicates 2.3-fold enhancement compared with plain drug (160.64 ± 7.63). Pharmacodynamic studies indicated that CLN NLCs were maintaining systolic blood pressure in a controlled manner without any signs of side effects. Conclusion CLN NLCs significantly improved lymphatic delivery and proved to be effective in the treatment and management of HT. It has been proved that CLN NLCs are found to be better than any traditional CLN dosage form due to enhancement in solubility, absorption, bioavailability, intestinal permeability, avoidance of first-pass metabolism, P-glycoprotein efflux and reduction in dose-related side effects, achievement of controlled and sustained release action.

Nanostructured Lipid Carrier-based Topical Gels as Novel Drug Delivery System: A Comprehensive Overview.

Nanostructured lipid carriers (NLCs) are lipidic nanocarriers that recover the permanency and capacity of drug payloads. NLCs are well-known as second-generation lipid nanocarriers with an unstructured matrix, presenting potentially advantageous nanocarrier systems with marketable opportunities because of reproducible production methodologies and biocompatible lipidic excipients. These (NLCs) are now recognized as a very promising nanocarrier structure for the efficient delivery of drugs via different administration routes. In recent years, several NLC-based gels have been developed and evaluated for topical delivery of many drugs and other therapeutic agents. This review article presents an overview of NLC-based topical gels investigated to deliver drugs via ocular, dermal, and transdermal routes. In addition, the classification, manufacturing, characterizations, advantages, and disadvantages of NLCs are addressed in this article. We also discussed different evaluations of NLC-based topical gels.

Hybrid Albumin-Decorated Lipid-Nanocarrier-Mediated Delivery of Polyphenol-Rich Sambucus nigra L. in a Potential Multiple Antitumoural Therapy.

The current research attempted to address the suitability of bioactive Sambucus nigra extract entrapped in albumin-decorated nanostructured lipid carriers (NLCs) as a promising "adjuvant" in improving tumour penetration for multiple antitumour therapy. The new hybrid albumin-decorated NLCs were characterised based on, e.g., the particle size, zeta electrokinetic potential, SambucusN entrapment efficiency, and fluorescence spectroscopy and tested for different formulation parameters. The antioxidant activity of NLC-SambucusN was significantly enhanced by a bovine serum albumin (BSA) polymer coating. According to the real-time cell analysis (RTCA) results, NLC-I-SambucusN-BSA behaved similarly to the chemotherapeutic drug, cisplatin, with cell viability for LoVo tumour cells of 21.81 ± 1.18%. The new albumin-NLC-SambucusN arrested cancer cells in G1 and G2 cycles and intensified the apoptosis process in both early and late phases. An advanced induction, over 50% apoptosis in LoVo colon cells, was registered for 50 μg/mL of NLC-II-SambucusN-BSA, a fourfold increase compared to that of untreated cells. RTCA and flow cytometry results showed that concentrations of the hybrid NLC-SambucusN up to 50 μg/mL do not affect the proliferation of normal HUVEC cells. This approach provides insightful information regarding the involvement of phytochemicals in future therapeutic strategies. Albumin-decorated NLCs can be considered a noteworthy strategy to be connected to antitumour therapeutic protocols.

Review of Lipid Nanoparticles for Breast Cancer Management: Targeting Strategies and Clinical Perspective

Abstract: Chemotherapy, a conventional breast cancer treatment, has limitations due to its nonspecific mechanisms and undesirable side effects. Lipid-based nanoparticles (LNPs) have emerged as a versatile and superior platform for targeted breast cancer treatment, offering several distinct advantages over traditional therapies. This class of nanocarriers, which includes solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), and liposomes, enhances the bioavailability and stability of therapeutic agents while minimizing systemic toxicity. LNPs can be engineered to precisely target breast cancer cells by exploiting tumor-specific markers, enabling selective delivery of chemotherapeutic agents and reducing off-target effects. SLNs provide controlled drug release and improved drug retention within the tumor, while NLCs offer higher drug-loading capacities and better stability. Liposomes, with their flexible design, allow for the encapsulation of both hydrophilic and hydrophobic drugs and can be modified for active targeting through surface functionalization. These lipid-based carriers also address the challenges of multi-drug resistance (MDR) by enhancing intracellular drug concentration and overcoming efflux mechanisms. In this review, we focus on lipid-based nanoparticles- a subtype of nanoparticles, and their potential advantages as drug delivery systems for breast cancer treatment. Results revealed that lipidbased nanoparticles have shown potential in breast cancer management, these include improved drug efficacy, enhanced ability to overcome cancer therapy resistance, and effective drug carrier for co-loaded drugs.

Enhancing resveratrol pharmacokinetics and cytotoxicity in ovarian cancer cells via nanostructured lipid carriers

Resveratrol (Res), a potent nutraceutical, holds promise in ameliorating cancer and catalyzing breakthroughs in cancer therapy. Despite numerous preclinical studies on its anticancer activity, translational research progress remains limited. Poor pharmacokinetics and low potency are primary bottlenecks of Res therapy. In this study, we aimed to enhance the pharmacokinetic profile of Res in a rat model and assess its cytotoxicity against human ovarian cancer cells by developing Res loaded Nanostructured Lipid Carriers (Res-NLCs). The Res-NLCs were synthesized using the solvent injection method, featuring a size of 177 nm, a PDI of 0.25, and an entrapment efficiency exceeding 80%. The formulation exhibited stability for three months at 4 °C and 40 °C. Cytotoxicity assessments using the MTT assay and cellular uptake studies on human ovarian cancer cells (PA1 and SKOV3 luc) revealed significantly superior time-dependent cytotoxic effects and cellular accumulation of Res-NLCs compared to free Res. Pharmacokinetic studies of intravenously administered Res in NLCs demonstrated prolonged plasma levels of Res for at least 48 h. Remarkably, Res-NLCs exhibited approximately 15- and 5-fold improvements in AUC and elimination half-life (t1/2), respectively, compared to Res in solution in rats. Moreover, Res tissue distribution from Res-NLCs in rats showed significantly higher accumulation in the liver, lungs, and ovaries over 48 h, underscoring the potential for targeted therapy. In conclusion, NLCs effectively mitigated premature reduction of Res in the bloodstream, prolonged circulation period, and enhanced tissue accumulation. These findings suggest promising prospects for improving therapeutic outcomes in ovarian cancer therapy using Res-NLCs.

Potential of Silymarin and Metformin Co-Loaded Nanostructured Lipid Carriers Containing Mucoadhesive Thermogel on KB Cells of Oral Cancer

Potential of Silymarin and Metformin Co-Loaded Nanostructured Lipid Carriers Containing Mucoadhesive Thermogel on KB Cells of Oral Cancer

Bio-Pesticidal Potential of Nanostructured Lipid Carriers Loaded with Thyme and Rosemary Essential Oils against Common Ornamental Flower Pests

The encapsulation of essential oils (EOs) in nanostructured lipid carriers (NLCs) represents a modern and sustainable approach within the agrochemical industry. This research evaluated the colloidal properties and insecticidal activity of NLCs loaded with thyme essential oil (TEO-NLC) and rosemary essential oil (REO-NLC) against three common arthropod pests of ornamental flowers: Frankliniella occidentalis, Myzus persicae, and Tetranychus urticae. Gas chromatography–mass spectrometry (GC-MS) analysis identified the major chemical constituents of the EOs, with TEO exhibiting a thymol chemotype and REO exhibiting an α-pinene chemotype. NLCs were prepared using various homogenization techniques, with high shear homogenization (HSH) providing the optimal particle size, size distribution, and surface electrical charge. A factorial design was employed to evaluate the effects of EO concentration, surfactant concentration, and liquid lipid/solid lipid ratio on the physicochemical properties of the nanosuspensions. The final TEO-NLC formulation had a particle size of 347.8 nm, a polydispersity index of 0.182, a zeta potential of −33.8 mV, an encapsulation efficiency of 71.9%, and a loading capacity of 1.18%. The REO-NLC formulation had a particle size of 288.1 nm, a polydispersity index of 0.188, a zeta potential of −34 mV, an encapsulation efficiency of 80.6%, and a loading capacity of 1.40%. Evaluation of contact toxicity on leaf disks showed that TEO-NLC exhibited moderate insecticidal activity against the western flower thrips and mild acaricidal activity against the two-spotted spider mite, while REO-NLC demonstrated limited effects. These findings indicate that TEO-NLCs show potential as biopesticides for controlling specific pests of ornamental flowers, and further optimization of the administration dosage could significantly enhance their effectiveness.

Guiding Therapeutics: Lipid Labyrinths and Nanostructures for Enhanced Drug Delivery

Abstract: Nanostructured lipid carriers (NLCs) offer a breakthrough platform for drug therapy, surpassing traditional limitations and delivering exceptional performance. Among various nanoparticulate systems, lipid nanoparticles stand out as one of the most promising options for medication delivery. NLCs stand out due to their solid matrix at ambient temperatures, setting them apart from conventional lipid-based carriers such as nanoemulsions and solid lipid nanoparticles. This paper thoroughly explores the makeup, classification, components, and various methods of preparing NLCs, based on extensive research findings. It emphasizes their numerous advantages, such as improved stability, minimal toxicity, extended storage capability, increased drug-loading capacity, and compatibility with biological systems. The review provides insights into the advantages and limitations of each method. Exploring the intricacies of drug loading and release, the review also addresses strategies to bolster NLCs’ stability. Moreover, it provides a detailed summary of both laboratory- based and animal studies demonstrating the efficacy of NLCs carrying cytotoxic drugs, particularly emphasizing their promise in targeted drug delivery to the brain. As the next-generation lipid nanocarriers, NLCs are composed of physiological and biocompatible lipids, rendering them novel pharmaceutical formulations. These colloidal drug delivery systems boast a solid lipid matrix with nanosized structures, offering superior drug loading capacity, physical stability, and bioavailability compared to conventional lipid nanoparticles. Several techniques, including high-pressure homogenization, microemulsion, solvent evaporation, and melt emulsification, add to the flexibility of nanostructured lipid carriers. Additionally, their exterior can be altered using coatings such as polyethylene glycol, chitosan, or antibodies to improve targeting ability and stealth characteristics. By elucidating the promising role of NLCs across diverse drug delivery systems, this review stimulates interest in their potential applications. It underscores the significance of understanding the structure, content, multiple formulation procedures, and characterization of NLCs, which are pivotal aspects for establishing stable drug delivery systems.

Modulation of IFN-γ induced macrophage inflammatory responses via indomethacin-loaded NLCs for OA management

Macrophages are the main cells present in the synovial membrane. They play an important role in the development and progression of osteoarthritis (OA). After the establishment of the disease macrophages mostly adopt a pro-inflammatory secretory phenotype (OA phenotype) further inducing cartilage degradation. Indomethacin (IND) is a non-steroidal anti-inflammatory drug (NSAID) able to inhibit the synthesis of prostaglandins mediated by both cyclooxygenase isoforms depicting a potent anti-inflammatory capacity. However, the lack of specificity and short half-like of free drugs within the joint cavity limits its utility in controlling inflammation after intra-articular administration. This study aims at developing IND loaded glycosylated nanostructured lipid carriers (NLCs) to selectively target macrophages and promote their reprogramming to an anti-inflammatory phenotype. This approach focused on the local administration of the NLCs, offers a promising therapeutic strategy for treating OA by modulating the inflammatory environment within the joint. NLCs will be designed by combining experimental and in silico docking analyses, and thoroughly characterized to obtain drug delivery systems with high stability and suitable physicochemical properties. The proposed mannose-functionalized systems exhibited adequate particle sizes (≈ 70 nm) and positive surface charges (> 20 mV) to be efficiently retained in the joint cavity. Moreover, the developed NLCs demonstrated effective and specific uptake by OA-like macrophages leading to a significant decrease in the secretion of the pro-inflammatory cytokines IL-6, IL-8 and TNF-α similarly to the free drug. Therefore, these systems effectively reprogrammed OA-associated macrophages to adopt a more regenerative phenotype, offering a promising strategy for managing inflammation in OA.