Nanostructured Lipid Carriers Research Articles

Development and Evaluation of Docetaxel-Loaded Nanostructured Lipid Carriers for Skin Cancer Therapy.

This study focuses on the design, characterization, and optimization of nanostructured lipid carriers (NLCs) loaded with docetaxel for the treatment of skin cancer. Employing a systematic formulation development process guided by Design of Experiments (DoE) principles, key parameters such as particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency were optimized to ensure the stability and drug-loading efficacy of the NLCs. Combined XRD and cryo-TEM analysis were employed for NLC nanostructure evaluation, confirming the formation of well-defined nanostructures. In vitro kinetics studies demonstrated controlled and sustained docetaxel release over 48 h, emphasizing the potential for prolonged therapeutic effects. Cytotoxicity assays on human umbilical vein endothelial cells (HUVEC) and SK-MEL-24 melanoma cell line revealed enhanced efficacy against cancer cells, with significant selective cytotoxicity and minimal impact on normal cells. This multidimensional approach, encompassing formulation optimization and comprehensive characterization, positions the docetaxel-loaded NLCs as promising candidates for advanced skin cancer therapy. The findings underscore the potential translational impact of these nanocarriers, paving the way for future preclinical investigations and clinical applications in skin cancer treatment.

Effects of Lipid Phase Content on the Technological and Sensory Properties of O/W Emulsions Containing Bemotrizinol-Loaded Nanostructured Lipid Carriers

Different lipid phase ratios (12, 14, and 16% w/w) were assessed for their ability to affect the technological and sensory properties of O/W emulsions in which bemotrizinol (BMTZ), a broad-spectrum sunscreen agent, was incorporated free or loaded into nanostructured lipid nanocarriers (NLC) to reduce its release from the vehicle and, hence, its skin permeation. The following technological properties were evaluated in vitro: spreadability, viscosity, pH, occlusion factor, BMTZ release, and sun protection factor (SPF). Sensory attributes were assessed by panelists in three different phases: before/during pick-up, rub-in, and after application. Raising the lipid phase ratio led to an increase in viscosity (from 8017 ± 143 cPs to 16,444 ± 770 cPs) and to a corresponding decrease in spreadability (from 9.35 ± 0.21 cm to 7.50 ± 0.10 cm), while the incorporation of BMTZ-loaded NLC determined a decrease in the occlusion factor (from 47.75 ± 1.16 to 25.91 ± 1.57) and an increase in SPF (from 6% for formulations containing 12% lipid phase to 15% for formulations containing 16% lipid phase). No BMTZ release was observed from all emulsions. Sensory attributes were mainly affected by the lipid phase ratio. These results suggest that the lipid phase ratio and BMTZ incorporation into NLC could contribute to determining the technological and sensory properties of O/W emulsions.

Feasibility of Nanostructured Lipid Carrier Loaded with Alpha-Mangostin and Clove Oil for Canine Periodontal Therapy.

Nanostructured lipid carriers (NLC) represent the second generation of nanoparticles, offering numerous advantages over conventional delivery systems. These include improved stability, enhanced drug-loading capacity, and controlled release profiles, making them highly attractive candidates for a wide range of therapeutic applications. Their suitability for hydrophobic drugs like a traditional medicinal plant of Thailand as clove oil and alpha-mangostin. We investigated into nanostructured lipid carriers loaded with Alpha-Mangostin and clove oil (NLC-AMCO) into the physicochemical and biological characteristics to identify the formulation with the highest efficacy for treatment. The particle size, charge, polydispersity index, and other characterizations were recorded. The realtime ex vivo penetration was explored using canine gingival tissue. Drug sustained release was assessed by HPLC. Moreover, the antibacterial properties were tested by conventional methods. The NLC-AMCO can be stored at up to 40 °C for 60 days without any alterations in particle characteristics. Gingival tissue penetration and sustained drug release were superior compared to unencapsulated counterparts. It exhibited greater effectiveness in inhibiting bacterial growth than the antibiotics tested, particularly against bacteria from the oral cavities of dogs. Therefore, this alternative treatment approach offers cost-effectiveness and ease of administration for pet owners and reduces discomfort for the animals during restraint.

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 > 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.

Functional Nanostructured Lipid Carrier-Enriched Hydrogels Tailored to Repair Damaged Epidermal Barrier.

In this study, a functional nanostructured lipid carriers (NLCs)-based hydrogel was developed to repair the damaged epidermal skin barrier. NLCs were prepared via a high-energy approach, using argan oil and beeswax as liquid and solid lipids, respectively, and were loaded with ceramides and cholesterol at a physiologically relevant ratio, acting as structural and functional compounds. Employing a series of surfactants and optimizing the preparation conditions, NLCs of 215.5 ± 0.9 nm in size and a negative zeta potential of -42.7 ± 0.9 were obtained, showing acceptable physical and microbial stability. Solid state characterization by differential scanning calorimetry and X-ray powder diffraction revealed the formation of imperfect crystal NLC-type. The optimized NLC dispersion was loaded into the gel based on sodium hyaluronate and xanthan gum. The gels obtained presented a shear thinning and thixotropic behavior, which is suitable for dermal application. Incorporating NLCs enhanced the rheological, viscoelastic, and textural properties of the gel formed while retaining the suitable spreadability required for comfortable application and patient compliance. The NLC-loaded gel presented a noticeable occlusion effect in vitro. It provided 2.8-fold higher skin hydration levels on the ex vivo porcine ear model than the NLC-free gel, showing a potential to repair the damaged epidermal barrier and nourish the skin actively.

Exploration of Abiraterone acetate loaded Nanostructured lipid carriers for bioavailability improvement and circumvention of fast-fed variability.

Abiraterone acetate (ABA), a biopharmaceutical class IV drug suffers from solubility and permeability pitfalls resulting in limited oral bioavailability and positive food effect, i.e. multi-fold enhancement in drug absorption in the presence of food. This poses difficulties to physicians towards the estimation of dose and dosage regimen required for efficacious therapy of prostate cancer (PCa). Nanostructured lipid carriers (NLC) have demonstrated tremendous outcomes in enhancing the oral bioavailability of various entities along with food effect attenuation. In this study, Quality by design and multivariate analysis was employed for optimization of ABA loaded NLC (ABA NLC). The optimal size, PDI and zeta potential obtained using QbD were 134.6nm, 0.163 and -15.7mV respectively. Ex vivo qualitative and quantitative intestinal permeability studies demonstrated improved traversion of NLC through the intestinal segments. In vitro dissolution profile in biorelevant fast and fed gastric and intestinal media revealed minimal differences for ABA NLC compared to ABA. In vivo pharmacokinetics was performed to decipher the efficacy of ABA NLC in mitigating the food effect of ABA. The studies demonstrated 14.51-fold and 1.94-fold improvement in oral bioavailability during fasted and fed state respectively as compared to free ABA. The absorption mechanism of ABA NLC using chylomicron flow blocking approach conveyed lymphatic uptake as the major mechanism. Cmax fast/fed ratio was 0.9758 whereas, AUC fast/fed ratio was 0.9386, which being nearly equivalent, confirmed the food effect attenuation. Therefore, the results of the study demonstrate optimal pharmacokinetics of ABA NLC and its utility in circumventing the fast fed variability.

Combinatorial Delivery of Docetaxel- and Erlotinib-Loaded Functionalized Nanostructured Lipid Carriers for the Treatment of Triple-Negative Breast Cancer Using Quality-by-Design Approach.

This study explored the combined administration of docetaxel (DOC) and erlotinib (ERL) using nanostructured lipid carriers (NLCs), with folic acid (FA) conjugation to enhance their synergistic anticancer efficacy against triple-negative breast cancer. NLCs were developed through hot melt homogenization-ultrasound dispersion, and optimized by a quality-by-design (QbD) approach using Plackett-Burman design and Box-Behnken design. Plots were generated based on maximum desirability. Spherical, nanosized dispersions (<200 nm) with zeta potential ranging from -16.4 to -14.15 mV were observed. These nanoformulations demonstrated ~95% entrapment efficiency with around 5% drug loading. Stability tests revealed that the NLCs remained stable for 6 months under storage conditions at 4 °C. In vitro release studies indicated sustained release over 24 h, following Higuchi and Korsmeyer-Peppas models for NLCs and FA NLCs, respectively. Additionally, an in vitro pH-stat lipolysis model exhibited a nearly fivefold increase in bioaccessibility compared to drug-loaded suspensions. The DOC-ERL-loaded formulations exhibited dose- and time-dependent cytotoxicity, revealing synergism at a 1:3 molar ratio in MDA-MB-231 and 4T1 cells, with combination indices of 0.35 and 0.37, respectively. Co-treatment with DOC-ERL-loaded FA NLCs demonstrated synergistic anticancer effects in various in vitro assays.

Antimicrobial Activity of Essential-Oil-Based Nanostructured Lipid Carriers against Campylobacter Spp. Isolated from Chicken Carcasses.

Campylobacter is a virulent Gram-negative bacterial genus mainly found in the intestines of poultry. The indiscriminate use of traditional antibiotics has led to drug resistance in these pathogens, necessitating the development of more efficient and less toxic therapies. Despite their complex biologically active structures, the clinical applications of essential oils (EOs) remain limited. Therefore, this study aimed to increase the bioavailability, stability, and biocompatibility and decrease the photodegradation and toxicity of EO using nanotechnology. The diffusion disk test revealed the potent anti-Campylobacter activity of cinnamon, lemongrass, clove, geranium, and oregano EOs (>50 mm). These were subsequently used to prepare nanostructured lipid carriers (NLCs). Formulations containing these EOs inhibited Campylobacter spp. growth at low concentrations (0.2 mg/mL). The particle size, polydispersity index, and zeta potential of these systems were monitored, confirming its physicochemical stability for 210 days at 25 °C. FTIR-ATR and DSC analyses confirmed excellent miscibility among the excipients, and FE-SEM elucidated a spherical shape with well-delimited contours of nanoparticles. The best NLCs were tested regarding nanotoxicity in a chicken embryo model. These results indicate that the NLC-based geranium EO is the most promising and safe system for the control and treatment of multidrug-resistant strains of Campylobacter spp.

Treatment of endometriosis with mifepristone mediated by nanostructured lipid carriers.

Mifepristone, a progesterone receptor antagonist, was initially used to terminate early pregnancy. As scientific research advanced, it emerged to be effective in the treatment of various tumors and tumor-like conditions such as endometriosis. Despite the therapeutic potential of mifepristone, its therapeutic effect is still far from ideal because the drug is difficult to dissolve and to accumulate in the target tissue sites. To address this issue, mifepristone-loaded nanostructured lipid carriers (Mif-NLC) were prepared by a simple solvent diffusion method and their anti-endometriosis performance and mechanisms were initially investigated. By optimizing the preparation protocol, we obtained uniform and spheroidal Mif-NLC with an average particle size of 280nm. The encapsulation rate and drug loading capacity were 64.67% ± 0.15% and 2.7% ± 0.014%, respectively, as measured by UV spectrophotometry. The in vitro release kinetics indicated that mifepristone was released from NLC in a sustained-release manner. Compared with free mifepristone, Mif-NLC exhibited enhanced cellular uptake and inhibition of invasion activity in primary mesenchymal cells of endometriosis. A certain reduction in the size of endometriotic cysts was observed in animals compared to controls. The induction of autophagy via Mif-NLC may serve as the molecular mechanism underlying this effect. Furthermore, observation of uterine structures showed negligible toxic effects. This suggested that mifepristone encapsulated in NLC can improve its bioavailability and anti-endometriosis efficacy, which provided a new strategy for the treatment of endometriosis.

Quality-by-Design-Driven Nanostructured Lipid Scaffold of Apixaban: Optimization, Characterization, and Pharmacokinetic Evaluation.

Apixaban, an anticoagulant, is limited in its efficacy due to poor solubility, low bioavailability, and extensive metabolism. This study investigates the application of nanostructured lipid carriers (NLCs) to enhance the bioavailability of Apixaban. NLCs were prepared using the high-pressure homogenization method. The influence of independent variables, viz., the amount of Tween 80, HPH pressure, and the number of HPH cycles, were studied using a 23 factorial design. The average particle size, PDI, zeta potential, and entrapment efficiency of the optimized NLCs were found to be 232 ± 23 nm, with 0.514 ± 0.13 PDI and zeta potential of about -21.9 ± 2.1 mV, respectively. Additionally, concerning the thermal and crystallographic properties of the drug, the NLCs showed drug entrapment without altering its potency. The in-vitro drug release studies revealed an immediate release pattern, followed by sustained release for up to 48 h. In-vivo pharmacokinetic experiments demonstrated that Apixaban-loaded NLCs exhibited higher values of t1/2 (27.76 ± 1.18 h), AUC0-∞ (19,568.7 ± 1067.6 ng·h/mL), and Cmax (585.3 ± 87.6 ng/mL) compared to free drugs, indicating improved bioavailability. Moreover, a decrease in the elimination rate constant (Kel) reflected the sustained effect of Apixaban with NLCs. NLCs offer improved oral absorption rates and enhanced therapeutic impact compared to free drugs, potentially reducing dose frequency and improving patient outcomes.

Preparation and characterization of a nanostructured lipid carrier for phenylethyl resorcinol

Phenylethyl resorcinol (PR) demonstrates inhibitory effects on multiple targets in the melanin synthesis pathway, resulting in a strong whitening effect. However, challenges such as limited solubility in water and susceptibility to oxidation and discoloration restrict its practical application in the cosmetics industry. In order to enhance stability and performance characteristics, a whitening nanostructured lipid carrier (NLC) was synthesized through high-pressure homogenization. This method entailed the incorporation of solid lipids, a liquid lipid, and a compound emulsifier, with deionized water fulfilling the roles of solid phase, liquid phase, and water phase, respectively. The NLC's particle size, Zeta potential, stability, encapsulation efficiency, and other parameters were assessed using techniques such as particle sizer, stability analyzer, and HPLC. The results showed that the NLC for phenylethyl resorcinol prepared by using the optimal formula (7.50 % solid lipids, 3.00 % ethylhexyl palmitate, and 2.00 % Tween 80 and soybean lecithin) has an encapsulation efficiency of 87.11 %, a particle size of 157.2 ± 0.70 nm, a kinetic instability of less than 1.2, and a greatly improved stability, thereby successfully solving the problems of unstable storage and poor solubility of phenylethyl resorcinol.

Resveratrol-loaded lipid-based nanocarriers for topical delivery: Comparative physical properties and antioxidant activity

Resveratrol (R) is an antioxidant that helps several aspects of aging skin. However, it is slightly soluble in water and unstable under light exposure, necessitating the use of suitable formulations for improved clinical efficacy. Therefore, this study aimed to prepare R-loaded lipid-based nanocarriers for topical delivery, i.e., nanostructured lipid carriers (NLCs) and nanoemulsions (NEs). R-loaded nanocarrier gels were further prepared to increase R loading. The comparative physical properties and antioxidant activity of nanocarriers were performed in terms of particle size, zeta potential, morphology, rheology, R content, in vitro release, antioxidant activity, cytotoxicity and stability. The results revealed that R was successfully loaded into NLCs and NE gels (NEGs), having different physical properties and antioxidant activity depending on the composition of lipid-based nanocarriers. R could be incorporated into NEs and the aqueous gelling phase, resulting in higher R loading. Furthermore, the gelling network was responsible for pseudoplastic flow behavior. The cumulative amount of R released from NEGs was significantly higher than that from NLCs due to the co-surfactant-like properties of NEGs, which resulted in smaller particle sizes. However, NLCs exhibited significantly more antioxidant activity and less cytotoxicity compared to NEGs. The stability of both nanosystems showed no significant change when stored at refrigerator temperature for over 3 months. In conclusion, the various compositions of lipid-based nanocarriers produced a range of physical properties and antioxidant activity. Nonetheless, these NLCs and NEGs have the potential to be nanocarriers for R, which has antioxidant properties for topical application.

Demystifying the potential of lipid-based nanocarriers in targeting brain malignancies.

Drug targeting for brain malignancies is restricted due to the presence of the blood-brain barrier (BBB) and blood-brain tumor barrier (BBTB), which act as barriers between the blood and brain parenchyma. Certainly, the limited therapeutic options for brain malignancies have made notable progress with enhanced biological understanding and innovative approaches, such as targeted therapies and immunotherapies. These advancements significantly contribute to improving patient prognoses and represent a promising shift in the landscape of brain malignancy treatments. A more comprehensive understanding of the histology and pathogenesis of brain malignancies is urgently needed. Continued research focused on unraveling the intricacies of brain malignancy biology holds the key to developing innovative and tailored therapies that can improve patient outcomes. Lipid nanocarriers are highly effective drug delivery systems that significantly improve their solubility, bioavailability, and stability while also minimizing unwanted side effects. Surface-modified lipid nanocarriers (liposomes, niosomes, solid lipid nanoparticles, nanostructured lipid carriers, lipid nanocapsules, lipid-polymer hybrid nanocarriers, lipoproteins, and lipoplexes) are employed to improve BBB penetration and uptake through various mechanisms. This systematic review illuminates and covers various topics related to brain malignancies. It explores the different methods of drug delivery used in treating brain malignancies and delves into the benefits, limitations, and types of brain-targeted lipid-based nanocarriers. Additionally, this review discusses ongoing clinical trials and patents related to brain malignancy therapies and provides a glance into future perspectives for treating this condition.

Intranasal delivery of doxepin: enhancing brain targeting efficiency utilizing nanostructured lipid carriers for a biopharmaceutics drug disposition classification system class-I drug

Doxepin, a Class-I Biopharmaceutics Drug Disposition Classification System (BDDCS) drug, exhibits poor bioavailability due to extensive first-pass metabolism. This research focuses on enhancing the delivery of doxepin by formulating nanostructured lipid carriers (NLCs) through the utilization of the Box–Behnken Design methodology. These optimized NLCs are intended for intranasal administration, with the ultimate goal of improving nose-to-brain drug delivery. NLCs were formulated using a high-speed homogenization technique. The optimized batch had a small particle size (75.80 ± 5.48 nm, PDI = 0.286), high entrapment efficiency (94.10 ± 0.16%), and sustained ex vivo release (82.25 ± 4.61% at 24 h). Characterization studies confirmed the conversion of doxepin from a crystalline to an amorphous state with uniform distribution in the lipid matrix. In vivo pharmacokinetic studies in rats showed significantly higher doxepin concentration in the brain tissue (Cmax = 16.77 µg/g, tmax = 30 min) after intranasal administration compared to intravenous administration (Cmax = 2.53 µg/g, tmax = 6 h). High-drug targeting efficiency (DTE = 284.3%) and direct transport percentage (DTP = 64.8%) suggested direct penetration of NLCs in the brain via olfactory and trigeminal pathways. In conclusion, the study highlights the potential of NLCs to improve the bioavailability of doxepin through nose-to-brain delivery and thereby potentially enable the treatment of neurological disorders.

A Review on Nanostructured Lipid Carriers as Promising Drug Delivery Vehicle to Target Various Cancers via Oral Route: A Step towards “Chemotherapy at Home”

Abstract: Oral drug administration is largely preferred owing to enhanced patient compliance, convenience of self-intake of dose, non-invasiveness, and low manufacturing cost. Cancer is a condition that starts with aberrant cell division at an uncontrolled rate. The clinical effectiveness of many anticancer drugs is limited by their physicochemical characteristics and physiological circumstances in the GI tract. Nanostructured lipid carriers have the potential to enhance the bio-availability of anticancer drugs by entrapping them. The NLCs, by virtue of their nanosize and their biocompatibility, can bypass the first-pass metabolism and be taken up by M cells of Peyer’s patches to deliver the drug to the deeper tumours. The proposed review highlights the potential of NLCs in oral drug delivery for the management of various cancers. It discusses various strategies, method of preparation, mechanism of uptake, and their applications in the treatment of cancer via oral delivery. Further, it explains the recent advances and future perspectives.

Recent Updates on Nanocarriers for Drug Delivery in Posterior Segment Diseases with Emphasis on Diabetic Retinopathy.

In recent years, various conventional formulations have been used for the treatment and/or management of ocular medical conditions. Diabetic retinopathy, a microvascular disease of the retina, remains the leading cause of visual disability in patients with diabetes. Currently, for treating diabetic retinopathy, only intraocular, intravitreal, periocular injections, and laser photocoagulation are widely used. Frequent administration of these drugs by injections may lead to serious complications, including retinal detachment and endophthalmitis. Although conventional ophthalmic formulations like eye drops, ointments, and suspensions are available globally, these formulations fail to achieve optimum drug therapeutic profile due to immediate nasolacrimal drainage, rapid tearing, and systemic tearing toxicity of the drugs. To achieve better therapeutic outcomes with prolonged release of the therapeutic agents, nano-drug delivery materials have been investigated. These nanocarriers include nanoparticles, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), dendrimers, nanofibers, in-situ gel, vesicular carriers, niosomes, and mucoadhesive systems, among others. The nanocarriers carry the potential benefits of site-specific delivery and controlled and sustained drug release profile. In the present article, various nanomaterials explored for treating diabetic retinopathy are reviewed.

Design and Characterisation of Curcumin-Loaded Nanostructured Lipid Carriers for Safe and Efficient Topical Drug Delivery in The Treatment of Pressure Ulcer

Pressure ulcers (PU) are chronic lesions with a high prevalence in at-risk populations. Although curcumin has various therapeutic properties, its use as a dermal therapeutic agent is limited by its poor solubility and permeability. This study aimed to develop nanostructured lipid carriers (NLCs) to facilitate the topical use of curcumin as wound healing agent in treating PU. The optimised curcumin-NLCs were characterised for their physicochemical properties, drug release, and skin permeation, while effectiveness and toxicity were investigated via cell viability, scratch assays, and an in vivo skin irritation test. The optimised curcumin-NLCs comprised 3.5% solid lipids, 1% surfactant, and 2% co-surfactant with an average particle size of 134.68±6.0 nm, polydispersity index of 0.248±0.00, zeta potential of −44.94±5.44, percentage of encapsulation efficiency of 93.42±0.32%, and drug loading of 0.11±0.00%. Curcumin-NLCs showed stable physicochemical properties and extended drug release for up to 48 h, with a cumulative release of 77.72% following a first-order kinetics. The formulation exhibited slower curcumin permeation than the free curcumin. Furthermore, the safe and non-toxic curcumin-NLCs were highly effective at 0.98 μM and showed a high rate of wound closure without skin irritation. Collectively, the NLCs developed for topical delivery of curcumin demonstrated prolonged and sustained release and improved wound healing activity, which indicates that curcumin-NLCs are a viable strategy for treating PU.

Integrating Natural Deep Eutectic Solvents into Nanostructured Lipid Carriers: An Industrial Look.

The industries are searching for greener alternatives for their productions due to the rising concern about the environment and creation of waste and by-products without industrial utility for that specific line of products. This investigation describes the development of two stable nanostructured lipid carriers (NLCs): one is the formulation of a standard NLC, and the other one is the same NLC formulation associated with a natural deep eutectic solvent (NaDES). The research presents the formulation paths of the NLCs through completeness, which encompass dynamic light scattering (DLS), zeta potential tests, and pH. Transmission electron microscopy (TEM) and confocal microscopy were performed to clarify the morphology. Cytotoxicity tests with zebrafish were realized, and the results are complementary to the in vitro outcomes reached with fibroblast L132 tests by the MTT technique and the zymography test. Infrared spectroscopy and X-ray diffractometry tests elucidated the link between the physicochemical characteristics of the formulation and its behavior and properties. Different cooling techniques were explored to prove the tailorable properties of the NLCs for any industrial applications. In conclusion, the compiled results show the successful formulation of new nanocarriers based on a sustainable, eco-friendly, and highly tailorable technology, which presents low cytotoxic potential.

Emu oil enriched nanostructured lipid carriers of lornoxicam burdened polymeric gel augmented drug delivery and assisted cartilage repairing in knee osteoarthritis: In-vitro and in-vivo studies

Lornoxicam (LRX) alleviates pain and inflammation associated with knee osteoarthritis (OAS). However, inadequate solubility, short half-life, and gastrointestinal side-effects on chronic use hinder the efficacy of LRX through oral route. Therefore, in present investigation, lornoxicam loaded nanostructured lipid carriers (LRX-NLCs) were scaled-up post optimization using hot homogenization method. The optimized F14 LRX-NLCs demonstrated particle size of 172.1 ± 2.0 nm with polydispersity index (PDI) of 0.293 ± 0.01, zeta (ζ) potential of −15.5 ± 1.21 mV, entrapment efficiency of 92.85 ± 0.25 % and drug release up to 18.9 ± 1.8 % at 3 h in addition to sustained release pattern throughout 24 h. Later, F14 LRX-NLCs were amalgamated with carbopol 940 LR gel as LRX-NLCs-Gel and evaluated for pH, spreadability, drug content, rheological behavior, texture properties, ex-vivo skin permeation and retention, and dermal distribution. Furthermore, pharmacodynamic studies of LRX-NLCs-Gel disclosed a substantial diminution in pain and inflammation in addition to amended radiographic and histopathological features in monosodium iodoacetate (MIA) induced OAS in Sprague Dawley rats. LRX-NLCs-Gel exhibited a remarkable decline in the levels of pro-inflammatory cytokines such as IL-1β, TNF-α, in addition to COX-2 in knee OAS. LRX-NLCs-Gel presented an epochal decrease in synovial hyperplasia, inflammation, and ameliorated cartilage structure. In addition, omega-3, omega-6, and omega-9 fatty acids enriched emu oil might have assisted in offering synergistic activity with LRX in cartilage repairing due to suppression of the proteolytic activity of MMP-2 and MMP-9. In conclusion, LRX-NLCs-Gel may be a prospective candidate for translating the product in to a clinically viable dosage form.

Improvement of Bioavailability of Bilastine Nanostructured Lipid Carriers for the Treatment of Allergic Rhinitis

Improvement of Bioavailability of Bilastine Nanostructured Lipid Carriers for the Treatment of Allergic Rhinitis