Unleashing the Potential of Cubosomes to Overcome Ocular Barriers in Precision Drug Delivery

The purpose of this research is to determine the optimum composition of solid lipid and liquid lipid in order to increase the penetration and effectiveness of Q10 as antioxidant in anti-aging cosmetics. Solid lipid and liquid lipid used in this study were cetyl palmitate and caprylic, which were combined to four (4) different ratios, namely 10:0; 9:1; 7:3 and 5:5. NLC Q10 in this study was produced by high shear homogenization method at 3400 rpm for 5 cycles and at 24000 for 1 cycle. The fourth formula was evaluated in term of characteristics, penetration and effectiveness. From the pH test , it was known that all formulas met the skin pH range (4.0-6.0). For the particle size test , all formulas (NLC 1 - NLC 4) were in the range from 269.13 to 354.77 nm with NLC 3 (7: 3) had the smallest particle size. The results of viscosity and surface tension test were also consistent with the theory, where the addition of liquid lipid reduced viscosity and surface tension of the system. The entrapment efficiency (EE) demonstrated the EE of NLC 1: 22.24%; NLC 2: 24.71%; NLC 3: 58.21% and NLC 4:36.94%. The penetration test showed all systems were able to penetrate the dermis layer at the 5th hour. NLC 3 (7:3) had more rapid onset, while the NLC Q10 with the ratio of lipid 9:1, had slower onset of action but can penetrate farther than the other NLC Q10 system. The result of Q10 effectiveness test showed NLC 2 (9:1) has lowest total macrophage (23.33) and very dense collagen observation (score : 4). From this research, it can be concluded that NLC 2 (9:1) had the most optimal lipid composition to increase the penetration and effectiveness of Q10 as an antioxidant in anti-aging cosmetics.

Nanostructured lipid carriers (NLCs) have attracted considerable interest as drug delivery systems capable of enhancing the solubility and oral bioavailability of poorly water-soluble drugs. In our previous work, cannabidiol (CBD)-loaded NLCs prepared by hot homogenization demonstrated improved dissolution and oral bioavailability. In the present study, hot-melt extrusion (HME) was investigated as a rapid and easily scalable alternative method for the preparation of CBD NLCs. Additionally, spray drying was used to convert the prepared CBD NLCs into a solid dosage form. CBD NLCs were prepared using HME at different screw speeds (100, 200, and 300rpm), followed by probe sonication, and characterized for particle size, entrapment efficiency (EE), and drug release. Spray drying was performed with different carriers (D-lactose, Kollidon® VA 64, maltodextrin 12, and Soluplus®) to evaluate their compatibility and performance. The results showed that the screw speed has an impact on the properties of the NLCs, while probe sonication further reduced particle size, resulting in enhanced entrapment efficiency, and drug release of all formulations. Although NLC produced at a screw speed of 300rpm was the most stable in both 4°C and 25°C. Among the carriers tested for spray drying, maltodextrin achieved nearly complete CBD release, while Soluplus® led to increased particle size and reduced release. Overall, HME combined with probe sonication proved to be a robust approach for the preparation of CBD NLCs, which were successfully converted into solid powder formulations by spray drying, offering a promising strategy for scalable production of CBD NLCs.

Spray drying of fenofibrate loaded nanostructured lipid carriers

Lipid nanoparticles as vehicles for topical psoralen delivery: Solid lipid nanoparticles (SLN) versus nanostructured lipid carriers (NLC)

Development of heat-stable gelatin-coated nanostructured lipid carriers (NLC): Colloidal and stability properties

Objective This review aims to explore innovative therapeutic strategies, with a particular focus on recent advancements in drug delivery systems using bioinspired nanomaterials such as solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for the idiopathic pulmonary fibrosis (IPF). Significance of the review Current treatments for IPF, including the FDA-approved anti-fibrotic agents pirfenidone and nintedanib, primarily aim to slow disease progression rather than reverse fibrosis. Bioinspired nanomaterials like SLNs and NLCs have shown promise in enhancing the efficacy of anti-fibrotic agents by improving drug solubility, stability, and targeted delivery. These systems not only minimize systemic side effects but also maximize therapeutic impact in lung tissues, offering a new hope for improved patient management and outcomes in this debilitating disease. Key findings SLNs facilitate sustained drug release and have demonstrated potential in delivering phosphodiesterase type 5 inhibitors effectively to lung cells. NLCs, on the other hand, exhibit superior biocompatibility and controlled release properties, making them suitable for pulmonary applications. Studies indicate that both SLNs and NLCs can enhance the bioavailability of drugs like ciprofloxacin and montelukast, thereby improving treatment outcomes in pulmonary conditions. Conclusion The integration of nanotechnology into anti-fibrotic therapy represents a significant advancement in addressing the challenges posed by IPF. By leveraging the unique properties of SLNs and NLCs, there is potential to overcome the limitations of current treatments and provide new therapeutic options that offer better management and improved outcomes for patients suffering from this debilitating disease.

Drug delivery via the oral route has always been challenging for poorly soluble drugs. Acid-induced hydrolysis, enzymatic degradation, and poor mucosal absorbency remain the primary hiccups for effective oral delivery of medications. With the advent of nanotechnology, nanostructured lipid carriers (NLCs) have emerged as a promising delivery carrier that can circumvent gastrointestinal tract (GIT) barriers hindering the solubility and bioavailability of such drugs. These NLCs can efficiently transport drug moieties across intestinal membranes shielding medications from intestinal pH and enzymatic degradation. Because they are composed of lipidic materials, they can be easily absorbed or taken up by various pathways such as transcellular absorption, paracellular transport, and M-cell uptake. Such mechanisms not only improve the absorption and solubility of drugs but also augment bioavailability and residence time and may bypass first-pass metabolism. This review explores the diverse applications of nanostructured lipid carriers (NLCs) in oral drug delivery for various medical conditions, shedding light on their current regulatory status, including FDA-approved options and those in pre/clinical stages. The review also features patented NLC formulations. It provides valuable insights into how NLCs can be harnessed for effective oral drug delivery and outlines recent advancements in optimizing their performance to tackle gastrointestinal barriers, thus opening new possibilities for NLCs in future pharmaceutical applications.

Objective: The aim of this study was to investigate physical characteristics of nanostructured lipid carriers (NLCs) mixture of alpha tocopheryl acetate, cetyl palmitate, Tween 80 and propylene glycol using high shear homogenization technique on NLC preparation to predict the optimum ratio of alpha tocopheryl acetate-cetyl palmitate to produce good characteristics of NLC loaded coenzyme, higher % EE, good penetration, controlled release, and stable.Methods: Lipid characterizations were conducted by diffraction scanning calorimetry, X-ray diffraction, and Fourier transforms infrared spectrophotometry. Coenzyme Q10 concentration was measured by spectrophotometer at 275 nm. NLC characteristics based on their morphology was determined using transmission electron microscope, particle size, and its polydispersity index which were measured with Delsa Nano™ particle size analyzer. Percentage of coenzyme Q10 entrapped in NLC was determined by dialysis bag method. Coenzyme Q10 release profile was measured using with Franz cell for 12 hrs. The penetration depth of NLC coenzyme Q10 in abdominal skin of Wistar rat was determined with fluorescence microscopy using rhodamine B as marker. NLC physical stability based on minimum of particle size variation, pH and viscosity during 90 days storage.Results: The result showed that formula with ratio of cetyl palmitate-alpha tocopheryl acetate 70:30 (% w/w) produce good characteristics of NLCloaded coenzyme, higher % EE, good penetration, controlled release, and stable in 90 days storage.Conclusion: The coenzyme Q10 NLC system with cetyl palmitate and alpha tocopherol acetate as lipid matrixare characterized by small particle size, low crystallinity, spherical morphology of particle and high coenzyme Q10 entrapment efficiency. Crystal modification led to the formation of a more amorphous thereby increasing the drug entrapmentKeywords: Coenzyme Q10, Nanostructured lipid carrier, Cetyl palmitate, Alpha tocopheryl acetate, High shear homogenization.

Background: The development of modern medical and pharmaceutical science has garnered lots of attention due to the development of targeted therapy and precision medicine. The current focus of the researchers is on developing strategies which provide the maximum therapeutic benefits with minimal adverse effects. In this scenario, nanostructured lipid carriers (NLC) have gained prominence because of their ability to improve the therapeutic properties of the drugs. Objective: In this review, we focus on some of the important methods involved in the preparation and characterization of the NLCs. We also discuss the application of NLC as a drug delivery system through different routes of administration and its role in overcoming the physiological and anatomical barriers. Methods: The literature was collected from different scientific browsers like sciencedirect, google scholar, pubmed and a total of 155 articles were read and analysed for the content. Results: The NLC improve the solubility and bioavailability of the drug, prolong the release and residence time and delay clearance. They also protect the drugs from enzymatic degradation and allow them to pass through different anatomical and physiological barriers. Conclusion: Though the use of NLCs has been reported across different therapeutic indications through various routes of administration, this success at the laboratory level has not gone to the next stage. One of the reasons for the failure of NLC formulations to progress to the next level could be due to toxicity caused by the accumulation of NLCs in organs. Hence, in order to utilize this strategy to its maximum potential, further research is inevitable.

The present study aimed to evaluate the effect of surfactant composition on the physical properties of nanostructured lipid carriers (NLCs) containing wheat germ oil (WGO) and to investigate the influence of both surfactant composition and pH on the oxidative stability of WGO encapsulated within the NLCs. The results showed that the smallest particle size (52.7 nm) was related to the NLC with the poloxamer-to-lipid ratio of 1:1 (Polox-NLC-1). Polox-NLC-1 not only showed good stability during storage, but also indicated a suitable physical structure from differential scanning calorimetry (DSC) analysis. The oxidative stability results indicated that the NLCs were more successful than O/W emulsion in protecting the WGO from oxidation. Additionally, the oxidative stability of the NLC with the poloxamer-to-lipid ratio of 2:1 (Polox-NLC-2) looked promising. Furthermore, NLCs prepared with the surfactant of poloxamer as a non-ionic surfactant had greater oxidative stability at high pH, and NLC prepared with sodium dodecyl sulfate (SDS) as an ionic surfactant had greater oxidative stability at low pH. These findings indicated that NLC could be an effective delivery and protection system for the WGO as a source of bioactive compounds.

Nanostructured lipid carriers loaded into in situ gels for breast cancer local treatment

Nanostructured lipid carriers (NLC) are based on mixture of solid lipids with spatially incompatible liquid lipids, which offer advantages of improving drug loading capacity and release properties. In the present study, hydroxycamptothecin (HCPT) loaded polyethylene glycol (PEG) modified NLC (PEG-NLC) was prepared by high pressure homogenize and spray drying method. PEG-NLC showed spherical particle with smooth surface in scanning electron microscopic (SEM) analysis. The crystallinity of lipid matrix within PEG-NLC was evaluated by powder X-ray diffraction and differential scanning calorimetry (DSC). The less ordered crystals or amorphous state of matrix were found in nanoparticles. A small, homogeneous particle size and high drug loading with fine entrapment efficiency of HCPT was obtained in PEG-NLC system. HCPT releasing from PEG-NLC showed a sustained release trend, and no significantly difference was found between two release curves of PEG-NLC before or after spray drying. After storage for 6 months, PEG-NLC powder after spray drying showed no significantly changes in particle size, drug loading and entrapment efficiency, crystal form and in vitro release. PEG modification statistically decreased the phagocytosis of NLC by RAW 264.7 cells, and spray drying process did not influence the cellular uptake of PEG-NLC. These results suggest that PEG-NLC prepared by spray drying is a stable and high-performance delivery system for HCPT.

Nanostructured lipid carriers of essential oils as potential tools for the sustainable control of insect pests

This study was aimed to determine the physical property and thermodynamic stability of nanostructured lipid carrier suspension incorporating ginsenoside F1 (GF1_NLC), and to evaluate its transport and antioxidant properties. GF1_NLC suspension possessed spherical particles with an average size of 98.9nm, and the encapsulation efficiency reached approximately 90%. There was a good compatibility between ginsenoside F1 (GF1) and the nanostructured lipid carrier (NLC) formulation, giving no contribution to the changes in the structural organization and crystallization behavior of lipid particles. However, the incorporation of GF1 reduced the thermodynamic stability of the lipid particles. The permeability of GF1_NLC (39.2%) across Caco-2 cell monolayer was higher than that of free GF1 (26.0%); however, no significant differences were observed in the radical scavenging activity (84.1% and 85.5%, respectively). In conclusion, NLC could be a potential candidate for the delivery of GF1 into the living body due to its small particle size, high encapsulation efficiency, and improved permeability. PRACTICAL APPLICATIONS: Poor water solubility in an aqueous solution and low absorption rate of ginsenoside F1 in the intestinal track limit its practical application in food systems. In this study, ginsenoside F1 was encapsulated in nanostructured lipid carrier to enhance its water solubility and absorption rate. The results of the encapsulated ginsenoside F1 showed high encapsulation efficiency of 90% with fine particle size of 98.9nm that could correspond to the enhancement of water solubility in an aqueous solution and permeability across Caco-2 cell monolayer. The results may encourage the food industry to utilize this encapsulation technique for the enhancement of the functional properties of poorly water-soluble bioactive compounds.

Topical ocular delivery of vancomycin loaded cationic lipid nanocarriers as a promising and non-invasive alternative approach to intravitreal injection for enhanced bacterial endophthalmitis management