Nanostructured Lipid Carrier System Research Articles

Nanostructured lipid carriers for enhanced batimastat delivery across the blood-brain barrier: an in vitro study for glioblastoma treatment.

Glioblastoma presents a significant treatment challenge due to the blood-brainbarrier (BBB) hindering drug delivery, and the overexpression of matrix metalloproteinases (MMPs), which promotes tumor invasiveness. This study introduces a novel nanostructured lipid carrier (NLC) system designed for the delivery of batimastat, an MMP inhibitor, across the BBB and into the glioblastoma microenvironment. The NLCs were functionalized with epidermal growth factor (EGF) and a transferrin receptor-targeting construct to enhance BBB penetration and entrapment within the tumor microenvironment. NLCs were prepared by ultrasonicator-assisted hot homogenization, followed by surface functionalization with EGF and the construct though carbodiimide chemistry. The construct was successfully conjugated with an efficiency of 81%. Two functionalized NLC formulations, fMbat and fNbat, differing in the surfactant amount, were characterized. fMbat had a size of 302nm, a polydispersity index (PDI) of 0.298, a ζ-potential (ZP) of -27.1mV and an 85% functionalization efficiency (%FE), whereas fNbat measured 285nm, with a PDI of 0.249, a ZP of -28.6mV and a %FE of 92%. Both formulations achieved a drug loading of 0.42μg/mg. In vitro assays showed that fNbat was cytotoxic and failed to cross the BBB, while fMbat showed cytocompatibility at concentrations 10 times higher than the drug's IC50. Additionally, fMbat inhibited MMP-2 activity between 11 and 62% across different cell lines and achieved a three-fold increase in BBB penetration upon functionalization. Our results suggest that the fMbat formulation has potential for enhancing GB treatment by overcoming current drug delivery limitations and may be combined with other therapeutic strategies for improved outcomes.

Preparation, Physicochemical, and Antibacterial Characterization of Nanostructured Lipid Carrier System Containing Tinidazole for Buccal Mucosa Delivery

Preparation, Physicochemical, and Antibacterial Characterization of Nanostructured Lipid Carrier System Containing Tinidazole for Buccal Mucosa Delivery

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.

Development and optimization of thyme-pennyroyal essential oils based active nanostructured lipid carrier (NLC) containing saffron extract with antioxidant and antimicrobial properties

The saffron extract-loaded nanostructured lipid carrier (NLC) was synthesized by the double emulsion (W/O/W) method for application as a preservative to increase the oxidative and microbial stability of French dressing. The optimization of the NLC system was carried out using a combined D-optimal design methodology and effect of thyme (TEOs)/pennyroyal (PEOs) essential oils, and polyglycerol ester (PGE)/polyglycerol polyricinolate (PGPR) surfactants ratios (independent variables) were investigated on the mean particle size, polydispersity, zeta potential, and encapsulation efficacy (dependent variables). The optimal formulation (NLC opt) was obtained as 90/10 thyme/pennyroyal essential oils and 90/10 polyglycerol esters/polyglycerol polyricinoleate ratio, which resulted in the lowest PDI and particle size (0.38 and 66.87 nm respectively), highest zeta potential and encapsulation efficiency (−26.7 mV and %78.88 respectively). Different techniques including transmission electron microscopy (TEM), Fourier transform-infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) analysis were used for the characterization of structure and physicochemical properties of the different NLC systems and confirmed successful incorporation of SE into NLC. The DPPH test showed decrement of antioxidant activity during 30 days of storage and IC50 value was lower in the SE-NLC (0.68 mg/ml) than in the free extract. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) tests against S. aureus, E. coli, and P. aeruginosa indicated that the SE did not have antibacterial properties. However, NLC formulations showed antimicrobial effect due to the presence of TEOs and PEOs essential oils. Peroxide value of control sample was the highest (8/35 O2/kg) and it was the lowest (3.75 O2/kg) in French dressing with SE-NLC.

Quality by design approach of apocynin loaded clove oil based nanostructured lipid carrier as a prophylactic regimen in hemorrhagic cystitis in vitro and in vivo comprehensive study

Apocynin (APO) is a naturally occurring acetophenone with eminent anti-inflammatory and anti-oxidant peculiarities. It suffers from poor bioavailability due to low aqueous solubility. Herein, APO was loaded in a Clove oil (CO) based Nanostructured lipid carrier (NSLC) system using a simple method (ultrasonic emulsification) guided by a quality-by-design approach (23 full factorial design) to optimize the formulated NSLCs. The prepared NSLCs were evaluated regarding particle size (PS), polydispersity index (PDI), zeta potential (ZP), and entrapment efficiency (EE%). The optimal formula (F2) was extensively investigated through transmission electron microscope (TEM), Fourier transform infrared (FT-IR) spectroscopy, Differential scanning calorimetry (DSC), X-ray diffractometry (XRD), in vitro release, and stability studies. Cytotoxicity against human urinary bladder carcinoma (T24) cell line and in vivo activity studies in rats with induced cystitis were also assessed. The results disclosed that the optimal formula (F2) had PS of 214.8 ± 5.8 nm with EE% of 79.3 ± 0.9%. F2 also exhibited a strong cytotoxic effect toward the T24 cancer cells expressed by IC50 value of 5.8 ± 1.3 µg/mL. Pretreatment with the optimal formula (orally) hinted uroprotective effect against cyclophosphamide (CP)-induced hemorrhagic cystitis (HC) in rat models, emphasized by histopathological, immunohistochemical, and biochemical investigations. In consideration of the simple fabrication process, APO-loaded CO-based NSLCs can hold prospective potential in the prophylaxis of oncologic and urologic diseases.

Evaluation of Emulgel and Nanostructured Lipid Carrier-Based Gel Formulations for Transdermal Administration of Ibuprofen: Characterization, Mechanical Properties, and Ex-Vivo Skin Permeation

In transdermal applications of nonsteroidal anti-inflammatory drugs, the rheological and mechanical properties of the dosage form affect the performance of the drug. The aim of this study to develop emulgel and nanostructured lipid carrier NLC-based gel formulations containing ibuprofen, evaluate their mechanical properties, bioadhesive value and ex-vivo rabbit skin permeability. All formulations showed non-Newtonian pseudoplastic behavior and their viscosity values are suitable for topical application. The particle size of the nanostructured lipid carrier system was found to be 468 ± 21 nm, and the encapsulation efficiency was 95.58 ± 0.41%. According to the index of viscosity, consistency, firmness, and cohesiveness values obtained as a result of the back extrusion study, E2 formulation was found to be more suitable for transdermal application. The firmness and work of shear values of the E2 formulation, which has the highest viscosity value, were also found to be the highest and it was chosen as the most suitable formulation in terms of the spreadability test. The work of bioadhesion values of NLC-based gel and IBU-loaded NLC-based gel were found as 0.226 ± 0.028 and 0.181 ± 0.006 mJ/cm2 respectively. The percentages of IBU that penetrated through rabbit skin from the Ibuactive-Cream and the E2 were 87.4 ± 2.11% and 93.4 ± 2.72% after 24 h, respectively. When the penetration of ibuprofen through the skin was evaluated, it was found that the E2 formulation increased penetration due to its lipid and nanoparticle structure. As a result of these findings, it can be said that the NLC-based gel formulation will increase the therapeutic efficacy and will be a good alternative transdermal formulation.Graphical

Development and physicochemical characterization of nanostructured lipid carriers for entrapment of vitamin D3 prepared at different lipid ratios

Development and physicochemical characterization of nanostructured lipid carriers for entrapment of vitamin D3 prepared at different lipid ratios

Antitumor activity of essential oils-based nanostructured lipid carriers on prostate cancer cells

Prostate cancer (PCa) is the second most frequent malignancy in men worldwide. Essential oils (EOs) are natural products which can act in cancer suppression by several mechanisms. In this work, a nanotechnological approach was used to develop and evaluate the antineoplastic effects of EOs loaded by nanostructured lipid carriers (NLCs). Three different NLC systems composed of cinnamon, sage or thyme EOs were optimized using factorial design (23). The optimal formulations were characterized in terms of biophysical parameters, structure, stability, in vivo safety and efficacy. All optimized NLC formulations exhibited excellent structural properties and stability over a year (25 °C). They proved to be in vitro and in vivo biocompatible on PNT2 normal prostate cells and on chicken embryos (CE), respectively. In PC3 PCa cells, optimized NLCs inhibited cell proliferation and migration and changed its morphology. In CE xenograft tumor, NLCs have inhibited tumor growth and angiogenesis. The results from this work suggested that all developed EO-based NLC formulations had their stability improved while the biological activity remains unchanged.

Pharmacokinetics and Pharmacodynamics of a Nanostructured Lipid Carrier Co-Encapsulating Artemether and miRNA for Mitigating Cerebral Malaria.

Cerebral malaria (CM), a severe neurological pathology caused by Plasmodium falciparum infection, poses a significant global health threat and has a high mortality rate. Conventional therapeutics cannot cross the blood-brain barrier (BBB) efficiently. Therefore, finding effective treatments remains challenging. The novelty of the treatment proposed in this study lies in the feasibility of intranasal (IN) delivery of the nanostructured lipid carrier system (NLC) combining microRNA (miRNA) and artemether (ARM) to enhance bioavailability and brain targeting. The rational use of NLCs and RNA-targeted therapeutics could revolutionize the treatment strategies for CM management. This study can potentially address the challenges in treating CM, allowing drugs to pass through the BBB. The NLC formulation was developed by a hot-melt homogenization process utilizing 3% (w/w) precirol and 1.5% (w/v) labrasol, resulting in particles with a size of 94.39 nm. This indicates an effective delivery to the brain via IN administration. The results further suggest the effective intracellular delivery of encapsulated miRNAs in the NLCs. Investigations with an experimental cerebral malaria mouse model showed a reduction in parasitaemia, preservation of BBB integrity, and reduced cerebral haemorrhages with the ARM+ miRNA-NLC treatment. Additionally, molecular discoveries revealed that nicotinamide adenine dinucleotide phosphate oxidase 2 (NOX2) and Interleukin-6 (IL-6) levels were reduced in the treated groups in comparison to the CM group. These results support the use of nanocarriers for IN administration, offering a viable method for mitigating CM through the increased bioavailability of therapeutics. Our findings have far-reaching implications for future research and personalized therapy.

Design of smart chemotherapy of doxorubicin hydrochloride using nanostructured lipid carriers and solid lipid nanoparticles for improved anticancer efficacy

Doxorubicin hydrochloride (DOX) is an anticancer agent used in cancer chemotherapy. The purpose of this study was to design nanostructured lipid carriers (NLCs) of DOX as smart chemotherapy to improve its photostability and anticancer efficacy. The characteristics of DOX and DOX-loaded NLCs were investigated using UV–Vis spectroscopy, Fourier transform infrared (FTIR) spectroscopy, particle size, and zeta potential study. The cytotoxicity of DOX was evaluated against three cancer cell lines (HeLa, A549, and CT-26). The particle size and zeta potential were in the range 58.45-94.08 nm and −5.80 mV - −18.27 mV, respectively. The chemical interactions, particularly hydrogen bonding and van der Waals forces, between DOX and the main components of NLCs was confirmed by FTIR. NLCs showed the sustained release profile of DOX. The photostability results revealed that the NLC system improved the photostability of DOX. Cytotoxicity results using the three cell lines showed that all formulations improved the anticancer efficacy of free DOX, and the efficacy was dependent on cell type and particle size. These results suggest that DOX-loaded NLCs are promising chemotherapeutic agents for cancer treatment.

Co-Delivery of siRNA and Docetaxel to Cancer Cells by NLC for Therapy.

The present study aims to develop a delivery system that can carry small interference RNA (siRNA) with small-molecule chemotherapeutic drugs, which can be used in cancer treatment. The drug delivery system combines the advantages of a therapeutic agent with two different mechanisms to ensure that it is used efficiently for cancer therapy. In this study, a nanostructured lipid carrier system was prepared, Docetaxel was loaded to these systems, and the Eph siRNA was adsorbed to the outer surface. In addition, DOTAP was added to the lipophilic phase to load a positive charge on the lipidic structure for interaction with the cells. Moreover, characterization, cytotoxicity, and transfection procedures were performed on the whole system. This candidate system was also compared to Taxotere, which is the first approved Docetaxel-containing drug on the market. Given the results, it was determined that the particle size of NLC-DTX was 165.3 ± 3.5 nm, the ζ potential value was 38.2 ± 1.7 mV, and the PDI was 0.187 ± 0.024. Entrapment efficacy of nanoparticles was found to be 92.89 ± 0.21%. It was determined that the lipidic system prepared in vitro release analyses were able to provide sustained release and exhibit cytotoxicity, even at doses lower than the dose used for Taxotere. The formulations prepared had a higher level of effect on cells when compared with pure DTX and Taxotere, but they also exhibited time-dependent cytotoxicity. It was also observed that the use of Eph siRNA together with the chemotherapeutic agent via formulation also contributed to this cell death. The results of the present study indicate that there is a promising carrier system in order to deliver hydrophilic nucleic acids, such as siRNA, together with lipophilic drugs in cancer treatment.

REVIEW: REVIEW ARTICLE LIPID-BASED NANOTECHNOLOGY

Nanotechnology is defined as engineering the creation of materials, functions, and devices on the nanometer scale. Nanoscience is increasingly developing and becoming a part of various fields, such as electronics, materials, and biology. Lipid nanoparticles are a major application in nanotechnology. In formulas II and III, smaller results were obtained compared with the other formulas. Based on the results of this study, it can be concluded that the nanostructured lipid carrier system with solid lipid poloxamer and stearic acid with liquid soybean oil lipids obtained good characteristics, and each test met the range. From the explanation above, it can be concluded that lipid-based nanotechnology has great potential in various fields such as medicine, cosmetics, and agriculture. Its use can provide great benefits such as increasing the effectiveness of drug administration, increasing the absorption of nutrients in food, and developing cosmetic products. which one is safer and more effective. To compare several types of nanoparticle methods, such as Liposomes, Neosomes, Etosomes, SLN, and NLC for selection of the lipid base, namely NLC. It is important to ensure that the use and development of this technology are safe and beneficial for humans and the environment. Keywords : Nanotechnology, Nanoparticles, Lipid-Based Nanoparticles

Co-administration of Adapalene loaded Nanostructured lipid carriers and Vitamin-E for management of acne

The present work is aimed to design, develop and characterize a novel nanostructured lipid carrier system based formulation for selective and customized delivery of adapalene and Vit-E for effective management of acne vulgaris. Adapalene loaded nanostructured lipid carriers were developed by modified melt dispersion ultrasonication technique, followed by cooling and high speed mechanical stirring. Principally in the process glyceryl tristearin was used as solid lipid and oleic acid as liquid lipid, phospholipid 90G was used as surfactant and carbopol was used as gelling material. The prepared nanocarriers were characterized in terms of particle size, zeta potential, polydispersity index, entrapment efficiency, transmission electron microscopy (TEM) and in-vitro drug release study. The particle size of optimized carrier was reported as 219.8nm. TEM analysis was also performed to assure particle size and shape of carrier system. Entrapment efficiency of optimized formulation was above 87.4%. The drug release from carrier have shown dual biphasic release pattern firstly the drug release rate was rapid which showed initial burst release pattern and subsequently sustained release pattern was observed which is required in treatment of acne. Then prepared and optimized formulation was subjected to skin permeation study in male Wistar rats. Formulation was also characterized for skin distribution study, skin irritation study and stability study of gel. So it was concluded in our research that this novel carrier system having adapalene and Vit-E can be a very innovative alternate of conventional antiacne therapy. In our research, drug is localized in superficial skin layer and systemic penetration of drug was avoided. Further, concrete research can open new avenues in antiacne treatment.

Guar gum series affect nanostructured lipid carriers via electrostatic assembly or steric hindrance: Improving their oral delivery for phytosterols

Surface modification of nanostructured lipid carriers (NLCs) can be an effective way to improve their oral delivery for active ingredients. In this study, four type of guar gum series modified NLCs for the delivery of phytosterols (PS) were constructed and the effects of the polysaccharides on their structure and physicochemical properties were studied. DLS and AFM results revealed that positively charged polysaccharides could bind to PS-NLCs through electrostatic attraction and made the complexes finally take positive charges, while negatively charged polysaccharides were more likely to fill in the gaps of NLC systems to achieve a balance between electrostatic repulsion and intermolecular forces. Although all four polysaccharides exhibited good storage stability and controlled release of PS in simulated intestinal digestion, PS-NLCs modified with partially hydrolyzed cationic guar gum (PHCG) at medium or high concentrations exhibited better gastric stability, mucoadhesion, and cellular uptake, which had considerable significance for improving the oral bioavailability of PS. This might be related to the coating structure of PHCG-PS-NLCs confirmed by AFM, FTIR, and Raman characterization. This study provide a reference value for designing suitable PS-NLC complexes without synthetic surfactants.

Propolis-Based Nanostructured Lipid Carriers for α-Mangostin Delivery: Formulation, Characterization, and In Vitro Antioxidant Activity Evaluation.

α-Mangostin (a xanthone derivative found in the pericarp of Garcinia mangostana L.) and propolis extract (which is rich in flavonoids and phenols) are known for their antioxidant properties, making them potential supplements for the treatment of oxidative stress-related conditions. However, these two potential substances have the same primary drawback, which is low solubility in water. The low water solubility of α-mangostin and propolis can be overcome by utilizing nanotechnology approaches. In this study, a propolis-based nanostructured lipid carrier (NLC) system was formulated to enhance the delivery of α-mangostin. The aim of this study was to characterize the formulation and investigate its influence on the antioxidant activity of α-mangostin. The results showed that both unloaded propolis-based NLC (NLC-P) and α-mangostin-loaded propolis-based NLC (NLC-P-α-M) had nanoscale particle sizes (72.7 ± 1.082 nm and 80.3 ± 1.015 nm, respectively), neutral surface zeta potential (ranging between +10 mV and -10 mV), and good particle size distribution (indicated by a polydispersity index of <0.3). The NLC-P-α-M exhibited good entrapment efficiency of 87.972 ± 0.246%. Dissolution testing indicated a ~13-fold increase in the solubility of α-mangostin compared to α-mangostin powder alone. The incorporation into the propolis-based NLC system correlated well with the enhanced antioxidant activity of α-mangostin (p < 0.01) compared to NLC-P and α-mangostin alone. Therefore, the modification of the delivery system by incorporating α-mangostin into the propolis-based NLC overcomes the physicochemical challenges of α-mangostin while enhancing its antioxidant effectiveness.

Formulation Development and Evaluation of Dry Adsorbed Nanoparticles of Curcumin and Piperine Dual Drug Loaded Nanostructured Lipid Carriers

Purpose: The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of curcumin (CUR) and piperine (PIP) loaded nanostructured lipid carriers (NLCs). Methods: CUR and PIP-loaded NLCs (CP NLCs) were prepared by modified hot-melt emulsification using precirol ATO5 (PRE) as solid lipid, labrafac lipophile WL1349 (LAF) as liquid lipid, and a combination of tween 80 (T80) with gelucire 50/13 (G50/13) as surfactants. The NLCs system was subjected to physical stability, particle size, zeta potential, thermal behaviour, crystallinity study and in-vitro drug release. Further, an evaporative drying technique converted the NLC system into stable DANs by adsorbing onto mannitol (Pearlitol 200SD). The DANs were characterized for redispersion properties, particle size, flow properties and in-vitro drug release. The stability studies were carried out for 30 days. Results: The optimized CP NLCs were of imperfect type and had a mean particle size of 248.5 ± 12.8 nm (size distribution of 0.216 ± 0.021), a zeta potential of -9.03 ± 0.53 mV, an entrapment efficiency (EE) of 99.80 ± 0.21% (CUR), 100.05 ± 0.07% (PIP) with a drug recovery of 99.70 ± 0.21% (CUR) and 100.36 ± 0.12% (PIP). The X-ray diffraction pattern and endothermic peaks confirmed the encapsulation of actives in lipid matrices. The in-vitro drug release showed controlled release for 24 h. The optimized DANs led to maximum redispersion and retained a particle size of 268.4 ± 23.1 nm (distribution 0.235 ± 0.037) with controlled release similar to CP NLCs. The CP NLCs DANs showed reasonable stability for 30 days. Conclusions: The developed CP NLCs DANs showed a controlled release profile, and the adsorption technique can be used to improve the stability of NLC dispersion. The DANs can be offered in patient-friendly dosage forms such as sachets, capsules, and compressed tablets.

Effect of Different Lipid Ratios on Physicochemical Stability and Drug Release of Nanostructured Lipid Carriers Loaded Coenzyme Q10

Background: For treatment or skin care via topical route, Coenzyme Q10 needs to permeate the epidermis which it is practically insoluble in water and a high molecular weight that make it difficult to penetrate the skin. Nanostructured Lipid Carriers (NLC) is chosen because of its ability to dissolve and solve the problem of low skin permeation. The type and ratio of solid and liquid lipids used in NLC affect the physicochemical characteristics, thus affecting the release profile and system stability. Objective: This study aimed to determine the effect of various ratios of Compritol 888 ATO as solid lipid and Miglyol 812 as liquid lipid on the physicochemical stability and Coenzyme Q10 release profile of NLC system. Methods: NLC was prepared using High Shear Homogenization method with three different lipid ratios. The ratio of Compritol 888 ATO : Miglyol 812 was 70:30, 80:20, and 90:10, respectively. NLC was evaluated for drug release and stability parameters including organoleptic, particle size, polydispersity index (PI), pH, viscosity, assay, and entrapment efficiency. Results: The stability test result for 90 days showed increments in the particle size and viscosity, whereas for assay and entrapment efficiency were decreased. The release test results showed no significant difference in the release parameters of the three tested formulas. Conclusion: During stability evaluation, NLC-CoQ10 systems did not significantly change pH and PI values, but statistically significantly changed particle size, viscosity, assay, and entrapment efficiency. The different in lipid ratios used in the formulas did not show significantly different results for release parameters.

A Dual Therapy of Nanostructured Lipid Carrier Loaded with Teriflunomide-A Dihydro-Orotate Dehydrogenase Inhibitor and an miR-155-Antagomir in Cuprizone-Induced C57BL/6J Mouse.

The effective treatment of central nervous system (CNS) disorders such as multiple sclerosis (MS) has been challenging due to the limited ability of therapeutic agents to cross the blood-brain barrier (BBB). In this study, we investigated the potential of nanocarrier systems to deliver miR-155-antagomir-teriflunomide (TEF) dual therapy to the brain via intranasal (IN) administration to manage MS-associated neurodegeneration and demyelination. Our results showed that the combinatorial therapy of miR-155-antagomir and TEF loaded in nanostructured lipid carriers (NLCs) significantly increased brain concentration and improved targeting potential. The novelty of this study lies in the use of a combinatorial therapy approach of miR-155-antagomir and TEF loaded in NLCs. This is a significant finding, as the effective delivery of therapeutic molecules to the CNS has been a challenge in treating neurodegenerative disorders. Additionally, this study sheds light on the potential use of RNA-targeting therapies in personalized medicine, which could revolutionize the way CNS disorders are managed. Furthermore, our findings suggest that nanocarrier-loaded therapeutic agents have great potential for safe and economical delivery in treating CNS disorders. Our study provides novel insights into the effective delivery of therapeutic molecules via the IN route for managing neurodegenerative disorders. In particular, our results demonstrate the potential of delivering miRNA and TEF via the intranasal route using the NLC system. We also demonstrate that the long-term use of RNA-targeting therapies could be a promising tool in personalized medicine. Importantly, using a cuprizone-induced animal model, our study also investigated the effects of TEF-miR155-antagomir-loaded NLCs on demyelination and axonal damage. Following six weeks of treatment, the TEF-miR155-antagomir-loaded NLCs potentially lowered the demyelination and enhanced the bioavailability of the loaded therapeutic molecules. Our study is a paradigm shift in delivering miRNAs and TEF via the intranasal route and highlights the potential of this approach for managing neurodegenerative disorders. In conclusion, our study provides critical insights into the effective delivery of therapeutic molecules via the IN route for managing CNS disorders, and especially MS. Our findings have significant implications for the future development of nanocarrier-based therapies and personalized medicine. Our results provide a strong foundation for further studies and the potential to develop safe and economic therapeutics for CNS disorders.

Application of sodium caseinate as protein based coating/stabilizing agent in development and optimization of vitamin D3-loaded nanostructured lipid carriers (NLCs)

Sodium caseinate is a food-grade protein that has several functional properties, such as acting as an emulsifying and stabilizing agent in a colloidal delivery system. Nanostructured lipid carriers (NLCs) have been proven to be highly effective carriers for encapsulating bioactive compounds. In this research, several novel food-grade NLC systems based on sodium caseinate (as a protein surfactant), anhydrous milk fat (as a solid lipid), and vitamin E acetate (as a liquid oil) were developed as an encapsulant for vitamin D3. The D-optimal combined design was employed to optimize the effects of lipid phase ratios and protein concentrations on particle size and loading efficiency. The optimized formulation obtained from the predicted model was composed of 1% w/v caseinate protein and a 73.23/26.78 solid lipid/liquid oil ratio with a desirability function of 0.983. This optimum formulation showed the smallest particle size at 120.16 nm with a narrow size distribution of 0.208 and an encapsulation efficiency of 96.14%. The cytotoxicity study showed that the anticancer effect of the vitamin was improved after incorporation into the NLC structure. The current study suggests that this composition of biopolymeric surfactant and applied lipid matrix could be an effective, health-promoting, and promising carrier system for developing food-grade bioactive delivery systems.

Screening and selection of formulation components of nanostructured lipid carriers system for Mitragyna Speciosa (Korth). Havil drug delivery

Nanostructured lipid carriers (NLC) have evolved as effective vehicles for improving the bioavailability of poorly water-soluble drugs as well as protecting them from degradation and metabolism. The present study investigated the preformulation and its impact on different liquid lipids and solid lipids with diverse chemical structures and hydrophilic-lipophilic balance (HLB) for the critical quality attributes of Mitragyna speciosa leaves extract (MS)-based nanostructured lipid carriers suitable for drug delivery system. The presence of bioactive alkaloids (mitragynine, 7-hydroxymitragynine, speciogynine), flavonoids (quercetin, apigenin, kaempferol), saponins (daucosterol, quinovic acid 3-o-beta-d-quinovopyranoside, 1-o-feruloyl-beta-d-glucose), and other bioactive phytochemicals (chlorogenic acid, umbelliferone, ursolic acid) in MS leaves extract was detected using LCMS/MS analysis to support its medicinal properties. The total phenolic content, total flavonoid content, and DPPH assay of MS were 90.88 ± 0.30 GAE mg/g, 50.43 ± 0.47 QE mg/g, and IC50 at 0.0397 ± 0.0035 mg/mL, respectively. The screening preparation of NLC requires the selection of liquid lipid (oil), solid lipid, and surfactant. Based on the solubility test, the maximum solubility of MS leaves extract in oleic acid (liquid lipid) and compritol ATO 888 (solid lipid) were 2.859 ± 0.010% and 53.02 ± 0.39% respectively at ratio 70:30. Tween 80 was selected as the main surfactant for the preparation of NLC due to its highest emulsification efficiency (51.53%). The antimicrobial study showed that MS leaves extract gives antimicrobial effect towards Streptococcus aureus bacteria. The preformulation information collected offers a better, efficient, and cost-effective choice for further formulation development of MS leaves extract in drug delivery systems.