Search

Summary: This article presents a switched‐capacitor‐based 13‐level inverter that exhibits step‐up property. The suggested converter makes use of a single DC source, 12 switches, three capacitors, and two diodes to accomplish the goal of producing a 13‐level output voltage while simultaneously achieving a boosting factor of six. Notably, inherent voltage balancing is attained for a wide variety of load types without the need of complex control methods or additional circuitry. In addition to this, the paper presents a comprehensive study of the power losses that occur across the different components of the converter. Multiple aspects of a topology's performance are taken into account during a comparison analysis with recent topologies that have a single and double DC sources connected to the input. The investigation incorporates simulations with both inductive and resistive loads. In order to validate that the proposed converter is effective, a prototype is built in the laboratory. The practicality of the suggested topology is shown by the collection of experimental result acquired under different loading situations. These findings include dynamic fluctuations in load and modulation indices. [ABSTRACT FROM AUTHOR]

This article examines the significance of Daniil Svyatskiy's research in unraveling the enigma of the Tunguska event. It aims to introduce a novel perspective on the origins and aftermath of the Tunguska Cosmic Body, alongside evaluating the potential hazards it poses to Earth. To achieve this goal, scientific papers addressing the Tunguska meteorite and its consequences, as well as chronicles describing the events under consideration, were analyzed. The chronicles support the hypothesis of a stable stream of comet fragments that could endanger Earth. Extensive areas between the 50th and 60th latitudes could be affected. The next manifestation of this stream is possible in 2038 or 2049. If the existence of the stream is confirmed in 2038 or 2049, it could pose a significant danger to the planet's population, emphasizing the need to monitor the Svyatskiy stream. The novelty of the study stems from the detailed examination of this hypothesis, which has not been taken seriously before. [ABSTRACT FROM AUTHOR]

Purpose: This study evaluated whether a nanostructured lipid carrier (NLC) delivery system could safely and accurately deliver nucleic acids to the cell nucleus using the enhanced green fluorescent protein (EGFP)-C1 plasmid model. Methods: The NLC was formulated using the emulsification method and equipped for cationic lipid-mediated transfection with 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP), which interacts electrostatically with nucleic acid. The NLC attributes, including size, polydispersity index, and zeta potential, were assessed by dynamic light scattering (DLS). The morphological structure was analyzed using transmission electron microscopy. Entrapment efficiency was evaluated by a direct method. Cellular uptake mechanisms of pEGFP-C1-NLC and the ability of pEGFP-C1 to penetrate the nucleus of TM4 cells to express EGFP were observed using confocal microscopy. Results: pEGFP-C1-NLC exhibited particle sizes in the range 56-88 nm with a particle charge range of -6.0 to+1.3 mV. The polydispersity index<0.5 showed good size uniformity, and entrapment efficiency of pEGFP-C1in the NLC was 92.06±2.295%. The NLC formulation was internalized predominantly via caveolae-mediated endocytosis, as indicated by EGFP expression following successful delivery of pEGFP by the NLC into the cells. Conclusion: NLC formulation could deliver genetic material to the nucleus and could be considered a gene therapy candidate for spermatogenesis. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

This paper presents a novel pentagonal structure dual-core photonic crystal fiber polarizing beam splitter (PS-DC-PCF PBS) filled with a nematic liquid crystal (NLC) in the central hole. Unlike previous designs with symmetric arrangements, the upper and lower halves of the structure have different air hole arrangements. The upper half consists of air holes arranged in a regular quadrilateral pattern, while the lower half features a regular hexagonal arrangement of air holes. By filling the central hole with birefringent liquid crystal, the birefringence of the structure is enhanced, reducing the coupling lengths along the x polarization and y polarization directions. The polarization properties, coupling characteristics, and the influence of different structural parameters on the extinction ratio of the polarizing beam splitter are analyzed using the full-vector finite element method. Simulation results demonstrate that the designed PS-DC-PCF PBS achieves a maximum extinction ratio (ER) of 72.94 dB with a splitting length of only 61.9 μm and a wide operating bandwidth of 423 nm (1.324–1.747 μm), covering most of the O, E, S, C, L, and U communication bands. It exhibits not only ultra-short splitting lengths and ultra-wide splitting bandwidth but also good manufacturing tolerances and anti-interference capabilities. The designed PS-DC-PCF PBS could provide crucial device support for future all-optical communication systems and has potential applications in fiber optic communication or fiber laser systems. [ABSTRACT FROM AUTHOR]

Background: We aimed to investigate the simultaneous effects of meloxicam and rifampin nanoformulations with solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC) substrates on inhibiting the quorum-sensing system of Pseudomonas aeruginosa and preventing biofilm formation by this bacterium. Methods: Antimicrobial activity of rifampin and meloxicam encapsulated with SLNs and NLCs against P. aeruginosa PAO1 was assessed by disk diffusion, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). Results: The SLN formulation was associated with lower doses for the MIC and minimum bactericidal concentration in comparison to NLC. Moreover, our results demonstrated that both nanoformulations were able to produce 100% inhibition of the biofilm formation of P. aeruginosa PAO1. Conclusion: All these findings suggest that meloxicam and rifampin encapsulated with SLNs could be the most effective formulation against P. aeruginosa. [ABSTRACT FROM AUTHOR]

Copyright of Farmacia is the property of Societatea de Stiinte Farmaceutice Romania and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

This work examines the negative impact of non-state actors in Nigeria. As a sovereign nation Nigeria ought to be under the firm control a legally constituted government, but this is apparently not the case as the government appears helpless in the face of daunting challenges orchestrated by the overbearing influence of both civil and uncivil non-state actors (NSAs). This unfortunate situation poses a grave security challenge on the country’s corporate existence. This work employing the expository, critical and historical methods examines the negative effects of the overbearing influence of NSAs on Nigeria’s security. The work critically appraises the negative effects of NSAs on the Nigerian socio-political and economic life as well as on the overall security of the country. In conclusion the work calls for strict governmental control of NSAs and the provision of good governance where equity, justice and the promotion of common good is basic. [ABSTRACT FROM AUTHOR]

Camila Folle,1 Ana M Marqués,2 Natalia Díaz-Garrido,3– 5 Paulina Carvajal-Vidal,1 Elena Sánchez López,1,6 Joaquim Suñer-Carbó,1,6 Lyda Halbaut,1,6 Mireia Mallandrich,1,6 Marta Espina,1,6 Josefa Badia,3– 5 Laura Baldoma,3– 5 Maria Luisa García,1,6 Ana Cristina Calpena1,6 1Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain; 2Department of Biology, Healthcare and Environment, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain; 3Department of Biochemistry and Physiology, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, Spain; 4Institute of Biomedicine of the University of Barcelona (IBUB), Barcelona, Spain; 5Research Institute Sant Joan De Déu (IR‑SJD), Barcelona, Spain; 6Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, Barcelona, SpainCorrespondence: Camila Folle; Elena Sánchez López, Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Barcelona, 08028, Spain, Email camilafolle@ub.edu; esanchezlopez@ub.eduPurpose: Acne vulgaris is one of the most prevalent dermal disorders affecting skin health and appearance. To date, there is no effective cure for this pathology, and the majority of marketed formulations eliminate both healthy and pathological microbiota. Therefore, hereby we propose the encapsulation of an antimicrobial natural compound (thymol) loaded into lipid nanostructured systems to be topically used against acne.Methods: To address this issue, nanostructured lipid carriers (NLC) capable of encapsulating thymol, a natural compound used for the treatment of acne vulgaris, were developed either using ultrasonication probe or high-pressure homogenization and optimized using 22-star factorial design by analyzing the effect of NLC composition on their physicochemical parameters. These NLC were optimized using a design of experiments approach and were characterized using different physicochemical techniques. Moreover, short-term stability and cell viability using HaCat cells were assessed. Antimicrobial efficacy of the developed NLC was assessed in vitro and ex vivo.Results: NLC encapsulating thymol were developed and optimized and demonstrated a prolonged thymol release. The formulation was dispersed in gels and a screening of several gels was carried out by studying their rheological properties and their skin retention abilities. From them, carbomer demonstrated the capacity to be highly retained in skin tissues, specifically in the epidermis and dermis layers. Moreover, antimicrobial assays against healthy and pathological skin pathogens demonstrated the therapeutic efficacy of thymol-loaded NLC gelling systems since NLC are more efficient in slowly reducing C. acnes viability, but they possess lower antimicrobial activity against S. epidermidis, compared to free thymol.Conclusion: Thymol was successfully loaded into NLC and dispersed in gelling systems, demonstrating that it is a suitable candidate for topical administration against acne vulgaris by eradicating pathogenic bacteria while preserving the healthy skin microbiome. Keywords: lipid nanoparticles, thymol, acne vulgaris, NLC, gels, antimicrobial

Nocturnal Leg Cramps (NLC) are involuntary lower limb contractions that are painful and occur during long rest periods. Magnesium is thought to have potential in the treatment of NLC as one of the precipitating factors of NLC is low levels of certain minerals, such as magnesium deficiency. This study aimed to assess the effectiveness of magnesium adjunctive therapy in reducing cramping pain intensity in patients with NLC. This study was a randomized clinical trial, open-label, controlled group that was followed up for 2 weeks. 30 subjects who have been diagnosed with the NLC short-form adaptation of ICSD 2005 were divided into 2 groups; (1) the intervention group who was given standard NLC therapy (calcium and gabapentin) with additional therapy of magnesium citrate 100 mg (Hi-Mg100) one tablet a day, (2) the control group who was only given standard NLC therapy. NLC cramping pain was measured using the Numeric Rating Scale (NRS) before the administration of therapy (baseline) and at week 2 after therapy. The results obtained were the addition of magnesium to standard therapy provided a significant reduction in cramping pain intensity between before and after treatment based on the Wilcoxon signed rank test (p=0.000). However, there was no statistically significant difference effect between the two therapy groups based on the Mann-Whitney test (p=0.073). In conclusion, magnesium adjunctive therapy was not significantly more effective in reducing cramping pain than standard drug therapy in patients with NLC. [ABSTRACT FROM AUTHOR]

In this study, bile acid-based vesicles and nanoparticles (i.e., bilosomes and biloparticles) are studied to improve the water solubility of lipophilic drugs. Ursodeoxycholic acid, sodium cholate, sodium taurocholate and budesonide were used as bile acids and model drugs, respectively. Bilosomes and biloparticles were prepared following standard protocols with minor changes, after a preformulation study. The obtained systems showed good encapsulation efficiency and dimensional stability. Particularly, for biloparticles, the increase in encapsulation efficiency followed the order ursodeoxycholic acid < sodium cholate < sodium taurocholate. The in vitro release of budesonide from both bilosytems was performed by means of dialysis using either a nylon membrane or a portion of Wistar rat small intestine and two receiving solutions (i.e., simulated gastric and intestinal fluids). Both in gastric and intestinal fluid, budesonide was released from bilosystems more slowly than the reference solution, while biloparticles showed a significant improvement in the passage of budesonide into aqueous solution. Immunofluorescence experiments indicated that ursodeoxycholic acid bilosomes containing budesonide are effective in reducing the inflammatory response induced by glucose oxidase stimuli and counteract ox-inflammatory damage within intestinal cells. [ABSTRACT FROM AUTHOR]

Nocturnal Leg Cramps (NLC) are involuntary lower limb contractions that are painful and occur during long rest periods. Magnesium is thought to have potential in the treatment of NLC as one of the precipitating factors of NLC is low levels of certain minerals, such as magnesium deficiency. This study aimed to assess the effectiveness of magnesium adjunctive therapy in reducing cramping pain intensity in patients with NLC. This study was a randomized clinical trial, open-label, controlled group that was followed up for 2 weeks. 30 subjects who have been diagnosed with the NLC short-form adaptation of ICSD 2005 were divided into 2 groups; (1) the intervention group who was given standard NLC therapy (calcium and gabapentin) with additional therapy of magnesium citrate 100 mg (Hi-Mg100) one tablet a day, (2) the control group who was only given standard NLC therapy. NLC cramping pain was measured using the Numeric Rating Scale (NRS) before the administration of therapy (baseline) and at week 2 after therapy. The results obtained were the addition of magnesium to standard therapy provided a significant reduction in cramping pain intensity between before and after treatment based on the Wilcoxon signed rank test (p=0.000). However, there was no statistically significant difference effect between the two therapy groups based on the Mann-Whitney test (p=0.073). In conclusion, magnesium adjunctive therapy was not significantly more effective in reducing cramping pain than standard drug therapy in patients with NLC.

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.

Nano-range bioactive colloidal carrier systems are envisaged to overcome the challenges associated with treatments of numerous diseases. Lipid nanoparticles (LNPs), one of the extensively investigated drug delivery systems, not only improve pharmacokinetic parameters, transportation, and chemical stability of encapsulated compounds but also provide efficient targeting and reduce the risk of toxicity. Over the last decades, nature-derived polyphenols, vitamins, antioxidants, dietary supplements, and herbs have received more attention due to their remarkable biological and pharmacological health and medical benefits. However, their poor aqueous solubility, compromised stability, insufficient absorption, and accelerated elimination impede research in the nutraceutical sector. Owing to the possibilities offered by various LNPs, their ability to accommodate both hydrophilic and hydrophobic molecules and the availability of various preparation methods suitable for sensitive molecules, loading natural fragile molecules into LNPs offers a promising solution. The primary objective of this work is to explore the synergy between nature and nanotechnology, encompassing a wide range of research aimed at encapsulating natural therapeutic molecules within LNPs. [ABSTRACT FROM AUTHOR]

Addressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. However, LC's high hydrophilicity poses challenges to its diffusion through bilayers, resulting in limited bioavailability, a short half-life, and a lack of storage within the body, mandating frequent dosing. In our research, we developed LC-loaded nanoparticle lipid carriers (LC-NLCs) using economically viable and tissue-localized nanostructured lipid carriers (NLCs) to address these limitations. Employing the central composite design model, we optimized the formulation, employing the high-pressure homogenization (HPH) method and incorporating Poloxamer® 407 (surfactant), Compritol® 888 ATO (solid lipid), and oleic acid (liquid oil). A comprehensive assessment of nanoparticle physical attributes was performed, and an open-field test (OFT) was conducted on rats. We employed immunofluorescence assays targeting CRP and PPAR-γ, along with an in vivo rat study utilizing an isolated fat cell line to assess adipogenesis. The optimal formulation, with an average size of 76.4 ± 3.4 nm, was selected due to its significant efficacy in activating the PPAR-γ pathway. Our findings from the OFT revealed noteworthy impacts of LC-NLC formulations (0.1 mg/mL and 0.2 mg/mL) on adipocyte cells, surpassing regular L-carnitine formulations' effects (0.1 mg/mL and 0.2 mg/mL) by 169.26% and 156.63%, respectively (p < 0.05). [ABSTRACT FROM AUTHOR]

[Display omitted] The most dangerous type of high-grade astrocytoma is glioblastoma multiforme. The objective of the work was to engineer lactoferrin conjugated temozolomide and resveratrol co-loaded NLC for the treatment of glioblastoma using intranasal delivery for brain targeting. Synergistic activity of temozolomide and resveratrol was determined using combination index method and 1:1 ratio was selected. QbD approach was used to formulate and optimize NLC, with minimum particle size, maximum transmittance and entrapment efficiency using Central Composite Rotable Design (CCRD) method. The optimized LTR-NLC had desired average particle size (209.3 nm), narrow PDI along, high percentage transmittance (>95%) and better entrapment efficiency (95.26% of TEM and 87.59% of RES). From ex-vivo permeation studies it was found that the permeation at 24 h was 77.43 %, and 88.55 % from LTR-NLC and 25.76 % and 31.10% from suspension for resveratrol and temozolomide respectively. In comparison to drug suspension, NLC had nearly 3-fold increase in drug penetration. IC50 value was also significantly better in the groups treated with LTR-NLC. Hence it can be concluded that LTR-NLC may be an effective formulation for the treatment of glioblastoma, according to the findings of this investigation. [ABSTRACT FROM AUTHOR]

Lung cancer is a formidable challenge in clinical practice owing to its metastatic nature and resistance to conventional treatments. The codelivery of anticancer agents offers a potential solution to overcome resistance and minimize systemic toxicity. The encapsulation of these agents within nanostructured lipid carriers (NLCs) provides a promising strategy to enhance lymphatic delivery and reduce the risk of relapse. This study aimed to develop an NLC formulation loaded with Gefitinib and Azacitidine (GEF-AZT-NLC) for the treatment of metastatic-resistant lung cancer. The physicochemical properties of the formulations were characterized, and in vitro drug release was evaluated using the dialysis bag method. The cytotoxic activity of the GEF-AZT-NLC formulations was assessed on a lung cancer cell line, and hemocompatibility was evaluated using suspended red blood cells. The prepared formulations exhibited nanoscale size (235–272 nm) and negative zeta potential values (−15 to −31 mV). In vitro study revealed that the GEF-AZT-NLC formulation retained more than 20% and 60% of GEF and AZT, respectively, at the end of the experiment. Hemocompatibility study demonstrated the safety of the formulation for therapeutic use, while cytotoxicity studies suggested that the encapsulation of both anticancer agents within NLCs could be advantageous in treating resistant cancer cells. In conclusion, the GEF-AZT-NLC formulation developed in this study holds promise as a potential therapeutic tool for treating metastatic-resistant lung cancer. [ABSTRACT FROM AUTHOR]

Solid–lipid nanoparticles and nanostructured lipid carriers are delivery systems for the delivery of drugs and other bioactives used in diagnosis, therapy, and treatment procedures. These nanocarriers may enhance the solubility and permeability of drugs, increase their bioavailability, and extend the residence time in the body, combining low toxicity with a targeted delivery. Nanostructured lipid carriers are the second generation of lipid nanoparticles differing from solid lipid nanoparticles in their composition matrix. The use of a liquid lipid together with a solid lipid in nanostructured lipid carrier allows it to load a higher amount of drug, enhance drug release properties, and increase its stability. Therefore, a direct comparison between solid lipid nanoparticles and nanostructured lipid carriers is needed. This review aims to describe solid lipid nanoparticles and nanostructured lipid carriers as drug delivery systems, comparing both, while systematically elucidating their production methodologies, physicochemical characterization, and in vitro and in vivo performance. In addition, the toxicity concerns of these systems are focused on. [ABSTRACT FROM AUTHOR]

In this paper, a novel integrated SHE-NLC control is proposed for the mitigation of unwanted lower-order harmonics in the cascaded H-bridge multilevel inverter. The proposed algorithm has been developed by hybridizing the NLC and SHE methods, in an attempt to keep the merits of both the individual control. The switching angles and nearest levels are calculated by applying the Genetic Algorithm (GA). The proposed technique reduces the calculation time and implementation complexity, thus can be a viable alternative to the real time implementation for SHE. Integrated NLC-SHE control is tested by varying the modulation index and load dynamics. This technique resulted in the reduction in Total Harmonic Distortion (THDs) in load voltage and current. Comparative analysis of NLC, SHE and Integrated NLC-SHE technique is also performed on the CHB nine-level inverter. There is significant reduction in voltage and current THD values and power losses. Efficiency of the inverter is increased. The efficacy of the proposed control CHB nine-level is tested on MATLAB Simulink environment and further validated by experimental results.

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. [ABSTRACT FROM AUTHOR]

Neurological disorders such as Alzheimer’s disease, Parkinson’s disease, dementia, epilepsy,depression, migraine etc. are affecting more and more elderly people’s day by day. Conventionalroute of administration to treat these diseases has to face a major hindrance that is bloodbrain and blood-cerebrospinal fluid (CSF) barrier to achieve desired concentration of drug atthe site of action for therapeutic effect. Hence, intranasal route of delivery is considered aspromising and alternative route to achieve desired goals. In last four decades, brain targetingstrategies are widely studied and considered having great potential by researchers; especiallyintranasal delivery owing to its benefits. Various nano formulations such as nanoemulsions,nanosuspensions, hydrogels, in situ gels, dendrimers and lipidic formulations are studiedwidely. Lipid nano formulations especially second generation nanostructured lipid carriersoffer greater advantages in terms of stability, fabrication techniques, scalability, drug loadingand drug targeting. Nanostructured lipid carrier (NLCs) constitute of two major componentsviz solid lipid and liquid lipid in a specific ratio. In this review, authors have discussed aboutthe possible synergistic actions of oils/liquid lipids with synthetic drugs resulting into greattherapeutic benefits.

Corticosteroids, although highly effective for the treatment of both anterior and posterior ocular segment inflammation, still nowadays struggle for effective drug delivery due to their poor solubilization capabilities in water. This research work aims to develop nanostructured lipid carriers (NLC) intended for periocular administration of dexamethasone acetate to the posterior segment of the eye. Pre-formulation studies were initially performed to find solid and liquid lipid mixtures for dexamethasone acetate solubilization. Pseudoternary diagrams at 65 °C were constructed to select the best surfactant based on the macroscopic transparency and microscopic isotropy of the systems. The resulting NLC, obtained following an organic solvent-free methodology, was composed of triacetin, Imwitor® 491 (glycerol monostearate >90%) and tyloxapol with Z-average = 106.9 ± 1.2 nm, PDI = 0.104 ± 0.019 and zeta potential = −6.51 ± 0.575 mV. Ex vivo porcine sclera and choroid permeation studies revealed a considerable metabolism in the sclera of dexamethasone acetate into free dexamethasone, which demonstrated higher permeation capabilities across both tissues. In addition, the NLC behavior once applied onto the sclera was further studied by means of multiphoton microscopy by loading the NLC with the fluorescent probe Nile red. [ABSTRACT FROM AUTHOR]

Marine sources contain several bioactive compounds with high therapeutic potential, such as remarkable antioxidant activity that can reduce oxidative stress related to the pathogenesis of neurodegenerative diseases. Indeed, there has been a growing interest in these natural sources, especially those resulting from the processing of marine organisms (i.e., marine bio-waste), to obtain natural antioxidants as an alternative to synthetic antioxidants in a sustainable approach to promote circularity by recovering and creating value from these bio-wastes. However, despite their expected potential to prevent, delay, or treat neurodegenerative diseases, antioxidant compounds may have difficulty reaching the brain due to the need to cross the blood–brain barrier (BBB). In this regard, alternative delivery systems administered by different routes have been proposed, including intranasal administration of lipid nanoparticles, such as solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), which have shown promising results. Intranasal administration shows several advantages, including the fact that molecules do not need to cross the BBB to reach the central nervous system (CNS), as they can be transported directly from the nasal cavity to the brain (i.e., nose-to-brain transport). The benefits of using SLN and NLC for intranasal delivery of natural bioactive compounds for the treatment of neurodegenerative diseases have shown relevant outcomes through in vitro and in vivo studies. Noteworthy, for bioactive compounds obtained from marine bio-waste, few studies have been reported, showing the open potential of this research area. This review updates the state of the art of using SLN and NLC to transport bioactive compounds from different sources, in particular, those obtained from marine bio-waste, and their potential application in the treatment of neurodegenerative diseases. [ABSTRACT FROM AUTHOR]

Nanotechnology takes the lead in providing new therapeutic options for cancer patients. In the last decades, lipid-based nanoparticles—solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), liposomes, and lipid–polymer hybrid nanoparticles—have received particular interest in anticancer drug delivery to solid tumors. To improve selectivity for target cells and, thus, therapeutic efficacy, lipid nanoparticles have been functionalized with antibodies that bind to receptors overexpressed in angiogenic endothelial cells or cancer cells. Most papers dealing with the preclinical results of antibody-conjugated nanoparticles claim low systemic toxicity and effective tumor inhibition, which have not been successfully translated into clinical use yet. This review aims to summarize the current "state-of-the-art" in anticancer drug delivery using antibody-functionalized lipid-based nanoparticles. It includes an update on promising candidates that entered clinical trials and some explanations for low translation success. [ABSTRACT FROM AUTHOR]

Gefitinib (GEF) is utilized in clinical settings for the treatment of metastatic lung cancer. However, premature drug release from nanoparticles in vivo increases the exposure of systemic organs to GEF. Herein, nanostructured lipid carriers (NLC) were utilized not only to avoid premature drug release but also due to their inherent lymphatic tropism. Therefore, the present study aimed to develop a GEF-NLC as a lymphatic drug delivery system with low drug release. Design of experiments was utilized to develop a stable GEF-NLC as a lymphatic drug delivery system for the treatment of metastatic lung cancer. The in vitro drug release of GEF from the prepared GEF-NLC formulations was studied to select the optimum formulation. MTT assay was utilized to study the cytotoxic activity of GEF-NLC compared to free GEF. The optimized GEF-NLC formulation showed favorable physicochemical properties: <300 nm PS, <0.2 PDI, <−20 ZP values with >90% entrapment efficiency. Interestingly, the prepared formulation was able to retain GEF with only ≈57% drug release within 24 h. Furthermore, GEF-NLC reduced the sudden exposure of cultured cells to GEF and produced the required cytotoxic effect after 48 and 72 h incubation time. Consequently, optimized formulation offers a promising approach to improve GEF's therapeutic outcomes with reduced systemic toxicity in treating metastatic lung cancer. [ABSTRACT FROM AUTHOR]

This study aimed to evaluate the effect of alginate-based edible coating incorporated with free thyme essential oil (EO) (thyme), unloaded NLC (NLC), 3000 mg/L thyme EO-loaded NLC (NLC 3000-thyme), 6000 mg/L thyme EO-loaded NLC (NLC 6000-thyme), and 6000 mg/L thyme EO-loaded emulsion (NLC 6000-emulsion) on the postharvest quality of tangerine fruit at 4 °C during 35 days of storage. Among the treatments, the NLC 3000-thyme, NLC 6000-thyme, and emulsion 6000-thyme showed the highest phenol content, DPPH radical scavenging activity, titrable acidity, and the lowest weight loss and TSS. However, the lowest mold injury (7.27% against 33.33% for control on day 35), the decay percentage, and the best sensorial quality retention were detected in the NLC 6000-thyme sample. Overall, our results indicated that the alginate-based edible coating incorporated with 6000 mg/L thyme EO-loaded NLC is an efficient way of extending the shelf life of tangerine fruit without no undesirable effects on its sensorial properties. [ABSTRACT FROM AUTHOR]

The major risk factor associated with the development of gastric cancer is chronic infection with Helicobacter pylori. The available treatments, based on a cocktail of antibiotics, fail in up to 40% of patients and disrupt their gut microbiota. The potential of blank nanostructured lipid carriers (NLC) for H. pylori eradication was previously demonstrated by us. However, the effect of NLC charge, size and protein corona on H. pylori-specific bactericidal activity herein studied was unknown at that time. All developed NLC formulations proved bactericidal against H. pylori. Although cationic NLC had 10-fold higher bactericidal activity than anionic NLC, they lacked specificity, since Lactobacillus acidophilus was also affected. Anionic NLC achieved complete clearance in both H. pylori morphologies (rod- and coccoid-shape) by inducing alterations in bacteria membranes and the cytoplasm, as visualized by transmission electron microscopy (TEM). The presence of an NLC protein corona, composed of 93% albumin, was confirmed by mass spectrometry. This protein corona delayed the bactericidal activity of anionic NLC against H. pylori and hindered NLC activity against Escherichia coli. Overall, these results sustain the use of NLC as a promising antibiotic-free strategy targeting H. pylori. [ABSTRACT FROM AUTHOR]

Dermatological conditions, such as acne, photoaging, psoriasis, and wounds, have been treated topically with all-trans retinoic acid (ATRA) for many years owing to its anti-inflammatory activity, comedolytic effect, and ability to increase collagen production. However, common side effects of ATRA known as the retinoid reaction can occur. These side effects are countered by ATRA encapsulation in solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLCs), and liposomes. Liposomes used to encapsulate ATRA include niosomes, ethosomes, and transfersomes. Side effects involving inflammatory reactions, such as irritation, redness, and erythema, were diminished using these approaches. The use of such carriers enhanced the efficacy of ATRA by enhancing its permeation into skin. These formulations have been compared in terms of improving the activity of ATRA and the ability to relieve the side effects. Further research into different delivery systems for ATRA using various formulations will improve the future of topical ATRA delivery. [ABSTRACT FROM AUTHOR]

Background: One of the vital variables affecting the stability and the characteristics of the Nanostructured Lipid Carrier (NLC) is the surfactant concentration. Using the two combinations of surfactants can cause higher stability and a better characteristic of NLC. Tween 80 and Span 20 are anionic surfactants whose combination has not been studied for use in NLC systems. Objective: Determine the effect of different surfactant ratios of Tween 80 and Span 20 on the physicochemical characteristics, stability, and irritability of NLC using the High Shear Homogenization (HSH) method. Methods: Four different surfactant ratios were used in the NLC formulation, in which the ratio of Tween 80:Span 20 were 5:5, 6:6, 7:7, and 8:8, respectively. In this NLC system, cetyl palmitate served as solid lipid, medium-chain triglyceride (CrodamolTM) as liquid lipid, Tween 80, and Span 20 as surfactant components. NLC was characterized for organoleptic, viscosity, pH, zeta potential, particle morphology, particle size, and polydispersity index (PDI), then evaluated for stability using the real-time and freeze-thaw method, and irritability effect. Results: The different ratios of Tween 80 and Span 20 had no significant effect on the particle size, PI, and irritation score of the NLC system. On the other hand, it influenced all formulas' pH value, viscosity, zeta potential, and stability. Conclusions: The different ratios of surfactant combination affect the characteristics and stability of the NLC system.

In this study, bile acid-based vesicles and nanoparticles (i.e., bilosomes and biloparticles) are studied to improve the water solubility of lipophilic drugs. Ursodeoxycholic acid, sodium cholate, sodium taurocholate and budesonide were used as bile acids and model drugs, respectively. Bilosomes and biloparticles were prepared following standard protocols with minor changes, after a preformulation study. The obtained systems showed good encapsulation efficiency and dimensional stability. Particularly, for biloparticles, the increase in encapsulation efficiency followed the order ursodeoxycholic acid < sodium cholate < sodium taurocholate. The in vitro release of budesonide from both bilosytems was performed by means of dialysis using either a nylon membrane or a portion of Wistar rat small intestine and two receiving solutions (i.e., simulated gastric and intestinal fluids). Both in gastric and intestinal fluid, budesonide was released from bilosystems more slowly than the reference solution, while biloparticles showed a significant improvement in the passage of budesonide into aqueous solution. Immunofluorescence experiments indicated that ursodeoxycholic acid bilosomes containing budesonide are effective in reducing the inflammatory response induced by glucose oxidase stimuli and counteract ox-inflammatory damage within intestinal cells.

Nano-range bioactive colloidal carrier systems are envisaged to overcome the challenges associated with treatments of numerous diseases. Lipid nanoparticles (LNPs), one of the extensively investigated drug delivery systems, not only improve pharmacokinetic parameters, transportation, and chemical stability of encapsulated compounds but also provide efficient targeting and reduce the risk of toxicity. Over the last decades, nature-derived polyphenols, vitamins, antioxidants, dietary supplements, and herbs have received more attention due to their remarkable biological and pharmacological health and medical benefits. However, their poor aqueous solubility, compromised stability, insufficient absorption, and accelerated elimination impede research in the nutraceutical sector. Owing to the possibilities offered by various LNPs, their ability to accommodate both hydrophilic and hydrophobic molecules and the availability of various preparation methods suitable for sensitive molecules, loading natural fragile molecules into LNPs offers a promising solution. The primary objective of this work is to explore the synergy between nature and nanotechnology, encompassing a wide range of research aimed at encapsulating natural therapeutic molecules within LNPs.

Addressing obesity is a critical health concern of the century, necessitating urgent attention. L-carnitine (LC), an essential water-soluble compound, plays a pivotal role in lipid breakdown via β-oxidation and facilitates the transport of long-chain fatty acids across mitochondrial membranes. However, LC’s high hydrophilicity poses challenges to its diffusion through bilayers, resulting in limited bioavailability, a short half-life, and a lack of storage within the body, mandating frequent dosing. In our research, we developed LC-loaded nanoparticle lipid carriers (LC-NLCs) using economically viable and tissue-localized nanostructured lipid carriers (NLCs) to address these limitations. Employing the central composite design model, we optimized the formulation, employing the high-pressure homogenization (HPH) method and incorporating Poloxamer® 407 (surfactant), Compritol® 888 ATO (solid lipid), and oleic acid (liquid oil). A comprehensive assessment of nanoparticle physical attributes was performed, and an open-field test (OFT) was conducted on rats. We employed immunofluorescence assays targeting CRP and PPAR-γ, along with an in vivo rat study utilizing an isolated fat cell line to assess adipogenesis. The optimal formulation, with an average size of 76.4 ± 3.4 nm, was selected due to its significant efficacy in activating the PPAR-γ pathway. Our findings from the OFT revealed noteworthy impacts of LC-NLC formulations (0.1 mg/mL and 0.2 mg/mL) on adipocyte cells, surpassing regular L-carnitine formulations’ effects (0.1 mg/mL and 0.2 mg/mL) by 169.26% and 156.63%, respectively (p < 0.05).

Objective(s): In this work, we loaded Auraptene (AUR) into nanostructured lipid carriers (NLCs) and performed an assessment on inhibitory activities of the obtained AUR-NLCs on melanogenesis. Materials and Methods: AUR-NLCs were prepared through a high shear homogenization and ultrasound method. Results: Entrapment efficiency and Particle size of the optimized formulation were 103.1±4.9 nm and 89.56±3.75. The TEM outcomes exhibited the spherical shape of our nanoparticles, while the DSC analysis revealed the lack of any drug-lipid incompatibility throughout the formulations. A prolonged drug-release was observed from AUR-NLCs when compared to the AUR-solution. According to results, this product can significantly attenuated the activity of cellular tyrosinase and ROS content with minimal cytotoxic effects in B16F10 cell line, which in contrast to AUR-solution. Moreover, the western blotting analysis was indicative of AUR-NLCs ability to inhibit melanogenesis through the suppression of MITF and act much more efficiently than AUR-solution.Conclusion: AUR-NLCs can offer merits as a natural anti-tyrosinase agent for the treatment of hyperpigmentory disorders.

Nanostructured lipid carriers (NLC) were prepared from solid lipid (glyceryl monostearate, GMS) and vegetable oils, including palm oil (PO), rice bran oil (RBO) or virgin coconut oil (VCO), at different ratios (95:5, 90:10 and 80:20), while nanoemulsions (NE) were prepared with sole vegetable oils. After production, the particle size of the lutein-free NLC and NE was found to be between 100 and 150 nm and increased after loading with lutein. An increase in oil loading in NLC reduced the particle size and resulted in a less ordered lipid matrix and an increase in % entrapment efficiency. From the stability study, it was observed that the types of oils and oil content in the lipid matrix had an impact on the chemical stability of lutein. Regarding the release study, lutein-loaded NE showed higher release than lutein-loaded NLC. Both NLC and NE prepared from VCO exhibited higher release than those prepared from PO and RBO, respectively (p < 0.05). In contrast, among the formulations of NLC and NE, both lutein-loaded NLC and NE prepared from RBO showed the highest permeation through the human epidermis due to the skin enhancement effect of RBO. Based on all the results, the lipid nanocarriers composed of RBO could effectively enhance the chemical stability of lutein and promote drug penetration into the skin. [ABSTRACT FROM AUTHOR]

Drug administration via the skin is one of the most conventionally used methods where the flux through the skin is the rate-limiting step. Safe carriers are used to provide the anticipated therapeutic effects, which play a vital role in drug delivery. A nanostructured lipid carrier (NLC) is a binary mixture of solid and liquid lipids and surfactants. The lipid nature and nano size of these carriers contribute to the skin penetration of therapeutic agents. These carriers have a wide variety of advantages, such as good biocompatibility, low cytotoxicity, high drug quality and increased stability. This paper deliberates the suitability of NLCs in transdermal drug delivery, their properties, the methods of preparation and their applications. [ABSTRACT FROM AUTHOR]

Neurological disorders such as Alzheimer's disease, Parkinson's disease, dementia, epilepsy, depression, migraine etc. are affecting more and more elderly people's day by day. Conventional route of administration to treat these diseases has to face a major hindrance that is blood brain and blood-cerebrospinal fluid (CSF) barrier to achieve desired concentration of drug at the site of action for therapeutic effect. Hence, intranasal route of delivery is considered as promising and alternative route to achieve desired goals. In last four decades, brain targeting strategies are widely studied and considered having great potential by researchers; especially intranasal delivery owing to its benefits. Various nano formulations such as nanoemulsions, nanosuspensions, hydrogels, in situ gels, dendrimers and lipidic formulations are studied widely. Lipid nano formulations especially second generation nanostructured lipid carriers offer greater advantages in terms of stability, fabrication techniques, scalability, drug loading and drug targeting. Nanostructured lipid carrier (NLCs) constitute of two major components viz solid lipid and liquid lipid in a specific ratio. In this review, authors have discussed about the possible synergistic actions of oils/liquid lipids with synthetic drugs resulting into great therapeutic benefits. [ABSTRACT FROM AUTHOR]

Purpose: Psoriasis is a chronic inflammatory skin disorder that poses significant challenges regarding effective and targeted drug delivery. Bioactive substances like betulin have shown tremendous utility in treating these conditions; however, they pose limited utility owing to their physicochemical characteristics. Here, we aimed to develop a novel topical dosage form for treating psoriasis, utilising betulin-loaded solid lipid nanoparticles (NLCs) incorporated into a hydrogel matrix., Methods: The optimization of the formulation was meticulously conducted using a design of experiments methodology, and its diverse physicochemical attributes were thoroughly examined. Evaluating betulin's in vitro release pattern from the NLC-hydrogel demonstrated consistent and regulated drug release properties. Additionally, the formulation demonstrated improved skin penetration abilities as determined by in vitro skin permeation experiments employing Franz diffusion cells- furthermore, the therapeutic effectiveness of the betulin-NLC-hydrogel was assessed by an in vivo experiment carried out using an imiquimod-induced psoriasis-like skin inflammation model in BALB/c female mice., Results: The NLCs exhibited a pH of 5.67±0.86, particle size of 148.16±12.66 nm, and zeta potential of -22.84±2.37 mV, ensuring stability and suitability for topical use. The gel, with a pH of 6.05±0.43 and viscosity of 17550±120 cPs, showed enhanced skin hydration and lipid restoration. Drug release studies indicated a slower release from NLCs and gel, improving skin retention. Stability tests revealed that the formulations were stable at room temperature but not at elevated temperatures. The in vitro safety profile of the formulation revealed no significant adverse effects on HaCaT cell lines. The NLC gel demonstrated significant anti-psoriatic activity, reducing inflammation and cytokine levels., Conclusion: The betulin-NLC-hydrogel formulation exhibited promising characteristics for the topical treatment of psoriasis, showcasing optimised drug delivery, sustained release, and notable therapeutic efficacy. The findings from this study provide a foundation for the potential clinical translation of this innovative topical dosage form for improved psoriasis management., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Abstract Background Magnesium supplements are widely used for prophylaxis and treatment of nocturnal leg cramps (NLC). However, there is little evidence in support of their effectiveness. The main impediment stems from the lack of assessments of cellular absorption. In the current study, we tested the efficacy and safety of a magnesium supplement – magnesium oxide monohydrate (MOMH), for which increased cellular absorption rates were demonstrated in an ex-vivo setting. Methods A randomized, double-blind, placebo-controlled multicenter study was conducted in hospitals and outpatient clinics in Ukraine, from February to August 2018. Eligible subjects received a capsule with MOMH 226 mg or placebo, once daily, at bedtime, for a 60-day period. The assessed parameters included frequency and duration of NLC episodes, quality of sleep, NLC-induced pain and quality of life sub-scores. The Fisher’s Exact Test for comparison of groups by categorical variables was used. The Student’s test or Mann-Whitney test were used for between-group comparison at different timepoints. ANCOVA followed by contrast analysis was used for comparison of groups at the end of the study. Results 175 (81%) out of 216 initially screened subjects completed the study. The number of NLC episodes has significantly decreased by the end of the study period as compared to baseline in both groups (p

Lung cancer is a formidable challenge in clinical practice owing to its metastatic nature and resistance to conventional treatments. The codelivery of anticancer agents offers a potential solution to overcome resistance and minimize systemic toxicity. The encapsulation of these agents within nanostructured lipid carriers (NLCs) provides a promising strategy to enhance lymphatic delivery and reduce the risk of relapse. This study aimed to develop an NLC formulation loaded with Gefitinib and Azacitidine (GEF-AZT-NLC) for the treatment of metastatic-resistant lung cancer. The physicochemical properties of the formulations were characterized, and in vitro drug release was evaluated using the dialysis bag method. The cytotoxic activity of the GEF-AZT-NLC formulations was assessed on a lung cancer cell line, and hemocompatibility was evaluated using suspended red blood cells. The prepared formulations exhibited nanoscale size (235–272 nm) and negative zeta potential values (−15 to −31 mV). In vitro study revealed that the GEF-AZT-NLC formulation retained more than 20% and 60% of GEF and AZT, respectively, at the end of the experiment. Hemocompatibility study demonstrated the safety of the formulation for therapeutic use, while cytotoxicity studies suggested that the encapsulation of both anticancer agents within NLCs could be advantageous in treating resistant cancer cells. In conclusion, the GEF-AZT-NLC formulation developed in this study holds promise as a potential therapeutic tool for treating metastatic-resistant lung cancer.

The present study aimed to engineer a nanoscale lipid-based lymphatic drug delivery system with D-α-Tocopherol polyethylene glycol 1000 succinate to combat the lymphatic metastasis of lung cancer. The nanoscale lipid-based systems including GEF-SLN, GEF-NLC, and GEF-LE were prepared and pharmaceutically characterized. In addition, the most stable formulation (GEF-NLC) was subjected to an in vitro release study. Afterward, the optimized GEF-NLC was engineered with TPGS (GEF-TPGS-NLC) and subjected to in vitro cytotoxicity, and apoptotic studies using the A549 cells line as a surrogate model for lung cancer. The present results revealed that particle size and polydispersity index of freshly prepared formulations were ranging from 198 to 280 nm and 0.106 to 0.240, respectively, with negative zeta potential ranging from − 14 to − 27.6.mV. An in vitro release study showed that sustained drug release was attained from GEF-NLC containing a high concentration of lipid. In addition, GEF-NLC and GEF-TPGS-NLC showed remarkable entrapment efficiency above 89% and exhibited sustained release profiles. Cytotoxicity showed that IC50 of pure GEF was 11.15 μg/ml which decreased to 7.05 μg/ml for GEF-TPGS-NLC. The apoptotic study revealed that GEF-TPGS-NLC significantly decreased the number of living cells from 67 to 58% when compared with pure GEF. The present results revealed that the nanoscale and lipid composition of the fabricated SLN, NLC, and LE could mediate the lymphatic uptake of GEF to combat the lymphatic tumor metastasis. Particularly, GEF-TPGS-NLC is a promising LDDS to increase the therapeutic outcomes of GEF during the treatment of metastatic lung cancer. [ABSTRACT FROM AUTHOR]

Aim: The current study was aimed to develop and validate a simple isocratic, precise, sensitive, accurate and robust reverse phase HPLC analytical method for the quantification of total, free and entrapped ritonavir in lipid nanocarriers and drug content of the filmcoated fixed-dose formulation. Materials and Methods: The method was developed by using Inertsil ODS-3V C18 column as stationary phase, orthophosphoric acid (OPA) in water (pH 3.0) and acetonitrile as mobile phase. Further, the method was validated following ICH Q2(R1) guidelines. Ritonavir loaded lipid nanocarriers were developed using hot-emulsion and probe-sonication method. A solid phase extraction (SPE) method was developed for the separation of free and entrapped ritonavir. Total ritonavir was extracted from lipid nanocarriers (LNCs) and film-coated tablets using methanol and analyzed with validated method. Results: The responses were found to be linear and precise over a range of 0.25 µg/mL to 16 µg/mL. The limit of detection (LOD) and limit of quantification (LOQ) of the RP-HPLC method were found to be 14.06 ng/mL and 42.60 ng/mL, respectively which emphasizes the sensitivity of the method. The recovery of ritonavir from LNCs was found to be within 3% of the total drug present in LNCs. Similar, amount of drug recovery was found from assay of marketed formulation i.e., > 97%. Conclusion: The SPE method is capable of separating free and entrapped ritonavir from LNCs. The developed HPLC method is sensitive, robust, economical and gives high recovery. The developed HPLC method can also be employed for routine quantitative analysis of ritonavir in bulk formulation. [ABSTRACT FROM AUTHOR]

High BP is one of the most predominant causes of heart diseases and cerebrovascular problems. Perinodopril is an ACE inhibitor that is a non sulfhydryl derivative that is used for the treatment of hypertension. To enhance the effect of the drug it was formulated into Lipid based nano carrier system (NLC) to improve the bioavailability and thereby the therapeutic potential. So the objective of the current work was to evaluate the NLC of perinodopril formulation and to evaluate the same. The invivo estimation of the activity was carried out on Albino wistar rats that are maintained under room conditions and the formulation was investigated for the Pharamcokinetic and pharmacodynamic paramteres in rat plasma. Also they were tested for their stability invitro. Results show that the nano particles measured as 0.207nm in size. The invitro drug release studies suggest that the formulations were releasing the drug in controlled fashion during 23 hrs. stability studies proves the drug is very stable in the formulation. With R2 = 0.9683, the in vitro-in vivo correlation research clearly shows good agreement between in vitro drug solubilization during lipolysis and in vivo drug absorption during pharmacokinetic studies. This in vitro lipolysis research, which has an R2 close to 1, suggests that this model can match the in vivo dissolution profile in the gut. [ABSTRACT FROM AUTHOR]

Hypertension is a serious cardiovascular event which refers to rise in the arterial blood pressure. Perinodopril which has been classified as calcium channel blocker is utilized in the treatment of hypertension. Perinodopril comes under BCS class II drug (low solubility/high permeability) which shows variable absorption pattern due to solubility limitation. Therefore, nanostructured lipid carrier (NLC) of Perinodopril was developed which is suitable for drug with high log P value as it offers the advantage of high drug entrapment and loading capacity to lipophilic drugs. Tween 80 and Poloxamer 188 were reportedly P-gp efflux inhibitors which would be an added feature to the property of Perinodopril -NLC thus enhancing drug availability across intestine. Therefore, the objectives of the present work were to develop an optimized Perinodopril -NLC using Quality by design (QbD) and evaluating it for enhancement in intestinal uptake and solubilisation fate (in physiologically simulating gastro intestinal milieu) of Perinodopril which would further enhance the oral bioavailability. Physicochemical characterization of the drug by means of UV spectra, DSC and FT-IR concluded that Perinodopril is pure and authentic. Both medium chain triglycerides (MCT) and long chain triglycerides (LCT) were used in the solubility studies of Perinodopril. The drug exhibited the highest solubility in Capryol 90 (35±3.51 mg/mL). Among solid lipids, solubility of drug in Emulcire 61 was found to be the highest (62.41±4.02 mg/g). The highest solubility of drug in Emulcire 61 could be attributed to its inherent selfemulsifying property. Presence of alcoholic group in Emulcire 61 and in Capryol 90 which acts as hydrogen bond donor and presence of 5 oxygen and 3 nitrogen atom in Perinodopril which acts as hydrogen bond acceptors could form a stable complex which enhances the solubility of drug in these solid and liquid lipids. [ABSTRACT FROM AUTHOR]

The management of the central nervous system (CNS) disorders is challenging, due to the need of drugs to cross the blood‒brain barrier (BBB) and reach the brain. Among the various strategies that have been studied to circumvent this challenge, the use of the intranasal route to transport drugs from the nose directly to the brain has been showing promising results. In addition, the encapsulation of the drugs in lipid-based nanocarriers, such as solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) or nanoemulsions (NEs), can improve nose-to-brain transport by increasing the bioavailability and site-specific delivery. This review provides the state-of-the-art of in vivo studies with lipid-based nanocarriers (SLNs, NLCs and NEs) for nose-to-brain delivery. Based on the literature available from the past two years, we present an insight into the different mechanisms that drugs can follow to reach the brain after intranasal administration. The results of pharmacokinetic and pharmacodynamics studies are reported and a critical analysis of the differences between the anatomy of the nasal cavity of the different animal species used in in vivo studies is carried out. Although the exact mechanism of drug transport from the nose to the brain is not fully understood and its effectiveness in humans is unclear, it appears that the intranasal route together with the use of NLCs, SLNs or NEs is advantageous for targeting drugs to the brain. These systems have been shown to be more effective for nose-to-brain delivery than other routes or formulations with non-encapsulated drugs, so they are expected to be approved by regulatory authorities in the coming years.

Solid–lipid nanoparticles and nanostructured lipid carriers are delivery systems for the delivery of drugs and other bioactives used in diagnosis, therapy, and treatment procedures. These nanocarriers may enhance the solubility and permeability of drugs, increase their bioavailability, and extend the residence time in the body, combining low toxicity with a targeted delivery. Nanostructured lipid carriers are the second generation of lipid nanoparticles differing from solid lipid nanoparticles in their composition matrix. The use of a liquid lipid together with a solid lipid in nanostructured lipid carrier allows it to load a higher amount of drug, enhance drug release properties, and increase its stability. Therefore, a direct comparison between solid lipid nanoparticles and nanostructured lipid carriers is needed. This review aims to describe solid lipid nanoparticles and nanostructured lipid carriers as drug delivery systems, comparing both, while systematically elucidating their production methodologies, physicochemical characterization, and in vitro and in vivo performance. In addition, the toxicity concerns of these systems are focused on.

The management of retinoblastoma (RB) involves the use of invasive treatment regimens. Paclitaxel (PTX), an effective antineoplastic compound used in the treatment of a wide range of malignant tumors, poses treatment challenges due to systemic toxicity, rapid elimination, and development of resistance. The goal of this work was to develop PTX-loaded, α-tocopherol succinate (αTS)-based, nanostructured lipid carrier (NLCs; αTS-PTX-NLC) and PEGylated αTS-PTX-NLC (αTS-PTX-PEG-NLC) to improve ocular bioavailability. The hot homogenization method was used to prepare the NLCs, and repeated measures ANOVA analysis was used for formulation optimization. αTS-PTX-NLC and αTS-PTX-PEG-NLC had a mean particle size, polydispersity index and zeta potential of 186.2 ± 3.9 nm, 0.17 ± 0.03, −33.2 ± 1.3 mV and 96.2 ± 3.9 nm, 0.27 ± 0.03, −39.15 ± 3.2 mV, respectively. The assay and entrapment efficiency of both formulations was >95.0%. The NLC exhibited a spherical shape, as seen from TEM images. Sterilized (autoclaved) formulations were stable for up to 60 days (last time point checked) under refrigerated conditions. PTX-NLC formulations exhibited an initial burst release and 40% drug release, overall, in 48 h. The formulations exhibited desirable physicochemical properties and could lead to an effective therapeutic option in the management of RB. [ABSTRACT FROM AUTHOR]