Flurbiprofen loaded ethosomes - transdermal delivery of anti-inflammatory effect in rat model.

BACKGROUND: Ethosomes have been widely used in Transdermal Drug Delivery System (TDDS) as they increase the permeation of drug across the skin. METHODS: Flurbiprofen loaded vesicular ethosomes were formulated, optimized and characterized for particle size, entrapment efficiency, poly dispersive index (PDI), microscopy using Atomic force microscopy (AFM), Scanning electron microscope (SEM) and Transmission electron microscopy (TEM) and Interaction of drug and excipients were studied using Fourier transform infra-red (FTIR) spectroscopy, Differential scanning colorimetry (DSC), Thermo gravimetric analysis (TGA). Further, ethosomal formulations of flurbiprofen were evaluated for stability study of three months and in vitro drug permeation study was carried out using albino rat skin. In addition, skin irritation test was evaluated by Draize test and in vivo study of prepared formulation was examined through paw edema assay by inducing carrageenan and cold plate method. RESULTS: Amongst all formulations, EF5 formulation exhibited ideal surface morphology, with maximum entrapment efficiency (95%) with optimal excipient concentration i.e. 200 mg phospholipid and 35% ethanol. The ideal vesicle size was achieved as 162.2 ± 2 nm, with zeta potential - 48.14 ± 1.4 mV with the PDI of 0.341. In-vitro permeation study shows a release of 82.56 ± 2.11 g/cm2 in 24 h and transdermal flux was found as 226.1 µg/cm2/h. Cold plate test indicates that the formulation EF5 showed a marked analgesic activity and Carrageenan induced paw edema test indicates that the formulation EF5 inhibits the increase in paw edema. Ethosomal suspension at 4 °C showed maximum stability. CONCLUSIONS: The overall study concluded that this ethosomal approach offers a new delivery system for sustained and targeted delivery for flurbiprofen.

PEG-PLGA- hybrid nanoparticles loaded with etoricoxib - phospholipid complex for effective treatment of inflammation in rat model.

The aim of the present study was to increase the bioavailability of the etoricoxib by making PEG-PLGA-Hybrid nanoparticles using emulsion solvent evaporation method. Then the prepared nanoparticles were further characterised using TEM, particle size, PDI, zeta potential, encapsulation efficiency and drug release study. Lipid (Phospholipon 90-G) and drug thermal behaviour were studied using DSC, TGA. The results of optimised formulation of Particle size, PDI and zeta potential was found 216.6 ± 4.0 nm, 0.24 ± 0.19 and +36.3 ± 1.9 mV. Encapsulation efficiency was found in the range of 77.15% w/v to 93.88% w/v. In-vivo study shows that the optimised formulation at a particular dose decreases the swelling index and number of writhes. Stability study indicated that the nanoparticles can be stored at a temperature of 4 ± 2 °C/60 ± 5% RH in well-closed container, away from heat and damp places. The prepared formulation has significantly increased the bioavailability of etoricoxib via oral administration.

Herbal ethosomal gel containing luliconazole for productive relevance in the field of biomedicine.

This study includes development, characterization, and optimization of herbal ethosomal formulation. The aim of the present study is to develop drug loaded ethosomes capped with Azadirachta indica (neem) which, was further incorporated in Carbopol 934 K thereby, resulting in the formation of ethosomal gel. The formulation is aimed to express effective treatment against fungal infection. The build was formulated using drug (Luliconazole), soyalecithin, ethanolic neem extract and propylene glycol. In total nine ethosomal, formulations of distinct concentrations of ingredients were processed, to determine out the optimized formulation among the all. Further the prepared drug loaded ethosomes were subjected to various evaluation parameters like particle size, zeta potential, polydispersity index (PDI) and % entrapment efficiency. For the evaluation of its surface morphology, transmission electron microscopy was executed whereas, atomic force microscopy was carried out which contributes in detail and depth information of surface morphology. For the analysis of thermal behavior Thermal gravimetric analysis graph was obtained for luliconazole, soyalecithin, neem extract, physical mixture and optimized formulation (LF5). Attenuated total internal reflection Fourier transforms infra-red spectroscopy was performed for luliconazole, soyalecithin, neem extract, physical mixture, and optimized formulation (LF5) to examine the interaction between the drug and the excipients. Viscosity, pH, spreadability and extrudability of the ethosomal gel were calculated to determine the suitability of the formulation for topical application. In vitro drug permeation study and antifungal activity was executed out with the aid of Wistar albino rat skin model and tube dilution assay respectively. The complete study wrap up, that this herbal ethosomal approach provides advanced sustained and targeted delivery of luliconazole. On analyzing the results, ethosomal formulation LF5 was found to be optimized one, due to its optimum concentration of soyalecithin (300 mg) and ethanol (35%). Hence it has maximum entrapment efficiency of 86.56 ± 0.74%. Optimum vesicle size, zeta potential, and PDI were found to be 155.30 ± 1.2 nm, - 42.20 ± 0.3 mV, and 0.186 ± 0.07 respectively. In vitro drug permeation study expresses release of 83.45 ± 2.51 in 24 h whereas; the in vivo activity proved that LF5 is more active and effective against Candida parapsilosis in comparison to Aspergillus niger. In the end, it was estimated that ethosomal suspension and lyophilized ethosomal suspension was utmost stable at 4 °C/60 ± 5 RH. The complete study clearly indicates that the buildup of ethosomal formulation with luliconazole and neem extract show synergistic effect thereby, expressing excellent result against the treatment of fungal infection.

Clitoria ternatea Mediated Synthesis of Graphene Quantum Dots for the Treatment of Alzheimer's Disease.

The main purpose of the present study was to synthesize graphene quantum dots (GQDs)from the flowers of Clitoria ternatea with the help of one-pot microwave-assisted green synthesis for the treatment of Alzheimer's disease. Further, the synthesized graphene quantum dots show a particle size of 10 nm ±1.3, a PDI of 0.354 ± 1.8, and a ζ potential of -46 ± 0.4, indicating the good stability of the quantum dots. With the help of scanning electron microscopy (SEM) and transfer electron microscopy (TEM) examination, the surface microscopic behavior of the synthesized quantum dots was determined. The presence of functional groups in the quantum dots was determined by Fourier-transform infrared spectroscopy (FTIR) study, the chemical state information on the sample was determined with the help of X-ray photoelectron spectroscopy (XPS), and the surface area of the dots was determined with the help of a surface area analyzer. With the help of a radial arm maze and water morris maze assay, the learning and memory capacity of the quantum dots was assessed, and the results show that the ctGQDs significantly decreased the transfer latency to reach the baited arm in 10.37 ± 1.65 s or to the hidden platform in 18.42 ± 0.99 s in 7 days. The synthesized quantum dots show more inhibition of the acetyl cholinesterase enzyme, i.e., 86.32 ± 1.52%, as compared to that of pure donepezil, i.e., 72.46 ± 2.21%. ctGQDs considerably increased the level of glutathione and protein and decreased the level of lipid peroxide and nitric oxide. The histopathological image of ctGQDs shows more preservation of small pyramidal cell and treats the disorganization of the cells. These results suggest that the quantum dots significantly crossed the blood-brain barrier since they were small in size and were effective in reducing Alzheimer-like symptoms in rodents, and thus, it can be concluded that Clitoria ternatea flowers can be used as an adjuvant in the treatment of Alzheimer's.

PEGylated Lipova E120 liposomes loaded with celecoxib: in-vitro characterization and enhanced in-vivo anti-inflammatory effects in rat models.

The goal of the current investigation was to prepare PEGylated Lipova E120 liposomes loaded with celecoxib for the effective treatment of rheumatoid arthritis (RA). PEGylated liposomes were prepared and were characterized using techniques such as particle size distribution, polydispersity index (PDI), zeta potential, encapsulation efficiency and in-vitro release, in-vivo and stability studies. The morphological study was characterized by scanning electron microscopy and transmission electron microscopy. To determine the interaction between drug and polymer Fourier transform infrared, Raman, thermogravimetric analysis and differential scanning calorimetry studies were performed. Results show that formulation F6 was optimized with a particle size of 92.12 +/- 1.7 nm, a PDI of 0.278 +/- 0.22, a zeta potential of - 40.8 +/- 1.7 mV with a maximum encapsulation of 96.6 +/- 0.05% of drug in the PEGylated liposomes. The optimized formulation shows a maximum release of drug i.e. 94.45 +/- 1.13% in 72 h. Tail immersion assay shows that the optimized formulation F6 significantly increases the reaction time and carrageenan-induced assay shows that the optimized formulation inhibits the increase in paw edema thus providing a pain relief treatment in RA. These results suggest that the PEGylated liposomes provide a sustained release of celecoxib and helps in effective treatment of RA.

Lipid-polymer hybrid nanoparticles: Synthesis strategies and biomedical applications.

This review article is an updated overview on lipid-polymer hybrid nanoparticles (LPHNs) including the various types of LPHNs polymers used in their preparation, various methods of preparation, their physiochemical, in-vitro and in-vivo evaluation parameters and their application in various delivery systems. LPHNs show a combined advantage of biodegradable polymeric nanoparticles and liposomes. LPHNs mainly consist of a biodegradable polymeric material core containing drugs or any substances which are to be encapsulated then this core is further enclosed by a phospholipid layer i.e. lipid PEG layer. LPHNs show good physical strength and biocompatibility. The hybrid structural design can offer various benefits such as controlled particle size, high drug loading, surface functionality with various ligands (antibody fragments, peptides, monoclonal antibodies, aptamers, and folate molecules), and encapsulation of combinational therapeutic agents, showing prolonged release of drug and drug circulates in the blood for longer duration. Significantly, the LPHNs have recently been confirmed as a better drug delivery route and good cellular delivery efficacy of various drugs as compared to polymeric nanoparticles and liposomes.

Green synthesis and characterization of copper nanoparticles by Tinospora cardifolia to produce nature-friendly copper nano-coated fabric and their antimicrobial evaluation.

Metallic nanoparticles such as gold, zinc, copper possess anti-microbial activity. These nanoparticles have a small size which provides a large surface area for the interaction with microbes and there are various mechanisms through which copper nanoparticles (CuNPs) act. The demand of these nanoparticles are increasing in the textile industry as they decrease the catalytic degradation property of various dyes as well as being helpful in the treatment of various topical infections. Our aim is to formulate the copper nanoparticle which is capped with Tinospora cardifolia and incorporate these nanoparticles on fabric and to study the anti-microbial activity of these nanoparticles formulated along with their study on the fabric. Formulated nanoparticles were tested for various characterizations such as SEM (Scanning Electron Microscope), TEM (Transmission Electron Microscope) for the microscopical study. The interaction of excipients with the drug was studied using FTIR, XRD, and Raman and the anti-microbial study was studied to determine the activity of the nanoparticles on gram-positive and gram-negative bacteria. Least particle size of 63.3 nm was used as optimized formulation (CuNPs-5) and further used for testing. Laundry durability, ZOI study and %efficacy of copper nanoparticles along with nanoparticle-coated fabric was tested and it was found that fabric was more efficacious for gram-positive bacteria as ZOI for gram positive and gram negative was 21.99 mm and 11 mm. The %efficacy of copper nanoparticle-coated fabric was 101% and 74% at the highest concentration for gram positive and gram negative bacteria respectively.

Flurbiprofen-loaded ethanolic liposome particles for biomedical applications.

Present study deals with the preparation, characterization and in-vivo evaluation of flurbiprofen loaded ethanolic liposome which provides predetermined and controlled release of drug through a transdermal drug delivery system. Ethanolic liposomes were prepared by using flurbiprofen, phospholipon 90-G, and ethanol in varied concentration ratio. The prepared ethanolic liposomes were optimized and characterized for particle size, zeta potential, polydispersive index and % entrapment efficiency. FTIR study was performed to analyze the interaction between drug and excipient. To study the thermal behavior of the formulation DSC and TGA were carried out. The surface morphology of ethanolic liposome was performed with the help of SEM, TEM, and AFM. In-vitro drug permeation study of the optimized formulation was carried out using the albino rat skin model and peripheral nociceptive activity was evaluated by writhing assay. In addition, formulations were also inspected for stability study for three months at a different temperature. The optimized formulation EF5 exhibited a particle size of 167.2 ±â€¯3.7 nm with a zeta potential of -51.6 ±â€¯0.2 mV and PDI of 0.209. The optimized formulation showed an ideal surface morphology with a maximum % entrapment efficiency i.e. 93.51 ±â€¯2.1. In-vitro permeation study shows a release of 70.23% in 24 h and transdermal flux was found as 238.2 µg/cm2/h. Writhing assay demonstrate that the optimized formulation decreases the number of writhes and thus shows the peripheral analgesic activity. In stability study, optimized formulation showed maximum stability at 4 °C. These results suggest that transdermal system mediated application of flurbiprofen loaded ethanolic liposome can be considered as an effective way to afford consistent and predictable release of flurbiprofen which could provide beneficial effects in the management of various inflammatory diseases.