Appraisal of Nano-lipidic Astaxanthin cum Thermoreversible Gel and its Efficacy in Haloperidol Induced Parkinsonism

2021 ◽  
Vol 18 ◽  
Author(s):  
Deepika Gautam ◽  
Samipta Singh ◽  
Priyanka Maurya ◽  
Manjari Singh ◽  
Sapana Kushwaha ◽  
...  
Keyword(s):  
Average Particle Size ◽  
Radical Scavenging ◽  
Nanostructured Lipid Carriers ◽  
Neuronal Uptake ◽  
Pharmacokinetic Studies ◽  
Average Particle ◽  
In Situ Gel ◽  
Thermoreversible Gel

Background: Parkinsonism has a toxic cascade of neurodegeneration, with akinesia as a major manifestation. Some antioxidants have shown promise against the disease. Astaxanthin is a powerful antioxidant, demonstrates free radical scavenging, and is also a potential neuroprotective agent Objective: To formulate astaxanthin laden nanostructured lipid carriers based thermoreversible gel for better neuronal uptake and better neuronal efficacy. Methods: The method for fabricating astaxanthin-nanostructured lipid carriers (ATX-NLC) was melt-emulsification, and these were optimized using factorial design and further evaluated for diverse parameters. Neurotoxicity was induced in rats by haloperidol. The treated and non-treated rats were then witnessed for their behaviour. TBARs and GSH levels were also determined. Pharmacokinetics was studied via HPLC. Results: The average particle size (by DLS), entrapment efficiency and zeta potential of optimized ATX-NLC were 225.6 ± 3.04 nm, 65.91 ± 1.22 % and -52.64 mV respectively. Astaxanthin release (after 24 h in simulated nasal fluid) from optimized ATX-NLC was 92.5 ± 5.42 %. Its thermo-reversible nasal gel (ATX-NLC in-situ gel) was prepared using poloxamer-127. The obtained gel showed in-vivo betterment in the behaviour of animals when studied using rotarod and akinesia test. Pharmacokinetic studies showed better availability of astaxanthin in the brain on the rats treated with ATX-NLC in-situ gel as compared to those treated with ATX-in-situ gel. Conclusion: Astaxanthin loaded lipidic nanoparticulate gel can be a hopeful adjuvant therapy for Parkinsonism and holds scope for future studies.

Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

2017 ◽  
Vol 6 (6) ◽  
pp. 517-526 ◽  
Author(s):  
Permender Rathee ◽  
Anjoo Kamboj ◽  
Shabir Sidhu
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Interaction ◽  
Precipitation Method ◽  
Pharmacokinetic Studies ◽  
Average Particle

AbstractBackground:Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats.Methods:Optimization studies of nanoparticles were performed using Taguchi L9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats.Results:The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats.Conclusion:The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.

scholarly journals Design of a Reversible Cholinesterase Inhibitor Mamentine HCL Nanogel: Formulation and In-vitro Evaluation

2021 ◽  
pp. 352-359
Author(s):  
Subhasri Mohapatra ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Particle Size ◽  
Cholinesterase Inhibitor ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Storage Period ◽  
Spherical Particles ◽  
Average Particle ◽  
In Situ Gel

Memantine hydrochloride is a is a reversible cholinesterase inhibitor used in the treatment of Alzheimer’s disease, low-moderate affinity, uncompetitive n-methyl-d-aspartate (NMDA) receptor antagonist, with strong voltage dependency and rapid blocking/unblocking kinetics. The present study was explore the potential of thermosensitive nanogel of mamentine loaded nanoparticle. In situ gel choosing due to restrict unwanted exposure in blood and other healthy tissues, thus eliminate hemolytic side effects of the drug and offer easy administration in vivo. Nanoparticle prepared by ionic gelation method and further the dried nanoparticle incorporates with in situ gel.  The in situ gel prepared by cold method using the solutions of Poloxamer-188 and Carbopol-934. The Transmission electron microscopy showed the spherical particles  with  smooth surface which was in conformity  with the SEM and Zetasizer  data for particle size. The pH of the formulations was found to be satisfactory and was in the range of 6.8±0.039 -7.4±0.053 and also mucoadhesive strength was show in table. The mucoadhesive strength of all formulations was varies from 2398±0.0004 to 4945±0.0002 dynes/cm2. In-vitro diffusion study of the in situ gel (N1-N8) was performed using modified Franz diffusion cell with dialysis membrane in phosphate buffer pH 6.5 for a period of 24 hours. The in vitro release study were fitted into various kinetic models viz zero order, first order, higuchi model and korsmeyer peppas equation. Stability studies for optimized formulations were carried out at 4.0 ± 0.5°C and 37 ± 0.5ºC for a period of four weeks. There was no significant variation found in physical appearance, average particle size and % drug content of the in situ nanogel N2. No visible changes in the appearance of the gel formulation were observed at the end of the storage period.

scholarly journals ABSOLUTE AND RELATIVE BIOAVAILABILITY STUDY FOR THE NEWLY DEVELOPED NASAL NANOEMULSION IN SITU GEL OF ONDANSETRON HCl IN COMPARISON TO CONVENTIONALLY PREPARED IN SITU GEL AND INTRAVENOUS DOSAGES FORMS

2018 ◽  
Vol 10 (5) ◽  
pp. 105
Author(s):  
Nidhal K. Maraie ◽  
Yasser Q. Almajidi ◽  
Ahmed Alshadher
Keyword(s):  
Relative Bioavailability ◽  
The Body ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Studies ◽  
Bioavailability Enhancement ◽  
In Situ Gel ◽  
Bioavailability Study ◽  
The Absolute

Objective: The aim of the work was to study the absolute and relative bioavailability (using rabbits) of ondansetron HCl (ONH)from our newly prepared intranasal mucoadhesive nanoemulsion in situ gel (NIG) in comparison to intranasal mucoadhesive in situ gel (IG) prepared by the conventional method and intravenous injection.Methods: Six male rabbits weighing 2.5-3 kg were used in this study, where the dose of ondansetron HCl (ONH) was calculated based on the body surface area (BSA) which is equivalent to 140μl (containing 10 mg/ml) of NIG and IG and 700μl of intravenous Zofran® injection (containing 2 mg/ml) were given to the rabbits, separated with one week washout period. Serial blood samples were withdrawn and analyzed for simultaneous determination of the drug using HPLC (Knaure; 150 ×4.6 mm; 5 μm particle size; 25 cm length) supported by guard column C18-4 mm diameter.Results: The pharmacokinetics parameters for NIG; Cmax, Tmax, AUC0-t, AUC0-∞were found to be greater than conventional in situ gel (IG). In vivo pharmacokinetic studies in rabbits showed a significant increase in Cmax and AUC 0-α(P<0.001) with shorter Tmaxusing NIG compared to IG containing the same NIG excipients, while the absolute bioavailability for NIG and IG (was 80.541 and 51.068 respectively).Conclusion: The present studies ratify the bioavailability enhancement potential of NE used to prepare NIG for the drug and significantly high absolute bioavailability to be used as a successful alternative route to the IV injection and improve patient compliance.

scholarly journals Formulation and Evaluation of A Nanoparticle Laden in Situ Gel System for Enhancing the Ocular Delivery of Ciprofloxacin

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Sourav Datta ◽  
Ratul Bhowmik ◽  
Ranajit Nath ◽  
Rajarshi Chakraborty ◽  
Apala Chakraborty
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Average Particle ◽  
Eye Drops ◽  
Physiological Factors ◽  
In Situ Gel ◽  
Gel System

The human eye can be a tricky issue for topical administration of the drugs due to its unique anatomical arrangements of surface tissue and corneal impermeability. Topical instillation of drugs in the form of eye drops is the major and well-accepted route of administration for the treatment of varied eye disorders. Conventional ophthalmic drug delivery systems often lead to poor bioavailability and thus reduced therapeutic response. Several new preparations are developed to enhance the contact time of the medicament on the surface of the eye. Successful results have been obtained in the form of inserts and collagen shields. However, these preparations have also some disadvantages, such as poor patient compliance, particularly in the case of elderly patients. These problems could be solved by using nanoparticles laden in situ gel-forming systems that exhibit phase transition from solution to gel. These nanoparticle in situ gel systems may be formulated as eye drops suitable for administration through instillation into the eye, which upon exposure to the eye, stimulated by various ocular physiological factors, converts to the gel phase. The advantage of those formulations is that unlike inserts and films they do not require complicated equipment for manufacture and that they are scalable without any difficulty. The objective of the present study was to prepare a pH-dependent nanoparticle-laden in situ gel system for Ciprofloxacin, to prolong the release of the drug into the ocular compartment. No incompatibility was found between the drug and the excipients. Nanoparticles were developed using the nanoprecipitation technique. Eudragit RL 100 was used as the polymer. While the in situ gel solution was formulated using chitosan as polymer. The Ciprofloxacin nanoparticles were measured for particle size and the average particle size was ranged from 295.3-458.7 nm. Entrapment efficiency ranged from 13.83% to 6.29%. Nanoparticleladen in situ gels had the pH of the formulati

scholarly journals Magnetically directed antioxidant and antimicrobial agent: synthesis and surface functionalization of magnetite with quercetin

PeerJ ◽  
2019 ◽  
Vol 7 ◽  
pp. e7651 ◽  
Author(s):  
Syed Tawab Shah ◽  
Wageeh A. Yehye ◽  
Zaira Zaman Chowdhury ◽  
Khanom Simarani
Keyword(s):  
Anticancer Agents ◽  
Magnetite Nanoparticles ◽  
Biological Activities ◽  
Average Particle Size ◽  
Radical Scavenging ◽  
Antibacterial Properties ◽  
Diffusion Method ◽  
Average Particle ◽  
Synthesis Technique

Oxidative stress can be reduced substantially using nanoantioxidant materials by tuning its surface morphological features up to a greater extent. The physiochemical, biological and optical properties of the nanoantioxidants can be altered by controlling their size and shape. In view of that, an appropriate synthesis technique should be adopted with optimization of the process variables. Properties of magnetite nanoparticles (IONP) can be tailored to upgrade the performance of biomedicine. Present research deals with the functionalization IONP using a hydrophobic agent of quercetin (Q). The application of quercetin will control its size using both the functionalization method including in-situ and post-synthesis technique. In in-situ techniques, the functionalized magnetite nanoparticles (IONP@Q) have average particles size 6 nm which are smaller than the magnetite (IONP) without functionalization. After post functionalization technique, the average particle size of magnetite IONP@Q2 determined was 11 nm. The nanoparticles also showed high saturation magnetization of about 51–59 emu/g. Before starting the experimental lab work, Prediction Activity Spectra of Substances (PASS) software was used to have a preliminary idea about the biological activities of Q. The antioxidant activity was carried out using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay. The antibacterial studies were carried out using well diffusion method. The results obtained were well supported by the simulated results. Furthermore, the values of the half maximal inhibitory concentration (IC50) of the DPPH antioxidant assay were decreased using the functionalized one and it exhibited a 2–3 fold decreasing tendency than the unfunctionalized IONP. This exhibited that the functionalization process can easily enhance the free radical scavenging properties of IONPs up to three times. MIC values confirms that functionalized IONP have excellent antibacterial properties against the strains used (Staphylococcus aureus, Bacillus subtilis and Escherichia coli) and fungal strains (Aspergillus niger, Candida albicans, Trichoderma sp. and Saccharomyces cerevisiae). The findings of this research showed that the synthesized nanocomposite has combinatorial properties (magnetic, antioxidant and antimicrobial) which can be considered as a promising candidate for biomedical applications. It can be successfully used for the development of biomedicines which can be subsequently applied as antioxidant, anti-inflammatory, antimicrobial and anticancer agents.

scholarly journals Physicochemical, Pharmacokinetic, and Toxicity Evaluation of Soluplus® Polymeric Micelles Encapsulating Fenbendazole

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 1000 ◽  
Author(s):  
Ik Sup Jin ◽  
Min Jeong Jo ◽  
Chun-Woong Park ◽  
Youn Bok Chung ◽  
Jin-Seok Kim ◽  
...  
Keyword(s):  
Polymeric Micelles ◽  
Drug Loading ◽  
Average Particle Size ◽  
A549 Cells ◽  
Pharmacokinetic Studies ◽  
Average Particle ◽  
Severe Toxicity ◽  
Blood Concentrations

Fenbendazole (FEN), a broad-spectrum benzimidazole anthelmintic, suppresses cancer cell growth through various mechanisms but has low solubility and achieves low blood concentrations, which leads to low bioavailability. Solubilizing agents are required to prepare poorly soluble drugs for injections; however, these are toxic. To overcome this problem, we designed and fabricated low-toxicity Soluplus® polymeric micelles encapsulating FEN and conducted toxicity assays in vitro and in vivo. FEN-loaded Soluplus® micelles had an average particle size of 68.3 ± 0.6 nm, a zeta potential of −2.3 ± 0.2 mV, a drug loading of 0.8 ± 0.03%, and an encapsulation efficiency of 85.3 ± 2.9%. MTT and clonogenic assays were performed on A549 cells treated with free FEN and FEN-loaded Soluplus® micelles. The in vitro drug release profile showed that the micelles released FEN more gradually than the solution. Pharmacokinetic studies revealed lower total clearance and volume of distribution and higher area under the curve and plasma concentration at time zero of FEN-loaded Soluplus® micelles than of the FEN solution. The in vivo toxicity assay revealed that FEN-loaded Soluplus® micelle induced no severe toxicity. Therefore, we propose that preclinical and clinical safety and efficacy trials on FEN-loaded Soluplus® micelles would be worthwhile.

scholarly journals Effect of soil textural characteristics on longitudinal dispersion in saturated porous media

2021 ◽  
Vol 69 (2) ◽  
pp. 161-170
Author(s):  
Mojtaba G. Mahmoodlu ◽  
Amir Raoof ◽  
Martinus Th. van Genuchten
Keyword(s):  
Particle Size ◽  
Dispersion Coefficient ◽  
Average Particle Size ◽  
Longitudinal Dispersion ◽  
Average Particle ◽  
Sand Sample ◽  
Average Pore ◽  
Advection Dispersion ◽  
Strong Positive Relationship

Abstract This study focuses on the effects of soil textural heterogeneity on longitudinal dispersion under saturation conditions. A series of solute transport experiments were carried out using saturated soil columns packed with two filter sands and two mixtures of these sands, having d50 values of 95, 324, 402, and 480 µm, subjected to four different steady flow rates. Values of the dispersion coefficient (D) were estimated from observed in-situ distributions of calcium chlo-ride, injected as a short nonreactive tracer pulse, at four different locations (11, 18, 25, 36 cm). Analyses of the observed distributions in terms of the standard advection-dispersion equation (ADE) showed that D increased nonlinearly with travel distance and higher Peclet numbers+. The dispersion coefficient of sand sample S1 with its largest average particle size (d 50) was more affected by the average pore-water velocity than sample S4 having the smallest d 50. Results revealed that for a constant velocity, D values of sample S1 were much higher than those of sample S4, which had the smallest d 50. A correlation matrix of parameters controlling the dispersion coefficient showed a relatively strong positive relationship between D and the Peclet number. In contrast, almost no correlation was evident between D and porosity as well as grain size. The results obtained with the four sandy matrices were consistent and proved that the dispersion coefficient depends mainly on the particle size.

scholarly journals FORMULATION AND EVALUATION OF DOXORUBICIN CONTAINING NANOGELS FOR DELIVERY TO CANCER CELLS

2018 ◽  
Vol 8 (5) ◽  
pp. 178-183
Author(s):  
Manish Kumar ◽  
Hemant K. Sharma
Keyword(s):  
Average Particle Size ◽  
Gellan Gum ◽  
Cross Linking ◽  
Average Particle ◽  
Scanning Calorimetry ◽  
Green Method ◽  
X Ray ◽  
Oppositely Charged ◽  
Chemical Cross Linking

The objective of this study is to prepare nanogels were prepared via charged gellan gum. It was prepared by in situ cross linking reaction between two oppositely charged materials by green method without use of chemical cross linking agents. The prepared nanogels were characterized by Dynamic light scattering, scanning electron microscopy, differential scanning calorimetry and X- Ray diffractometry. The prepared formulation had average particle size of 226 nm with polydispersity index of 0.3. The doxorubicin loaded nanogel demonstrated sustained release for 20 h. The prepared nanogels were hemocompatible and cyctocompatible as revealed by hemocompatibility and MTT assay respectively. All results confirmed that these nanogels can be used for cancer treatment. Keywords: Nanogel, Chitosan, Gellan gum, Doxorubicin, Cancer.

Sign in / Sign up

Export Citation Format

Share Document