Resveratrol and Puerarin loaded polymeric nanoparticles to enhance the chemotherapeutic efficacy in spinal cord injury

Abstract Introduction:Spinal cord injury includes inflammation and apoptosis of neurons, which is difficult to cure by systemic drug administration. Administration of natural active compounds (resveratrol and also Puerarin) by advance drug delivery technology improves the patient’s conditions.Material and Methods: Oil-in-water emulsion method was utilized to prepare resveratrol as well as puerarin loaded PLGA nanoparticles. The nanoparticles were subjected to mean zeta potential, mean particle size, encapsulation efficiency as well as in vitro drug release studies. The biochemical parameters i.e. malondialdehyde (MDA), reduced glutathione (GSH), superoxide dismutase (SOD), advanced oxidation products (AOPP), catalase (CAT) and nitrite/nitrate levels were tested for the loaded nanoparticles. Reperfusion injury induced rats treated with 10 mg/kg resveratrol and puerarin loaded nanoparticles protects spine from ischemia injury and supports biological parameters.Results: The mean particle size varies from 238 nm to 274 nm and also particle size distribution was mono-dispersed (0.239 to 0.318). Zeta potential value of nanoparticles was observed to be -12.6 ± 2.1 mV. Optimized nanoparticles reveals 72% -79% of drug release over 36 h by diffusion mechanism. Significantly, lowers the levels of plasma nitrite/nitrate level as well as phosphorylation of p38MAPK pathways in reperfusion injury induced rats.Conclusion: The resveratrol and puerarin loaded nanoparticles decreases free radicals produced by reperfusion injury induced rats, as well as decrease of oxidative stress because of IRI. Resveratrol and puerarin loaded nanoparticles decreases GSH, SOD and CAT antioxidant level, which helps in overall health improvement of patients.

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Mechanism of Hydrogen Sulfide Drug-Loaded Nanoparticles Promoting the Repair of Spinal Cord Injury in Rats Through Mammalian Target of Rapamycin/Signal Transducer and Activator of Transcription 3 Signaling Pathway

Science of Advanced Materials ◽

10.1166/sam.2021.4109 ◽

2021 ◽

Vol 13 (9) ◽

pp. 1691-1698

Author(s):

Hongzhe Liu ◽

Kai Tong ◽

Ziyi Zhong ◽

Gang Wang

Keyword(s):

Spinal Cord ◽

Spinal Cord Injury ◽

Particle Size ◽

Dispersion Coefficient ◽

Drug Loading ◽

Average Particle Size ◽

Mammalian Target Of Rapamycin ◽

Average Particle ◽

Recovery Effect ◽

Cord Injury

To explore the effect of hydrogen sulfide (H2S) drug-loaded nanoparticles (H2S-NPs) on the mTOR/STAT3 signaling pathway in rats and its mechanism on repair of spinal cord injury (SCI), a new H2S-NP (G16MPG-ADT) was prepared and synthesized. The rats were selected as the research objects to explore the mechanism of SCI repair. The G16MPG-ADT NPs were evaluated by average particle size (APS), dispersion coefficient (DC), drug loading content (DLC), drug loading efficacy (DLE), in vitro release (IV-R), and acute toxicity (AT). It was found that G16MPG-ADT nanoparticles had a uniform particle size distribution with a unimodal distribution, with an average particle size of 186.5 nm and a dispersion coefficient of 0.129; within the concentration range of 8~56 μg/L, there was a good linear relationship with the peak area; and the release rate of the nanoparticles within 16 h~32 h was higher than 50%. G16MPG-ADT NP injection treatment was performed on rats with SCI. Western blotting (WB) and immunofluorescence staining were adopted to analyze the expression levels of mammalian target of rapamycin (mTOR) and signal transducers and activators of transcription (STAT3) protein and the growth of neurites. It was found that G16MPG-ADT can increase mTOR and STAT3 protein levels and promote nerve growth after SCI. Finally, the Basso, Beattie and Bresnahan locomotor rating (BBB) score was to evaluate the recovery effect of rats after treatment. It was found that the recovery effect was excellent after G16MPG-ADT treatment. In summary, G16MPG-ADT has a good effect on SCI repair in rats and can be promoted in the clinic.

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FORMULATION AND EVALUATION OF CURCUMIN LOADED LIPOSOME AND ITS BIO-ENHANCEMENT

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v9i4-a.3505 ◽

2019 ◽

Vol 9 (4-A) ◽

pp. 425-437

Author(s):

Khushboo Verma ◽

Jhakeshwar Prasad ◽

Suman Saha ◽

Surabhi Sahu

Keyword(s):

Thin Film ◽

Particle Size ◽

Drug Release ◽

Zeta Potential ◽

High Performance ◽

Encapsulation Efficiency ◽

Mean Particle Size ◽

Liposome Formulation

The aim of this work was to develop and evaluate curcumin loaded liposome and its bio- enhancement. Curcumin was selected as a natural drug for liposome formulation. Curcumin show variety of biological activity but it also shows poor bioavailability due to low aqueous solubility (1 µg/ml), poor absorption and rapid metabolism so that piperine was selected as bio enhancer to improve curcumin bioavailability. Soy lecithin and cholesterol were used to prepared curcumin and curcumin-piperine loaded liposome at different ratio by thin film hydration method because of easy to perform, and high encapsulation rates of lipid. The all liposome formulations (F1-F5) were evaluated by mean particle size, polydispersity index, zeta potential, encapsulation efficiency and drug release. Bioavailability was also determined on rat. Blood samples were collected at specific intervals, and plasma was separated by ultracentrifugation. Plasma was analyzed by high-performance liquid chromatography at 425 nm taking acetonitrile: water (75:25 v/v) acidified with 2% acetic acid as a mobile phase at a flow rate of 0.5 ml/min using C18 column. The mean particle size was found in the range between 800-1100 that indicate liposome are large unilamellar vesical types. By zeta potential study its conform that the all formulation was stable. The encapsulation efficiency of all liposome formulation are varied between 59-67%. In vitro drug release was analyse in 7.4 pH phosphate buffer, the maximum %CDR observed at the 12 hrs., and formulation are follow sustained release thus they reduce metabolism, good absorption rate which improve bioavailability of drug. From in-vivo study, it is clear that curcumin-piperine liposomal formulation, increases Cmax, area under the curve, and mean residence time significantly as compared to pure curcumin and pure curcumin liposome. Keywords: liposome; Curcumin; Piperine, Thin film hydration method; Bioavailability

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The selective poly(ADP)ribose-polymerase 1 inhibitor INO1001 reduces spinal cord injury during porcine aortic cross-clamping-induced ischemia/reperfusion injury

Intensive Care Medicine ◽

10.1007/s00134-007-0585-3 ◽

2007 ◽

Vol 33 (5) ◽

pp. 845-850 ◽

Cited By ~ 18

Author(s):

Christian Maier ◽

Angelika Scheuerle ◽

Balázs Hauser ◽

Hubert Schelzig ◽

Csaba Szabó ◽

...

Keyword(s):

Spinal Cord ◽

Spinal Cord Injury ◽

Reperfusion Injury ◽

Ischemia Reperfusion Injury ◽

Ischemia Reperfusion ◽

Cord Injury

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Abdominal Adiposity and Insulin Level Influence Lipoprotein Particle Size and Concentration in Spinal Cord Injury

Medicine & Science in Sports & Exercise ◽

10.1249/01.mss.0000385305.65733.f8 ◽

2010 ◽

Vol 42 ◽

pp. 532

Author(s):

Racine R. Emmons ◽

Christopher M. Cirnigliaro ◽

Steven C. Kirshblum ◽

Marinella D. Galea ◽

Ann M. Spungen ◽

...

Keyword(s):

Spinal Cord ◽

Spinal Cord Injury ◽

Particle Size ◽

Insulin Level ◽

Abdominal Adiposity ◽

Lipoprotein Particle ◽

Cord Injury ◽

Lipoprotein Particle Size

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Efficacy of Virtual Reality in Neurorehabilitation of Spinal Cord Injury Patients: A Systematic Review

10.17488/rmib.42.2.8 ◽

2021 ◽

Author(s):

◽

B. A. Orsatti-Sánchez

Keyword(s):

Systematic Review ◽

Spinal Cord ◽

Spinal Cord Injury ◽

Virtual Reality ◽

Methodological Quality ◽

Emotional Health ◽

Functional Improvement ◽

Health Improvement ◽

Positive Effects ◽

Cord Injury

This systematic review (SR) analyzed the effectiveness of interventions using virtual reality (VR) technology as a neurorehabilitation therapy in people with spinal cord injury (SCI). The SR was developed under the guidelines of the PRISMA statement and the recommendations of the Cochrane Collaboration, along with the PEDro and National Institute of Health scales to assess the risk of bias and methodological quality. The Cochrane, IEEE, BVS/LILACS, MEDLINE/PubMed, and Web of Science databases were browsed to identify studies that, between 2010 and 2020, evaluated the efficacy of these therapies. Out of 353 retrieved studies, 11 were finally selected after the application of the defined inclusion and exclusion criteria. These articles presented good methodological quality as they were mostly controlled clinical trials that analyzed mixed therapies with conventional therapies. Interventions based on non-immersive or immersive VR technology that achieved functional motor, balance, and psycho-emotional health improvement with positive effects on motivation, self-confidence, commitment, and active participation were identified in a total sample of 155 SCI patients. It was concluded that such VR technology is an effective tool of neurorehabilitation complementary to conventional therapies, which promotes functional improvement in SCI patients both in the clinic and at home.

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Optimization of Microemulgel for Tizanidine Hydrochloride

Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry ◽

10.2174/1871523018666190308123100 ◽

2020 ◽

Vol 19 (2) ◽

pp. 158-179

Author(s):

Swati Jagdale ◽

Sujata Brahmane ◽

Anuruddha Chabukswar

Keyword(s):

Spinal Cord ◽

Drug Release ◽

Zeta Potential ◽

Ternary Phase Diagram ◽

Ex Vivo ◽

Research Work ◽

Isopropyl Myristate ◽

Globule Size ◽

Cord Injury

Background: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis or spinal cord injury and treatment of muscle spasticity in spinal cord disease. Tizanidine hydrochloride belongs to BCS class II. It has low oral bioavailability and short halflife. Incorporating this drug in microemulgel is an excellent way to overcome problems associated with the drug. Objective: Present research work was aimed to develop and optimize a microemulsion based gel system for tizanidine hydrochloride. Methods: Screening of oil, surfactant and co-surfactant was carried out. Ternary phase diagram was constructed to obtain concentration range of components. The prepared microemulsion was evaluated for pH, globule size, zeta potential, conductivity, density and viscosity. 32 level factorial design was applied to study the effect of concentration of carbopol 934 and HPMC K15M on % cumulative drug release and viscosity of microemulgel using software Design Expert. Microemulgel was evaluated for pH, spreadability, viscosity, syneresis, drug content, bioadhesive strength, in-vitro as well as ex-vivo diffusion study. Results: Microemulsion was prepared by using isopropyl myristate as oil, tween 80 as a surfactant and transcutol P as cosurfactant. Largest transparent microemulsion region was found with Smix ratio of 1:1. FE-SEM showed globule size 28μm for batch B1 and zeta potential was -1.27mV indicating good stability of the microemulsion. Optimised batch was F6 which showed 92% drug release within 8 hours. It followed the Korsmeyer-Peppas model. Conclusion: A stable, effective and elegant microemulgel formulation, exhibiting good in-vitro and ex-vivo drug release was formulated.

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