Novel treatment for refractory rheumatoid arthritis with total glucosides of paeony and nobiletin codelivered in a self-nanoemulsifying drug delivery system

Author(s):  
Biao Qu ◽  
Xiao-lin Wang ◽  
De-chong Zheng ◽  
Chu-tian Mai ◽  
Zhong-qiu Liu ◽  
...  
Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.


YMER Digital ◽  
2022 ◽  
Vol 21 (01) ◽  
pp. 41-55
Author(s):  
L Tamilselvi ◽  
◽  
R Senthamarai ◽  
A.M. Ismail ◽  
T Shri Vijaya Kirubha ◽  
...  

Novel herbal drug delivery system opens new vistas for delivery of herbal drugs at right place, at right concentration, for right period of time and also gives scientific angle to verify the standardization of herbal drug. Herbal Transdermal patches can develop valuable assessment and drug safety by additional site specific the way and temporal position in the body’s imperative to reduce the number and size of doses required to achieve the objective of systemic medication during topical application to the intact skin surface. Rheumatoid Arthritis (RA) is a chronic, progressive autoimmune disease of unknown cause. It is characterized by persistent inflammation that primarily affects the peripheral joints. In the present study, herbal transdermal patch was developed by using ethanolic extract of leaves of Cardiospermum halicacabum and rhizomes of Drynaria quercifolia that had already been widely used for the treatment of arthritis in conventional dosage forms. Evaluation of the developed patch for the effectiveness against RA was done by in vitro methods in terms of inhibition of albumin denaturation, measurement of Interleukin-6 cytokines by Enzyme-Linked Immuno Assay (ELISA). IC-50 value was determined from albumin denaturation inhibition assay. The herbal patch significantly and dosedependently inhibited Interleukin–6 cytokines. The present study revealed that the formulated polyherbal Transdermal patch will be the better drug of choice for the treatment of Rheumatoid Arthritis as compared to the conventional dosage forms.


2017 ◽  
Vol 34 (3) ◽  
pp. 654-667 ◽  
Author(s):  
Vijay Kumar ◽  
Ankita Leekha ◽  
Aakriti Tyagi ◽  
Ankur Kaul ◽  
Anil Kumar Mishra ◽  
...  

2020 ◽  
Author(s):  
Feili Yan ◽  
Zhirong Zhong ◽  
Yao Wang ◽  
Hui Li ◽  
Zhiqiang Mei ◽  
...  

Abstract Backgroud: Glucocorticoids (GCs) show powerful treatment effect on rheumatoid arthritis (RA). However, the clinical application is limited by their nonspecific distribution after systemic administration and serious adverse reactions during long-term administration. To achieve better treatment and reduce side effect, we here established a biomimetic exosome (Exo) encapsulating dexamethasone sodium phosphate (Dex) nanoparticle (Exo/Dex), whose surface was modified with folic acid (FA)-polyethylene glycol (PEG)-cholesterol (Chol) compound to attain FPC-Exo/Dex active targeting drug delivery system. Results The size of FPC-Exo/Dex was 128.43 ± 16.27 nm, with a polydispersity index (PDI) of 0.36 ± 0.05, and the Zeta potential was − 22.73 ± 0.91 mV. The encapsulation efficiency (EE) of the preparation was 10.26 ± 0.73%, with drug loading efficiency (DLE) of 18.81 ± 2.05%. In vitro study showed this system displayed enhanced endocytosis and excellent anti-inflammation effect against RAW264.7 cells by suppressing pro-inflammatory cytokines and increasing anti-inflammatory cytokine. Further biodistribution study showed the fluorescence intensity of FPC-Exo/Dex was stronger than other Dex formulations in joints, suggesting its enhanced accumulation to inflammation sites. In vivo pharmacodynamic experiment displayed FPC-Exo/Dex could preserve the bone and cartilage of CIA mice better and significantly reduce inflamed joints. Next in vivo safety evaluation demonstrated this biomimetic drug delivery system had no obvious hepatotoxicity and exhibited desirable biocompatibility. Conclusion The present study provides a promising strategy for using exosome as nanocarrier to enhance the therapeutic effect of GCs against RA.


Author(s):  
KARISHMA KAPOOR ◽  
VINAY PANDIT ◽  
UPENDRA NAGAICH

Objective: Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are essential part of the administration of Rheumatoid Arthritis (RA). Methotrexate (MTX) is effective for tumor necrosis factor alpha (TNF-a) biologic agents, indicated only in minority of patients suffering from severe RA. MTX remains the "anchor drug" in the treatment of RA. For delivery improvement, novel pharmaceutical drug delivery system i.e. MTX-Cubosomes were developed. Methods: Poloxamer 407 and Glycerol monooleate (Monoelin, MO) used and the formulation were characterized as a sustained release drug delivery system for Methotrexate. Different ratios of Monolein, Poloxamer 407 and water were used to develop the different cubosomes using homogenization and emulsification method. Characterization of formulations for morphology was performed and also particle size distribution by Transmission Electron Microscopy (TEM). Results: Formulation showed the internal cubic structures of the vesicles. The particle size of the formulations was found to be ranging from 53.21 to 185.32 nm, zeta potential of the formulations varied from-18.20-36.10 mV. The cubosomal formulation exhibited good entrapment efficiency along with high drug loading. Compatibility with the excipients was also established. An in vitro release study was done using Franz Diffusion cell indicated sustained release of the formulation at a rate of 1.25 %/h. Cubosomes proved to be reliable system for sustained transdermal drug delivery system. Conclusion: Methotrexate cubosomes is a novel medication delivery framework and in this examination it has been developed and characterized. The formulations were found to be promising in terms of its characterization parameters like particle size, zeta potential, entrapment efficiency, loading capacity, release kinetics, and stability, suitable for topical delivery.


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