scholarly journals Preparation and Evaluation of Amino Acid Conjugates of Celecoxib as Prodrugs to Improve the Pharmacokinetic and Therapeutic Properties of Celecoxib

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1043
Author(s):  
Yonghyun Lee ◽  
Jungyun Kim ◽  
Wooseong Kim ◽  
In-Soo Yoon ◽  
Yunjin Jung
Keyword(s):  
Systemic Absorption ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Linear Pharmacokinetic ◽  
Conversion Rates ◽  
Edema Model ◽  
Intestinal Contents ◽  
Therapeutic Properties ◽  
Rat Paw ◽  
Preparation And Evaluation

Although celecoxib is quite effective in the management of inflammation-related diseases, especially arthritis, its use is limited by concerns including low bioavailability (BA), non-linear pharmacokinetic (PK) profile, and peak concentration-related toxicity. To overcome these issues, we designed and prepared hydrophilic celecoxib prodrugs, namely N-glycyl-aspart-1yl celecoxib (N-GA1C), glutam-1-yl celecoxib (G1C), and aspart-1yl celecoxib (A1C), for the sustained release of celecoxib in the intestine with limited systemic absorption. The celecoxib derivatives were converted to celecoxib in the intestinal contents. The conversion rates were in order of N-GA1C > G1C > A1C. Oral administration of the celecoxib derivatives (oral celecoxib derivatives) sustained the plasma concentration of celecoxib for 24 h, improving the BA and linearity of the PK profile of celecoxib. The peak concentrations (Cmax) of celecoxib after oral celecoxib derivatives were lower than that after oral celecoxib. In a carrageenan-induced rat paw edema model, oral N-GA1C exhibited greater anti-inflammatory activity for a longer duration compared with oral celecoxib. The order of efficacy of the celecoxib derivatives was N-GA1C > G1C > A1C. Taken together, the prodrug approach is a feasible strategy to improve the PK and therapeutic properties of celecoxib, and among the celecoxib derivatives, N-GA1C may be the most promising prodrug of celecoxib.

scholarly journals Retraction Note: Release-Active Dilutions of Diclofenac Enhance Anti-inflammatory Effect of Diclofenac in Carrageenan-Induced Rat Paw Edema Model

Inflammation ◽  
2020 ◽  
Author(s):  
Sachin S. Sakat ◽  
Kamaraj Mani ◽  
Yulia O. Demidchenko ◽  
Evgeniy A. Gorbunov ◽  
Sergey A. Tarasov ◽  
...  
Keyword(s):  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inflammatory Effect

scholarly journals Ufasomes Mediated Cutaneous Delivery of Dexamethasone: Formulation and Evaluation of Anti-Inflammatory Activity by Carrageenin-Induced Rat Paw Edema Model

2013 ◽  
Vol 2013 ◽  
pp. 1-12 ◽  
Author(s):  
Rajkamal Mittal ◽  
Arvind Sharma ◽  
Sandeep Arora
Keyword(s):  
Oleic Acid ◽  
Entrapment Efficiency ◽  
Inflammatory Activity ◽  
Molar Ratio ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Transmission Electron ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw

The purpose of study is to formulate and evaluate ufasomal gel of dexamethasone. Ufasomal suspension was made by sonication method using different concentrations of Span 80, Span 20 and cholesterol along with 25 mg of drug. Ufasomal gel was formulated by hydration method using carbopol 940. Ufasomal vesicles appeared as spherical and multilamellar under Transmission Electron Microscope. Ufasomal formulation prepared with drug to oleic acid molar ratio 8:2 (UF-2) produced greater number of vesicles and greater entrapment efficiency. UF-2 was optimized for further evaluation. The transdermal permeation and skin partitioning of from optimized formulation was significantly higher () as compared to plain drug and plain gel formulation which is due to presence of surfactant acting as permeation enhancer. Permeation of optimized formulation was found to be about 4.7 times higher than plain drug gel. Anti-inflammatory activity evaluated by inhibition Carrageenan induced rat paw edema model. Significant reduction of edema () was observed in comparison to the commercial product. Hence oleic acid based vesicles can be used as alternate carrier for topical delivery.

scholarly journals RETRACTED ARTICLE: Release-Active Dilutions of Diclofenac Enhance Anti-inflammatory Effect of Diclofenac in Carrageenan-Induced Rat Paw Edema Model

Inflammation ◽  
2013 ◽  
Vol 37 (1) ◽  
pp. 1-9 ◽  
Author(s):  
Sachin S. Sakat ◽  
Kamaraj Mani ◽  
Yulia O. Demidchenko ◽  
Evgeniy A. Gorbunov ◽  
Sergey A. Tarasov ◽  
...  
Keyword(s):  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Retracted Article ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inflammatory Effect

scholarly journals Inhibition of carrageenan-induced expression of tissue and plasma prekallikreins mRNA by low level laser therapy in a rat paw edema model

2011 ◽  
Vol 15 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Moisés P. Silva ◽  
Flávia Bortone ◽  
Marcelo P. Silva ◽  
Thiago R. Araújo ◽  
Maricília S. Costa ◽  
...  
Keyword(s):  
Laser Therapy ◽  
Low Level Laser Therapy ◽  
Paw Edema ◽  
Induced Expression ◽  
Low Level ◽  
Low Level Laser ◽  
Rat Paw Edema ◽  
Level Laser ◽  
Edema Model ◽  
Rat Paw

scholarly journals Therapeutic effects of Smilax glabra and Bolbostemma paniculatum on rheumatoid arthritis using a rat paw edema model

2018 ◽  
Vol 108 ◽  
pp. 309-315 ◽  
Author(s):  
Yarigui Bao ◽  
Hui Li ◽  
Qi-Yan Li ◽  
Yong Li ◽  
Fei Li ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Therapeutic Effects ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Rat Paw

scholarly journals Lipid Nanocapsule-Based Gels for Enhancement of Transdermal Delivery of Ketorolac Tromethamine

2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Valiollah Hajhashemi ◽  
Sindokht Soltanzadeh
Keyword(s):  
Oleic Acid ◽  
Transdermal Delivery ◽  
Cold Water ◽  
Penetration Enhancers ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Permeation Studies ◽  
Rat Paw

Previous reports show ineffective transdermal delivery of ketorolac by nanostructured lipid carriers (NLCs). The aim of the present work was enhancement of transdermal delivery of ketorolac by another colloidal carriers, lipid nanocapsules (LNCs). LNCs were prepared by emulsification with phase transition method and mixed in a Carbomer 934P gel base with oleic acid or propylene glycol as penetration enhancers. Permeation studies were performed by Franz diffusion cell using excised rat abdominal skin. Aerosil-induced rat paw edema model was used to investigate the in vivo performance. LNCs containing polyethylene glycol hydroxyl stearate, lecithin in Labrafac as the oily phase, and dilution of the primary emulsion with 3.5-fold volume of cold water produced the optimized nanoparticles. The 1% Carbomer gel base containing 10% oleic acid loaded with nanoparticles enhanced and prolonged the anti-inflammatory effects of this drug to more than 12 h in Aerosil-induced rat paw edema model.

Anti-Inflammatory and Cytotoxic Activities of Chichipegenin, Peniocerol, and Macdougallin Isolated from Myrtillocactus geometrizans (Mart. ex Pfeiff.) Con.

2011 ◽  
Vol 66 (1-2) ◽  
pp. 24-30 ◽  
Author(s):  
Juan Rodrigo Salazar ◽  
Mariano Martínez-Vazquez ◽  
Carlos L. Cespedes ◽  
Teresa Ramírez-Apan ◽  
Antonio Nieto-Camacho ◽  
...  
Keyword(s):  
Human Cancer ◽  
Cytotoxic Activities ◽  
Dependent Manner ◽  
Paw Edema ◽  
Medicinal Uses ◽  
Human Cancer Cell Lines ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw

The oleanane-type triterpene chichipegenin and the sterols peniocerol and macdougallin, isolated from Myrtillocactus geometrizans, showed anti-inflammatory activities in both the 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema model and the carrageenan- induced rat paw edema model. All tested compounds inhibited the TPA-induced edema in a dose-dependent manner, with ED50 values less than or equal to that shown by indomethacin. Among them, peniocerol was the most active compound. However, only peniocerol and macdougallin reduced carrageenan-induced rat paw edema. On the other hand, peniocerol and macdougallin showed cytotoxicity against several human cancer cell lines. These results indicate that compounds isolated from M. geometrizans possess antiinflammatory and cytotoxic properties, and the presence of chichipegenin in the aerial parts could justify the medicinal uses attributed to the plant.

scholarly journals TO STUDY OF ANTI-INFLAMMATORY EFFECT OF CALCIUM CHANNEL BLOCKERS IN RAT PAW EDEMA MODEL

2016 ◽  
Vol 3 (14) ◽  
pp. 493-500
Author(s):  
Anil Kumar Sharma ◽  
Azmatulla Shaik ◽  
Chitti Babu G ◽  
Khizer Hussain Afroze M ◽  
Praveen Agarwal
Keyword(s):  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Channel Blockers ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Inflammatory Effect

scholarly journals EVALUATION OF ANTI-INFLAMMATORY (IN VIVO) ACTIVITY OF ARIFLEX LINIMENT IN COMPARISON WITH DICLOFENAC GEL IN CARRAGEENAN INDUCED RAT PAW EDEMA MODEL

2021 ◽  
pp. 67-70
Author(s):  
SANJAY NIPANIKAR ◽  
S. S. CHITLANGE
Keyword(s):  
Significant Inhibition ◽  
Lateral Malleolus ◽  
Inflammatory Activity ◽  
Control Group ◽  
Paw Edema ◽  
Rat Paw Edema ◽  
Edema Model ◽  
Anti Inflammatory ◽  
Rat Paw

Objective: The present study was conducted to evaluate anti-inflammatory activity of Ariflex liniment (conceptualized and developed by Ari Healthcare Pvt. Ltd) in comparison with Diclofenac gel in carrageenan induced rat paw edema model. Methods: Wistar rats of either sex weighing 150-180 g were taken and divided into 3 groups with 6 animals in each group i.e. Group 1 (Controlled Group), Group 2 (Diclofenac gel) and Group 3 (Ariflex liniment). The study drugs were topically applied 30 min prior to carrageenan injection. After 30 min 1% w/v of 0.05 ml carrageenan was injected subcutaneously in the paw. The paw was marked with ink at the level of lateral malleolus and immersed in mercury up to the lateral malleolus mark. The paw volume was measured plethysmographically, immediately after injection i.e. on 0 min, and then on 30 min,1h, 2h,3h, 4h and 5hr after injection. Results: Diclofenac gel sodium treated group showed significant inhibition (p<0.01) of paw edema at 30 min, 1, 2, 3, 4 and 5th hrs as compared to control group. Ariflex Liniment showed significant inhibition (p<0.05) of paw edema at 30 min, 1, 2, 3, and 4th hrs as compared to the control group. Group treated with Ariflex Liniment did not show any significant decrease in paw edema volume at 5th hrs when compared to the control group. Conclusion: Ariflex Liniment possesses anti-inflammatory activity.

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