In-vitro release and in-vivo performance of tolmetin from different topical gel formulations

Auda, Sayed H.; El-Rasoul, Saleh Abd; Ahmed, M. M.; Osman, Shaaban K.; El-Badry, Mahmoud

doi:10.1007/s40005-015-0174-3

Cited by 21 publications

(13 citation statements)

References 22 publications

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“…The calculated amounts of each HPMC (3, 5, 7, 10% w/v), HEC (2, 3, 4% w/v) and CMC (2, 3, 4% w/v) were separately weighed and added gradually to the drug solution with gentle stirring (120 rpm) using a magnetic stirrer (Dubuque, Iowa, USA). Stirring was continued until no lumps were observed and the content left overnight in refrigerator (4 °C) to complete solubility and gel formation (Auda et al 2015).…”

Section: Methodsmentioning

confidence: 99%

Pharmaceutical and pharmacokinetic evaluation of novel rectal mucoadhesive hydrogels containing tolmetin sodium

Ramadan

Elbakry

Esmaeil

et al. 2017

J. Pharm. Investig.

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The objective of the present study was to develop rectal mucoadhesive hydrogels loaded with Tolmetin Sodium, a nonsteroidal anti-inflammatory drug, for prolonged duration of action and increased bioavailability. Fourteen formulae were prepared with different types and concentrations of polymers as hydroxypropylmethyl cellulose, hydroxylethyl cellulose, carboxymethyl cellulose and sodium alginate. Each formulation contain Tolmetin Sodium equivalent to 5% w/w active drug. The effect of the employed gel bases on pH, gel strength, mucoadhesion, viscosity and the in vitro release profile of drug was examined. In addition, hydrogel formulations were subjected to rheological and stability studies. The physicochemical characterization revealed that all hydrogels had a suitable pH (6.64-7.75) and gel strength (15.5-65.29 s) for rectal application. The in-vitro drug release from the formulations showed a controlled drug release pattern, reaching 72-92.6% after 8 h. The kinetic analysis of the release data revealed that the drug release from all tested hydrogel bases obeyed the diffusion mechanism. The degradation of Tolmetin Sodium from its rectal hydrogel formulations was found to be a zero-order reaction. All formulations except sodium alginate hydrogel were quite stable. Considering the in-vitro release, rheological properties and shelf life, (CMC; 2%w/w) hydrogel formula was the best among the studied formulations. Therefore, further histopathological and bioavailability studies were carried out to detect different pharmacokinetic parameters of the established formulations compared with commercially available capsules. Formula containing 2% CMC showed relative bioavailability 357.93%. Finally, good correlation was observed between in-vitro and in-vivo profile.

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Section: Methodsmentioning

confidence: 99%

Pharmaceutical and pharmacokinetic evaluation of novel rectal mucoadhesive hydrogels containing tolmetin sodium

Ramadan

Elbakry

Esmaeil

et al. 2017

J. Pharm. Investig.

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“…According to the International Council for Harmonization of technical requirements for pharmaceutical for human use (ICH) guidelines, the stability studies of the prepared quercetin loaded nanosponges gel and quercetin pure gel were conducted. The prepared gels were studied under two variations 25±2 °C (refrigerator temperature) and 40±2 °C (accelerated stability condition) for a period of three months [34,35]. Parameters like pH, drug content, homogeneity, in vitro drug release studies were conducted.…”

Section: Stability Studiesmentioning

confidence: 99%

“…For this study male Wistar albino rats were used. They were grouped into five and all the animals were kept at an optimum weight of 150-200g and age of 10-12 w [35,36]. Group I was treated as the control without any treatment, Group II was normal with only carrageenan (1%w/v) inducer, Group III was treated with marketed Voveran gel, Group IV with pure quercetin gel and Group V with quercetin loaded nanosponges gel.…”

Section: In Vivo Anti-inflammatory Activitymentioning

confidence: 99%

Formulation and Optimization of Quercetin Loaded Nanosponges Topical Gel: Ex Vivo, Pharmacodynamic and Pharmacokinetic Studies

Sujitha

Muzib

2019

Int J App Pharm

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Objective: Quercetin is therapeutically hampered because of its poor solubility. The present investigation was aimed to prepare quercetin loaded nanosponges topical gel to enhance the solubility and efficacy of the drug. Methods: Quercetin nanosponges were prepared by emulsion solvent diffusion method. Developed nanosponges optimized by particle size, SEM, entrapment efficiency, FT-IR, DSC, P-XRD, In vitro studies. The optimized formulation of nanosponges was loaded into a topical gel and it was characterized by ex-vivo, in vivo Pharmacodynamic and kinetic studies. Results: The particle size and zeta potential of optimized nanosponges were found to be 188.3 nm and-0.1mV. Surface morphology was studied using SEM Analysis which showed tiny sponge-like structure and entrapment efficiency was found to be 96.5 %. In vitro drug release of optimized nanosponges was found to be 98.6% for 7hours. Optimized nanosponges entrapped gel was prepared by using carbopol 934 and hydroxypropyl methylcellulose as gelling agents. The prepared nanogels were homogenous and ex-vivo skin permeation studies of the optimized nanosponges gel was found to be 98.1% for 5 h, quercetin loaded nanosponges has shown higher skin permeation efficiency (18.4µg/cm2±2.1) compared to pure quercetin gel. The pharmacokinetic and pharmacodynamic studies showed that the quercetin loaded nanosponges has shown more effective when compared to marketed formulation. Conclusion: Quercetin loaded nanosponges gel has shown a significant increase in activity (p<0.05) compared to the marketed formulation (Voveran Emulgel).

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“…The maximum concentration of EG in the supernatant was determined by determining UV absorbance of soluble EG as described above. According to the previous reports, 25,26 EG/CMC hydrogel and EG–β-CD/CMC hydrogel were prepared as follows: 0.5 g CMC was dissolved in 25 ml of 1% NaOH solution. Next, 100 mg of EG and EG–β-CD was dispersed into 25 ml PBS (pH 7.4) gradually and individually added to CMC solution for ensuring the complete dispersion of EG and EG–β-CD between the polymer chains with gentle stirring (120 r/min) using a magnetic stirrer at room temperature.…”

Section: Methodsmentioning

confidence: 99%

Fabrication of carboxymethylcellulose hydrogel containing β-cyclodextrin–eugenol inclusion complexes for promoting diabetic wound healing

Wang

et al. 2019

J Biomater Appl

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The difficult healing of wounds caused by diabetes remains a challenging clinical problem. The activation of nuclear factor kappa-B as a key factor contributes to prolonged inflammation and inhibition of angiogenesis. As a natural antioxidant, eugenol may downregulate the lectin-like oxidized low-density lipoprotein receptor-1 and inhibit the activation of nuclear factor kappa-B in endothelial cells. However, eugenol shows poor solubility, pungent odor, and volatility, thus impeding its clinical application as a potential therapeutic agent. This study developed a novel bioactive carboxymethylcellulose hydrogel loaded with inclusion complexes of eugenol with b-cyclodextrin (eugenol-b-cyclodextrin/ carboxymethylcellulose hydrogel) to regulate lectin-like oxidized low-density lipoprotein receptor-1-induced activation of nuclear factor kappa-B to enhance angiogenesis and inhibit inflammation for accelerating diabetic wound healing in vivo. It was found that eugenol-b-cyclodextrin/carboxymethylcellulose hydrogel exhibited remarkable antibacterial activity in vivo and in vitro. Furthermore, it accelerated diabetic wound healing by reducing the lectin-like oxidized low-density lipoprotein receptor-1/nuclear factor kappa-B-induced dysfunction in endothelial cells and promoting angiogenesis.

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In-vitro release and in-vivo performance of tolmetin from different topical gel formulations

Cited by 21 publications

References 22 publications

Pharmaceutical and pharmacokinetic evaluation of novel rectal mucoadhesive hydrogels containing tolmetin sodium

Pharmaceutical and pharmacokinetic evaluation of novel rectal mucoadhesive hydrogels containing tolmetin sodium

Formulation and Optimization of Quercetin Loaded Nanosponges Topical Gel: Ex Vivo, Pharmacodynamic and Pharmacokinetic Studies

Fabrication of carboxymethylcellulose hydrogel containing β-cyclodextrin–eugenol inclusion complexes for promoting diabetic wound healing

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