Drug development and industrial pharmacy · 2025
A new approach for the development of etodolac emulgels for rheumatic arthritis cure: in vitro and in vivo assessments.
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Osman Shaaban K, Mohammed Ahmed M, Saleh Khaled I, Yassin Taher M, Abdelsalam Ahmed M, Marzouk Adel A, Ahmed Fatma, Ibrahim Mohamed A
Аннотация
OBJECTIVES: Etodolac (ETD), an insoluble anti-inflammatory drug, undergoes first-pass metabolism, which limits its oral bioavailability. The current study presents the trials for improvement of drug solubility on one hand and formulation of different emulgel systems loaded with modified drug on the other hand.
SIGNIFICANCE: The Prolonged oral administration of ETD results in serious gastrointestinal problems. Therefore, the improvement of its solubility and modifying an alternative route of administration will increase its bioavailability and lessen its adverse effects, providing an alternative safe delivery system for inflammatory signs treatment.
METHODS: The current study focused on the formulation of different emulgel systems since medicated emulgels were constructed by loading the emulgels with either pure ETD or modified ETD adsorbate (ETD/Avicel, 1:2 ratio). Finally, the in vivo studies were accomplished by studying the anti-inflammatory activity of ETD emulgels using albino rats.
RESULTS: All the prepared emulgels showed acceptable physical properties since sodium alginate emulgel showed superior drug release compared with other gelling agents. The drug release profile was affected significantly by both emulsifying and gelling agents' concentration. The release kinetics data showed that the main mechanism of drug release was the Higuchi diffusion model. concerning the in vivo results, the extreme edema inhibition was obtained upon using emulgel formulae containing modified ETD with penetration enhancer (5% PG + 5% oleic acid). The modified emulgels did not show any sign of irritation on rats' dorsal skin.
CONCLUSION: The obtained results highlighted the promising application of topical ETD emulgels as an alternative anti-inflammatory drug delivery system.
SIGNIFICANCE: The Prolonged oral administration of ETD results in serious gastrointestinal problems. Therefore, the improvement of its solubility and modifying an alternative route of administration will increase its bioavailability and lessen its adverse effects, providing an alternative safe delivery system for inflammatory signs treatment.
METHODS: The current study focused on the formulation of different emulgel systems since medicated emulgels were constructed by loading the emulgels with either pure ETD or modified ETD adsorbate (ETD/Avicel, 1:2 ratio). Finally, the in vivo studies were accomplished by studying the anti-inflammatory activity of ETD emulgels using albino rats.
RESULTS: All the prepared emulgels showed acceptable physical properties since sodium alginate emulgel showed superior drug release compared with other gelling agents. The drug release profile was affected significantly by both emulsifying and gelling agents' concentration. The release kinetics data showed that the main mechanism of drug release was the Higuchi diffusion model. concerning the in vivo results, the extreme edema inhibition was obtained upon using emulgel formulae containing modified ETD with penetration enhancer (5% PG + 5% oleic acid). The modified emulgels did not show any sign of irritation on rats' dorsal skin.
CONCLUSION: The obtained results highlighted the promising application of topical ETD emulgels as an alternative anti-inflammatory drug delivery system.