Formulation Optimization and Ex Vivo and In Vivo Evaluation of Celecoxib Microemulsion-Based Gel for Transdermal Delivery

Abstract

Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Transcutol-P (co-surfactant) was screened respectively and optimized by using orthogonal experimental design. The Km value and concentration of oil, S, and water were confirmed by pseudo-ternary phase diagram studies and central composite design. One percent carbopol 934 was added to form CXB microemulsion-based gel. The final formulation was evaluated for its appearance, pH, viscosity, stability, drug content determination, globule size, and zeta potential. Its ex vivo drug permeation and the in vivo pharmacokinetic was investigated. Further research was performed to ensure the safety and validity by skin irritation study and in vivo anti-inflammatory activity study. Ex vivo permeation study in mice was designed to compare permeation and transdermal ability between microemulsion formulation and conventional gel. The results revealed that optimized microemulsion-based gel gained higher permeation based on smaller globule size and high drug loading of microemulsion. Transdermal ability was also greatly improved. Bioavailability was compared to market Celebrex® by the in vivo pharmacokinetic study in rabbits. The results indicated that CXB microemulsion-based gel had better bioavailability than Celebrex®.

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

“…A nanosponge showing a high percentage of drug release F4 was converted into a topical gel using polymers carbopol 934 and hydroxypropyl methylcellulose (HPMC). Carbopol934 and hydroxypropyl methylcellulose [16] were weighed and soaked for 24h in the required quantity of water and stirred using a mechanical stirrer at 1000 rpm [16,17]. In the above-formed gel required quantities of glycerin, methylparaben, propylparaben, and triethanolamine were added with continuous and slow stirring for 30 min.…”

Utilization of active and passive constructions in English academic writing

“…Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID) (Cao, Ren, and Chen, 2017).…”

“…Hence, the formulation of CXB was selected for solubilisation and bioavailability (Cao, Ren, and Chen, 2017).…”

Efficiency of the combination of physical therapy modalities with topical nonsteroidal anti-inflammatory drugs for treatment of pain in rheumatology

“…В іншому рандомізованому клінічному дослідженні за допомогою біопсії післяопераційного біоматеріалу (артропластика колінних суглобів) підтверджено вплив ультразвуку на ефективність транспорту кетопрофену в навколосуглобові тканини та синовіальну рідину [13]. Не менш ефективною ця комбінація була в лікуванні стенозуючого тендовагініту, латерального епікондиліту та синдрому субакроміального конфлікту [19,20,21,22].…”