Etoricoxib Emulgel: In Vitro and Ex Vivo Characterization for Development of Novel Topical Formulation—A Preclinical Study
摘要
Emulgel is a novel topical formulation for the delivery of hydrophobic drugs. Etoricoxib is a cyclooxygenase II inhibitor by reducing the prostaglandins generation from Arachidonic acid. The present research aimed to formulate and develop an emulgel for the topical delivery of Etoricoxib for the management of inflammation. Emulgel was prepared by a combination of oil (Etoricoxib) and water phases in different proportions by homogenization. The drug excipient compatibility was confirmed by the FTIR study. The manufactured emulgels were characterized for pH, viscosity, drug content, spreadability, extrudability, bioadhesive, haemocompatibility, stability and drug diffusion as well as permeation studies. The optimized Etoricoxib emulgel was studied for skin irritation test and its potency to inhibit the inflammation by carrageenan-induced paw edema method. FTIR study revealed that Etoricoxib was compatible with excipients. The pH and viscosity of emulgels were found in the ranges of 5.5 to 6.2 and 2.2 to 2.8 × 104 cp. The drug content was more than 90% for all emulgels. As the oil amount was increased in emulgel, the spreadability was increased with good extrudability and bioadhesion properties. The emulgel was much potent to inhibit the inflammation as compared with the marketed gel. The emulgel containing 40 ml of olive oil at the 4:6 ratio of oil and aqueous phase (F4) was found to be haemocompatible and non-irritant to animal skin. The emulgel was stable at various storage conditions as per ICH guidelines. The emulgel (F4) diffuses and permeates (7.956 ± 0.97 and 1.591 ± 0.88% in 3 h) the drug in a more controlled and constant manner. Etoricoxib emulgel (F4 with oil and aqueous phase ratio of 4:6) was found to be the best emulgel formulation for the effective management of inflammation.