Abstract
The present study aimed to investigate the delivery potential of Etodolac (ETD) containing topical niosomal gel. Niosomal formulations were prepared by thin film hydration method at various ratios of cholesterol and Span 60 and were evaluated with respect to particle size, shape, entrapment efficiency, and in vitro characteristics. Dicetyl phosphate (DCP) was also added in the niosomal formulation. Mean particle size of niosomal formulation was found to be in the range of 2 μm to 4 μm. Niosomal formulation N2 (1 : 1) ratio of cholesterol and surfactant displayed good entrapment efficiency (96.72%). TEM analyses showed that niosomal formulation was spherical in shape. Niosomal formulation (N2) displayed high percentage of drug release after 24 h (94.91) at (1 : 1) ratio of cholesterol : surfactant. Further selected niosomal formulation was used to formulate topical gel and was characterized with respect to its various parameters such as pH, viscosity, spreadability, ex vivo study, and in vivo potential permeation. Ex vivo study showed that niosomal gel possessed better skin permeation study than the plain topical gel. Further in vivo study revealed good inhibition of inflammation in case of topical niosomal gel than plain gel and niosomal formulation. The present study suggested that topical niosomal gel formulations provide sustained and prolonged delivery of drug.
Highlights
Etodolac (ETD) is a nonsteroidal anti-inflammatory drug (NSAID) of selective COX-2 inhibitor class used for osteoarthritis and rheumatoid arthritis
Shape and morphology of niosomal formulations were determined by optical microscopy and Transmission Electron Microscopy (TEM) and result were shown in Figures 1 and 2
The viscosity of gel formulations was determined by Brookfield viscometer. 25.0 g gel was taken in beaker and spindle number 4 was rotated at 50 rpm and viscosity of the sample was determined (“as discussed by Jain et al [13]”)
Summary
Etodolac (ETD) is a nonsteroidal anti-inflammatory drug (NSAID) of selective COX-2 inhibitor class used for osteoarthritis and rheumatoid arthritis. Prostaglandins are the chemicals which are responsible for pain and the fever and tenderness that occur with inflammation It possesses poor solubility and undergoes extensive first pass metabolism that could be the reason of its low bioavailability. Continuous oral use of ETD causes serious gastrointestinal disturbance such as ulcer, stomach, or intestinal bleeding and chest pain which can be fatal To avoid such problem there are other alternatives like coating of polymer that avoid release of drug molecule in gastrointestinal tract (GIT). Transdermal route avoid first pass metabolism associated with conventional route of drug administration It provides easy elimination of drug in case of toxicity and reduced fluctuation in plasma drug concentration level and decreased side effect. Various novel delivery technologies including ethosomes (“as discussed by Chintala and Padmapreetha [2]”), microsphere (“as discussed by Kumar et al [3]”), thermogels for rectal delivery (“as discussed by Barakat [4]”), and hydrophilic gel (“as discussed by Tas et al [5]”) have been reported for delivery of Etodolac
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