Department of Pharmaceutics, Rajiv Academy for Pharmacy, Mathura (U.P.), India.
Department of Pharmacology, Rajiv Academy for Pharmacy, Mathura (U.P.), India.
Antiinflamm Antiallergy Agents Med Chem. 2024;23(2):129-137. doi: 10.2174/0118715230276597240207070306.
Emulgel combines the qualities of an emulsion with those of a gel. In order to create an emulgel w/o or o/w, emulsions have to be formulated, which are then combined with a gelling agent, resulting in a dual-control drug release. Celecoxib exhibits analgesic, antipyretic and anti-inflammatory activities and is used to treat osteoarthritis, severe pain, rheumatoid arthritis, and other medical conditions.
Celecoxib Emulgel was developed and evaluated by using natural oil and carbopol- 940 as a gelling agent in different concentrations. The screening of various oils, co-surfactants and surfactants was performed to determine the solubility. The essential oils (eucalyptus oil and turpentine oil) were used as penetration modifiers. Studies on compatibility with polymers have been conducted, and the results indicate that there should be no physical or chemical interactions between the polymers and the drug substance. For the preparation of emulgel, various emulsions were prepared with Smix (cosurfactant and surfactant) ratios (1:1, 2:1 and 3:1). The selection of a gelling agent was done by incorporating the selected emulsion system ratio of 1:1 with the combinations of polymers carbapol 940, carbapol 934, and HPMC (0:1:0, 0:0.5:1, 0:0:3, 0.5:0:1, 1:0:0) gel base to make a homogenous emulgel.
The emulgel was examined visually to see if it had any phase behaviour, feel, spreadability, and grittiness by applying its thin layer to a slide. Then, all six formulations of emulgel were prepared with the selected gelling agent. All emulgels were evaluated for pH, physical properties (consistency, homogeneity, colour, texture), drug content, spreadability, extrudability, swelling index, viscosity, stability and centrifugation. A Franz diffusion cell and an egg membrane were used to perform drug release.
Among all prepared formulations, EG1 had a better release, higher viscosity, higher drug content, and a higher swelling index than the others. The formulation EG1 showed higher drug release (91.25%) within 8 hours.
乳凝胶结合了乳液和凝胶的特性。为了制备 w/o 或 o/w 型乳凝胶,必须先制备乳液,然后再与成胶剂结合,从而实现双重控制药物释放。塞来昔布具有镇痛、解热和抗炎作用,用于治疗骨关节炎、严重疼痛、类风湿性关节炎和其他医疗条件。
采用天然油和卡波姆-940 作为成胶剂,以不同浓度研制并评价塞来昔布乳凝胶。对各种油、助表面活性剂和表面活性剂进行筛选,以确定溶解度。桉叶油和松节油等精油被用作渗透改性剂。对与聚合物的相容性进行了研究,结果表明聚合物与药物之间不应存在物理或化学相互作用。为制备乳凝胶,用 Smix(助表面活性剂和表面活性剂)比例(1:1、2:1 和 3:1)制备各种乳液。选择成胶剂时,将选定的乳液系统比例 1:1 与卡波姆 940、卡波姆 934 和 HPMC(0:1:0、0:0.5:1、0:0:3、0.5:0:1、1:0:0)凝胶基的组合相结合,制成均匀的乳凝胶。
通过将薄层涂在载玻片上,目视检查乳凝胶是否有任何相行为、感觉、铺展性和粗糙感。然后,用选定的成胶剂制备六种乳凝胶制剂。对所有乳凝胶进行 pH 值、物理性质(稠度、均匀性、颜色、质地)、药物含量、铺展性、挤出性、溶胀指数、粘度、稳定性和离心等评价。用 Franz 扩散池和鸡蛋膜进行药物释放。
在所制备的制剂中,EG1 的释放更好,粘度更高,药物含量更高,溶胀指数更高。制剂 EG1 在 8 小时内显示出更高的药物释放(91.25%)。