Background: Wound occurs when integrity of the skin is compromised. Healing of wounds occur in various phases namely hemostasis, inflammation, proliferation, granulation, contracture remodelling. Neolamarckia cadamba leaves had been used by the tribal people for the treatment of wounds. Objectives: To formulate a gel of Neolamarckia cadamba which contains carbopol 934 as a gelling agent and to determine its wound healing activity by topical application of gel of Neolamarckia cadamba on surgically induced wounds in Swiss albino mice. Materials and Methods: To study the wound healing properties, free radical scavenging activity by DPPH, nitric oxide, total phenolic content estimation, antibacterial activity, excision and incision studies and histopathology were done. Ethyl acetate fraction of methanolic leaves extract of Neolamarckia cadamba (EAFNC) was applied topically as a 2% gel. Percentage of wound contraction and tensile strength was determined in excision and incision wound model respectively. Results: The animals treated with EAFNC showed significant percentage inhibition of nitric oxide and DPPH as compared to ascorbic acid. Antibacterial activity of EAFNC against Bacillus subtilis and Pseudomonas aeruginosa was also seen. Also, there was increase in wound contraction on 12 th post wounding day (81.33 ± 0.574), tensile strength (4.645 ± 0.1345). Histopathology of regenerated skin of EAFNC showed prominent collagen networks, mononuclear cells and fibroblasts. Conclusion: The ethyl acetate fraction of methanolic leaves extract of Neolamarckia cadamba (EAFNC) showed significant increase in wound healing activity validating its use by the tribal people.
Kumar et al.: Synthesis and Evaluation of Aceclofenac-Urea CocrystalsAceclofenac is one of the commonly used Nonsteroidal anti-inflammatory drugs representing the variety of therapeutic applications including management of pain, inflammation, rheumatoid arthritis, and osteoarthritis, etc. But very low solubility and dissolution rate of aceclofenac compromise its therapeutic effectiveness. So, current work focuses on the improvement of solubility and dissolution of aceclofenac by the cocrystal approach. Aceclofenac was screened with various coformers selected from Generally Recognized as Safe and Everything Added to Foods in the United States list using Molecular orbital package 2016 software to find out novel cocrystals of aceclofenac with improved biopharmaceutical properties. Novel cocrystals of aceclofenac with urea were synthesized by mechanochemical grinding method. The synthesized cocrystals (Aceclofenac-Urea neat grinding and Aceclofenac-Urea liquid assisted grinding) were characterized carefully by Differential scanning calorimetry, infrared spectroscopy and powder X-ray diffraction to verify the formation of the cocrystals. Pharmaceutically significant properties such as powder dissolution rate, solubility, and stability of the synthesized cocrystals were evaluated. Compared to aceclofenac, the synthesized cocrystals showed improved solubility and dissolution rate. The synthesized cocrystals were found to be non-hygroscopic and stable under ambient conditions.
Aim: Present research work focuses on the improvement of biopharmaceutical properties of aceclofenac (ACF) by the cocrystal approach.\ Background: ACF is one of the frequently used Nonsteroidal Anti-Inflammatory Drug (NSAID). ACF is a BCS Class - II drug (low solubility and high permeability) with poor solubility and low oral bioavailability. Hence, the improvement in solubility and bioavailability of ACF is very crucial for successful product development. Now a day’s pharmaceutical cocrystals are considered a novel solid form of drugs. These cocrystals may have different physicochemical as well as biopharmaceutical properties as compared to the parent drug. In a previous study, the cocrystal of ACF (ACF-l-CYS NG and ACF-UREA NG) were successfully prepared and characterized. These cocrystals have shown superior solubility and dissolution rate than pure ACF in HCl buffer (pH 1.2). The synthesized cocrystals were also found non-hygroscopic and stable for 6 months under standard test settings. However pharmacokinetic evaluation of these cocrystals have not been explored yet. Objective: The specific objective of this research work was the measurement of bioavailability and other pharmacokinetic parameters of ACF cocrystals prepared by the mechanochemical grinding method. Methods: Cocrystals of ACF with l-cystine and urea were prepared by neat grinding (NG) method and in-vivo oral bioavailability of prepared cocrystals was measured in Wistar rats. The plasma drug concentration was measured by high-performance liquid chromatography (HPLC) and the pharmacokinetic data was analyzed by “PK solver” software. Results : Percent relative bioavailability of ACF-l-CYS NG and ACF-UREA NG cocrystals in Wistar rats was found to be 242.05 ± 65.27and 178.93 ± 45.21 respectively, which were significantly higher (ANOVA, P < 0.05) than that of pure ACF. Conclusion: The present study indicates that the enhanced aqueous solubility of the prepared cocrystals leads to enhanced oral bioavailability of ACF. Thus, the cocrystals may be an alternative crystalline form of the drug that can enhance the solubility, dissolution rate, and oral bioavailability of many poorly soluble drugs.
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