In this study, sulfoxyamine derivative of chitosan was carried out by reaction with thionyl chloride and further treated with ammonia. FT-IR, 1H NMR, elemental analysis and DSC methods are used for confirmation of modification. The results revealed that the modified chitosan exhibits better water solubility than chitosan. The evaluation of the applicability of sulfoxyamine modified chitosan in the treatment of dermal wound in rats was performed by induction of transcutaneous wound. The antibacterial activity was tested on Gram-negative and Gram-positive strains. It was found that the modified chitosan showed grater activity against Gram-negative stains as compared to Gram-positive strains. The superior wound healing and antibacterial activity might be due to the grafting of additional cationic group on the polymeric backbone and their ionic interaction with anionic cell wall of skin or bacteria. Modified chitosan also showed significant physical properties like mucoadhesion and film forming or coating properties. The modified chitosan forms film with good adhesion on wound which will protect the wound and also allows gas exchange. These properties are beneficial for treatment of wounds. Similar to chitosan, modified chitosan showed non-toxicity in skin irritation, oral acute toxicity and cytotoxicity.
Aims: The aim this research work is to formulate and evaluate thermoreversible gel of antifungal agent Clotrimazole for treatment of vaginal infection. Place and Duration of Study: Department of Biopharmaceutics, Government College of Pharmacy, Karad, Maharashtra, India, between June 2009 and July 2010. Methodology: Different Formulations of thermoreversible gel of antifungal agent Clotrimazole were prepared by using various concentrations of ethanol, PEG 400, sodium dodecyl sulphate, polycarbophil and pluronic F 127 and pluronic F 68. The gel formulations were subjected for evaluation on the basis of rheological behaviour, mucoadhesive behaviour, in-vitro performance. Results: The results indicate that Polymers such as polycarbophil, PEG- 400 in various concentrations to prepare formulations were found to release drug for period over 12 hrs. Without getting dislodged. The formulations have satisfactory rheological behavior and their diffusion profile is comparable to the marketed gel formulation. Significant difference was observed in the rheological behavior of formulations. Gel strength, spreadability, mucoadhesive strength of formulation B and C were desirable. Drug diffusion of formulation B and C were 95.2% release after 11 hrs 98.5% release after 11 hrs, respectively which was good as compared to marketed formulation showing drug diffusion of 102.2% after 10 hrs. Conclusion: On basis of the results we concluded that developed thermoreversible gel of Clotrimazole will be better alternative to conventional dosage form Clotrimazole & will improve patient compliance.
Recently different series of compounds have been designed that utilize the 1,5-diaryl-3-oxo-1,4-pentadinenyl pharmacophore for the development of novel cytotoxic and anticancer agents. These compounds interact with cellular thiols and thiols are not part of nucleic acids. Hence, these compounds are free from the problem of mutagenicity and carcinogenicity. The Claisen-Schmidt reaction is used for synthesizing furfurylidene analogs in a basic medium. The title compounds were prepared by reacting furfurylidenes with aryl sulfonyl, benzoyl, acroylyl, or acetyl chloride. The resulting synthesized compounds were screened for their in vitro cytotoxic properties by MTT and SRB assays against leukemic and colon cancer cell lines. Acute toxicity was determined by OECD-423 guidelines. The in vivo anticancer activities were evaluated against Ehrlich ascites carcinoma (EAC)-bearing Swiss albino mice. The MTT assay showed that compounds 2d and 3d have significant cytotoxicity against the Molt-4 human cell line as compared to the standard, 5-fluorouracil. In addition, the SRB assay indicated that the compounds 2, 2a, 2d, and 3d showed equipotent cytotoxicity against human leukemia cell lines as compared to the standard, doxorubicin. Compounds 2a and 2d showed significant anticancer activity against EAC in Swiss albino mice. This study revealed the potential of these molecules for further development as anticancer agents.
Aim: The aim this research work is to formulate and characterize Poly Sulfoxyamine Grafted Chitosan Coated contact Lens. Methodology: Poly Sulfoxyamine Grafted Chitosan was used for coating the Lens & converting it in to Antimicrobial Lenses. Poly Sulfoxyamine Grafted Chitosan was performed in the presence of pyridine and further treatment with ammonia during reaction of Thionyl chloride & chitosan. The UV light interference, visible light transmission and antimicrobial evaluation were studied. Results: The results indicate that Contact lenses prepared with Modified Poly Sulfoxyamine Grafted Chitosan absorbed some UV radiation & does not interfere with visible region. Due to the antimicrobial activity of modified Chitosan, the growth and transmission of micro organisms are reduces in coated Lens as compared to uncoated Lens. Conclusion: On basis of the results we concluded that Modified Poly Sulfoxyamine Grafted Chitosan might be used as coating material or material for making contact Lenses which will be less susceptible for microbial contamination.
INTRODUCTION 5-Fluorouracil (5-FU) is one of the most potent antimetabolites, which have been widely used in the treatment of advanced solid tumours. As an anticancer agent, because of its low efficacy and high toxicity, numerous modifications of 5-fluorouracil structure have been performed [1]. The most of currently available anticancer alkylating agent suffer from a number of significant disadvantages because of their interactions with nucleic acids [2]. In contrast, various α,βunsaturated ketones react preferentially or exclusively with thiols but not with amino or hydroxy groups present in nucleic acid [3,4]. Since thiols are not part of the nucleic acid structures, hence such conjugated enones may be having less mutagenic and carcinogenic than conventional alkylating agents [5,6]. The theory of sequential cytotoxicity state that successive chemical attack may lead to greater damage in cancer cell compared to normal cell [7]. Initially only one conjugated arylidene keto group was utilized in the molecules. However, recently the 1,5-diaryl-3-oxo-1,4-pentadienyl pharmacophore has been incorporated into various cyclic systems which permit two successive alkylations of thiols [8-10]. The pH of a number of tumours is lower than the corresponding normal cells [11]
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