Posted by admin on Jul 31, 2019 in |
Objective: The Failure in chemotherapy is mainly because of the resistance of the chemotherapeutic drugs towards the neoplastic cells. The main reason behind this study was to develop a novel combination of 5-Fluorouracil (5-FU) lipid curcumin conjugates for the treatment of cancer. Methods: In this study, the lipid group stearic acid and oleic acid was conjugated with the parent drug moiety 5-Fluorouracil to acquire lipophilicity. The next step involves the conjugation of curcumin with 5-Fluorouracil lipid to form a lipid dual drug conjugate. The characterization of conjugates followed the synthesis part by using FT-IR, DSC, and LCMS. The conjugates hence obtained were further carried for formulation aspect. After the successful completion of the formulation part, in-vitro studies and MTT Assay was performed. Results: The results depict the successful synthesis of the conjugates, and its characterization was successfully done. The conjugates are formulated into Self Nanomulsifying drug delivery system (SNEDDS). The results obtained from the MTT assay also shown a significant cytotoxic effect in both the conjugation. Conclusion: The in-vitro...
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Posted by admin on Jul 31, 2019 in |
Degradation studies are important to know the potentials degradation products and to develop a stability indicating method. Ranolazine active pharmaceutical ingredients subjected to in detailed forced degradation study using several stressing agents (HCl, NaOH, H2O2). Degradation products of Ranolazine under hydrolytic and oxidative stress conditions were identified, and their stabilities were assessed. Three degradation products were formed when the drug was subjected to acid stress and two products were formed in oxidative stress condition. Ranolazine was stable to base hydrolysis. The degradants were separated on a C-8 column employing preparative HPLC using gradient elution. The structures of all the five degradation products (DP-1, DP-2, DP-3, DP-OX1, and DP-OX2) were established by extensive 1D (1H, 13C) and 2D (COSY, HSQC and HMBC) NMR spectroscopic studies and mass spectra. The products were identified as 2-(4-(2-hydroxy-3-(2-hydroxyphenoxy) propyl) piperazine-1-yl) acetic acid (DP-1), 2-(4-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine-1-yl) acetic acid (DP-2), N-(2,6-dimethylphenyl)-2 -(4-(2-hydroxy-3 (2-hydroxyphenoxy) propyl) piperazine-1-yl) acetamide (DP-3), 1-(2-((2,6-dimethylphenyl)amino)-2oxoethyl)-4-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine 1, 4-dioxide (DP-OX1), 4-(2-((2, 6 dimethyl phenyl) amino)-2-oxoethyl)-1-(2-hydroxy-3-(2-methoxy phenoxy) propyl) piperazine 1-oxide (DP-OX2)....
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Posted by admin on Jul 31, 2019 in |
A novel synthesis of N-(2, 4′-dioxo-1, 2-dihydro-3′H-spiro [indole-3, 2′-[1, 3] thiazolidin]-3′-yl)-2 -hydroxybenzamide derivatives were synthesized by cyclization of isatin hydrazones with thioglycolic acid. The synthesized compounds were characterized by spectral data (IR, 1H-NMR, Mass) and evaluated for antibacterial activity against various strains of bacteria at the concentrations of 200 µg/ml. Among the tested compounds X(i) is highly active against E. coli, X(f) is active against B. subtilis, X(h) is active against S. aureus and X(c) is active against S....
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Posted by admin on Jul 31, 2019 in |
Garcinia mangostana L. pericarp (GMP) has been known as a traditional medicine in Asian countries. The bioactive from GMP has been recognized to be related to complex phenolic compounds linked with free radical scavenging activity. This research aimed to study the effects of topical formulation types (gel, oil in water cream and water in oil cream) of GMP extract on the in-vitro release and in-vitro shed snake skin penetration. The formulations were evaluated for viscosity and pH. The extent of GMP extracts released and penetrated shed snake skin were evaluated based on stable radical 2, 2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and expressed by Radical Scavenging activity equivalent GMP Extract concentration (RSGMPE). Mangostin skin penetration was quantified using UV spectrophotometric method. GMP extract exhibited significantly higher DPPH scavenging activity compared to α-mangostin which is known as the major constituent in the GMP extract. RSGMPE released and penetrated through the skin was significantly influenced by the type of formulations. GMP extract loaded gel provided highest RSGMPE amount transported through the skin than...
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Posted by admin on Jul 31, 2019 in |
One of the major problems faced by the pharmaceutical industry is to maintain the quality and efficacy of herbal drugs due to the lack of purity of herbal raw materials. Furthermore, using traditional identification methods to identify the correct plant part needed for the preparation of herbal medicine can be difficult. Creating a novel system to assess the quality of a medicinal herb and to discriminate adulterants from authentic raw material is essential. There is a lot of confusion regarding nomenclature and originality of Valerian available in the market. The objective of the present work is to develop a molecular tool for accurate identification of dry root samples. The isolation of DNA is the first step in developing this technology. The methods employed for extracting DNA from fresh and dried root samples of medicinal plants, however, are time-consuming and yield DNA in lesser quantity and low purity due to the presence of high levels of polysaccharides, phenolics and other secondary metabolites in these samples. In this study, an easy...
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