Isradipine (ISDP) is an effective calcium channel blocker used in the treatment of hypertension. It undergoes extensive first pass metabolism and bioavailability through the oral route is only about 15 to 24%. Hence we attempted to develop a matrix type controlled transdermal drug delivery system for ISDP. Formulations A1, A2, A3 were composed of Eudragit RL100 and hydroxypropyl methyl cellulose (HPMC) in 1:3, 1:1, 3:1 ratios; A4, A5, A6 were composed of Eudragit RS100 and HPMC in 1:3, 1:1, 3:1 ratios. All six formulations carried 5 mg of ISDP/patch area, 5% v/w of D-limonene, 15 % v/w of propylene glycol in methanol:dichloromethane (1:1). The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy and differential scanning calorimetry. The results suggested no physicochemical incompatibility between the drug and the polymers. The prepared transdermal drug delivery system were evaluated for physicochemical characteristics, mainly in vitro release and ex vivo permeation. The ex vivo permeation studies were carried out across excised rat skin using Franz diffusion cell. All the formulations exhibited satisfactory physicochemical characteristics. Cumulative amount of the drug released in 36 h from the six formulations were 1695.32, 1527.89, 1455.54, 1485.65, 1282.81 and 916.88 microg/cm(2) respectively. Corresponding values for the cumulative amounts of drug permeated across the rat skin for the above matrix films were 1456.29, 1284.70, 1182.99, 1212.72, 1046.05, and 782.60 microg/cm(2) respectively. By fitting the data into zero order, first order and Higuchi models, it was concluded that drug release from matrix films followed Higuchi model and the mechanism of drug release was diffusion mediated. Based on the physical evaluation, in vitro drug release and ex vivo permeation characteristics, it was concluded that for potential therapeutic use, monolithic drug matrix films A1, may be suitable for the development of a transdermal drug delivery system of ISDP.

Nasal cavity is lined by vascularized epithelium which provides larger surface area useful for drug absorption. It has low enzymatic activity in contrast to the di-ABSTRACT The objective of this study was to develop novel intranasal microemulsion containing oxcarbazepine (OXC) for treatment of epilepsy. Optimized ratio of Tween 80: Polyethylene glycol and isopropyl myristate was selected after developing pseudoternary phase diagrams and microemulsions were prepared. The prepared microemulsions were characterized for drug content, pH, particle size, polydispersity index, zeta potential, conductivity, viscosity and in vitro release. Ex vivo permeation study for selected microemulsion was performed through sheep nasal mucosa. Further pharmacodynamic performance was evaluated in mice by electrically induced seizures. It was found that selected microemulsion was transparent with average globule size of 20.5 nm and cumulative percentage drug permeated was 95.60 %. Pharmacodynamic evaluation of selected formulation also indicated lesser intensity of seizures with low dose in mice in comparison to oral suspension of OXC. OXC intranasal delivery system is an effective alternate therapy for treatment of epilepsy.

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A series of potential bioactive compounds, 4-Amino-5-mercapto-3-(4-chlorophenyl)-1, 2, 4-triazole (1d), 4-Amino-5-mercapto-3-(4-nitrophenyl)-1, 2, 4-triazole (2d) , 4-Amino-5-mercapto-3-(2, 4-dichlorophenyl)-1, 2, 4-triazole (3d), 4-Amino-5-mercapto-3-(2-chlorophenyl)-1, 2, 4-triazole (4d), 4-Amino-5-mercapto-3-(2-methylphenyl)-1, 2, 4-triazole (5d), 4-Amino-5-mercapto-, 2, 4-triazole (6d) were synthesized according to the 1 literature methods. The synthesized compounds were characterized by FT-IR, H NMR spectroscopy, C H N analysis and anticancer activity was evaluated.Male Swiss albino mice has been used as test animal. Tumor cells used for anticancer activity were EAC (Ehrlich Ascites Carcinoma). Compounds were given at a dose of 25 mg/kg body weight intraperitoneally. groups were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition and non-viable cell count and increase in life span (%ILS). All the compounds exhibited the significant (P< 0.01) anticancer activity compared to control and the compound 4d is found to be the most potent one. The standard drug was used as 5-Fluorouracil (20mg/kg, body weight).Keywords: 1, 2, 4-triazole, anticancer activity, tumor cell count, tumor weight inhibition. 3-(4-methoxyophenyl)-1 Compounds treated (III-VIII)ABSTRACT

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