In vivo evaluation of newly developed losartan potassium sustained release dosage form using healthy male Indian volunteers

Sustained release (SR) matrix tablets of losartan potassium were prepared by wet granulation using xanthene as the polymer. The studies indicated that the drug release can be modulated by varying the concentration of the polymer and the fillers. The estimation of losartan potassium from human plasma method involves simple protein precipitation techniques using nifedipine as internal standard. Chromatographic separation was carried out on a reversed phase C18 column using mixture of 0.5% triethyl amine (pH 3.5) and acetonitrile (60:40, v/v) at a flow rate of 1.0 mL/min with UV detection at 225 nm. The method was validated and found to be linear in the range of 20-300 ng/ml. An open, randomized, two-treatment, two period, single dose crossover, bioavailability study in 24 fasting, healthy, male, volunteers was conducted. Various pharmacokinetic parameters including AUC0–t, AUC0–∞, Cmax, Tmax, T1/2, and elimination rate constant (Kel) were determined from plasma concentration of both formulations. These results indicated that the analytical method was linear, precise and accurate. The sustained and efficient drug delivery system developed in the present study will maintain plasma losartan potassium levels better, which will overcome the drawbacks associated with the conventional therapy

Targeted drug delivery system:- formulation and evaluation of chitosan nanospheres containing doxorubicin hydrochloride

A chitosan molecule form self-assembled nanoparticles that can encapsulate a quantity of drugs and deliver them to a specific site. Chemical attachment of drug to chitosan throughout the functional linker has possibility to produce useful prodrugs, exhibiting biological activity at target site. In vivo residence time of the dosage form in the gastrointestinal tract and bioavailability of various drugs increases by mucoadhesive and absorption enhancement properties of chitosan. Antitumour activity of doxorubicin(DOX)-incorporated nanoparticles in vitro on DOX- resistant C6 glioma cells. Nanoparticles showed increased cytotoxicity compared to DOX alone. These results suggest that doxorubicin (DOX) was unable to penetrate into cells and did not effectively inhibit cell proliferation. In contrast, nanoparticles can penetrate into cells and effectively inhibit cell proliferation. There are 3 batches of drug loaded nanospheres in which 2.5mg,5mg and 10mg of DOX were loaded into nanospheres where the concentration of chitosan is 1%w/v. Anticancer drugs without targeting a specific site cause side effects. The objective of this research is to reduce side effects. HPLC device was used to quantitatively analyze amount of doxorubicin loaded in nanospheres. The result had showed concentration of anticancer drug loaded in nanospheres is directly proportional to the drug payload capacity until saturation point. The in vitro drug release studies was carried out for 48 hours to obtain a more precise result by carrying out this studies in a medium resembling our body environment such as pH7.4, 37ºC with analytical grade water for this studies. In vitro release of doxorubicin is of zero order kinetic. This shows that release is independent of the concentration of drug loaded in the nanospheres. Besides that, the graphs also show a sustained release manner, indicating these nanospheres formulation are suitable for targeting drug delivery system and for efficient treatment of cancerous cells

Simple and sensitive method development and validation of Econazole in human plasma by RP-HPLC

A simple and accurate method was developed for the validation of the Econazole using Fluconazole as internal standard with short time of 10 minutes .Optimization of chromatography technique was used during the preparation of this analysis.  The method carried out using reversed phase of HPLC. Chromatography using Phenomenex Luna C18 Column (250mm x 4.6mm i.d, 5µm) as the stationary phase and mobile phase of solvent A and B of 0.5% Triethylamine at pH 6.5 and Acetonitrile at pH 3.5. Wavelength was fixed at 260nm and flow rate at 0.6mL/min. Validation studies was achieved by using the fundamental parameters, including accuracy, precision, selectivity, sensitivity, linearity and range, stability studies, limit of detection (LOD) and limit of quantitation (LOQ). Retention time obtained for Econazole and Fluconazole are 7.7 minutes and 5.18 minutes. It shows recovery at 93.5% which is more precise and accurate compared to the other Econazole method. Hence, a simple and accurate method of validation of Econazole in drug free plasma was developed and validated

Simple and sensitive method development and validation of Econazole in human plasma by RP-HPLC

A simple and accurate method was developed for the validation of the Econazole using Fluconazole as internal standard with short time of 10 minutes .Optimization of chromatography technique was used during the preparation of this analysis.  The method carried out using reversed phase of HPLC. Chromatography using Phenomenex Luna C18 Column (250mm x 4.6mm i.d, 5µm) as the stationary phase and mobile phase of solvent A and B of 0.5% Triethylamine at pH 6.5 and Acetonitrile at pH 3.5. Wavelength was fixed at 260nm and flow rate at 0.6mL/min. Validation studies was achieved by using the fundamental parameters, including accuracy, precision, selectivity, sensitivity, linearity and range, stability studies, limit of detection (LOD) and limit of quantitation (LOQ). Retention time obtained for Econazole and Fluconazole are 7.7 minutes and 5.18 minutes. It shows recovery at 93.5% which is more precise and accurate compared to the other Econazole method. Hence, a simple and accurate method of validation of Econazole in drug free plasma was developed and validated

Targeted drug delivery system:- formulation and evaluation of chitosan nanospheres containing doxorubicin hydrochloride

A chitosan molecule form self-assembled nanoparticles that can encapsulate a quantity of drugs and deliver them to a specific site. Chemical attachment of drug to chitosan throughout the functional linker has possibility to produce useful prodrugs, exhibiting biological activity at target site. In vivo residence time of the dosage form in the gastrointestinal tract and bioavailability of various drugs increases by mucoadhesive and absorption enhancement properties of chitosan. Antitumour activity of doxorubicin(DOX)-incorporated nanoparticles in vitro on DOX- resistant C6 glioma cells. Nanoparticles showed increased cytotoxicity compared to DOX alone. These results suggest that doxorubicin (DOX) was unable to penetrate into cells and did not effectively inhibit cell proliferation. In contrast, nanoparticles can penetrate into cells and effectively inhibit cell proliferation. There are 3 batches of drug loaded nanospheres in which 2.5mg,5mg and 10mg of DOX were loaded into nanospheres where the concentration of chitosan is 1%w/v. Anticancer drugs without targeting a specific site cause side effects. The objective of this research is to reduce side effects. HPLC device was used to quantitatively analyze amount of doxorubicin loaded in nanospheres. The result had showed concentration of anticancer drug loaded in nanospheres is directly proportional to the drug payload capacity until saturation point. The in vitro drug release studies was carried out for 48 hours to obtain a more precise result by carrying out this studies in a medium resembling our body environment such as pH7.4, 37ºC with analytical grade water for this studies. In vitro release of doxorubicin is of zero order kinetic. This shows that release is independent of the concentration of drug loaded in the nanospheres. Besides that, the graphs also show a sustained release manner, indicating these nanospheres formulation are suitable for targeting drug delivery system and for efficient treatment of cancerous cells