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 DELIVERY OF SILYMARIN TO LIVER CELLS BY GALACTOSYLATED NANOPARTICLES: IN-VITRO & IN-VIVO EVALUATION STUDIES

Targeted delivery of drug to hepatic can be successfully achieved by binding to asialoglycoprotein receptor which is present in liver cells. For the targeting of liver cells, galactosylated chitosan nanoparticles were prepared and silymarin drug was loaded for the treatment of liver cirrhosis. The prepared galactosylated and chitosan nanoparticles were evaluated by physiochemical parameters like particles size, morphology, entrapment efficiency, zeta potential and invitro release studies. The successful formulation was subjected to invivo evaluation studies like organ drug distribution studies and Hepatoprotective activity by calculating SGOT, SGPT concentration. Based on plasma drug concentration profile, pharmacokinetics parameters like AUC, AUMC, Cmax, Tmax, t1/2, MRT & clearances were evaluated. The above results indicate galactosylated chitosan nanoparticles might be the best suitable carrier to target liver cells in treating liver cirrhosis

Therapeutic Significance of Polymeric Nano Particles as Carriers for Sustained Ocular Therapy: An Overview

ABSTRACT Effective delivery of drug to the eye poses many problems through conventional eye drops due to its poor ocular retention and bioavailability. The use of nanocarriers provides interesting opportunities for topical ocular drug delivery. The association of an active drug to nanocarriers allows the drug to closely interact with specific ocular structures, also to overcome ocular barriers and to prolong its residence in the target area. Hence delivery of a drug through nanoparticles can accomplish main benefits like enhancement of drug permeation, controlled release, and targeting. Though several non polymeric and colloidal drug delivery systems, such as Prodrugs, Polymeric micelles, liposomes, neosome, nanoemulsions, nanocrystals and nanoparticles have been largely investigated and reported to enhance ocular bioavailability of ocular drugs. Owing to the submicron size of polymeric nanoparticles they are well tolerated and have the tendency to deposit in the cul-de-sac for prolonged period. In the present review our objective is focused on the fundamental aspects of polymeric nanoparticles as carrier for ocular drugs and its therapeutic applications with special emphasis to research studies in ocular delivery of polymeric nanoparticles with anti-infectious and anti inflammatory drugs

Pharmacokinetic evaluation of newly developed isradipine sustained release formulation

A specific and efficient method using High Performance Liquid Chromatography (HPLC) has been developed to validate the pharmacokinetics of sustained-release formulation containing Isradipine. The objective of the present study is to develop and validate PK of sustained release formulation containing Isradipine. The plasma samples of Isradipine were extracted using the protein precipitation technique (PPT). The detection wavelength of Isradipine, which was 325nm, was determined using UV spectrophotometer. Reversed phase Thermos c18 column was used for separation. 10mM ammonium acetate buffer (pH 4) and acetonitrile at a ratio of 20:80% v/v was used as the mobile phase with the flow rate of 1.0 ml/min. The linearity achieved in this method was in the range of 10-120 ng/ml. HPLC method provides extremely precise results and is an excellent and efficient method compared to others. The development of a sustained release formulation offers advantages such as prolonged blood levels of the drug and improved patient compliance. The formulated sustained release tablets containing Isradipine is capable of exhibiting sustained release properties, stable and feasible for industrial scale production. Thus they are capable of reducing the dose intake, minimize the blood level oscillations, dose related adverse effects, cost and ultimately improve the patient compliance in the hypertension

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