International Journal of Pharmaceutical Sciences and Drug Research

90-94

Authors: D. Nagasamy Venkatesh*, K. Kalyani, K. Tulasi, V. Swetha Priyanka, Shaik Abid Ali, S. Shashi Kumar

Lipid based drug delivery systems have been examined in various studies and exhibited their potential in controlled and targeted drug delivery. Pharmacosomes, a novel vesicular drug delivery system, offering a unique advantage over liposomes and niosomes, and serve as potential alternative to these conventional vesicles. They constitute an amphiphilic phospholipid complex with drug bearing an active hydrogen atom covalently that bind to phospholipids. They provide an efficient delivery of drug required at the site of action, which ultimately reduces the drug toxicity with reduced adverse effects and also reduces the cost of therapy by imparting better biopharmaceutical properties to the drug, resulting in increases bioavailability, especially in case of poorly soluble drugs. As the system is formed by binding the drug (pharmakon) to carrier (soma), they are termed as pharmacosomes. Depending upon the chemical structure of the drug lipid complex they may exist as ultrafine vesicular, micellar and hexagonal aggregate. Drug having active hydrogen group such as carboxyl, hydroxyl group can be esterified to lipids, resulting in amphiphilic compound. Pharmacosomes are widely used as carriers for various non-steroidal anti-inflammatory drugs, proteins, cardiovascular and antineoplastic drugs. The release of drug from pharmacosomes is generally governed by the process of enzymatic reaction and acid hydrolysis. Here, in the present review paper we have discussed the potential of pharmacosomes as a controlled and targeted drug delivery system and highlighted the method of preparation and characterization.

102-108

Authors: Aliya Parveen1, Iizhar Ahmed Syed2*

The aim of the present work was to prepare and evaluate mucoadhesive microspheres of Lamivudine. Microspheres were formulated using sodium alginate (5%) with mucoadhesive polymer (Chitosan 1%) and copolymer Sodium CMC HPMC, Xanthan gum (XG) in concentration of 1% (Chitosan1% + HPMC1%) (1%) retarding agents and 10% of Calcium chloride (CaCl2), Aluminum sulphate (AlSO4) as cross linking agents by employing Ionic Gelation Technique. The particle size was characterized for by scanning electron microscopy (SEM) and drug excipients compatibility was determined by FT-IR spectroscopy. Percentage drug content, Entrapment efficiency and in-vitro dissolution studies were also carried out. Among the prepared microspheres (F8) formulation in which AlSO4 was used as cross linking agent, portray better sustained release for more than 12hrs. The dissolution profile followed the near zero order profile and Hixon-crowell as “best fit” model. SEM shows that prepared microspheres were of spherical in shape and free flowing. FT-IR results showed compatibility of Lamivudine with excipients used.

114-119

Authors: Ebere I. Okoye1*, Chinenye Edochie2, Jacob O. Adegbemi2

The study focused on the extraction and utilization of Delonix regia seed gum as a suspending agent in amoxicillin dry granules for reconstitution. The seeds were dehauled, defatted with diethyl ether and the gum extracted from its aqueous dispersion by antisolvent precipitation method. Delonix regia gum (DRG), sodium carboxymethyl cellulose (CMC) and hydroxylpropylmethyl cellulose at 0.50, 0.75 and 1.00% (with or without NaCl at 0.02% or 0.04%) were separately used to formulate amoxicillin granules. The granules were reconstituted and characterized using standard protocols for suspension dosage forms. Results revealed that at similar concentrations, products viscosities were: CMC>HPMC>DRG; and pourability: DRG>HPMC>CMC. At 1.00%, DRG gave the best product and flocculation with NaCl was better at 0.02%. The order of degree of flocculation at 1.00% suspendant and 0.02% NaCl was DRG>HPMC>CMC, while at 0.04% NaCl, it was CMC>HPMC>DRG. Ease of redispersion for DRG products was significantly better (p<0.05) than those of CMC, HPMC and two popular commercial products in Nigeria. Particles shapes and interaction with the excipients as revealed by photomicrographs illuminated some of the observed properties of the products, in that the ones whose particles were planar or acicular shaped had significantly higher (p<0.05) degree of flocculation than products containing mostly circular particles. In conclusion, the qualities of products formulated with DRG compared very well and for redispersibility is significantly better (p<0.05) than products formulated with standard suspending agents and the two popular commercial products in Nigeria markets.

124-127

Authors: Abhishek Kumar*, Jennifer Fernandes, Pankaj Kumar

A series of novel substituted 1-amino-3-(5-phenyl-4,5-dihydroisoxazol-3-yl) quinolin-2(1H)-one (AJI1-AJI8) have been synthesized upon reaction with 1-amino-3-cinnamoyl-quinolin-2(1H)-one by using hydroxylamine hydrochloride as cyclising agent in alcohol medium. The intermediate chalcones 1-amino-3-cinnamoyl-quinolin-2(1H)-one (AJC1-AJC8) were synthesized by condensing 3-acetyl-1-amino-quinolin-2-one with different substituted benzaldehyde in presence of 40% ethanolic KOH. The title compounds obtained were characterized by IR, 1H NMR, mass spectra and elemental analysis. The synthesized compounds were screened for their antimicrobial and anti-inflammatory activity.

132-136

Authors: V. S. Nade *, L. A. Kawale, P. S. Deshmukh, S. S. Zambare, Y. B. Wale

Endothelial dysfunction is associated with diabetes mellitus and hypertension. Oxidative stress and augmented activity of associated enzymes like cyclooxygenase (COX) and xanthine oxidase (XO) is a major culprit. In this study, diabetes mellitus (DM) was induced by alloxan (75 mg/kg, i.v) and hypertension was induced by left renal artery (LRA) ligation in male Wistar rats. Treatment with COX inhibitors, etoricoxib (10 mg/kg, p.o), lornoxicam (4.5 mg/kg, i.p) and XO inhibitor, allopurinol (50 mg/kg, p.o) was initiated after confirming induction of diabetes and hypertension and continued for 6 weeks. Vascular reactivity to catecholamines like adrenaline (1 µg/kg), noradrenaline (1 µg/kg), and phenylephrine (1 µg/kg), was evaluated in both models wherein treated rats expressed better responses than untreated groups. In an in vitro study, relaxant response to acetylcholine (ACh) and sodium nitroprusside (SNP) was observed on isolated aortas. Relaxation to ACh was impaired in untreated groups but treated groups produced near to normal relaxant responses. In case of SNP, no significant results were obtained. Diabetes and hypertension induced significant oxidative stress reflected by increase in lipid peroxidation level and decrease in antioxidant enzymes like catalase and superoxide dismutase. Drugs treatment reversed these effects on oxidative stress indices and ameliorated endothelial dysfunction.

140-144

Authors: Zahi Mohammad Turabi*, O’hood Atef Khatatbeh

A stability-indicating reverse phase-HPLC method has been developed and validated for the simultaneous determination of Clobetasol propionate (CLOB) and Chlorocresol (CHLOR) in pharmaceutical dosage form (cream). Beclomethasone dipropionate monohydrate (BEC) was used as internal standard. The column (Luna) C18 (250 mm × 4.6 mm, 5μm particle size) was used for chromatographic separation. The gradient elution system was performed using mobile phase A: Ammonium dihydrogen phosphate pH 4.5 and methanol in the ratio of 80:30 respectively, and Acetonitrile as mobile phase B. The flow rate was adjusted to 1.5 ml/min. The column oven was set at 25°C and the detection wavelength at 240nm. The retention times of CHLOR, CLOB and BEC were found to be 8.86 min, 13.36 min and 15.6 min respectively. The linearity was performed in the concentration ranges of 64.0-96.0μg/ml (CHLOR), 32.0-48.0μg/ml (CLOB), and 80μg/ml (BEC) with squared correlation coefficient of 0.9995 and 0.9996 for CHLOR and CLOB respectively. The percentage purity of CHLOR and CLOB was found to be > 99.5 %. The analytical method has been validated for specificity, linearity, precision, accuracy, ruggedness and robustness which were found to be within the acceptance limit according to ICH guidelines. The developed method was successfully employed for routine and stability analysis of CHLOR and CLOB in pharmaceutical cream.

154-159

Authors: Zahi Mohammad Turabi*, O’hood Atef Khatatbeh

A stability indicating, accurate, specific, linear and sensitive reverse phase-HPLC method has been developed and validated for the determination of Rosuvastatin as calcium, (ROS) in pharmaceutical dosage form. The chromatographic separation was performed using end capped (Luna) C18 Column (250 mm × 4.6 mm, 5μm particle size). Mobile phase A was prepared by mixing 3.0g/l Ammonium dihydrogen phosphate in distilled water: Methanol: Acetonitrile: Tetrahydrofuran in the ratios (400:20:100:5v/v). To 1000 ml of the resulting solution 1 ml of triethylamine was added then the pH was adjusted to 6.3 with 5% v/v orthophosphoric acid. Mobile phase B was prepared by mixing Acetonitrile: Methanol: Tetrahydrofuran in the ratios (500:50:5v/v). Other chromatographic conditions such as flow rate set at 2.0 ml/min and 30°C column temperature with the detection wavelength at 243nm. The retention times of Rosuvastatin was found to be about 16 min. The linearity was performed in the concentration range of 40.0-60.0μg/ml with a squared correlation coefficient of 0.99998. The percentage purity of ROS was found to be >99.8%. The percentage recovery was determined for ROS and was found to be 100.067%. The developed analytical method has been validated for specificity, linearity, precision, accuracy, ruggedness and robustness which were within the acceptance limit according to ICH guidelines. All the degradation products obtained by stress conditions were found to be well separated from the principal peak, which means that the ROS peaks were highly pure in all chromatograms obtained. The developed method was successfully employed for routine quality control and stability analysis of ROS in pharmaceutical dosage forms.

164-168

Authors: Nesy E A1*, Lizzy Mathew2

To evaluate the significance of Thevetia neriifolia in folk medicine for curing skin infections, an efficacy study was conducted using bacterial (Staphylococcus aureus, Streptococcus pyogenes, Nocardia asteroids, Proteus mirabilis and Pseudomonas aeruginosa) and fungal pathogens (Candida albicans and Trichophyton rubrum) that cause various dermatological disorders. For antimicrobial properties, different fractions of hot extracts of shade dried leaves were assessed by Agar well diffusion method using concentrations ranging from10 mg/50µl/well and compared with reference antibiotics Gentamicin and Fluconazole (25-50µg/well). Of these, petroleum ether fraction was almost ineffective; chloroform fraction showed better efficiency at very low dozes (0.05-0.0125 mg/well) against C. albicans (19.00±1.00) and N. asteroids (14.5±0.71), ethyl acetate fraction was sensitive at higher doses against both fungal cultures T. rubrum (17.67±0.58), C. albicans (15.33±0.58) followed by bacterial strain N. asteroids (15.67±1.52), where as methanol division inhibited colony growth moderately against all the tested organisms (10-13mm). Better DPPH free radical scavenging activity was shown by EA and MT fractions of hot extract with IC50 values 0.72 and 0.81mg/ml respectively. Similarly, cold methanol extract also acted as powerful free radical scavengers of DPPH, super oxide and nitric oxide with low IC50 Values (DPPH-0.46 mg/ml, SOD-0.91 mg/ml, NO-0.88 mg/ml). In conclusion, higher antimicrobial and antioxidant compounds in the leaf add more value to the therapeutic field in drug development for curing many cutaneous bacterial and fungal infections.

174-177

Authors: Mirza Danish Baig*, Syed Basheeruddin, Silpa. S, A. Venkateshwara Reddy

The aim of the present study was to conduct phytochemical screening, perform acute oral toxicity effect and to evaluate the anti-inflammatory effect of ethanolic extracts of leaf and stem bark of Calophyllum inophyllum on albino Wistar rats. Carrageenan induced paw edema and cotton pellet granuloma techniques were applied to determine anti-inflammatory properties of the extracts. Extracts were administered orally. Acute oral toxicity studies were conducted using the OECD guidelines 423 Annexure – 2d. The results indicate the mortality was not observed during the toxicity studies and maximum safe does was determined. The anti-inflammatory effect of the extracts showed significant dose dependent effect (200 mg/kg b.w and 400 mg/kg b.w) on both acute and chronic models of inflammation i.e., carrageenan induced paw edema and cotton pellet granuloma respectively. Additionally, Calophyllum inophyllum leaves extract showed more activity compared to Calophyllum inophyllum stem bark extract.