International Journal of Pharmaceutical Sciences and Drug Research

63-70

Authors: Jagan Mohan Kandukuri, Venkatesham Allenki*, Chandra Mohan Eaga, Vasu Keshetty, Kiran Kumar Jannu

Multiparticulates are discrete particles that make up a multiple unit system. Although pellets have been used in the pharmaceutical industry for more than four decades, with the advent of controlled release technology, that the full impact of the inherent advantages of pellets over single unit dosage forms have been realized, not only has focused on refining and optimizing existing pelletization techniques, but also focused on the development of novel approaches and procedures for manufacturing of pellets. The present review outlines the manufacturing and evaluation of pellets. The manufacturing techniques include layering, cryopelletization, freeze pelletization, extrusion spheronization and hot melt extrusion have been discussed. Characterization of pellets is discussed with reference to the particle size distribution, surface area, porosity, density, hardness, friability and tensile strength of pellets.

74-79

Authors: K.P.R. Chowdary1, K. Sree Deepthi2, Y. Srinivasa Rao2*

Mucoadhesive microcapsules of indomethacin were prepared by an emulsification-ionic gelation process employing sodium carboxy methylcellulose, methylcellulose, Carbopol and hydroxy propyl methyl cellulose along with alginate and the microcapsules were evaluated for release kinetics and ulcerogenic activity. The resulting microcapsules were discrete, free flowing, multinucleate, monolithic and spherical. Microencapsulation efficiency was 41-70 % and relatively high with alginate-sodium carboxymethylcellulose. Indomethacin release from these mucoadhesive microcapsules was found to be slow and extended over longer periods of time and depended on the composition of coat and size of the microcapsules. Drug release was diffusion controlled and followed first order kinetics. Alginate-methyl cellulose and alginate-sodium carboxymethylcellulose microcapsules were found suitable for oral controlled release. The microcapsules exhibited good mucoadhesive property in the in vitro wash-off test. Release from some microcapsules fulfilled the official (USP 23) drug release test-2 requirement of indomethacin extended release capsules. A 62-80 % reduction in ulcerogenic activity was observed with these microcapsules when compared to pure drug indomethacin.

83-84

Authors: Dinesh Kaushik1, Satish Sardana1, D. N. Mishra2*

The present investigation was aimed to develop a new formulation containing chemically cross-linked guar gum microspheres loaded with 5-fluorouracil for targeting of colorectal cancer. The emulsification polymerization method involving the dispersion of aqueous phase of guar gum in castor oil was used to prepare spherical microspheres. Cytotoxicity analysis on HT-29 human colon cancer cell lines indicated that 5-FU loaded guar gum microspheres leads to sustained releases of drug and thus delayed apoptosis over a long period of time. In this way, 5-fluorouracil loaded guar gum microspheres have shown promising results in the management of colorectal cancer, warranting thorough in vivo study for scale up technology.

91-99

Authors: Nandy B. C.a,b*, Gupta R. N.a, Rai V. K.b, Das S.c, Tyagi L. K.d, Roy S.e, Meena K. C.b

In the present investigation, we prepared Atenolol (1.5 % w/w) solution and various polymer formulations by incorporating the tween-20 or L-menthol, as a penetration enhancers and its effect on permeation of the drug through the excised abdominal rat skin were used to examined by using the vertical Franz-type diffusion cell. The physicochemical interactions between Atenolol and various polymers were investigated by performing the assay, ultra violet absorption maxima, Fourier transform infrared spectroscopy and it was further confirmed by thin layer chromatography studies, from which drug did not show any evidence of interaction with the polymers. We found that, L-menthol was superior than tween-20 to iontophoresis [current density applied 0.5 mA/cm2 and 90:10 (on: off) ratio], in enhancing the transdermal permeation of Atenolol; it enhanced the flux of Atenolol by more than 2-folds, comparison to the preparations without penetration enhancer via passive diffusion, and 3 folds increased using iontophoresis alone with a shorter lag time. Atenolol also showed good stability in gel formulations. The basic parameters like % loading dose released at the end of the study, permeation coefficient and steady state flux (Jss) were calculated and showed statistically significant difference (p<0.05). The results indicated that suitable iontophoretic delivery with desired permeability could be appeared and the cumulative amount-time curves were suitable to fit by a zero order equations which indicated a steady state permeation rate or sustained effect could be achieved from hydrogel; when it is combined with penetration enhancer, L-menthol. The results demonstrate that the semisolid gel formulations are more applicable than solution as a transdermal iontophoretic delivery system to administer clinically. Electrically assisted transdermal delivery of Atenolol significantly increased transport compared to passive delivery. Also, rapid and modulated delivery was shown to be feasible by programming the electrical parameters.

103-106

Authors: R. K. Gupta1*, U. K. Singh2, S. Kumar2, B. Moothan3

A simple, precise and reproducible reverse phase, isocratic high performance liquid chromatographic method was developed and validated for the quantitative determination of sodium valproate in bulk and enteric coated tablet dosage form. The quantification was carried out using a Nova-pack phenyl, 4µm, 150 mm × 3.9 mm i.d. column, with a mobile phase consisting of acetonitrile: buffer (30:70, v/v) (pH 2.5) at a flow rate of 1.2 ml/min and UV detection at 210 nm. The method was validated for specificity, linearity, accuracy, precision, limit of detection, limit of quantification, robustness and solution stability. The linearity of the proposed method was investigated in the range of 50-1500 µg/ml (r = 0.9999). Mean inter- and intra-assay relative standard deviations (RSD) were less than 2.0 %. The proposed method was successfully applied for the analysis of sodium valproate in bulk and pharmaceutical dosage forms. Also, the method was extended for determination of sodium valproate release from in-vitro dissolution studies.

110-112

Authors: Guno Sindhu Chakraborthy*, Vidhu Aeri1

Extracts of leaves and stems of Chlorophytum borivilianum were subjected to preliminary phytochemical screening and in-vitro antimicrobial studies. The results of the preliminary investigation revealed the presence of alkaloids, glycosides, steroidal nucleus, saponins and tannins in both parts. The methanolic extract of leaf and stems part were investigated for antimicrobial activity using agar disc diffusion method. Six clinical strains of human pathogenic microorganisms, comprising 3 Gram +ve, 1 Gram -ve and 2 fungi were utilized in the studies. The leaf extract of Chlorophytum borivilianum displayed overwhelming concentration dependent antimicrobial properties, inhibiting the growth of Staphylococcus aureus and Bacillus cereus, far above that of ampicillin used in a concentration of 1.0 g/ml. The extract was less sensitive to 2 Gram -ve bacteria in the assay. In antifungal assay, the growth of Aspergillus niger and Candida albicans, were inhibited in the same manner comparable to voriconazole the reference drug used in the study. The methanol extract of stem also displayed a concentration related antibacterial activity, inhibiting the growth of S. aureus comparable to ampicillin at 1.0 g/ml. The extract was least active against Escherichia coli with a mild activity at 1.0 g/ml. The extract exhibited weak activities against C. albicans as well as A. niger. Both plant parts seem to justify their ethno medical uses.

116-118

Authors: Akanksha D1*, Vikas G1, Neetesh K. J1, Shailendra S2, Neelam B1, Dinesh K. J1

Present investigation was to develop novel ointment formulation in combination of natural wound healing agent curcuma longa, which is reported to possess wound healing and anti-bacterial activities. Combination of neomycin sulphate and curcuma longa is good rational, where curcuma longa produces synergistic wound healing effect with neomycin sulphate. Formulations containing fixed concentration (0.5 %) of neomycin sulphate and 3 %, 4 % and 5 % of curcuma longa were prepared. To assess the efficacy of formulations anti-bacterial activity, rheology, stability, spreadability and other physical characteristics were evaluated. The results obtained were encouraging and formulation containing neomycin sulphate (0.5 %) with 5 % of curcuma longa was found better than other formulations.

121-123

Authors: Guno Sindhu Chakraborthy*

Plants are the best source of active secondary metabolites which are beneficial to mankind. Many plant origin drugs have been reported with biological properties like Analgesic, Anti-inflammatory, Antioxidant, hypoglycemic agents and many more. The successive extracts of Aesculus indica leaves were screened for in vitro antioxidant properties using the standard procedures. The successive extracts such as petroleum ether, ethyl acetate, methanol and water and 50% crude methanol extracts exhibited IC 50 values of respectively in DPPH and respectively in nitric oxide radical inhibition assays. The values are comparable with the standards such as ascorbic acid and quercetin. The Aesculus indica leaves are showing significant antioxidant activity.