Journal of Pharmaceutical Technology, Research and Management
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Synthesis,Characterization and Biological studies on Mannich Bases of 2-Substituted Benzimidazole Derivatives
Get PDFIn the present study novel derivatives of 2-substituted benzimidazoles were prepared via Mannich reaction and evaluated for their in vitro antimicrobial activity against two gram negative strains (Escherichia coli and Pseudomonas aeruginosa), two gram positive strains (Bacillus subtilis and Staphylococcus aureus) and fungal strains (Candida albicans and Aspergillus niger).The synthesized compounds were also screened for antioxidant activity.The newly synthesized compounds were characterized by spectral and analytical techniques.The results revealed that all the synthesized compounds have a significant antioxidant and biological activity against the tested microorganisms
Development, physicochemical characterization and in-vitro evaluation of herbal sunscreen lotion
Get PDFUltraviolet radiations have shorter wavelengths and can reach earth’s surface through penetrating clouds. UV-A rays leads to aging while UV-B rays causes burning of skin. Sunscreens protect the skin from harmful effects of sun including appearance of erythema, premature photo-ageing and facilitate to diminish the manifestation of facial red veins and blotchiness. In this investigation, herbal sunscreen was prepared using Shea butter, almond oil, raspberry oil, jojoba oil, zinc oxide and titanium dioxide as active ingredients. Fabricated lotions were evaluated for physicochemical parameters i.e. color, pH, viscosity and spreadability. Sun protection efficacy of lotion was determined in term of sun protection factor (SPF) by in-vitro spectrophotometric method. Total 10 formulations were made with different compositions F1-F10. The pH of formulations ranges from 6.10 (F6) to 8.34 (F5). The viscosity of formulations ranges from 1500 (F1) to 3586 (F10). The spreadability of formulations ranges from 10.56±0.8 (F1) to 30.65±0.7 (F10). The physicochemical parameters of formulation F6 and F10 were found to be in controlled range justifying its compatibility with skin and confirming good cosmetological property. Stability study of optimized lotion was performed after storage of formulation at 25°C and 60 % RH as well as 40°C and 75 % RH for three months. Stability of lotion was evaluated on the basis of changes in physicochemical parameters i.e. color, pH, viscosity and spreadability and SPF. F10 has SPF value of 15.71±0.07 (medium protection sunscreen). The optimized formulations might provide good moisturizer, emollient, anti-ageing and anti-wrinkle effect with good sun protection
Formulation and Evaluation of Moxifloxacin Hydrochloride Niosomes for Controlled Ophthalmic Drug Delivery
Get PDFThe objective of present invesigation was to formulate and evaluate a niosomal delivery system of moxifloxacin hydrchloride for the treatment of ocular infections. Moxifloxacin-loaded niosomes were prepared by using thin film hydration technique and were investigated for surface pH, morphology, entrapment, in-vitro release, TEeM (transmission electron microscopy), physical stability & ocular irritancy test. The release study profile was subjected to release kinetics models. Aall the vesicles were uniform and spherical in size. The drug relaese pattern of all formulation follows decreasing order: MN3 > MN6 > MN9 > MN5 > MN2 > MN1 > MN8 > MN4 > MN7. The formulation MN3 (span 60: cholesterol) molar ratio produce faster release of drug i.e. 77.98% after 12 hours, concluded less sustained action. The study concluded that the moxifloxacin loaded niosomes to be effective in sustaining the drug release leading to decreased side effects and increased patient complianc
Antiamnesic Activity of Extracts and Fraction of Desmodium Gangeticum
Get PDFDesmodium gangeticum D.C. (Salpani; family – Papilionaceae) has been traditionally used in the treatment of various ailments especially in dementia. Thus, it was planned to screen antiamnesic activity of D. gangeticum to validate its traditional claims. Properly identified powdered plant material was extracted successively using solvents in increasing order of polarity viz., n-hexane, chloroform, methanol and water. All the extracts were administered at the doses of 200 or 400 mg/kg, p.o. for six successive days to mice. The antiamnesic activity of crude extracts was evaluated against scopolamine (0.6 mg/kg, i.p.) induced amnesia using well established exteroceptive behavioural model, i.e., elevated plus maze (EPM). The efficacy of test drugs was statistically compared with the standard memory enhancing drug, piracetam (100 mg/kg, p.o.). A standardized procedure was adopted to prepare alkaloidal fraction from D. gangeticum roots, which was also evaluated for antiamnesic activity at the doses of 25 or 50 mg/kg, p.o. The chloroform extract and alkaloidal fraction of the plant significantly reversed the amnesia induced by the scopolamine at the dose of 400 and 50 mg/kg, respectively, with respect to control. The antiamnesic activity shown by the chloroform extract and alkaloidal fraction of the plant was statistically equivalent to the standard drug. It is concluded that alkaloids are responsible for antiamnesic activity of D. gangeticum roots
A Review on Role of Advanced Glycation End products (AGEs) in Rheumatoid Arthritis
Get PDFRheumatoid arthritis (RAa) is a systemic inflammatory connective tissue disease with polyarthritis as a prominent feature; however, extra-articular symptoms and signs are always present. Aadvanced glycation end products with ability of cross-linking of proteins characteristic fluorescence and reaction with AaGEe-specific receptor RAaGEe (receptor for AaGEes). AaGEes action as well as AaGEe formation is directly related to both to inflammation and oxidative stress. RAaGEe is a 35-kDa polypeptide whose gene is located at the junction of the class II and III HLAla regions on chromosome. ligation of RAaGEe has been shown to activate p21ras and mitogen-activated protein (MAaP) kinase, and stimulate nuclear translocation of the transcription factor NF-κB, thereby, resulting in the transcription of target genes thus may induce chronic cellular activation and tissue damage
Evaluation of Antioxidant and Anti-Inflammatory Activities of Justicia neesii Ramam Whole Plant Extract
Get PDFThe plant Justicia neesii is rich in polyphenolic compounds like lignans which can exhibit anti-inflammatory properties. In this study ethanolic extracts of Justicia neesii was screened for elucidating its antioxidant potential using various methods. In all the methods it has shown good antioxidant nature and reducing ability. The IC50 values against DPPH, H2O2, NO and lipid peroxidases were found to be 55.72μg/mL, 133.35μg/mL, 29.65μg/mL and 271.02μg/mL respectively. The total phenolic content in the ethanolic extract was found to be 99.8mg per gram dry plant in gallic acid equivalents. The anti-inflammatory nature of Justicia neesii was tested using carrageenan induced paw edema model in rats. The extract has shown significant inhibition of paw volume at all the three gradient doses of the extract. The percent inhibition of paw volume is correlating with the standard diclofinac sodium. From this study we concluded that Justicia neesii is a plant with potent anti-inflammatory molecules
Synthesis, antimicrobial evaluation and QSAR studies of p-amino benzoic acid derivatives
Get PDFA series of Schiff bases (1-16) and esters (17-27) of p-amino benzoic acid (PABA) was synthesized and its in vitro antimicrobial potential was evaluated by using tube dilution method. Compound 11 was found to be most promising antibacterial agent (pMICbs = 2.11 μM/ml) having antibacterial potential comparable to standard drug norfloxacin (pMICbs = 2.61 μM/ml) and may be taken as a lead compound for the development of novel antibacterial agents. QSAR analysis indicated that electronic parameters, total energy (Te) and energy of lowest unoccupied molecular orbital (LUMO) were found dominant in explaining the antimicrobial activity of synthesized compounds
Sustained Release Solid Dispersions of Pentoxyfylline: Formulation and Optimization
Get PDFObjective: The purpose of the study is to formulate and optimize sustained release solid dispersions of pentoxyfylline using a combination of eudragit polymers and ethyl cellulose. Methods: Solid dispersions were formulated by solvent evaporation method.Preliminary batches were formulated using various drug to polymer ratio; with eudragit S100 and L100 (1:1 to 1:5 ratio), and with ethyl cellulose(1:1 to 1:3 ratio) and evaluated for solubility analysis. Based on results of preliminary batches, Box Behnken design was further applied and three factors (X1- concentration of Eudragit S100, X2- concentration of Eudragit L100, X3- concentration of Ethyl Cellulose) were selected with three levels (+1, 0, -1). Multiple linear regression was applied to generate polynomial equations and statistical evaluation. Prepared solid dispersions were investigated for sustained release properties via in vitro dissolution studies. Fourier transform infrared spectroscopic analysis (FTIR), X-ray diffraction analysis (X-RD), Differential scanning calorimetry (DSC) studies were carried out to evaluate drug polymer interactions. Scanning Electron Microscopy (SEM) analysis of optimized solid dispersion was carried out to evaluate surface morphology of the particles. Results: Batch F5 showed maximum sustained release (65.46% in 24 h) characteristics out of all solid dispersions. DSC studies indicated drug integrity when mixed with the polymeric carriers. FTIR and X-RD studies also ruled out any drug polymer interaction. A change in crystalline habit was observed in solid dispersion particles (F5 batch) as seen in SEM micrographs. Polynomial mathematical model generated using multiple regression analysis was found to be statistically significant (p<0.05). Conclusion: Release retarding effect was found to be dependent on polymer concentration. Therefore, an optimized combination may lead to better sustaining effect
Development And Characterization of Inhaled Chitosan Nanoparticles Loaded with Isoniazid
Get PDFThe objective of our study is to load first line anti-tubercular drug, Isoniazid in chitosan Nanoparticles in order to enhance bioavailability and to reduce dose frequency. The chitosan nanoparticles containing the drug Isoniazid were prepared by the method of spontaneous emulsification. Chitosan gel containing drug is cross linked with Glutaraldehyde and nanoparticle suspension obtained was centrifuged at 5000 rpm. It was then evaluated for Drug loading, swelling index, Mucoadhesive force, Zeta potential, DLS studies, DSC studies, SEM studies, In vitro Drug release, Pharmacokinetic Studies and Stability studies.Formulation 1(F1) shows maximum Drug Loading, Swelling index and mucoadhesive force. The positive zeta value was obtained for all formulations due to positive charge of polymer used in preparation of dispersion. The DLS plot of Formulations shows that Average particle diameter are in the range of 661.8-823.8nm. The SEM study revealed that the micrographs of cross linked chitosan nanoparticles have smooth surface. The thermogram of the formulations showed the shifting of endotherm. This indicates the possible change in the release kinetics and bioavailability of the drug. In vitro drug releases was found to be maximum for formulation F6. Pharmacokinetic evaluation shows all the formulation shows first order rate release profile and release mechanism from nanoparticles is diffusion controlled. Stability studies indicated that the developed chitosan nanoparticles are physically and chemically stable and retain their pharmaceutical properties at various environmental conditions over a period of 3 months
Preparation and Evaluation of Chitosan and PLGA Based Implants for the Delivery of Cefotaxime
Get PDFThe poor bioavailability of cefotaxime and limitation of conventional system limits the delivery of antibacterial drug cefotaxime for bone infection treatment. In the current study in situ chitosan implant containing cefotaxime was developed. Injectable implantable drug delivery system containing Cefotaxime was prepared by physically mixing β-glycerophosphate with chitosan in different concentrations. The objective of this study was to standardize the concentrations of the ingredients so as to develop formulation that remains liquid when stored at 4ºC but forms a gel, in minimum time, when injected or when its temperature is raised to 37oC. Injectable in-situ implant before injection was clear and transparent. Gelation temperature significantly increase from 32.6°C ±0.1 to 48.43°C ±0.1 of all formulation. Percentage drug content of all formulation were found in the range of 82.42±1.93 to 99.43±0.55. The syringeability of the final solutions greatly decreased with the increase of chitosan concentration. The release pattern for all formulations was biphasic, comprising an initial burst effect followed by an almost sustained continuous phase. After an initial burst release, the drug entrapped into the chitosan/Gp gel was released slowly. Local delivery of chemotherapeutic agent by controlled- release polymers is a new strategy with the potential to maximize the antibacterial effect of a drug to treat bone infection. The system formulated with cefotaxime was found to be stable and the release profiles of a formulation with chitosan and beta-GP showed almost Higuchi equation release kinetics. The drug release of chitosan imlant containing cefotaxime was found to be more as compare to PLGA implant