Paclitaxel delivery by micro/nano encapsulation using layer-by-layer assembly

A novel formulation of paclitaxel (PTX) has been developed by providing multilayer assembly over drug loaded porous CaCO3 microparticles (CaCO3 MP) using combination of biocompatible and biodegradable polyelectrolytes (PE’s). PTX was encapsulated into the nanopores of preformed CaCO3 MP prepared by the co-precipitation method. Infrared (IR) and X-ray diffraction (XRD) provides evidences that PTX has been encapsulated into nanopores of CaCO3 MP and not crystallized on the surface. PTX loaded CaCO3 MP (CaCO3-PTX) was found to be highly stabilized against thermal decomposition as evinced by thermo gravimetric analysis (TGA) indicating decomposition at 600°C and 250°C for CaCO3-PTX and PTX respectively. The multilayer assembly over CaCO3-PTX was effectuated by alternate deposition of protamine sulfate (PRM) and sodium alginate (SA) using LBL technique followed by subsequent core removal [PTX- (PRM/SA)5]. The pay load efficiency of PTX in this system was found to be 78.98±2.14%. The developed system was further evaluated for surface morphology, size and size distribution, surface charge, core removal and layer-by-layer growth due to sequential adsorption of PE’s. The release data of PTX-(PRM/SA)5 was comparable with marketed formulation of PTX (PTX-M) and CaCO3-PTX when performed in simulated intestinal fluid (SIF pH=7.4). The release profile of PTX-(PRM/SA)5 indicates that PEs based multilayer matrix is capable to provide barrier to PTX release as it has been found to follow first order matrix diffusion kinetics with 64±4.8% release within 24 hrs. The t50% of PTX-M, CaCO3-PTX and PTX-(PRM/SA)5 was found to be 70, 90 and 480 minutes respectively. This alternative delivery system of PTX disguised in the form of LBL assembly could have immense application for the treatment of metastasized mammary glands vis-à-vis existing formulation of PTX which is by and large criticized for having certain toxic excipients to be given parentrally. Moreover, the proposed system provides ample of opportunity to modify the surface for targeted application of PTX.
&#xa

Status of automation in special libraries and information centers of Gwalior: a survey

Paper has been published in Proceedings of the National Conference on Information Management in Digital Libraries held on 2-4 August, 2006, organized by central library, IIT Kharagpur.The study presents the status of automation in special libraries and information centers of Gwalior District in Madhya Pradesh. Aims at understanding and analyzing the various problems faced by the authorities and the staff during the process of automation. The methodology adopted for the present study is survey using a structured questionnaire. The lack of staff, hesitancy and lack of attitude towards automation and unsatisfactory library software problems are the major hindrances to speedy automation. However, 50% of special libraries opting for automation show that the libraries have a mind to adapt to the new changes and the other libraries will follow the suit.Central Librar

Extraction, Phytochemical Screening and Anti-Inflammatory Activity of Hydro-Ethanolic Extract of Roots of Dactylorhiza hatagirea

The present work showed phytochemical screening, anti-inflammatory activities and sub-acute toxicity of hydro-ethanolic extract of roots of Dactylorhiza hatagirea (D. hatagirea) and rhizomes of Curcuma angustifolia (C. angustifolia). The anti-inflammatory activity was evaluated by Carrageenan-Induced Rat Paw Edema method. Acute toxicity of the extract (2000 mg/kg) was examined in Swiss albino mice for 14 days. Qualitative analysis of various phytochemical constituents and quantitative analysis of total phenolics and flavonoids were determined by the well-known test protocol available in the literature. Quantitative analysis of phenolic and flavonoids was carried out by Folins Ciocalteau reagent method and aluminium chloride method respectively. Phytochemical analysis revealed the presence of phenols, flavonoids, tannins, saponins, alkaloids. The total phenolics content of roots of Dactylorhiza hatagirea and rhizomes of Curcuma angustifolia extract was (0.675, 0.456mg/100mg), followed by flavonoids (0.832, 1.091mg/100mg) respectively. Hydro-ethanolic extract up to 2000 mg/kg did not produce any toxic effects. The hydro-ethanolic extract of Dactylorhiza hatagirea and Curcuma angustifolia (100 and 200 mg/kg) inhibited the inflammation induced by carrageenan in rats in a dose dependent manner. After anti-inflammatory activity tablet formulation was prepared of the extract and evaluated as per IP.  The hydro-ethanolic extract of Dactylorhiza hatagirea and Curcuma angustifolia possesses a strong anti-inflammatory activity and may be considered an interesting source of effective anti-inflammatory compounds. Keywords:   Sub-acute toxicity, anti-inflammatory effect, Dactylorhiza hatagirea, Curcuma angustifolia, Herbal tablet formulatio

Characterization And Optimization Of Recombinant Gm-Csf Protein: Expression And Functional Analysis

Background: Granulocyte Macrophage Colony Stimulating Factor (GM-CSF) emerges as a key influencer, wielding its impact over haematopoiesis and immune modulation. It can address an array of intricate physiological and pathological scenarios. Objective: The present study is aimed to characterize and optimize the recombinant GM-CSF protein and to carry out its expression and functional analysis. Methods: GS115 (Pichia pastoris) strain was double digested with restriction enzymes 5’AOX1 and 3’AOX1α and ligated to the pPICZα vector. The positive clones were screened using PCR, mobility shift, Kex2 signal cleavage and restriction digestion. Further, the Pichia strain with pPICZα A was transformed into yeast cells, and its expression was studied using Spectroscopy and SDS-PAGE. In addition, the resulting Protein was purified using reverse-phase column chromatography and functional characterization was performed using a Pichia pastoris HCP kit. Results: The GM-CSF protein was successfully transformed into yeast cells, andtheSDS-PAGE profile confirmed the presence of GM-CSF in the expression system. A purified form of recombinant GM-CSF protein was obtained using HPLC, and the obtained chromatograms of both reference and test samples were comparable. Further, from the functional analysis, about9.67 ppm of the functional hematopoietic cell phosphatase (HCP) was observed in the purified GM-CSF sample. Conclusion: The Recombinant GM-CSF has been successfully prepared and confirmed for their expression and functional characteristics. The developed Protein can regulate production, cell differentiation and granulocytic functions

HPLC Method Development and Validation for the Estimation of Esomeprazole in Bulk and Pharmaceutical Dosage Form

A reversed-phase high performance liquid chromatography (RP-HPLC) method was developed and validated for the estimation of esomeprazole in bulk and tablet dosage forms. The separation was achieved on Thermo C18 analytical column (250 mm × 4.6 mm i.d., 5.0 μm) using acetonitrile and methanol in the ratio 50:50 v/v as mobile phase and at a flow rate of 1.0 ml/min. Detection was carried out using a UV detector at 300nm. The total chromatographic analysis time per sample was about 8.0min with esomeprazole eluting at retention time of about 6.863±0.3 min. The method was validated for accuracy, precision, specificity, linearity and sensitivity. Validation studies demonstrated that this HPLC method is simple, specific, rapid, reliable and reproducible. The standard curve was linear over the concentration range of 5-25μg/ml with r2 close to one (0.999). The limit of detection (LOD) and limit of quantitation (LOQ) obtained for esomeprazole were 0.100μg/ml and 0.314μg/ml respectively. The developed and validated method was successfully applied for the quantitative analysis of ESOMZ 20 Tablet. The high recovery and low relative standard deviation confirm the suitability of the proposed method for the determination of esomeprazole in tablets dosage form. Keywords: Analytical method development, Reversed phase HPLC method, ICH guidelines, Tablet dosage forms, Accuracy and precisio

Adamantinoma: A clinicopathological review and update

Adamantinoma is a primary low-grade, malignant bone tumor that is predominantly located in the mid-portion of the tibia. The etiology of the tumor is still a matter of debate. The initial symptoms of adamantinoma are often indolent and nonspecific and depend on location and extent of the disease. Histologically, classic adamantinoma is a biphasic tumor characterized by epithelial and osteofibrous components that may be intermingled with each other in various proportions and differentiating patterns. To assure the histological diagnosis, pathologists should employ immunohistochemistry for demonstrating the sometimes sparse epithelial cell nests when the radiological features are suggestive of adamantinoma. There is paucity of compiled data over adamantinoma in the literature, hence authors tried to make a comprehensive review which must be of use to beginners and trained pathologists. Our objective is to further define the clinicoradiologic features and pathologic spectra of adamantinoma

FORMULATION AND EVALUATION OF GEL CONTAINING ETHOSOMES ENTRAPPED WITH TRETINOIN

A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. One of the best options for successful drug delivery to the affected area of skin is the use of ethosomes which can be transported through the skin through channel-like structures. Tretinoin is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Drug loaded ethosomes had been prepared using phospholipid and ethanol, were optimized and characterized for entrapment efficiency, vesicular size, shape, In-vitro skin permeation, skin retention, drug‐membrane component interaction and stability. The ethosomal formulation having 0.5 %w/v of phospholipid and 20 %v/v of ethanol (F2) showing the greatest entrapment efficiency (80.25±0.23) with small particle size (205.40±2.31nm) was selected for further skin permeation studies. The skin permeation and skin retention studies were performed on ethosomal formulation, liposomal formulation (0.5 %w/v of phospholipid without alcohol), hydroethanolic drug solution and phosphate buffer saline (pH7.4) drug solution. Among them, ethosomal formulation showed higher cumulative percentage of drug permeation (93.36±0.45%) and 8 hours than the other formulations. Scanning electron microscopy confirmed the three dimensional nature of ethosomes. Dynamic light scattering technique proved that the ethosomes has smaller vesicular size than the liposomes prepared without alcohol. FT‐IR studies revealed no interaction between the drug and membrane components. The ethosomal vesicles were incorporated in carbopol gel base and its anti‐acne was compared with the marketed gel. Our results suggest that the ethosomes are an efficient carrier for dermal and transdermal delivery of tretinoin. Keywords: Tretinoin, Ethosomes, Diffusion, Carbopol gels, Transdermal delivery

Formulation Development and Evaluation of Emulgel of Clindamycin Phosphate for Effective Treatment of Acne

Emulgel have emerged as one of the most interesting topical delivery system as it has dual release control system i.e. gel and emulsion. The topical applications of the drug offers the potential advantages of delivering the drug directly to the site of action and delivering the drug for extended period of time at the effected site that mainly acts at the related regions. The major objective behind this formulation is enhancing the topical delivery of hydrophobic drug (clindamycin phosphate) by formulating clindamycin phosphate emulgel using carbopol 941 as a gelling agent. In addition, light liquid paraffin as oil, tween-20 and span-20 as emulsifiers and propylene glycol as co-surfactant were selected for preparation of emulgel. Clindamycin phosphate is an antibiotic useful for the treatment of a number of infections. It is of the lincosamide class. Clindamycin phosphate is a semi synthetic lincosamide antibiotic that has largely replaced lincomycin due to an improved side effect profile. Clindamycin inhibits bacterial protein synthesis by binding to bacterial 50S ribosomal subunits. Topical clindamycin phosphate reduces free fatty acid concentrations on the skin and suppresses the growth of Propionibacterium acnes (Corynebacterium acnes), an anaerobe found in sebaceous glands and follicles.  The prepared emulgel were evaluated for their physical appearance, pH determination, viscosity, spreadability, extrudability, in vitro drug release, anti acne activity and stability. All the prepared emulgel showed acceptable physical properties, homogeneity, consistency, spreadability, viscosity and pH value. The best formulation F4 showed better antiacne activity when compared with all formulation. Keywords: Emulgel, Clindamycin phosphate, Extrudability, Spreadability, Antiacne activit

Formulation Development and Evaluation of Sustain Release Gastroretentive Floating Tablets of Prochlorperazine Dimaleate

Floating drug delivery systems are the gastroretentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of Prochlorperazine dimaleate (PCZ) were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of PCZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of PCZ shown that the formulation F9 was found to be the best formulation as it releases 98.89% in a controlled manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. The optimized formulation (F9) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months.  Prepared floating tablets of PCZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Prochlorperazine dimaleate, Floating tablet, Gastro retentive, Total floating time

Phytochemical Screening and Evaluation of Antiulcer Activity of Hydroalcoholic Extract of Lilium Candidum Flowers

Peptic disorders like gastro esophageal reflux disease, gastritis, peptic ulcer, duodenal ulcer etc., are the common in today’s life style. This may be due to stressful life style or improper balance diet. The pathology behind these disorders may be discrepancy between offensive and defensive mechanisms either by excess secretion of acid and pepsin or diminished ability of the gastro-duodenal mucosal barrier to protect against stomach acid-pepsin secretion. Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of the most commonly used medicines and proven to be effective for certain disorders. Some people use NSAIDs on daily basis for preventive purpose. But a variety of severe side effects can be induced by NSAIDs. Studies have shown that edible natural ingredients exhibit preventive benefit of gastric ulcer. Therefore present study was designed to evaluate antiulcer activity of hydroalcoholic extract of Lilium candidum flowers in rats. Qualitative analysis of various phytochemical constituents and quantitative analysis of total phenolics and flavonoids were determined by the well-known test protocol available in the literature. The in vivo anti-ulcer activity of hydroalcoholic extract was assessed against Aspirin-induced gastric ulcer in rats. Depending on the model, outcome measures were pH of gastric fluid and ulcer index as well as percent inhibition of ulcer index. Preliminary phytochemical screening revealed the presence of flavonoids, carbohydrates, saponins, polyphenols and amino acids. The total phenolics content of L. candidum extract was (1.039mg/100mg), followed by flavonoids (0.941mg/100mg) respectively. Further hydroalcoholic extract of 100 and 200mg/kg/p.o significantly (p˂0.01) reduced the gastric pH, ulcer index in aspirin induced ulcer models in rats. The findings of this study confirmed that L. candidum extract has anti-ulcer pharmacologic activity due to one or more of the secondary metabolites present in it. Therefore, this study validates its anti-ulcer use in Indian folk medicine. Further investigations on isolation of specific phytochemicals and elucidating mechanisms of action are needed. Keywords: Lilium candidum, Phytochemical constituents, Antiulcer, Non-steroidal anti-inflammatory drugs, Aspirin-induced gastric ulcer