Volume 6

July-September 2014

Review Articles

Upadhyayasupriya, Chauhanbisht Seema, Kothiyal Preeti

Human skin offer ideal and multiple sites to administer therapeutic agent for both local and systemic action. Emulgel is one such emerging topical drug delivery system that incorporates properties of both gel and emulsion and shows dual release control system. The main objective behind emulgel is delivery of hydrophobic drug via skin so that a hydrophobic moiety can enjoy the unique properties of gels. Most of the hydrophobic drugs cannot be incorporated directly into gel base because solubility act as a barrier and problem arises during the release of the drug. Emulgel helps in the incorporation of hydrophobic drugs into the oil phase and then oily globules are dispersed in aqueous phase resulting in o/w emulsion which can be mixed into gel base. Emulgels provide better stability, better loading capacity and controlled release of drug with short half life.

Keywords: Emulgel, Hydrophobic Drugs, Topical Delivery.

Hussain Hamid, Juyal Divya, Dhyani Archana

Microsponge and Nanosponge delivery System was originally developed for topical delivery of drugs can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Microsponge delivery system (MDS) can entrap wide range of drugs and then release them onto the skin over a time by diffusion mechanism to the skin. It is a unique technology for the controlled release of topical agents and consists of nano or micro porous beads loaded with active agent and also use for oral delivery of drugs using bioerodible polymers.

Keywords: Microsponge Drelivery System (MDS), Nanosponge, Bioerodible.

Neha Bisht, Laxmi Goswami, Preeti Kothiyal

In-situ forming polymeric gelling systems has become prominent among novel drug delivery system (NDDS) in recent years due to advantages such as sustained and prolonged drug action, improved patient compliance and reduced frequency of administration of the drug in comparison to conventional drug delivery system (DDS). This is a type of mucoadhesive DDS where the polymeric formulation is in sol form before administration and once comes in contact with body fluids; it undergoes gelation to form a gel. The formulation of gel depends upon factors like temperature modulation, pH changes, presence of ions and ultraviolet irradiation from which drug gets released in sustained and controlled manner. Conventional formulation for the treatment of dental diseases has certain drawbacks. A new concept of in situ gel was developed to overcome the shortcoming of conventional formulation which deals with dental diseases. Conventional oral formulations like solution, suspension, and ointments have many disadvantages which result into poor bioavailability of drug in the buccal cavity. In-situ forming polymeric formulation drug delivery systems is in sol form before administration in the body, but once administered, undergoes gelation in-situ to form a gel.

Keywords: In-Situ Dental Gel, Periodental Diseases, Gingivitis, Periodontitis.

Bhatt Akanksha, Kumar Ganesh, Kothiyal Preeti

Targeted drug delivery through macrophages is an attractive and modified technique to improve therapeutic efficacy for various infection, viral and inflammatory disease and macrophages are the differentiating cell having precursor monocytes, promocytes and monoblast. In liver 80-90% of total body macrophages are present RES and kupffer cells are the site of macrophages in liver where they present and RES having the sugar receptor highly phagocytosed and important for determination of foreign particles, macrophages having self defense mechanism. Other techniques are receptor mediated targeting, negatively charged drug delivery Opsonization means the process by which a particular antigen are rendered more susceptible to phagocytosed. Opsonic material are used to enhance the extent of phagocytosis. Mannose binding lectins coat the microbes as opsonins and enhance neutrophil reactivity against them. RES, phagocytosis membrane having negative charge in it and so as its target, which make it difficult to come closer. So at the time of evaluation one must check the negative charged of target by zeta potential.

Keywords: Liver Macrophages, Kupffer Cells, RES, Opsonization.

Kanika Bahuguna, Ganarajan, Preeti Kothiyal

Among the other route of drug administration, the oral cavity is an attractive site for the drug delivery of the drugs. However, disadvantages such as hepatic first pass metabolism and enzymatic degradation within the GI tract limits its use for certain drugs. Buccal drug delivery involves the administration of drug through buccal mucosal (the lining in the oral cavity). By the buccal route the drug are directly pass through into systemic circulation, less hepatic metabolism and high bioavailability. The buccal mucosa is very suitable for a bioadhesion system because of a smooth and relatively immobile surface and accessibility. The oral cavity is easily accessible for self medication and can be promptly terminated in case of toxicity just by removing the dosage form from buccal cavity. This drug delivery system utilizes the property of larger surface area and rich blood supply. Certain water soluble polymer become adhesive on hydration and hence can be used for targeting a particular site. Buccal drug delivery prolongs the residence time of dosage form at the site and thus improved the therapeutic performance of drug. This drug delivery also called mucoadhesive drug delivery. It shows better stability, patient compliance, and uniform and sustained drug release. Buccal dosage forms are meant to be placed between gingival and cheek. Buccal adhesive dosage forms are those dosage forms which can deliver drugs either locally to treat conditions within the buccal cavity or systemically via the mucosa

Keywords: Buccal Drug Delivery, Bioadhesion.

Swarnali Das Paul, Divya Dewangan

This paper provides an insight of some of the growing number of nano-applications being researched and commercialized in nutraceuticals. Recently Nanotechnology, has a number of applications in dairy and food processing, preservation, packaging and development of functional foods. Several critical challenges, including discovering of beneficial compounds, establishing optimal intake levels, developing adequate food delivering matrix and product formulation including the safety of the products need to be addressed. And also the potential negative effects of nanotechnology- based delivery systems on human health need to be considered.

Keywords: Nanotechnology, Neutraceuticals.

Research Articles

Sandip Prajapati, Abhay Dharamsi

Pregabalin has a short elimination half-life and is absorbed in the small intestine and the ascending colon in humans but is poorly absorbed beyond the hepatic flexure. The purpose of this study was to develop a gastro retentive effervescent controlled release drug delivery system with swelling and floating properties. Tablet formulations were designed using hydroxyl propylmethylcellulose (HPMC K15M) and sodium alginate (Na alginate) as release-retarding polymer(s) and sodium bicarbonate (NaHCO3) as a gas former. Floating behavior, swelling study and drug release studies were performed in 0.1 N HCl (pH1.2) at 37 ± 0.5°C. The tablets showed acceptable physicochemical properties. Drug release profiles of all the 12 batches formulated followed zero order. Statistical analysis of data done by design expert software revealed that the desired physicochemical properties of effervescent matrix tablets could be achieved by optimization through 32 full factorial designs. The optimized batch was promising and exhibited excellent floating properties, swelling properties and sustained drug release characteristics. This optimized batch was stored at 40˚C /75% RH for 3 months according to ICH guidelines. It was concluded that combination of HPMC K15M, sodium alginate, and sodium bicarbonate showed good swelling, floating and drug release characteristics.

Keywords: Pregabalin, Gastric Emptying Time, Floating Matrix Tablets, Release-retarding Polymers, 32 Full Factorial Design.

Ajit C Bhadage, ‎Saurabh C Khadse, ‎Deepak l Rokade, ‎Pradum P Ige ‎

The aim of the present investigation was to develop sustained release Glipizide matrix pellets for Type II diabetis mellitus. The Glipizide matrix pellets were prepared by extrusion-spheronization method using different hydrophilic polymers such as pectin, microcrystalline cellulose (MCC) and Eudragit L-100 in various proportions to retard and prolong the release of Glipizide. The prepared matrix pellets were characterized through Infrared Spectroscopy (FTIR), Differential Scanning Colorimetry (DSC), circularity, roundness, pellips, percent drug content, percent production yield, and in vitro drug release. The in vitro dissolution studies showed that GSR 6 formulation had released (90.07±0.67) the drug in a controlled profile for 12 h which containing pectin (30%), MCC PH-101 (35%), Eudragit L-100 (26%) and Polyvinylpyrrolidone (PVP) K-30 (5%) w/w. The DSC and FTIR studies revealed that there was no interaction between drug and excipients. Stability studies were carried out for optimized formulation GSR 6 according to ICH guidelines. Stability studies (40±20C/75±5% RH) for a period of 3 months indicated that Glipizide was stable in matrix pellets. In comparison, drug dissolution profile with marketed Glipizide (Glytop 10®) SR Tablet (98.23±0.88 % release), formulation GSR 6 drug release was found to be lesser up to 12 h. In conclusion, different hydrophilic polymers (Pectin, Microcrystalline Cellulose, Eudragit L-100 and Polyvinylpyrrolidone K-30) at optimum ratios in matrix pellets had a promising potential for sustained release.

Keywords: Glipizide, Extrusion-Spheronization, Pectin, Sustained Release Matrix Pellets, Pelletization.

Attama A A, Ofokansi K C, Kenechukwu F C, Ugwueze M E

The objective of the research was to study the hepatoprotective activity of ethanol and aqueous root extracts (EREMA and AREMA) of Milletia aboensis Hook F. (Fabaceae) against paracetamol-induced liver damage in rats. Preliminary phytochemical screening of the extracts (AREMA and EREMA) was carried out using standard procedures while oral acute toxicity was evaluated using a modified Lorke’s method. Hepatotoxicity was induced by administration of paracetamol (350 mg/kg) and the biochemical parameters such as serum glutamate oxalate transaminase (SGOT/AST), serum glutamate pyruvate transaminase (SGPT/ALT), alkaline phosphatase (ALP), total and conjugated bilirubin and histopathological changes in liver were studied along with Liv-52®, a standard hepatoprotective agent. Alkaloids, glycosides, resins, steroids, flavonoids, terpenoids and saponins were detected in the phytochemical screening. LD50 of the extracts was determined to be 2,154 mg/kg. The extracts at a dose level of 215 mg/kg and 431 mg/kg produced significant (P<0.05) hepatoprotection by dose-dependently decreasing the levels of serum enzymes (for EREMA), total and conjugated bilirubin (for AREMA). Overall, while the hepatoprotective effect of AREMA was less than that of EREMA, at all dose levels, hepatoprotective effect of the latter (431 mg/kg) was comparable to the standard reference Liv-52® (1 mL/kg). The hepatoprotective effect was confirmed by histopathological examination of the liver tissue of control and treated animals. Millettia aboensis root conferred hepatoprotection against paracetamol-induced liver damage in rats and this activity was better in ethanol than aqueous extract.

Keywords: Millettia aboensis, Hepatoprotective Effect, Paracetamol, Liv-52®, Paracetamol-induced Hepatotoxicity.

Yuan-Mei Huang, Ping Li, Yu-Min Li, Ai-Qin Wang

The aim of the present study was to prepare magnetic/pH sensitive alginate-chitosan beads loaded with the water-soluble traditional Chinese medicine Sophora alopecuroides L. total alkaloids by the ionic gelation method. Beads formulations based on the electrostatic interactions between alginate and chitosan were prepared via single factor design experiments, which were employed to investigate the combined effect of seven formulation variables, i.e., % of alginate, Fe3O4 nanoparticles to polymer, CaCl2 and chitosan and the volume ratio of alginate to CaCl2 and the crosslinking time and the polymer to drug on beads encapsulation efficiency and loading efficiency, considered as the responses to be optimized. Then, we characterized the optimal beads using SEM, FTIRS, XRD, and VSM, respectively, and investigated the influence of the swelling characteristic on the multifactorial relationships among formulation parameters. Furthermore, the delivery behavior of SATA from the optimal dry beads was evaluated in vitro. We found that the beads exhibited good pH-sensitive swelling, magnetic-response and controlled release properties due to their electrostatic interaction. The results together demonstrated that the beads can realize the goal of magnetic-target and have the potential to be used as a vehicle of SATA in the gastrointestinal administration.

Keywords: Sophora alopecuroides L., Total Alkaloids, Magnetic/pH Sensitivity, Hydrogel Beads, Swelling Characteristic, Delivery Property.

Sujan Banik

The present study was undertaken to develop a spectrophotometric method for the determination of Dapoxetine in pharmaceutical dosage forms. This paper reports a simple, rapid, accurate and precise UV-Spectrophotometric method for the assay of Dapoxetine in bulk and marketed tablet dosage form has been developed. The validation of the designed method was also carried out in terms of linearity, precision, accuracy, specificity, limit of detection, limit of quantification and by performing recovery study. Beer’s law was obeyed in the concentration range of 5- 35 µg/ml with a good correlation coefficient (r=0.999). Method is validated as per ICH guidelines and this study is statistically significant as all the statistical parameters are within the acceptance range (% RSD < 2.0 and SD < 2.0) for both accuracy and precision.

Keywords: Dapoxetine, UV Spectrophotometer, Method Validation, Dosage Form.

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