ABSTRACT

The blood brain barrier represents an insurmountable obstacle for a large number of drugs including antibiotics, anti neoplastics and a variety of CNS active drugs especially neuropeptides. One of the possibilities to overcome this barrier is a drug delivery to brain using nanoparticles. The use of nanoparticles to deliver drugs to the brain across the blood brain barrier may provide a significant advantage to current strategies. The primary advantage of nanoparticles carrier technology is that nanoparticles mask the blood brain barrier limiting the characteristics of the therapeutics, drug molecules and it also decreasing peripheral toxicity by causing slow drug release in the brain. The nanoparticles may be especially helpful for the treatment of the disseminated and very aggressive brain tumors. The mechanism of nanopraticles mediated transport of drugs is mostly endocytosis by endothelial cells lining the brain blood capillaries.

Keywords: Targeted drug delivery, Blood Brain Barrier, Central nervous system, Reticuloendothelium system, Neuroletics.

ABSTRACT

The present study is an attempt to formulate microspheres of Glimepiride, an orally administered ant-diabetic drug with a view of improving its oral bioavailability and giving a prolonged release of drug, where here the microspheres with polymers such as Ethyl cellulose and Eudrajit RS 100 and Eudrajit RL 100 were successfully prepared by emulsification solvent evaporation method and the particle size analysis revealed that the size of microspheres was increased with increase in the concentration of polymer. Formulation with combination of Ethyl cellulose, Eudrajit RS 100 and Eudrajit RL 100 gave large particles in the range of 250.6±1.34 µm, Scanning electron microscopy showed that microspheres of drug with combination of Ethyl cellulose, Eudrajit RS 100 and Eudrajit RL 100 showed smooth surface and a good spherical shape where the in-vitro drug release studies showed that drug release was more in case of formulations MP_9- MP₁₂ containing both hydrophilic and hydrophobic polymers as compared to formulations MP_1- MP₈ only hydrophobic polymer.

Keywords: Glimepiride, Eudrajit RS 100, Eudrajit RL 100, Oral Bioavailability.

ABSTRACT

In present times, the pelletization technologies are giving much attention as they represent an efficient pathway for manufacture of new drug delivery system .It has good advantage over the conventional dosage form. Pelletization technique help in the formation of spherical beads or pellets having a diameter 0.5 -1.5 mm which can be eventually coated for preparation of modified release dosage form. These pelletized dosage forms have gained popularity considerably from then because of their distinct advantages, such as ease of capsule filling because of better flow properties of the perfectly spherical pellets; enhancement of drug dissolution; ease of coating; sustained, controlled, or site-specific delivery of the drug from coated pellets; uniform packing; even distribution in the GI tract; and less GI irritation. The aim of this study is to provide detailed and different techniques of pelletization. Pelletized dosage forms can be prepared by a number of techniques, including drug layering on nonpareil sugar or microcrystalline cellulose beads, spray drying, spray congealing, roto granulation, hot-melt extrusion, and spheronization of low melting materials or extrusion-spheronization of a wet mass. The techniques namely extrusion-spheronization, hot melt extrusion, freeze pelletization, cryopelletization have been discussed along with formulation requirements for the process, parameters affecting pelletization. Evaluation of quality of the pellets is discussed with reference to the size distribution, shape, surface morphology, specific surface area, friability, tensile strength.

Keywords: Pelletization, Extrusion, Spheronization, Cryopelletization, Hot melt extrusion.

ABSTRACT

The objective of the present investigation was to develop a bilayer-floating tablet (BFT) for Verapamil Hydrochloride using direct compression technology using floating and viscosity enhancing polymers such as HPMC K100 and Carbopol 940. Sodium bicarbonate and citric acid were used as a gas generating agent. All the bi-layered floating tablet formulations were subjected to post-compression evaluation parameters such as hardness, friability, weight variation, thickness, drug content, lag time subsequently buoyancy time, and in-vitro dissolution studies. The assay of the formulation revealed that the drug content was within the limits. In-vitro floating revealed that all the formulations showed buoyancy of more than 12 hours. Dissolution tests were performed using USP dissolution apparatus at 75 rpm in pH 1.2 buffer. The tablet split in to 2 layers i.e. floating and immediate layer in the dissolution medium, which exhibited biphasic release of Verapamil Hydrochloride. The formulation F3 released 98.24% of drug at the end of 12hr. The invitro drug release data was fitted into various kinetic models and the best fit release kinetics was achieved with Peppas model.

Keywords: Verapamil hydrochloride, HPMC, Carbopol, Bilayer floating tablet.

ABSTRACT The aim of present work is to prepare microsponges of Erythromycin using Ethyl cellulose as polymer. Erythromycin has bacteriostatic activity which inhibits growth of bacteria. They mainly act by binding to the 50s subunits of bacteria, 70s r-RNA complex, and protein synthesis. Erythromycin is also used topically to treat acne. They are used to treat moderate to severe inflammatory acnes or acne that isn’t getting better with other treatments. Erythromycin works to treat acne by reducing the amount of acne causing bacteria called “propionibacteria” acnes on the skin, it also lessens inflammation and redness. Erythromycin is easily inactivated by the gastric environment and produce gastric disturbances such as diarhoea, nausea, abdominal pain and vomiting. Erythromycin microsponges were prepared using quassi emulsion solvent diffusion method. In order to standardize the microsponge formulation, factors affecting the physical properties of microsponges were determined. The SEM and DSC studies were carried out to study shape, morphology of microsponges and thermal analysis respectively Thus it was concluded that erythromycin can be formulated as microsponge gel that can release the drug up to 8hrs with reduced side effects.

Keywords: Acne, Erthromycin, Microsponges, Gel.

ABSTRACT

Supramolecular chemistry refers to the area of chemistry beyond the molecules and focuses on the chemical systems made up of a discrete number of assembled molecular sub-units or components. A Super molecule is an organized, complex entity that is created from the association of two or more chemical species held together by intermolecular forces. There is a wide scope for supramolecular chemistry in improving the characteristics of chemical entities. The technique is pharmaceutically used to increase the bioavailability, solubility and stability of the active pharmaceutical ingredients by formation of complexes, inclusion complexes and co crystals. This article highlights the role of supramolecular chemistry in design and synthesis of novel pharmaceutical multiple component crystalline phases.

Keywords: Supramolecular chemistry, Complexes, Chemical entities.

ABSTRACT

The intention of the present research work was to develop once daily controlled release floating microballoons of pantoprazole using different polymers like HPMC, EC and gelatin for GRDDS along with the loading dose granules with superdisintegrants. The immediate release (IR) granules were prepared by wet granulation method by using Sodium starch glycolate, Cross povidone as superdisintegrants and evaluated for the flow property and release studies. The granules showed good flowability and in vitro release of pantoprazole IR granules was found to be 96-102%. The floating microballoons were prepared by emulsion solvent diffusion method. The prepared microballoons were characterized for scanning electron microscopy (SEM), drug content, entrapment efficiency, production yield, floating ability, buoyancy percentage, in vitro drug release and release kinetics studies. The prepared microballoons were spherical and showed good flow properties. DSC studies revealed that the drug is having a very good compatibility with the polymers. SEM revealed that the microballoons had smooth surface and hollow cavity in the middle. The entrapment efficiency of microballoons was found to be 72-95 % and the drug release from the microballoons in simulated gastric fluid (SGF) was found to be 54-68 % up to 12 h. The floating ability and buoyancy percentage of the microballoons were found to be 75-88 % and it remains buoyant up to 12 h. The release kinetics study revealed that the prepared microballoons were best fitted to the zero order kinetics and indicates that the drug release obeys diffusion – controlled mechanism. Thus it conclude that GRDDS of pantoprazole (an anti-ulcer drug) loaded microballoons along with IR granules loaded capsule was an ideal drug delivery system for ulcer protective activity as both controlled and immediate release drug delivery systems.

Keywords: Buoyancy percentage, Emulsion solvent diffusion method, Floating Microballoons, Gastro retentive drug delivery system, Pantoprazole.