Volume 4, Issue 4, Oct-Dec 2012

Volume 4

October-December 2012

Nanocarriers as novel nose-to-brain targeted drug delivery platforms

Sagar Patel, Brijesh Patel, Zarna Patel, Chandrakantsing Pardeshi

Abstract:
The present review is designed to provide an insight on how nanoparticulate carriers are finding niche as promising drug vectors. In the era of controlled and site specific drug delivery systems, use of nanocarriers has became a revolutionary approach. Nanocarriers are at forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery, clinical medicines and research. The success of nanocarriers as targeted drug delivery platforms depends on their ability to incorporate drugs of different kinds, penetrate through several anatomical barriers, sustained release of incorporated drugs, and stability in nanoscale size. Such prototypic traits of nanocarriers offer a new breakthrough in drug delivery and therapeutics that holds great promise for achieving the goal of controlled and site-specific drug delivery. Delivery of drugs to the brain is a major challenge due to presence of physiological barriers that restricts the delivery of drugs to CNS. Thus, since last few decades, nasal route has been attracted a wide attention of researchers as a convenient, reliable, and safe, being non-invasive, route to achieve faster and higher levels of drug absorption in the brain. It is thought to do so through olfactory route of drug transport which bypass the blood-brain barrier (BBB) and allow the direct transport of drug from nose to brain. Herein, authors has tried to highlight over the frontline aspects relevant to nanoparticulate carriers and their potential as drug delivery systems for targeting the brain via nasal route of drug administration. The present discussion embodies the various nanocarriers and their utility as nose to brain targeted drug delivery vehicles, in the core areas of pharmaceutical sciences, thereby alarming the pharmaceutical industries to enhance their scale up.

Keywords: Nanoparticulate Drug Carriers, Polymeric Micelle, Nanoemulsion, Macroemulsion, Carbon Nanotubes (CNTs), Dendrimer, Solid Lipid Nanoparticles (SLNs), Polymer-Lipid Hybrid Nanoparticles (PLN), Liposome.

A review on fast dissolving drug delivery systems- A pioneering drug delivery technology

Soumya M, Madhu Babu M, Aparna K, Himabindu P

Abstract:
The Fast Dissolving Drug Delivery Systems was an advancement that came into existence in the early 1970’s and combat over the use of the tablets, syrups, capsules which are the other oral drug delivery systems. Fast Dissolving Drug Delivery Systems serves as a major benefit over the conventional dosage forms since the drug gets rapidly disintegrated & dissolves in the saliva without the use of water. Inspite of the downside i.e.., lack of immediate onset of action; these oral dosage forms have beneficial purposes such as self medication, increased compliance, ease of manufacturing and lack of pain. Hence Fast Disintegrating Tablet (FDT) technology has been gaining significance now-a-days with wide variety of drugs serving many purposes. Fast Disintegrating Tablets (FDT) have ever increased their demand in the last decade since they disintegrate in saliva in less than 60 seconds.

Keywords: Fast Dissolving Drug delivery Systems, Patented Technologies, Conventional Technologies, Evaluation of FDTs.

A review on ethanomedical uses, phytochemicals and pharmacological profile of Bambusa arudinacea Retz:

Vishal Soni, Arun Kumar Jha, Jaya Dewedi

Abstract:
India has a great wealth of various naturally occurring plant drugs which have great potential pharmacological activities. Bambusa arundinacea is one amongst them. Bambusa arundinacea has been proven to have great pharmacological potential with a great utility and usage as folklore medicine. Various parts of this plant such as Leaf, root, shoot and seed possess Anti inflammatory, Antiulcer, Antidiabetic, Anti-oxidant, anthelmintic, astringent, emmengogue activity. Various phyto-pharmacological evaluations have been reported in this literature for the important potential of the Bambusa arundinacea. This review mainly focuses on the traditional, phytochemical and pharmacological information of Bambusa arundinacea.

Keywords: Bambusa arundinacea, Phytopharmacological Properties, Phytochemicals, Traditional Uses.

Intellectual property rights (IPRs) and mechanisms for intellectual property protection (IPP): A review

Dogra Rahul, Dhiman Vijay, Gupta Nipun

Abstract:
We have experienced a growing importance of intellectual capital and intangible assets and an increased tendency for firms and public institutions to privatize, by the use of patents or copyrights, their knowledge assets and creative expressions. Because control over the use of an intellectual property right (IPR) requires ownership or a licence, the growing importance of knowledge-based assets and creative expressions has been accompanied by recognition that patents and copyrights represent strategic assets for those who own and control them. It is therefore not surprising that, in recent years, the pace at which individuals, firms and the public sector are using IPRs to privatize knowledge-based assets and creative expressions has been accelerating. This trend has been enhanced by the view of many industry, government and international agencies that the privatization of the intellectual capital and knowledge-based assets of individuals and firms provides many advantages (for example, competitive advantage), and we have seen an increased enforcement of IPR regimes worldwide. Protection of undisclosed information is least known to players of IPR and also least talked about, although it is perhaps the most important form of protection for industries, R&D institution and agencies dealing with IPR. Undisclosed information generally known as trade secrets or confidential information includes formula, pattern, compilation, programme, device, method, technique or process. Protection of undisclosed information or trade secret is not really new to humanity; at every stage of development people have evolved methods to keep important information secret, commonly by restricting the knowledge to their family members.

Keywords: Copyright, IPP, Industrial Designs, Patent, Trade Mark.

Solid dispersion as an approach for dissolution enhancement and delivery of trandolapril, a poorly water-soluble ace inhibitor

Ofokansi K C, Kenechukwu F C, Isah A B, Ogbonna J D N

Abstract:
This study was designed to formulate and evaluate solid dispersions as novel carrier system for the delivery of trandolapril. Trandolapril-loaded solid dispersions (SDs) were prepared by fusion method using varying combination ratios of Eudragit RL 100 and polyethylene glycol (PEG) 8000 with or without urea as a hydrophilic carrier. Characterization based on surface morphology, particle size, absolute drug content and moisture sorption properties were carried out on the SDs. The in vitro release of trandolapril from the SDs was performed in 0.1 N HCl (pH 1.2) and phosphate buffered saline (PBS, pH 7.4). To evaluate the mechanism of release of trandolapril from the SDs, the in vitro release data from different batches of the SDs were fitted into different kinetic models. Results indicate that discrete and irregular SDs of mean particle size range 3.87 ± 0.15 to 22.14 ± 1.09 µm, which were stable over 3 months, were obtained. SDs containing urea entrapped greater amounts of drug in comparison with SDs containing only Eudragit RL 100 and PEG 8000. The moisture sorption studies indicate that both amorphous and microcrystalline state of trandolapril are present in the SDs. In vitro release studies revealed that there was marked increase in the dissolution rate of trandolapril from the solid dispersions when compared to pure trandolapril. The improved dissolution, which was better in PBS than in 0.1 N HCl, was highest in the SDs containing Eudragit RL 100, PEG 8000 and urea. The increased dissolution rate of trandolapril may be due to the formation of microcrystals, increased wettability and dispersibility in systems containing Eudragit RL 100, PEG 8000 and urea. The release pattern of the drug was found to follow predominantly the Higuchi square root model. This study has shown that a formulation of trandolapril SDs could offer a better and more effective approach of increasing the dissolution rate of the poorly water-soluble prodrug, trandolapril.

Keywords: Trandolapril, Solid Dispersion, Urea, PEG 8000, Dissolution, Eudragit RL 100, Moisture Sorption.

Design and development of floating gastro retentive tablets for mosapride citrate dihydrate: In vitro-in vivo evaluation

Ige Pradum Pundlikrao, Patel Kalpesh Mohanbhai

Abstract:
The aim of the current work is to develop stable formulation of mosapride citrate dihydrate in the form of floating matrix tablet, in combination with two different polymers hydroxy propyl methyl cellulose (HPMC K4M) and Eudragit RS. The Mosapride citrate dihydrate in a form of gastro retentive floating sustained release dosage forms, which provides enhanced bioavailability. In the present study mosapride citrate dihydrate controlled release tablet were prepared with the help of the direct compression method, using sodium bicarbonate and citric acid as the gas forming agent. It was characterized by FTIR spectroscopy, floating ability, swelling ability, in vitro drug release, in vivo x-ray imaging and stability studies. The physical characterization of the floating matrix tablets was examined by SEM and results showed that the shape and texture of the tablets were uniform. Percent drug content from the tablets was determined by UV spectrophotometer and exhibited about 99.32 ± 0.08. The in vitro drug release from the tablets was found to have 78.3 ± 0.2 to 99.04 ± 0.12 for 12 h. The optimized formulations F3 were kept for 90 days at 40°C / 75% RH. After 90 days of exposure the percent drug content was found to be 99.70 ± 0.04. In conclusion, the combination of eudragit RS and HPMC K4M at the 1.0:4.5 w/w ratios could be the effective carrier for the sustained release floating matrix tablets of mosapride citrate dihydrate.

Keywords: Mosapride Citrate Dihydrate, Floating Matrix Tablets, HPMC K4M, Eudragit RS, Gas Forming Agent.

In vitro anthelmintic potentials of Bambusa vulgaris (L.) Leaf extracts using adult african earthworm (Eudrilus eugeniae) from southern Nigeria

Gideon Ikechukwuogu

Abstract:
Bambusa vulgaris leaf is used traditional among the aborigines of South-Western Nigeria to manage intestinal helminths with paucity of scientific evidence to the practice. This study was undertaken to evaluate the in vitro anthelmintic activities of the aqueous and methanolic extracts of B. vulgaris leaf (at doses 10, 20 and 30 mg/ml) using adult African earthworm (Eudrilus eugeniae) which has similar anatomy and physiology to human intestinal helminths. Albendazole (commercial anthelmintic drug) was used as a standard reference and saline as control. Both extracts displayed concentration-dependent and significant (P<0.05) vermicidal activities against the worms. The paralysis time of aqueous fraction of the plant at 10, 20 and 30 mg/ml concentrations were respectively observed at 14.42, 9.01 and 8.53 min followed by death at 21.03, 14.59 and 12.43 min post-exposure. Methanolic fraction caused paralysis at 12.33, 8.27, 7.52 min and post-exposure death time of 21.12, 14.57, 10.29 min. Both extracts (at 20 and 30 mg/ml) were more effective in promoting paralysis and death of the earthworms than the 10 and 20mg/ml treatments of the standard reference drug (Albendazole). The observations from this study therefore suggest that the bioactive principles of B. vulgaris leaf extracts possess significant anthelminthic activity against E. eugeniae, and possibly potent against human intestinal helminths that has similar anatomy and physiology to E. eugeniae. The ethno-medicinal claim of B. vulgaris as anthelminthic plant is thus substantiated.

Keywords: African Earthworm, Bambusa vulgaris, Intestinal Helminths, Vermicidal Activities.

Preparation and characterization of lipid vesicles of thiocolchicoside for transdermal drug delivery system

Abhishek Rathod, Ankit Mishra, Shelesh Jain

Abstract:
The aim of the current investigation is to evaluate the transdermal potential of novel vesicular carrier, liposomes, ethosomes, transferosomes, having thiocolchicoside, a potent, water soluble muscle relaxant drug with lesser transdermal permeation. Drug loaded liposomes, ethosomes, transferosomes had been prepared using phospholipid and ethanol, were optimized and characterized for entrapment efficiency, vesicular size, zeta potential, in vitro skin permeation and stability. The ethosomal formulation having 10 mg of phospholipid and 10 ml of ethanol showing the greatest entrapment efficiency (23.16 ± 1%) with small particle size (502 ± 5nm) then liposomes, and transferosomes. The skin permeation studies were performed on ethosomal formulation, liposomal formulation, transferosomes formulation, aqueous drug solution. Among them, ethosomal formulation showed higher cumulative percentage of drug permeation (90 ± 5%) after 24 hours than the other formulations. Differential scanning colorimetery shows no intraction between lipid and drug. Zeta seizer revealed that the ethosomes has smaller vesicular size than the liposomes and transferosomes. FT‐IR studies revealed no interaction between the drug and membrane components. The ethosomes, liposomes, transferosomes vesicles muscle relaxant efficiency was compared with the marketed thiocolchicoside gel. The pharmacodynamic studies showed that the muscle relaxant activity of ethosomes was more then liposomes, transferosomes suspension and less than the marketed gel formulation. Our results suggest that the ethosomes are an efficient carrier for dermal and transdermal delivery of thiocolchicoside.

Keywords: Transdermal, Ethosomes, Phospholipid, Liposomes, Thiocolchicoside.

Indian Journal of

Novel Drug Delivery ISSN 0975-5500

Indian Journal of Novel Drug Delivery ISSN 0975-5500