Bioaccumulation and Toxic Profiling of Nanostructured Particles and Materials

Use of nanotechnological based formulations and nanomaterials are increasing day-by-day in wide range covering a broad typology of applications, from design and development of targeted drug delivery systems, manufacturing of pesticides, domestic appliances, textiles, to bioremediation engineering. There are therefore concerns about the environmental risks or bioaccumulation-related issues that may arise particularly resulting from the application of drug-loaded nanocarriers or effect of pesticides that reach the natural ecosystems. This is a major threat in the present era and needs to be balanced against their undoubted benefits to human society. The assessment of the physical and chemical properties of nanoparticles and nanomaterials influencing their toxic manifestation due to accumulation in human or in animal organs is still poorly investigated. This chapter reviews the possibilities of bioaccumulation of different nanoscale particles and materials, their potential acute and subacute toxicological profile and their identification and characterization in different organs and tissues of vertebrates

FORMULATION AND IN-VITRO/IN-VIVO ASSESSMENT OF ENHANCED BIOAVAILABILITY OF LACIDIPINE USING NANO PURE TECHNIQUE

The objective of this study was to formulate and evaluate a novel drug solubilization platform (so called Nano-suspension prepared by comminution method using High pressure homogenizer; GEA Niro soavi) and further use the nano-suspension as granulating fluid admixed with excipients for further tablet production. The solid state characterization of Lacidipine along with the excipients   reveal compatibility , as confirmed X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR) and Differential scanning calorimetry (DSC). The performance of Nano suspension is highly dependent on the selection of polymer stabilizer; hence different polymers such as hydroxy propyl cellulose, propylene glycol and poly vinyl pyrollidone were used in the study and evaluated. The results revealed hydroxy propyl cellulose as a suitable stabilizer compared to others polymer. The dissolution studies of Lacidipine shows complete release of drug within 45 minutes using hydroxy propyl cellulose as stabilizer in comparison to  available marketed product. Hydroxy propyl cellulose was better adsorbed with the drug compared to other polymers resulting in better mechanical interaction during comminution which causes the drug particle size to reach in nano-meter scale. The particle size of the nano suspension as confirmed by Zeta sizer revealed a particle size of 293.7 nm. The appearance of the nano suspension shows a bluish opalescence and the morphology revealed by Transmission electron microscope shows a particle size of 200.0 nm. The In-Vivo pharmacokinetic study was performed on rabbits to assess the bioavailability, since the bioavailability is directly proportional to the particle size. The In-Vivo pharmacokinetic results revealed that the AUC and Cmax were increased to two and six folds respectively in comparison to conventional market tablet. This may be recognized to increase solubility and permeability of the drug due to this novel formulation approach

Solid Lipid Based Nano-particulate Formulations in Drug Targeting

Recently, targeted drug delivery systems have gained much more interest for delivering varieties of drugs as well as imaging agents specifically to the targeted disease cells or tissues. These are well known for their increased precision and accuracy in mode of drug delivery along with reduced side effects. Though numerous carriers are being employed for drug targeting, the solid lipid based nanoparticles (SLNs) are preferred over them owing to their ability to encapsulate wide varieties of drugs, biocompatibility, ease of surface modification, scaling up feasibility, and possibilities of both active as well as passive targeting to various organs. Surface of these drug loaded SLNs can be modified by conjugating different ligands to enhance their tissue/organ targeting ability and therapeutic efficacy to much higher extent. In this chapter, we have discussed about the SLNs and their different surface modified forms for passive as well as active targeting to different organ such as (colon, breast, lungs, liver, kidney, brain, eyes, etc.) in combating different diseases

ANTI-TUBERCULOSIS DRUG RESISTANCE IN ETHIOPIA: A MATA- ANALYSIS

Tuberculosis is one of the most dangers of health in the world. Ethiopia ranked seventh from the 22 high burden counties in the world. The main problem is development of resistance to the major anti-tuberculosis drugs actually increasing in Ethiopia. The aim was to review studies done on anti-tuberculosis drug resistance in Ethiopia. Literatures were searched for published articles on anti-tuberculosis drug resistance using the combination of terms; resistance, anti-tuberculosis and Ethiopia. Fifteen studies done in different parts of Ethiopia from 1978-2005 G.C were retrieved without restriction of place & design of study. The primary resistance of the fifteen studies done in various parts of Ethiopia (Addis Ababa, Harar, Bahir Dar, Sidamo, Arsi, and Hosanna) from1978-2005 G.C showed: Isoniazid (H) 1.9%-21.4%, Streptomycin (S) 1.9%-26%, Rifampicin (R) 0%-1.9%, Ethambutol (E) 0%-6.3%, Thiacetazone (T) 2.2%-6.3%, H+S 1.9%-26%, H+T 0%-4.4%, S+T 0%-1.8%, H+R 0%-1.1%, S+R 0%-0.7%, R+T 0%-0.4%, H+E 0%-0.9%, S+E 0%-0.6% ,H+S+T 0%-2.4%, H+S+R 0%-1.1%, H+T+R 0%-0.4%, H+S+E 0%-1.7%, R+H+T+S 0%-0.6% and Multi Drug Resistance 0%-1.3%.Acquired drug resistance: H 5.3%-66.7%, S 1.2%-46%, R 0%-12%, E 0%-5.6%, T0%-29%, H+T 0%-20%, H+S 4.8%- 28%, R+H 0%-8%, R+S 0%-3.5%, S+T 0%-2.3%, H+E 0%-3.6%, R+E 0%-5.6%, S+E 0%- 11.2%, H+S+T 0%-16%, R+S+T 0%-2.3% , R+S+H 0%-4%, H+S+E 0%-3.6%, H+R+E 0%- 3.6%, H+R+S+E 0%-14.3% and Multi Drug Resistance 0%-26.3%. It can be concluded that resistance to the anti-tuberculosis drugs is increasing. National level drug resistance survey is recommended to design policies and strategies to prevent increase of drug resistance. Key words: Resistance, tuberculosis, anti-tuberculosis drugs and Ethiopia

LITERATURE REVIEW ON ENSET STARCH: PHYSICO-CHEMICAL PROPERTIES AND PHARMACEUTICAL APPLICATIONS

ABSTRACT Enset (Ensete Ventricosum, Family Musaceae) is a plant indigenous to Ethiopia, it is often called ‘false banana†for its close resemblance to banana plant. The plant is the most important staple food for millions of people in the south and southwestern parts of Ethiopia. Enset plant contains starch as its major contents. The starch has been investigated for its physico-chemical properties including granule size, X-ray diffraction pattern, amylose content, gelatinization behavior, stability and various rhelogical properties of the gel. Based on its physico-chemical properties the starch was evaluated for various pharmaceutical applications such as in tablet binder and disintegrant. Several modifications were also attempted on the native enset starch so as to improve and modulate its physiochemical properties. Hence, this review aims to summarize the knowledge on the properties of enset starch and its pharmaceutical applications. Key words: Enset, Starch, properties, Pharmaceutical applicationÂ

Priprava, in vitro i in vivo evaluacija bioadhezivnih mikrosfera s algino-pektinom: ispitivanje utjecaja polimera pomoću multiple poredbene analize

Ionotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigated in vitro for possible sustained drug release and their use in vivo as a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunett\u27s multiple comparison analyis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.U radu je opisana priprava algino-pektinskih bioadhezivnih mikrosfera protuupalnog lijeka aceklofenaka metodom ionotropnog geliranja. In vitro je ispitivana mogućnost postupnog oslobađanja ljekovite tvari iz mikrosfera te mogućnost upotrebe mikrosfera kao gastroprotektivnog sustava za isporuku aceklofenaka in vivo. Ispitivan je utjecaj koncentracije polimera i omjera polimera i lijeka na svojstva mikrosfera. Mikrosfere su bile bioahezivne i sadržavale su veliki udio lijeka. Oslobađanje aceklofenaka iz alginatnih mikrosfera bilo je brže, a iz mikrosfera s algino-pektinom usporeno. Dunnetova multipla analiza ukazuje na značajnu razliku u postotku inhibicije edema šape kada se usporede optimizirana formulacija i čista ljekovita tvar. Može se zaključiti da su bioadhezivne mikrosfere s algino-pektinom povoljne za usporeno oslobađanje aceklofenaka te da pružaju umjerenu zaštitu sluznice želuca

Studies on some psychopharmacological activities of <i>Ocimum sanctum </i>root extract

284-288The petroleum ether (60-80°C) extract of Ocimum sanctum root was tested for pentobarbitone induced hypnosis in mice. The root extract or vehicle was administered (i.p.) and after 30 minutes pentobarbitone sodium (35 mg/kg) was administered. The exploratory behaviour like Water Maze Test was studied by imparting training to mice in a rectangular tank having holes to escape, filled with water and the number of mistakes were recorded. The extract was found to produce a significant alteration in general behavioural pattern by Water Maze Test. Besides this the extract also potentiated the pentobarbitone induced hypnosis in mice. The potentiation of pentobarbitone sodium induced hypnosis and reduction of mistakes to escape by Water Maze Test indicates that the extract may have some CNS depressant as well as tranquilizing activity

A Systematic Study on Processing Problems and In-vitro Release of Saraca indica Caesalpiniaceae Bark Powder Tablets

Purpose: To examine the original flowability, compressibility and compactibility of Saraca indica bark powder and its tablet formulations. Methods: Saraca indica bark powder was subjected to various quantitative tests including acid insoluble ash, total ash, foreign organic matter, alcohol soluble extractive and water soluble extractive. Its flowability and compressibility were determined using Kawakita, Heckel and Leuenberger relationships. Tablets were prepared from the powder by direct compression and wet granulation techniques and characterized. Results: Kawakita analysis revealed lower cohesiveness of granules (3.877 ± 0.890) compared to the powder (6.176 ± 1.030), and hence improved flowability. From Heckel analysis, the higher value of intercept (A) for granules (4.38 ± 0.45) implies higher degree of fragmentation than direct compression DC formulation (2.90 ± 0.33) and powders (2.44 ± 0.12). The compression susceptibility parameter obtained from Leuenberger equation for compacts formed by wet granulation technique (0.183 ± 0.045 1/kg/cm2) indicate that maximum crushing strength is reached faster at lower pressures of compression than for Saraca indica bark powder (0.073 ± 0.025 1/kg/cm2) and DC formulation (0.105 ± 0.033 1/kg/cm2). In-vitro dissolution study showed that more than a 90% of tannin was released within 30 and 60 min from tablets prepared by wet granulation and DC, respectively. Brittle fracture index data indicate that tablets prepared from granules showed less fracture, capping and lamination tendencies. Conclusion: It is concluded that the desired flowability, compressibility and compactibility of Saraca indica bark powder can be obtained by direct compression and wet granulation techniques