Volume 6

October-December 2014

Review Articles

Kapoor D, Vyas RB, Lad C, Patel M, Tyagi BL

By using these nanoparticles, multiple tasks can be carried out simultaneously, e.g., early and accurate diagnosis, efficient cataloguing of patient groups of personalized therapy and real-time monitoring of disease progress. In this paper, we describe various types of nanoparticles for drug delivery systems, as well as theranostic systems. Because of these features, therapeutic efficacy can be improved and unwanted side effects can be reduced. Nanotechnology based delivery system would allow faster drug absorption, controlled dosage release into the human body and would have other unique properties of minimizing side-effects by eliminating requirement of co-solvent as used in conventional dosage form. These drug nanocarriers have the potential to enhance the therapeutic efficacy of a drug, since they can be engineered to modulate the release and the stability and to prolong the circulation time of a drug, protecting it from elimination by phagocytic cells or premature degradation. Moreover, nanoscale carriers can be tailored to accumulate in tumour cells and tissues, due to enhanced permeability and a retention effect or by active targeting using ligands designed to recognize tumour-associated antigens. Several anti-cancer drugs including paclitaxel, doxorubicin, 5-fluorouracil and dexamethasone have been successfully formulated using nanomaterials. Quantom dots, chitosan, Polylactic/glycolic acid (PLGA) and PLGA-based nanoparticles have also been used for in vitro RNAi delivery. Anti-cancer drugs such as loperamide and doxorubicin bound to nanomaterials have been shown to cross the intact blood-brain barrier and released at therapeutic concentrations in the brain. The use of nanomaterials including peptide-based nanotubes to target the vascular endothelial growth factor (VEGF) receptor and cell adhesion molecules like integrins, cadherins and selectins, is a new approach to control disease progression.

Keywords: Drug Delivery, Nanotechnology, Nanoparticle, Active Targeting, Hyperthermia.

Anupriya Adhikari, Ganesh Bhatt, Preeti Kothiyal

Chronotherapeutics is the purposeful timing of medications, with or without the utilization of special drug-release technology, to proportion serum and tissue concentrations in synchrony with known circadian rhythms in disease processes and symptoms as a means of enhancing beneficial outcome sand/or attenuating or averting adverse effects. The concept of chronotherapeutics, although relatively new to hypertension and cardiovascular medicine, was first introduced and proven worthy in clinical medicine in the 1960s; the morning alternate-day corticosteroid tablet dosing schedule was introduced as a convenient means of minimizing the adverse effects of such anti-inflammatory medications as prednisolone and methylprednisolone. The chronotherapy of hypertension takes into account the clinically relevant features of the 24-hour pattern of blood pressure (BP) (i.e., the accelerated morning rise at the commencement of diurnal activity and the extent of decline during nighttime sleep) plus potential administration-time (circadian rhythm) determinants of the pharmacokinetics and dynamics of individual antihypertensive medications. Herein, we focus on the chronotherapy of hypertension; however, as necessary background we first present the major concepts and mechanisms of biologic timekeeping

Keywords: Chronotherapy, Biological Rhythm, Circadian Rhythm.

Rakhi Negi, Laxmi Goswami, Preeti Kothiyal

The purpose of this review is to accumulate the recent study on floating drug delivery system with special emphasis on microballoons as drug delivery. Microballoons are emerging as the most promising drug delivery as it overcome many limitations of conventional drug delivery system. As microballoons delivery system provides longer retention in gastric pH, hence longer is the residence time and therefore enhance the solubility of drugs that are less soluble in high pH environment. The formation of cavity inside the microsphere depends upon the preparation temperature and the surface smoothness determines the floatability and the drug release rate of the microballoons. The review includes the classification, advantages, disadvantages, method of preparation and future aspects of microballoons. Basic anatomy and physiology of stomach is also studied.

Keywords: Gastric Retention, Floating Drug Delivery, Microballoons, Solvent Evaporation.

Research Articles

Mahajan Hitendra S, Patil Sandeep K, Nerkar Pankaj P

Drug actions can be improved by developing new drug delivery systems; one such Liquisolid compact of gliclazide was prepared with the intension of improving the dissolution properties of gliclazide. Polyethylene glycol (PEG), Propylene glycol (PG) and mixture of both were used as non volatile liquid. The dissolution studies of the liquisolid compacts were performed in vitro, and the results obtained showed that the dissolution rate of gliclazide was considerably improved when formulated in liquisolid compact with PG and PEG as compared to original drug, and the increased dissolution rate favorable for further oral absorption. In the comparative pharmacokinetic study with gliclazide suspension, a reference drug product, liquisolid system (LS1-A3) showed improved bioavailability with higher Cmax and faster Tmax. We conclude that liquisolid system (LS1-A3) is a good candidate for the development of oral solid dosage forms.

Keywords: Liquisolid Compact, Gliclazide, Dissolution Rate.

Hai-Xuan Zhang, Ping Li, Yu-Min Li, Ai-Qin Wang, Jun-Ping Zhang, Qin Wei, Xun Meng

A simple light-responsive azobenzene-N-Succinylchitosan (AZO-NSC) polymer has been investigated for its ability to act as a drug carrier. The AZO-NSC hydrogel bead was prepared by the ionic gelation method for the controlled delivery of kojic dipalmitate. The structure and surface morphology of the hydrogel were characterized by FTIR and SEM, respectively. The hydrogel showed good light-responsive. The release of the encapsulated drug from the hydrogel was regulated by (trans–cis) photoisomerization of azobenzene moiety. The in vitro release behavior of drug from these hydrogel systems is revelative of the potential of the hydrogel for controlled drug delivery.

Keywords: Kojic Dipalmitate, Light-Responsibility, Hydrogel, N-Succinylchitosan Azobenzene.

Amir Mehdizadeh, Mohammad Reza Rouini, Tayebeh Toliyat

The objective of this study was to determination of critical manufacturing parameters (CMP) and their influences on drug release of fentanyl transdermal reservoir patches (RPs). Fentanyl as a common drug administered by RPs was used as a model for drug release testing. Drug release studies were carried out using paddle over disk (USP apparatus 5). The critical manufacturing parameters (CMP) may potentially influence on rheological properties of hydroxyethyl cellulose (HEC) gels include gelation temperature and hydration time of polymer. Rheological characterizations were examined using a spindle type rheometer with a thermostatic water pump bath. The results indicated that the viscosity and consistency of 3% gel made in 60°C was suitable for fentanyl RPs and showed desired drug release over 72 h. While the release of fentanyl from gel made in 40°C reached its maximum within 48 h. Increasing the HEC concentration or in gelation temperature, both significantly decreased the release rate of fentanyl. In contrast, the hydration time of polymer did not affect significantly on drug release. Flow curve of HEC gels showed non-Newtonian characteristics, pseudo-plasticity for 2% gel and Bingham behavior for 3% or more. Gels with 3% concentrations showed some thixotropy. The thixotropic coefficient (M) and yield value (f) were 417 mPa s and 820 dynes cm-2.

Keywords: Fentanyl, Critical Manufacturing Parameters, Rheological Properties, Transdermal Patches, Drug Release.

Eidangbe G O, Oluba O M, Josiah S J, Adekunle A S, Onyeneke E C

The nutritional composition and anti-nutritive contents of wild Ganoderma lucidum fruit bodies were determined and its aqueous extract assessed for subchronic oral toxicity in mice. The matured fruit body contained per 100 g total carbohydrate (42.10 g), crude fibre (32.10 g), moisture (10.80 g), crude protein (7.18 g), ash (6.02 g) and crude fat (3.50 g). The antinutritive factors content per 100 g were cyanide (0.005 mg), oxalate (0.36 mg) and phytate (0.018). Crude aqueous extract of Ganoderma lucidum at 100, 250 and 500 mg/kg body weight for 21 days did not significantly affect the relative liver, kidney and spleen weights compared with control but relative heart weights were significantly higher compared with control in mice administered 100 and 500 mg/kg extract. Hematological indices, serum markers of liver and kidney status and serum lipid profile showed no statistically significant differences in the extract treated mice compared with control. It was therefore concluded that fruit body of G. lucidum contained good nutritional profile and its consumption both for nutritional and pharmaceutical purposes in the short-term could be said to be relatively safe.

Keywords: Proximate Composition, Anti-Nutritive Factors, Medicinal Mushroom, Ganoderma lucidum, Toxicity.

Kotta Kranthi Kumar, K Kavitha, V Saikishore

The objective of this study was to design Ramipril sustain release bi layer tablets containing immediate release layer and sustain release layer. Tablets were prepared by wet granulation technique using various polymers such as Hydroxy propyl methyl cellulose (HPMC K 100), Sod.CMC, Xanthum gum and Guar gum as release rate retardant and tablets were evaluated for hardness, friability, weight variation, thickness and drug content uniformity. In vitro release studies were performed using USP type II apparatus (paddle method) in 900 mL of pH 6.8 at 50 rpm for 8 hours and compared with USP specification. In vitro release studies revealed that the release rate decreased with increase of polymer loading. The maximum drug release was found to be 98.9% over a period of 8 hours in Xanthum gum based tablets (F11). Drug release was analyzed using zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain the mechanism of drug release from the bi layer matrix tablets. Mathematical analysis of the release kinetics indicated that release from the matrix tablets followed diffusion. So the bi-layer tablets could be a potential dosage form for delivering Ramipril.

Keywords: Ramipril, Bilayer Tablets, Hydrophilic Polymers, Wet Granulation.

Short Communications

Charles O Ezeh, Uzoma J Ngene, Kenechukwu C Onyekwelu

Antibacterial activity of leaf extracts of Heinsia crinita was observed in this work. Heinsia crinita was evaluated for antibacterial activity on Staphylococcus aureus which was gotten from skin surfaces of students of Renaissance University, 26 males and 24 females making a total number of 50 samples through swabbing. Organisms isolated include Staphylococcus aureus, Staphylococcus epidermidis and Bacillus, and because Staphylococcus aureus was the organism of interest it was sub cultured into Nutrient agar plates after which the antibacterial sensitivity testing was carried out. The organism was sensitive to Methanol and Aqueous extract but N-hexane showed no inhibition. The result obtained indicated that female isolates showed more significant effect of antimicrobial activities of leaf extracts of Heinsia crinita against staphylococcus aureus with the value of 25.76MM while for the male showed least significant effect with the value of 22.34MM. It was also found out that for the males: Aqueous extract inhibited the most with the mean value of 4.53MM followed by Methanol extract with the mean value of 3.93MM and N-hexane extract showed no inhibition. For the females, aqueous extract inhibited the most with the mean value of 4.67MM followed by methanol extract with the mean value of 3.93MM while N-hexane extract showed no inhibition. This study justifies the necessity of using Heinsia crinita for medicinal purposes.

Keywords: Antibacterial Activity, Heinsia crinite, Staphylococcus Aureus.

Md Tanwir Alam, Izharul Hasan, Md Zeyauddin, Aisha Perveen

Unani (Greco-Arabian-Indian) System of Medicine (USM) is one of the classic and prestigious therapies among Indian system of medicine. It offers full range of medication through natural products. Various plants and their parts & products are the main source of drugs in USM. Black pepper is the commonest drug being used for range of diseases. Although it is considered as one of the well known spice as well as medicinal plant throughout the Globe but it is the most famous spice used in Indian and Indian sub-continent kitchens. Black Pepper in various forms is good home remedies for lot of common ailments. In USM it is best drug for common cold and cough. In this paper authors try to explain the medicinal aspects of Black pepper in USM.

Keywords: Filfile Siyah, Unani System of Medicine, Kali Mirch, Piper nigrum, Herbal Medicine.

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