Volume 4

January-March 2012

Review Articles

Zaheer Abbas, Sachin, Swamy N G N

Drug actions can be improved by developing new drug delivery systems; one such formulation being a mucoadhesive system. These systems remain in close contact with the absorption tissue, the mucous membrane, releasing the drug at the action site leading to increased bioavailability for both local and systemic effects. Over the last few decades, the application of mucoadhesive polymers in nasal drug delivery systems has gained interest among pharmaceutical scientists as a means of promoting dosage form residence time in the nasal cavity as well as for improving intimacy of contact with absorptive membranes of the biological system. In addition, the enhanced paracellular absorption following the swelling of the mucoadhesive polymers on the nasal membranes provides an important way for the absorption of the macromolecules through the nasal cavity. This review describes some aspects of mucoadhesion related to the nasal drug delivery system. On the first count, the theories of the adhesion of mucoadhesive polymers to the mucosa epithelium are described. Secondly, the characteristics and application of several widely used mucoadhesive polymers in nasal drug delivery are presented. The mucoadhesive polymers have enormous potential for the delivery of therapeutic macromolecules, genes, and vaccines through the nasal cavity with enhanced bioavailability.

Keywords: Mucoadhesion, Mucoadhesive Polymers, Mucociliary Clearance, Nasal Drug Delivery, Absorption Enhancers.

Anita Patel, Jayvadan Patel

The vagina, distinct than other systems like buccal or gastrointestinal, is highly dynamic with respect to its physiology, which renders the vaginal environment an uncertainty factor with respect to retention of vaginal dosage forms, absorption of drugs, their metabolism and their elimination from the vagina. Conventionally, vaginal delivery was restricted to locally acting drugs such as antibacterial, antifungal, anti-viral, spermicidal, labour-inducing agents, prostaglandins and steroids. Although with time, the potential for systemic delivery through vagina was explored because of its large surface area, high vascularity, and permeability to a wide range of compounds including peptides and proteins. It suggests a constructive substitute to oral and parenteral route. On the other hand, several drawbacks like cultural sensitivity, personal hygiene, gender specificity, local irritation need to be addressed during the design of a vaginal formulation. Presently available vaginal formulations have limitations, such as leakage, messiness and low residence time, which contribute to poor subject or patient compliance. Attempts are being made to develop novel vaginal drug delivery systems that can meet the clinical as well as the user’s requirements. This review will focus on the various aspects, scope and potential of vaginal drug delivery.

Keywords: Vaginal Drug Delivery, Vaginal Formulation, Retention, Mucoadhesion.

Neha Singh, Tamizh Mani T, Dev Prakash, Prashant Singh

Ichnocarpus frutescens, is a large, much-branched twining shrub, containing white latex in its all parts. Leaves 4.5-7.5 cm long, elliptic-oblong, acute or acuminate. Flowers small, greenish white, numerous, in axillary and terminal rusty-pubescent trichotomous pedunculate cymes. Fruit a follicle, 10-15 cm long, slender, cylindric. English name: Black Creeper. The roots are employed as a substitute for Sarsaparilla; it is cooling, demulcent, alterative, tonic, diaphoretic and diuretic; used in fever, dyspepsia, skin troubles, diabetes and stone in the bladder. A decoction of the stems and leaves is used in fevers. Leaves are applied to headaches, wounds and sore between fingers. Marma use root in dental caries and stems and leaves for scabies. In the present review an attempt has been made to explore a literature survey on its pharmacological properties. The whole plant as well as specific parts such as roots, leaves and flowers have been widely used and claimed against different activities.

Keywords: Ichnocarpus frutescens, Black Creeper, Sarsaparilla, Marma, Pharmacological Properties.

Research Articles

Lucky Lebgosi Nwidu, Paul Alozie Nwafor, Wagner Vilegas

The leaf of Carpolobia lutea G. Don (Polygalaceae) is widely used among the Ibibio and Efik in Nigeria to control psychotic patient by sedation. This antipsychotic effect among other uses of the plant is yet to be investigated pharmacologically. This is a first report of neuropharmacological screening of the leaf. Gradient extraction was executed after maceration of air-dried leaf of C. lutea in n-hexane, chloroform, ethyl acetate and ethanol solvent for 72 hours to obtain the four fractions. The effects of these four fractions of the leaf (192.5-770mg/kg) were investigated on thiopentol-induced sleeping time, locomotor activity, pentylenetetrazole (PTZ) – and strychnine (STN)-induced convulsion in mice. The most active fraction, ethyl acetate fraction, was submitted to semi- preparative HPLC to structurally isolate and characterized active compounds. The ethyl acetate fraction reveal a dose dependent significant (P < 0.01) prolongation of sleeping time duration but no effect on sleeping time latency when compared with control group. The ethyl acetate fraction reveals a dose dependent significant (p < 0.05- 0.001) decrease on locomotor activity. In the anticonvulsant assay, it demonstrates 60% and 40% protection in the PTZ- and strychnine-induced convulsion in mice respectively. The effects of other fractions were not as significant compared to the ethyl acetate fraction. Five polyphenols were isolated, the first four molecules is reported for the first time. The neuropharmacological screening results and isolated compounds could in part lend credence to antipsychotic ethnomedical uses of C. lutea in management of mad people in Akwa Ibom State of Nigeria.

Keywords: Carpolobia lutea, Psychopharmacology, Neuropharmacology, Anticonvulsant.

K Bhaskar Reddy, M Jyostna, N Audinarayana, C Madhavi Latha, E Mohanambal

Nitrendipine (NDP), a dihydropyridines calcium antagonist which has a very low solubility in vitro was used as a poorly water-soluble model drug. The percutaneous permeation of nitrendipine was investigated in rat skin after application of a water–propylene glycol (50:50% v/v) using a diffusion cell technique. The effect of various surfactants such as sodium lauryl sulphate (SLS), benzalkonium chloride and Tween 80 with different concentrations on skin permeability were evaluated. Flux, Kp, lag time and enhancement ratios (ERs) of nitrendipine were measured over 12 h and compared with that of control sample. Furthermore, solubility in presence of surfactants was determined. The in vitro permeation experiments with rat skin revealed that the surfactant enhancers varied in their ability to enhance the flux of nitrendipine and the flux of benzalkonium chloride provided the greatest enhancement for nitrendipine flux (5.858±0.145 μg/cm2/h, 3 fold over control) at 1% w/w of the surfactant. SLS at a concentration of 5% w/w (the highest concentration) exhibited the greatest increase in flux of nitrendipine compared with control (6.103±0.221 μg/cm2/h, 3.5 fold over control). Tween 80 at a concentration of 1% w/w exhibited significant increase in flux of nitrendipine compared to control (5.607±0.187, 1.9 fold over control). The results also showed that the highest ER was obtained in presence of 1% w/w surfactant with the exception of SLS. The increase in flux at low enhancer concentrations is normally attributed to the ability of the surfactant molecules to penetrate the skin and increase its permeability. The results showed that the nature of enhancer greatly influences cutaneous barrier impairment. The surfactants have shown ability to enhance the permeation of nitrendipine across rat skin.

Keywords: Nitrendipine, Tween 80, Sodium Lauryl Sulfate, Permeability.

Kuntal Das, Raman Dang, Manjunath U Machale, Ugandar R E, Lalitha B R

In the present work, herbal vanishing cream based drug formulations (2.5% and 5.0%) were designed and prepared for the skin moisturizer with Stevia white extract. The creams were O/W emulsion based formulations containing suitable combination of oil phase and aqueous phase along with preservatives. Both the creams were non greasy, coolant and pearl like appearance. They were subjected to various physicochemical parameters i.e. pH, viscosity, spreadability, tube extrudability and drug content studies. Stability studies of creams were also done at different temperature for the period of 3 months as per ICH guideline and results revealed both the formulations showed good stability over control preparation. Amount of active constituent present, pH, spreadability, tube extrudability of the formulation were found to be 7.47 mg and 3.64 mg; 6.70-6.80, 16.11- 16.12 gm.cm/sec; 92.38% – 92.40 % for 5% and 2.5% Stevia cream respectively. Furthermore, both the formulations were studied for primary skin irritation test in rabbit and 30 numbers of healthy human volunteers for 48 hours and observed for skin rashes, inflammation, itching or redness on applied portions. Results revealed no adverse skin reactions with all the formulations. It was proved that vanishing cream containing Stevia extract is pleasant, effective, easily washable and completely safe for human use.

Keywords: Physicochemical Parameters, Patch Test, Stevia Extract, Skin Irritation.


Nwachukwu C Daniel, Okwuosa N Chukwugozie

The gastroprotective ability of chloroform leaf extract of Aspilia africana against ulcer was investigated using male albino wistar rats. Aspirin was used to induce ulcer in the gastric mucosa while omeprazole was the standard anti-ulcer drug used. Phytochemical analysis revealed the presence of alkaloids, saponins, flavonoids, steroids, terprenoids, proteins and tannins. Acute toxicity test showed an oral LD50 greater than 5000mg/Kg. Results showed that chloroform leaf extract at different doses of 250mg/Kg and 500mg/Kg demonstrated significant protection against ulcer with mean ulcer indices of 5.04 ± 1.20 and 0.84 ± 0.15 respectively compared with negative control (3% Tween 80) with mean ulcer index of 9.42 ± 0.73. The higher dose of the extract demonstrated greater protective ability with percentage ulcer protection (91.1%) similar to that of omeprazole (92.8%). Thus, chloroform extract of Aspilia africana was able to protect the stomach against ulceration caused by aspirin.

Keywords: Aspilia Africana, Chloroform Extract, Ulcer, Omeprazole, Gastroprotection.

Aliasgar J Kundawala, Vishnu A Patel, Harsha V Patel, Dhaglaram Choudhary

Microparticles containing antitubercular agent, Rifampicin, was prepared and evaluated for its suitability as respirable dry powder formulation for lung delivery. Chitosan solution containing rifampicin, lactose and leucine in different ratio was spray dried. Ascorbic acid was used in concentration of 200µg/ml as antioxidant. The other physical properties of prepared microparticles like Particle size, morphology, densities and aerodynamic diameter were determined. Solid state of microparticles was characterized by Differential scanning calorimetry (DSC) and X-ray diffraction studies. The fine particle fraction and emitted dose required for a good aerosol performance was determined by Andersen Cascade Impactor. Microparticle with maximum drug loading of 98.31 and particle size in range 5-7µm was obtained with % yield of ≤ 43 %. Satisfactory aerosol properties like FPF (47.29 %), emitted dose up to 92 % and theoretical aerodynamic diameter less than 3.62 µm were obtained. The in vitro drug release from chitosan microparticles was found to be slow and up to 68 to 84 % in 6 hrs. When drug release data were plotted in Ritger and Peppas model, all formulations except controlled formulation showed fickian diffusion kinetic. The present study revealed that the rifampicin loaded chitosan microparticles produced by spray drying showed good physicochemical properties deemed suitable for inhalation therapy.

Keywords: Respirable Dry Powder, Chitosan Microparticle, Rifampicin, Spray Drying.

Suman Malik, Vinod Gauttam, Krishna Reddy V Bijjem, Ajudhia Nath Kalia

The present study was aimed to screen Cassia obtusifolia leaves for antiinflammatory potential using carrageenan-induced paw edema and cotton pelletinduced granuloma models in Wistar rats. In this study, 90% methanol extract at two dose levels (250 and 500 mg/kg, p.o.) and n-Butanol fraction of methanol extract (50 and 100 mg/kg, p.o.) were studied in carrageenan-induced paw edema model. The methanol extract (500 mg/kg) and n-Butanol fraction of methanol extract (50 and 100 mg/kg) showed significant (p<0.05) anti-inflammatory potential in this model, Moreover, the anti-inflammatory effect of n-Butanol fraction of methanol extract at the dose of 100 mg/kg was comparable to diclofenac sodium (20 mg/kg, p.o). Therefore, n-Butanol fraction of methanol extract (50 and 100 mg/kg, p.o.) have been further evaluated in cotton pellet induced granuloma model. Preliminary phytochemical screening of the n-Butanol fraction of methanol extract revealed the presence of glycosides, steroids, flavonoids and triterpenoids. The present study hence proved the anti-inflammatory potential of methanol extract of Cassia obtusifolia leaves. On further fractionation, the n-Butanol fraction has potentiated the therapeutic efficacy.

Keywords: Anti-inflammatory, Granuloma, Cassia obtusifolia, Carrageenan.

Shete A S, Yadav A V, Sfurti Sakhare

Niosomes have been extensively investigated for drug delivery, drug targeting, controlled release and enhancing solubility. The aim of present investigation was to develop and characterize the 5-flurouracil niosomal drug delivery system that will-protect from body immune system (stealth niosomes), prolong drug release. The niosomes were prepared by ether injection method using span 60 as a nonionic surfactant, niosomal dispersion was bath sonicated for different period of time to reduce particle size at or above the phase transition temperature of surfactant. The preformed niosomes were incubated with PEGylated lipid (5mol %) for 30 minuites. The un-entrapped drug was separated by centrifugation. It was observed that with increase in total molar concentration of surfactant and cholesterol, % entrapment efficiency increased. To formulate formulations total concentration of lipid 300µ moles was selected. It was observed that increase in sonication time reduces the particle size of the niosomes. After 15 minutes of sonication average particle size was found to be 244nm. PEGylated lipid coated niosomes were found larger than the conventional ones. In 6-hrs in vitro drug release study PEGylated lipid coated niosomes showed controlled release of 5- FU. Stability study indicates that the PEGylated niosomes showed more drug retention stability than conventional niosomes.

Keywords: Niosomes, 5-flurouracil, Stability, Drug Release.

Devprakash, Sreenivasan K K, Subburaju T, Parag S Mahadik

Primary sources of naturally occurring antioxidants are whole grains, fruits and vegetables. Most of the antioxidant compounds in a typical diet are derived from plant sources and belong to various classes of compounds with a wide variety of physical and chemical properties. Some compounds, such as gallates, have strong antioxidant activity, while others, such as the mono-phenols are weak antioxidants. The main characteristic of an antioxidant is its ability to trap free radicals. These free radicals may oxidize nucleic acids, proteins, lipids or DNA and can initiate degenerative disease. Antioxidant compounds like phenolic acids, polyphenols and flavonoids scavenge free radicals such as peroxide which inhibit the oxidative mechanisms that lead to degenerative diseases. Oxidative damage plays a significantly pathological role in human disease. Free radicals lead to cellular necrosis, which is implicated in some membrane pathophysiological conditions including atherosclerosis, rheumatoid arthritis as well as toxicity of many xenobiotic, ischemia and injury of many tissues, central nervous system injury, gastritis, ageing, inflammatory response syndrome, respiratory diseases, liver diseases, and cancer. Many herbal plants contain antioxidant compounds and these compounds protect cells against the damaging effects of reactive oxygen species (ROS), such as singlet oxygen, superoxide, hydroxyl radicals and peroxy nitrite. The plant Tinospora cordifolia was selected based on Ayurvedic literature claim many medicinal uses. So the plant was subjected to antioxidant studies. Result shows better activity in case of aqueous extract prepared from fresh plants compared to ethanolic extract of dried plant. The plant Tinospora cordifolia was selected based on Ayurvedic literature claim many medicinal uses. So the plant was subjected to antioxidant studies. Result shows better activity in case of aqueous extract prepared from fresh plants compared to ethanolic extract of dried plant.

Keywords: Antioxidant, Aqueous Fresh Extract, Ethanolic Extract, DPPH, Cavenging.

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