Volume 3

October-December 2011

Review Articles

Ashish Kumar Verma, M C Bindal

Vesicular system such as liposomes, niosomes, transferosomes, pharmacosomes and ethosomes provide an alternative to improve the drug delivery. Niosomes play an important role owing to their nonionic properties, in such drug delivery system. During the past decade formulation of vesicles as a tool to improve drug delivery, has created a lot of interest amongst the scientist working in the area of drug delivery systems. Design and development of Novel Drug Delivery system (NDDS) has two prerequisites. First, it should deliver the drug in accordance with a predetermined rate and second it should release therapeutically effective amount of drug at the site of action. Conventional dosage forms are unable to meet these requisites. Niosomes are essentially non-ionic surfactant based multilamellar or unilamellar vesicles in which an aqueous solution of solute is entirely enclosed by a membrane resulting from the organization of surfactant macromolecules as bilayer. Niosomes are formed on hydration of non-ionic surfactant film which eventually hydrates imbibing or encapsulating the hydrating aqueous solution. This paper deals with composition, characterization/evaluation, merits, demerits and applications of niosomes. The main aim of development of niosomes is to control the release of drug in a sustained way, modification of distribution profile of drug and for targeting the drug to the specific body site.

Keywords: Niosomes, Lipid Hydration Method, Film Hydration Method, Nonionic Surfactant, Novel Drug Delivery system, Encapsulation, Surfactants, Vesicles.

Gannu Praveen Kumar, A Saraswathi

Niosomes represent a promising targeted drug delivery system for hydrophilic and lipophilic drugs. They present a structure similar to liposome and hence they can be an alternative vesicular system with respect to liposomes. Due to the niosome ability to encapsulate different type of drugs within their multi environmental structure they can be exploited for various treatments of various diseases. Niosomes can be a better drug delivery system as compared to liposomes due to various factors like cost, stability. Various routes of drug delivery and drug targeting can be achieved using niosomes.

Keywords: Niosomes, Liposome, Targeting, Ophthalmic, Topical, Parentral.

J S Mulla, Naveen Kumar Sharma, I M Khazi


Solid lipid nanoparticles (SLN) have been established as an alternative particulate carrier system. Recently, increasing attention has been focused on these SLN as colloidal drug carriers combining advantages of polymeric nanoparticles, fat emulsions, and liposomes, but simultaneously avoiding some of their disadvantages. Under optimized conditions, SLNs can be produced to incorporate lipophilic or hydrophilic drugs and seem to fulfill the requirements for an optimum particulate carrier system. This review describes the characterization of SLN such as particle size, zeta potential, surface morphology, lipid crystallinity, rheological properties etc.

Keywords: Solid Lipid Nanoparticles, Particle Size, Zeta Potential, Differential Scanning Calorimetry.

Research Articles

Tarek A Ahmed, Basher E Abd Elaziz, Mamdouh M Elmoemen, Abd Elmoniem H Hotah

The rationale behind this study was to develop a topical tea tree oil formulation and to evaluate its usefulness as a new therapy in the treatment of burns. Melaleuca alternifolia (tea tree) oil 5% cream was prepared, characterized, and compared to silver sulphadiazine (SSD) 1% which is the most frequently used topical therapy as regard the pain, infection, healing and epithelization. The healing was achieved in 90% of patients of study group within two weeks, in comparison to 80% of patients of control group. No local irritation of skin was reported in study group but two patients were reported in control group. Melaleuca alternifolia (tea tree) oil topical formulation showed an apparent anti-inflammatory effect , reduce edema and erythema that occurs after burn, and showed analgesic effect by relief the pain shortly after use, so the patient would not need further analgesic treatment as those under treatment with SSD cream.

Keywords: Tea Tree Oil, Topical, Silver Sulphadiazine, Burns.

Hitendra S Mahajan, Sonali B Dinger

Nanoemulsion system with Tween 80, campul PG8 as surfactant and ethyl oleate as oil was developed for intranasal delivery of artemether. The selected nanoemulsion system is evaluated for particle size, zeta potential and stability. Ex vivo studies like permeation and histological examination were also carried out. The oil in water type nanoemulsion system was obtained containing 2:1 ratio of surfactant and co surfactant. The nanometric size of globule was retained even after 100 times dilution with water. The negative zeta potential reveals anionic charge on surface of globule. The ex vivo permeation of artemether across nasal mucosa is rapid. This improved permeation of artemether was result of presence of surfactant which reduces the interfacial tension at the mucosal surface nearly to zero. The enhanced permeation also explained in terms of large surface area of the nanoemulsion droplets. Histological examination of nasal mucosa did not detect any damage during in vitro permeation studies. This study points to the potential of nasal nanoemulsion in terms of ease of administration, improved permeation across the nasal mucosa and safety. This novel mode of administration may consider as an alternative to conventional treatment of cerebral malaria.

Keywords: Nanoemulsion, Nasal, Malaria, Artemether.


Ravi Kumar Nayak, Narayana Swamy V B, Senthil A, Mahalaxmi R

In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of Losartan Potassium. Sustained release matrix tablets were developed using different drug polymer ratios and prepared by direct compression method. The influence different concentrations and nature of polymer was studied. The tablets were evaluated for preformulation studies like angle of repose, bulk density, compressibility index and physical characteristics like hardness, weight variation, friability and drug content. In-vitro release of drug was performed in PBS pH 6.8 for 24 hours. All the physical characters of the fabricated tablet were within acceptable limits. Drug-excipient interaction was evaluated by Differential scanning calorimetry and FTIR. There was no drug excipient interaction. The tablet with xanthan gum (F4) in the ration of drug: polymer (1:2) exhibited greater swelling index and better dissolution profile than those with pectin, xanthan gum, sodium alginate and pectin. Optimized tablet formulation (F4) containing xanthan gum showed no change in physical appearance and dissolution profile upon storage at 40°C/75% relative humidity for three months. The drug release of optimized formulation follows the Higuchi kinetic model, and the mechanism is found to be non-Fickian /anomalous according to Korsmeyer–Peppas equation. Compared to conventional tablets, release of losartan potassium from these matrix tablets was prolonged, leading to achieve an effective therapy with low dosage of the drug, to reduce the frequency of medication.

Keywords: Guar Gum, Pectin, Xanthan Gum, Sustained Release Matrix Tablets, Losartan Potassium.

J S Mulla, A Y Khan, S I Panchamukhi, M A Khazi, M B Kalashetti, I M Khazi


A series of 5,6-disubstituted imidazo[2,1-b][1,3,4]thiadiazoles were synthesized. The structures of newly synthesized compounds were characterized by spectral and analytical data. All the title compounds were tested for their in-vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using AlamarBlue susceptibility test, and the activity is expressed as the minimum inhibitory concentration (MIC) in μg/mL. Among the series, compounds 3a, 3c, 4a, 5c and 6a displayed an encouraging antitubercular activity profile as compared to the reference drug, rifampicin.

Keywords: imidazo[2,1 -b][1,3,4]thiadiazole, Mannich Reaction, Antitubercular Activity.

Natasha Sharma, Neelam Balekar, D K Jain

The present investigation concerned with the development of Hydrodynamically Balanced Tablets of Ranitidine, which after oral administration are designed to prolong the gastric residence time and there by increase drug bioavailability. Preliminary trial batches were prepared and the best combination was selected on the basis of the floating behavior (floating time, total floating lag time). Than Ten batches of tablets were fabricated containing drug, and various grades of polymers HPMC K4M, HPMC K15M, HPMC K100M, HPMC 15cps, HPMC 3cps, and carbopol, along with gas generating agent sodium bicarbonate and calcium carbonate with acidulent adipic acid by using wet granulation technique to study the effect on these polymers on floating behaviors. The physicochemical properties of different formulations, their buoyancy lag time and total floatation time and swelling index were evaluated. It is found that the high viscosity grade polymers given better controlled release drug profile. The in vitro release studies (USP XXIII) indicated that the floating dosage forms containing (F9) HPMC K100M high viscosity grade polymer with calcium carbonate (effervescing compound) instead of sodium bicarbonate showed good drug release rate up to 12 h in comparison to other batches. The results indicate that gas powered hydrodynamically balanced tablets of ranitidine containing HPMC K100M provides a better option for controlled release action and improved bioavailability.

Keywords: Gastric Residence, Gas Generation, Swelling Index, HPMC, Floating Tablet.

Ashutosh Meher, Sanjaya Kumar Panda, Anuj Kumar Agrahari, Amiya Ranjan Pradhan, Ranjan Bhoi

The plant Heliotropium indicum L. commonly known as “Hatisundha” in Oriya belongs to family Boraginaceae, a small fragrant evergreen annual herb. The plant is medicinnaly important which is used to cure various diseases like fever, inflammation, wound, tumour and flatulence in Indian traditional system of medicine. Pharmacognostical investigation of fresh, powdered and anatomical section of stem was carried out to determine its macromorphological, micromorphological and chemomicromorphological profiles. Phytochemical evaluation indicated the preparation of extract and preliminary phytochemical screning carried out for identification of alkaloids, glycosides and carbohydrates, saponins, phenolic compounds, flavonoids, phytosterols. The result of the study can be useful in the identification of the drug and establishing pharmacopoeia standards.

Keywords: Hatisundha, Heliotropium indicum L., Boraginaceae, Pharmacognostical, Phytochemical Evaluation.

Short Communications

Prakash Dabadi, B C Koti, A H M Vishwanath Swamy, Chandrakala

Antianthelmintic activity of successive extracts (petroleum ether chloroform, acetone and ethanol) of Mimusops elengi bark were evaluated separately on adult Indian earthworm (Pheretima posthuma) and compared with that of albendazole. It was found that the extracts exhibited respectively dose-dependent action and inhibition of spontaneous motility (paralysis) and death of earthworms. The results indicated that the alcoholic and chloroform extracts were more potent.

Keywords: Anthelmintic Activity, Mimusops Elengi, Paralysis and Death, Pheretima Posthuma.

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