Volume 6

April-June 2014

Review Articles

Patil J S, Gurav P B, Mandave S V, Jadhav S M, Kulkarni R G

Hydrogels made from hydrophilic and three dimensional crosslinked polymers are discovered by Wichterle and Lim, since then they have been offered indispensible applications to the biomedical field including pharmaceutical sciences. As these systems have similarity with biological tissues more than any other class of synthetic materials and due to this hydrogels succeeded in attracting the attention of pharmaceutical scientists to explore their use in development of drug delivery systems for various bioactive molecules. The soft consistency, high water content and low interfacial tension with biological fluids of the hydrogel materials made them biocompatible. The unique property of the different sized molecules has an ability to diffuse in and out of hydrogels permitted their use as a carrier for drug delivery system. Further research on these systems resulted into invention of variety of hydrogel forms which are having versatile applications. There is an ampoule scope for preparing these systems as physiological stimuli materials so as to get the desired benefit as and when necessary. The present concise review emphasized mainly on the pharmaceutical and biomedical applications along with other properties of this unique system.

Keywords: Hydrogels, Biocompatible, Stimuli Materials, Pharmaceutical Applications.

Amit Gupta, Pallavi R Khamkar, Sushama Chaphalkar

The immune System is the most complex biological systems in the body. At the time of infection related to viruses, bacteria and fungi only the immune system is able to detect the pathogen by using a specific receptor to produce immediate response by the activation of immune components such as cytokines, chemokines and release of inflammatory mediators to modulate and potentiate the immune system. Modulation of immune response, as a possible prophylactic or therapeutic measure, by using various medicinal plant products has become a subject of scientific investigation. According to Ayurveda, most of the commonly used active ingredients i.e. plant derived materials (alkaloids, glycosides, proteins, lectins, polysaccharides, etc.) are extracted from Indian medicinal plants for the treatment of various ailments and have so many advantages over the conventionally used drugs, which are so expensive and known to have harmful side effects.

Keywords: Cytokines, Pathogen, Ayurveda, Medicinal Plant.

A Krishna Sailaja, P Sashikala

Liposomes have been widely investigated since 1970 as drug carriers for improving the delivery of therapeutic agents to specific sites in the body. There are numerous improvements for the treatment of certain diseases by using this technology. Liposomes can be defined as simple microscopic vesicles in which lipid bilayer structures are present with an aqueous volume entirely enclosed by a membrane, composed of lipid molecule. Liposomes are biodegradable and essentially non‐toxic vehicles. They can encapsulate both hydrophilic and hydrophobic materials, and are utilized as drug carriers in drug delivery. Liposomes are generally classified based upon structure, method of preparation, composition and application. The prepared liposomes are characterized for visual appearance, liposomal size distribution, lamillarity, liposome stability, entrapped volume and surface charges. The liposomes have many applications which increase its importance over other formulations. The current pharmaceutical preparations of liposome-based therapeutic systems mainly result from our understanding of lipid-drug interactions and liposome disposition mechanisms. This review mainly focuses on the advantages and limitations of liposomes, different methods for the preparation and applications of liposomes. In this review discussion was made about the stability problems of liposomes.

Keywords: Multi Lamellar Large Vesicles, Stable Plurilamellar Vesicles, Dehydration‐ rehydration Vesicles, Reverse Phase Evaporation Technique.

Izharul Hasan, Tanwir Alam, Suboohi Irshad

Solanum lycopersicum are widely known for their outstanding antioxidant content, including, of course, their oftentimes rich concentration of lycopene. Researchers have recently found an important connection between lycopene, its antioxidant properties, and bone health. Solanum lycopersicum is low in Sodium, and very low in Saturated Fat and Cholesterol. It is also a good source of Vitamin E (Alpha Tocopherol), Thiamin, Niacin, Vitamin B6, Folate, Magnesium, Phosphorus and Copper, and a very good source of Dietary Fiber, Vitamin A, Vitamin C, Vitamin K, Potassium and Manganese.

Keywords: Solanum lycopersicum, Lycopene.

Research Articles

Ranjitha, Zaheer Abbas, N G N Swamy

A sustained release drug delivery system for acebutolol hydrochloride was designed to increase its residence time in the stomach without establishing contact with the mucosa. This was made possible through the preparation of microballoons by emulsion solvent diffusion-evaporation technique. The prepared microballoons were characterized for physical characteristics such as particle size, particle shape and surface morphology by scanning electron microscopy. Further, percentage yield determination, drug entrapment efficiency, in vitro buoyancy test, micromeritic investigations and in vitro drug release studies were carried out. The obtained microspheres were free flowing, spherical and displayed a particle size ranging from 52.37 to 67.5µm suitable for oral delivery. The drug entrapped in the hollow microspheres increased with the increase in eudragit RSPO content. Scanning electron microscopy and particle size analysis revealed differences in the formulations in respect to their appearance and size distribution. The Fourier Transform Infrared spectroscopy technique and Differential Scanning Calorimetry were carried out to rule out drug – excipients interactions. From the results obtained, it was concluded that there was no interaction between drug and the excipients. The formulation containing acebutolol: eudragit RSPO (1:3 and 1:4) exhibited higher percentage values for buoyancy time. The drug release was found to follow Higuchi kinetics with non-fickian diffusion mechanism, from all the four batches. These preliminary results indicate that acebutolol hydrochloride loaded microballoons could be effective in sustaining drug release for prolonged periods of time.

Keywords: Microballoons, Acebutolol Hydrochloride, Emulsion Solvent Diffusion-evaporation Method, Drug Entrapment Efficiency, Sustained Release.

Attama A A, Ofokansi K C, Kenechukwu F C, Ugwueze M E

The entire plant including the root of Millettia aboensis Hook F. (Fabaceae) has been used in Nigerian folkloric medicine for treatment of veneral diseases, acute malaria, ulcer and liver disorder. The aim of this research was to evaluate the hepatoprotective effect of aqueous and ethanol root extracts of Millettia aboensis (AREMA and EREMA) on carbon tetrachloride-induced liver damage in rats. The extracts (AREMA and EREMA) were studied for their hepatoprotective effect on carbon tetrachloride-induced acute liver damage on Wistar albino rats. The degree of protection was measured using biochemical parameters such as serum enzymes and bilirubin levels. Further, the effects of both extracts on histopathological changes in liver were studied and compared with Liv-52®, a standard hepatoprotective agent. The extracts (AREMA and EREMA) at a dose level of 215 mg/kg and 431 mg/kg produced significant (P<0.05) hepatoprotection by dose dependently decreasing the activity of serum enzymes and bilirubin. While hepatoprotective effect of AREMA was less than that of EREMA, at all dose levels, hepatoprotective effect of the latter (431 mg/kg) was comparable to that of Liv52® (1 mL/kg). The hepatoprotective effect was confirmed by histopathological examination of the liver tissue of control and treated animals. This study has shown that Millettia aboensis root possesses hepatoprotective activity, which resides more in ethanol than aqueous extract. Further experiments are underway to identify the active constituent(s) responsible for the observed hepatoprotective effect and the mechanism(s) of action.

Keywords: Millettia aboensis, Hepatoprotective Effect, Carbon Tetrachloride, Liv-52®.

Yashoda Kambar, ‎Vivek M N, ‎Prashith Kekuda T ‎R, Vinayaka K S ‎

Urinary tract infections are the common infections in community and hospital settings and infect millions of people worldwide every year. The present study was undertaken to determine antibacterial efficacy of extracts of three Parmotrema species viz., P. tinctorum, P. grayanum and P. praesorediosum, macrolichens from Western Ghats of Karnataka, India. The powdered lichen materials were extracted using methanol in soxhlet assembly. Antibacterial activity of lichen extracts was determined against five clinical isolates viz., Staphylococcus aureus, Enterococcus faecalis, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli of urinary tract infection by agar well diffusion assay. The lichen extracts showed dose dependent inhibition of test bacteria. Inhibitory efficacy was highest against Gram positive bacteria than Gram negative bacteria. Overall, high and least inhibitory activity was observed against E. faecalis and K. pneumoniae respectively. The MIC of extracts was found to be least for Gram positive bacteria (0.3 to 0.6mg/ml) than Gram negative bacteria (0.6 to 2.5mg/ml). Thin layer chromatogram revealed the presence of Lecanoric acid, Atranorin, Orsellinic acid, Protolichesterinic acid, Chloroatranorin, Protopraesorediosic acid and Praesorediosic acid in lichen materials. The antibacterial potential of lichen extracts could be ascribed to the presence of secondary metabolites. The Parmotrema species appears to be promising source of agents with inhibitory activity against antibiotic resistant urinary tract pathogens.

Keywords: Western Ghats, Parmotrema, Antibacterial Activity, Urinary Tract Infections.


J N Ravi Varma, M Kranthi Kumar Reddy, C H Pavan Kumar, A Koushik Reddy, P Prudhvi Raju

Present investigation aims colon specific, pulsatile device to achieve time release of Diltiazem, based on chrono-pharmaceutical consideration. Formulations of modified pulsincapdrug delivery of Diltiazem microspheres to achieve timed release in colon. The design consists of an insoluble hard gelatin capsule body, filled with Diltiazem Microspheres prepared by Emulsion-solvent evaporation method employing chitosan in varying ratio and sealed with a hydrogel plug; capsules were coated with 5% ethyl cellulose to prevent variable gastric emptying. Microspheres were evaluated for particle size, entrapment efficiency, SEM, IR and in vitro release study. Optimized microspheres were formulated as pulsatile device with different hydrogel polymers (Sodium alginate, Xanthan gum, Guar gum) and evaluated for dimensions, thickness of CAP and in vitro release kinetics study. Results: Spherical microspheres were confined by SEM with average particle size in range 260 – 360µm. Hydrogel plug showed a lag time of 4-8 hours with release of 83% at the end of 20 hours and followed zero order kinetics. Conclusion: Diltiazem microspheres can be formulated with chitosan. Desired lag period can be achieved and the order of sustaining capacity of pulsatile device is Sodium alginate, Guar gum and Xanthan gum for better maintenance of Angina Pectoris.

Keywords: Angina Pectoris, Chitosan, Diltiazem Microspheres, Pulsatile, Lag time.

Shelke Dattatraya, Vilegave Kailash, Uma A Patil, Vilegave Pratibha

Recent developments in technology have presented viable dosage alternatives for patients who may have difficulties in swallowing tablets or capsules. Conventional tablets and capsules administered with water may be inconvenient or impractical for other patients. In such conditions there is a requirement of fast disintegrating/dissolving tablets (FDT) which can be administered without water. In the present study an attempt to formulate fast dissolving tablets containing Nizatidine-Eudragit E100 complex using direct compression method. The main objective is prepare the Nizatidine complexes with Eudragit E100 to mask the bitter taste of the drug and to prepare fast dissolving tablets containing these complexes to improve patient compliance. The complexes were prepared by solvent evaporation method and spray drying method and were characterized by IR, SEM and DSC to check for chemical integrity, crystallinity and stability. FDTs were prepared by direct compression method using various superdisintegrants like crospovidone(CRP), croscarmellose sodium(CSS) and soypolysaccharide (SYP) in varying range (6-15%). The formulated tablets were evaluated for thickness, hardness, friability, weight variation, wetting time, drug content uniformity, disintegration time and In-vitro dissolution study. It was concluded that CRP was beneficial in decreasing disintegration time of tablets. Solvent Evaporation technique was found to be more suitable and cost effective than spray drying to prepare solid dispersions of Nizatidine in small scale.

Keywords: Eudragit E 100, Nizatidine, Fast Disintegrating/Dissolving Tablets, Crospovidone, Croscarmellose Sodium, Soypolysaccharide.

Saripilli Rajeswari, Sravya Kudamala, Kolapalli Venkata Ramana Murthy

The objective of the present investigation is to formulate gastro retentive floating tablets (GRFT) of clarithromycin for the treatment of Helicobacter pylori, to prolong the gastric residence time after oral administration, at a particular site. Controlled release of drug is especially useful for achieving controlled plasma level as well as for improving bioavailability. The effect of formulation variables on floating lag time, t50 and t90 are also studied. The GRFT contains hydroxypropyl methylcellulose (HPMC) and hydroxyl ethyl cellulose (HEC) as release retarding polymers. The concentration of sodium bicarbonate (NaHCO3) was initially optimized. The tablets were prepared by wet granulation method and evaluated for all their physicochemical properties, in vitro buoyancy, drug release and rate order kinetics. From the results, FHM4 was selected as an optimized formulation based on the polymer concentration, 12 hrs drug release, minimal floating lag time and maximum total floating time. The optimized formulation followed first order rate kinetics with erosion mechanism. The optimized formulation was characterized with FTIR studies and no interaction between the drug and the polymers was observed.

Keywords: Clarithromycin, Gastro Retentive, Hydroxylethyl Cellulose, Hydroxypropyl Methylcellulose, Microcrystalline Cellulose, Sodium Bicarbonate.

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