The blood brain barrier (BBB) represents one of the strictest barriers of in vivo therapeutic drug delivery. The barrier is defined by restricted exchange of hydrophilic compounds, small proteins and charged molecules between the plasma and central nervous system (CNS). For decades, the BBB has prevented the use of many therapeutic agents for treating Alzheimer's disease, stroke, brain tumor, head injury, spinal cord injury, depression, anxiety and other CNS disorders. Different attempts were made to deliver the drug across the BBB such as modification of therapeutic agents, altering the barrier integrity, carrier-mediated transport, invasive techniques, etc. However, opening the barrier by such means allows entry of toxins and undesirable molecules to the CNS, resulting in potentially significant damage. An attempt to overcome the barrier in vivo has focused on bypassing the BBB by using a novel, practical, simple and non-invasive approach i.e. intranasal delivery. This method works because of the unique connection which the olfactory and trigeminal nerves (involved in sensing odors and chemicals) provide between the brain and external environments. The olfactory epithelium acting as a gateway for substances entering the CNS and peripheral circulation is well known. Also, it is common knowledge that viral infections such as common cold, smallpox, measles, and chicken pox take place through the nasopharynx. The neural connections between the nasal mucosa and the brain provide a unique pathway for the non-invasive delivery of therapeutic agents to the CNS. This pathway also allows drugs which do not cross the BBB to enter the CNS and it eliminates the need for systemic delivery and thereby reducing unwanted systemic side effects. Intranasal delivery does not require any modification of therapeutic agents and does not require that drugs be coupled with any carrier. A wide variety of therapeutic agents, including both small molecules and macromolecules can be rapidly delivered to the CNS using this method. The present review discusses the various applications, advantages and limitations of this novel approach.

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OBJECTIVE: To evaluate the antiinflammatory and analgesic activities of the aqueous extract of Spilanthes acmella (SPA) in experimental animal models. MATERIAL AND METHODS: SPA was evaluated for antiinflammatory action by carrageenan-induced rat paw edema. The analgesic activity was tested by acetic acid-induced writhing response in albino mice and tail flick method in albino rats. RESULTS: The aqueous extract of SPA in doses of 100, 200 and 400 mg/kg showed 52.6, 54.4 and 56.1% inhibition of paw edema respectively at the end of three hours and the percentage of protection from writhing was 46.9, 51.0 and 65.6 respectively. In the tail flick model, the aqueous extract of SPA in the above doses increased the pain threshold significantly after 30 min, 1, 2 and 4 h of administration. SPA showed dose-dependent action in all the experimental models. CONCLUSION: The present study indicates that SPA has significant antiinflammatory and analgesic properties.

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Platelets play a key role in atherosclerosis, thrombosis and acute coronary syndromes. Drugs that dissolve blood clot (thrombolytic agents) and that prevent clot propagation (antiplatelet and anticoagulant agents) are used to treat a broad array of cardiovascular diseases. Therapeutic manipulation of platelet function has focused principally on the use of aspirin which has proved effective in many clinical situations, despite its relatively weak antiplatelet action as compared to newer agents like ticlopidine, clopidogrel and more recently, platelet glycoprotein (GP) IIb/IIIa receptor inhibitors. The platelet GP IIb/IIIa receptor has been identified as a pivotal mediator of platelet aggregation, making it a logical target for the control of the platelet response to vascular injury. The primary mechanism of GP IIb/IIIa antagonists is the inhibition of the final common pathway of platelet aggregation: fibrinogen binding to the GP IIb/IIIa complex. Various antagonists of the GP IIb/IIIa receptor are currently receiving considerable attention and are being investigated for various clinical settings including angina, myocardial infarction and interventional cardiology.

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OBJECTIVE: To evaluate the cardiac effects of extracts derived from the aerial parts of Ocimum basilicum Linn. MATERIAL AND METHODS: The aerial parts of Ocimum basilicum Linn. were extracted with 95% ethanol and double distilled water. The extracts were screened for their effects on frog-heart in situ preparation. Enzyme studies such as Na+/K+ ATPase, Ca2+ATPase and Mg2+ATPase were done on the heart tissue aspartate transaminase (AST), alanine transaminase (ALT), lactate dehydrogenase (LDH) and creatine phosphokinase (CPK) were estimated in the heart tissue and serum of albino rats after administering the extracts for 7days. RESULTS: The alcoholic extract produced significant positive ionotropic and negative chronotropic actions on frog heart. The positive ionotropic effect was selectively inhibited by nifedipine. A significant decrease in membrane Na+/K+ ATPase, Mg2+ATPase and an increase in Ca2+ATPase pointed the basis for the cardiotonic effect. The aqueous extract produced positive chronotropic and positive ionotropic effects which were antagonized by propranolol indicating that these might have been mediated through ß-adrenergic receptors. Nifedipine also blocks the action of the aqueous extract. CONCLUSION: The alcoholic extract exhibited a cardiotonic effect and the aqueous extract produced a ß-adrenergic effect.

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OBJECTIVE: To investigate the neuropsychopharmacological effect of a polyherbal formulation Bramhi Ghrita (BG) on learning and memory processes in rats by elevated plus maze, and in mice by Morris water maze model. MATERIAL AND METHODS: BG contains Bacopa monneri (Bramhi), Evolvulus alsinoids, Acorus calamus, Saussurea lappa and cow's ghee. Its effect (30, 50 and 100 mg/kg, p.o.) was tested on learning and memory processes. The activity of BG on memory acquisition and retention was studied using elevated plus maze model (EPM) in rats, and on spatial memory using Morris water maze model (MWM) in mice. The alcoholic extract of Bacopa monneri (40 mg/kg, p.o.) was also administered to one group of animals. The results were compared with the vehicle-treated group. RESULTS: Administration of Bramhi Ghrita (50 and 100 mg/kg, p.o.) showed significant reduction in transfer latency in EPM and escape latency in MWM as compared with the control group. CONCLUSION: BG may act as a memory enhancer formulation and may also be useful as a supportive adjuvant in the treatment of impaired memory functions.

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OBJECTIVE: To determine the opinion of students regarding the teaching of pharmacology, the best way of knowing and retaining the subject and application of the subject in future practice. MATERIAL AND METHODS: A questionnaire was designed and given to Second-year medical students who were due to appear for examination. They were supposed to fill in and make suggestions according to the options given and were also free to express their own opinion at various places. RESULTS: Fifty-one out of sixty-three students (81%) wanted introduction of case studies and therapy as part of regular teaching. They wanted the teachers to make use of audiovisual aids during the lectures. About one third of the students (22/63; 35%) felt that more group discussions should be introduced during teaching sessions. Even fewer (7/63; 11%) opted for finer aspects of clinical pharmacology including drug schedules, dosage calculations, and drugs used in special situations. According to them students' seminars should be discouraged. CONCLUSION: Students are interested in learning the subject from a futuristic practical therapeutic point of view.

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OBJECTIVE: To study whether the increasing doses of omeprazole, lansoprazole and famotidine afford protection against ethanol-induced gastric damage and to compare their antioxidant effect with that of melatonin. MATERIAL AND METHODS: Mucosal damage was evaluated by macroscopic examination and by the measurement of lipid peroxidation (LPO), glutathione (GSH) levels and myeloperoxidase (MPO) activity. RESULTS: Ethanol administration-induced significant gastric damage, increased gastric acidity, and LPO and MPO activities, while tissue GSH levels decreased. The antiulcer drugs decreased the gastric acidity in a dose-dependent manner, whereas melatonin had no effect on this parameter. Biochemical parameters of oxidative damage, namely gastric LPO and GSH levels and MPO activities were reversed by both the antiulcer drugs and melatonin in a dose-dependent manner. CONCLUSION: These findings suggest that, parallel to increased acidity, reactive oxygen species have an important role in the pathogenesis of ethanol-induced gastric damage, and that melatonin, famotidine, lansoprazole and omeprazole are protective by their antioxidant property. However, according to our findings, inhibition of acid secretion is as important as the inhibition of oxidative damage in affording protection against ethanol-induced damage, and in this aspect melatonin seemed to be less efficient than the antiulcer drugs.

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OBJECTIVE: To evaluate the gastroprotective effects of 3-adrenoceptor agonists CGP 12177A and SR 58611A, on water immersion plus restraint stress (WIRS)-induced gastric ulceration in rats. MATERIAL AND METHODS: Drugs were administered (5, 10 and 15 mg/kg, p.o.) 30 min prior to the ulcerogenic procedure. Ulcer index and the score for intensity of intraluminal bleeding were determined. Gastric wall mucus content (GWMC) and mast cell counts were determined in the glandular portion of the stomach. RESULTS: A dose-dependent reduction in the ulcer index was observed with both the drugs. A significant rise in the GWMC in the glandular tissue at 15 mg/kg dose was caused by the 3-adrenoceptors agonists. In the glandular tissue the mast cell count was significantly decreased at 10 and 15 mg/kg dose with both drugs. CONCLUSION: The present study shows the gastroprotective effect of 3-adrenoceptor agonists CGP 12177A and SR 58611A against WIRS-induced gastric ulceration in rats. The gastroprotective effect may be mediated by the enhancement of mucin activity and the decrease in mast cell degranulation.

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OBJECTIVE: To develop Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) method for the estimation of adenosine A1 receptor mRNA levels in rat kidney. MATERIAL AND METHODS: Total cellular RNA was isolated from whole rat kidney by small-scale total RNA preparation protocol and it was reverse transcribed into cDNA. The cDNA was subjected to PCR amplification using gen specific primers. The amplified cDNA was evaluated by gel electrophoresis and the intensity of the bands were visualized and quantitated with a FujiBAS 1000 PhosphorImager. Then the adenosine A1 receptor mRNA levels were extrapolated from the standard curve. RESULTS: Adenosine A1 receptor mRNA levels in rat kidney were measured as: 1.30 ± 0.17 X 107 copies of adenosine A1 receptor transcript/mg total RNA. CONCLUSION: The RT-PCR method developed for the estimation of adenosine A1 receptor mRNA levels in rat kidney is sensitive and reliable.

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