Awani K Rai

Cyclodextrins in delivery systems: Applications.

Cyclodextrins (CDs) are a family of cyclic oligosaccharides with a hydrophilic outer surface and a lipophilic central cavity. CD molecules are relatively large with a number of hydrogen donors and acceptors and, thus in general, they do not permeate lipophilic membranes. In the pharmaceutical industry, CDs have mainly been used as complexing agents to increase aqueous solubility of poorly soluble drugs and to increase their bioavailability and stability. CDs are used in pharmaceutical applications for numerous purposes, including improving the bioavailability of drugs. Current CD-based therapeutics is described and possible future applications are discussed. CD-containing polymers are reviewed and their use in drug delivery is presented. Of specific interest is the use of CD-containing polymers to provide unique capabilities for the delivery of nucleic acids. Studies in both humans and animals have shown that CDs can be used to improve drug delivery from almost any type of drug formulation. Currently, there are approximately 30 different pharmaceutical products worldwide containing drug/CD complexes in the market.

Stimuli sensitive hydrogels for ophthalmic drug delivery: A review

Amongst the various routes of drug delivery, the field of ocular drug delivery is one of the most interesting and challenging endeavors facing the pharmaceutical scientist for past 10-20 years. As an isolated organ, eye is very difficult to study from a drug delivery point of view. Despite this limitation, improvements have been made with the objective of maintaining the drug in the biophase for an extended period. A major problem in ocular therapeutics is the attainment of an optimal drug concentration at the site of action. To achieve effective ophthalmic therapy, an adequate amount of active ingredient must be delivered and maintained within the eye. The most frequently used dosage forms, i.e., eye solution, eye ointments, eye gels, and eye suspensions are compromised in their effectiveness by several limitations leading to poor ocular bioavailability. Ophthalmic use of viscosity-enhancing agents, penetration enhancers, cyclodextrins, prodrug approaches, and ocular inserts, and the ready existing drug carrier systems along with their application to ophthalmic drug delivery are common to improve ocular bioavailability. Amongst these hydrogel (stimuli sensitive) systems are important, which undergo reversible volume and/or sol-gel phase transitions in response to physiological (temperature, pH and present of ions in organism fluids, enzyme substrate) or other external (electric current, light) stimuli. They help to increase in precorneal residence time of drug to a sufficient extent that an ocularly delivered drug can exhibit its maximum biological action. The concept of this innovative ophthalmic delivery approach is to decrease the systemic side effects and to create a more pronounced effect with lower doses of the drug. The present article describes the advantages and use stimuli sensitive of hydrogel systems in ophthalmic drug delivery.

Carbon nanotubes as a novel drug delivery system for anticancer therapy: a review

Carbon nanotubes (CNTs) were discovered in 1991 and shown to have certain unique physicochemical properties, attracting considerable interest in their application in various fields including drug delivery. The unique properties of CNTs such as ease of cellular uptake, high drug loading, thermal ablation, among others, render them useful for cancer therapy. Cancer is one of the most challenging diseases of modern times because its therapy involves distinguishing normal healthy cells from affected cells. Here, CNTs play a major role because phenomena such as EPR, allow CNTs to distinguish normal cells from affected ones, the Holy Grail in cancer therapy. Considerable work has been done on CNTs as drug delivery systems over the last two decades. However, concerns over certain issues such as biocompatibility and toxicity have been raised and warrant extensive research in this field.

Pharmacist involvement in the patient care improves outcome in hypertension patients

Objective: The main objective of this study was to assess the effects of pharmaceutical care interventions in patients with essential hypertension in Lakshmi Pat Singhania Institute of Cardiology, Kanpur, India. Methods: The study was carried out from July 2010 to August 2011. Pharmaceutical care was provided for 54 patients (intervention group) which was comprised of the patient education, the prescription assistance and the life style modifications and motivation for health. Then the clinical outcome as well as health related quality of life (HRQOL) were compared with the control group (48 patients) in which the pharmaceutical care was not provided. Furthermore, the effect of pharmaceutical care intervention on HRQOL was assessed using Short Form-36 (SF-36), a general health related quality of life questionnaire used to evaluate the QOL of patients. Blood pressure (BP) measurements and QOL survey was performed at baseline and at the follow-up session. Findings: The difference between blood pressure readings from the baseline to the second follow-up was significant for systolic [(P = 0.0001), 12.24 mmHg] and diastolic BP [(P = 0.001), 5.17 mmHg] in the intervention group. The questionnaire used to evaluate the QOL of patients also showed improvement in the mean score for intervention group. Conclusion: Results from our study showed that applying pharmaceutical care to hypertensive patients can help in the control of these patients’ blood pressure, and consequently lower the risk that hypertension poses in cardiovascular disease. Successful implementation of pharmaceutical care has the potential to increase patients’ satisfaction with their pharmacists’ activities and may increase patients’ expectations that pharmacists will work on their behalf to assist them with their healthcare needs.

FTIR spectroscopy: A tool for quantitative analysis of ciprofloxacin in tablets

A simple, accurate and sensitive spectroscopic method has been proposed for the assay of ciprofloxacin in tablet by least square treatment of fourier transform infrared spectrometric data obtained at the wavenumber corresponding to the carbonyl group centered at 1707 cm-1. The method involves the extraction of the active ingredient with methanol followed by phosphate buffer pH 6.0. The excipients in the commercial tablet preparation did not interfere with the assay. The specifity, linearity, detection limits, precision and accuracy of the calibration curve, drug extraction, infrared analysis and data manipulation were determined in order to validate the method. Moreover, the statistical results were compared with other methods for quantification of ciprofloxacin.

Aliskiren: An orally active renin inhibitor

Renin inhibitors are antihypertensive drugs that block the first step in the renin-angiotensin system. Their mechanism of action differs from that of the angiotensin-converting enzyme inhibitors and angiotensin-receptor antagonists, but like these drugs, renin inhibitors interrupt the negative feedback effects of angiotensin II on renin secretion. The renin–angiotensin–aldosterone system (RAAS) has long been recognized to play a significant role in hypertension pathophysiology. Certain agents that modify the RAAS can control blood pressure and improve cardiovascular outcomes. Optimization of this compound by Novartis led to the development of aliskiren – the only direct renin inhibitor which is clinically used as an antihypertensive drug. Aliskiren is the first of a new class of antihypertensive agents. Aliskiren is a new renin inhibitor of a novel structural class that has recently been shown to be efficacious in hypertensive patients after once-daily oral dosing. In short-term studies, it was effective in lowering blood pressure either alone or in combination with valsartan and hydrochlorothiazide, and had a low incidence of serious adverse effects. It was approved by the Food and Drug Administration in 2007 for the use as a monotherapy or in combination with other antihypertensives. Greater reductions in blood pressure have been achieved when aliskiren was used in combination with hydrochlorothiazide or an angiotensin-receptor blocker. The most common adverse effects reported in clinical trials were headache, fatigue, dizziness, diarrhea, and nasopharyngitis. Aliskiren has not been studied in patients with moderate renal dysfunction; as an RAAS-acting drug, it should be prescribed for such patients only with caution.

Studies on development of controlled delivery of combination drug(s) to periodontal pocket

AIM The aim of this study to develop the controlled delivery of combination drug(s) to periodontal pocket. MATERIALS AND METHODS In the present investigation mucoadhesive gel formulations were prepared using carboxy methylcellulose (CMC), methylcellulose (MC), hydroxyethylcellulose (HEC), polyvinylpirrolidone (PVP), polycarbophil (PC), and poloxamer. Each formulation was characterized in terms of polarizing light microscopy, gelation, gel melting, hardness, compressibility, adhesiveness, cohesiveness, syringeability, adhesion to a mucin disk, rheological studies, drug release, and antibacterial activities. Addition of CMC and PVP to the gel favored hexagonal phase formation. The gelation temperature was decreased linearly with an increasing concentration of drug(s), whereas, the melting temperature increased with the concentration of drug(s). Increasing the concentrations of each polymeric component significantly increased formulation hardness, compressibility, adhesiveness, mucoadhesion, and syringeability, yet a decreased cohesiveness. Increased time of contact between the formulation and mucin significantly increased the required force of detachment. Drug release from all formulations was non-diffusion controlled and significantly decreased as the concentration of the polymer was increased, due to the concomitant increased viscosity of the formulations and the swelling kinetics of PC, following contact with the dissolution fluid. RESULT Antibacterial studies revealed that a gel with 30% HEC had a growth inhibition zone on agar with all three strains. CONCLUSION Formulations containing HEC exhibited superior physical characteristics for improved drug delivery to the periodontal pocket and are now the subject of long-term clinical investigations.

Management of coronary artery disease in a Tertiary Care Hospital

Aims: The objective of the study was to study the prescribing patterns of drugs used in the coronary artery disease (CAD) and to identify, which drug is mostly prescribed at that hospital. Settings and Design: This was a prospective observational survey including case series analysis of patients with CAD who met the inclusion criteria. It was conducted in the cardiology unit of multidisciplinary Tertiary Care Hospital in Kanpur. Materials and Methods: Data of patients who met the inclusion criteria was collected in specially designed case record forms. It was designed to include the patient data such as, demographics, risk factors, clinical and biochemical characteristics, procedures and investigations performed during the hospital stay, in-hospital and discharge drug therapy. Statistical Analysis Used: Descriptive statistics were performed for baseline characteristics, risk factors and medication use. All the analyses were performed using Statistical Package for Social Sciences version 16.0. Results: Subjects of age groups 65-74 (33.34%) were found to be more susceptible to CAD. In this study, we see that Aspirin, Clopidogrel and Statins were mostly prescribed in this hospital. Conclusions: In this study, Aspirin and Clopidogrel were mostly prescribed. According to 2009 focused updates of American College of Cardiology/American Heart Association (ACC/AHA) guidelines for the management of patients with ST-elevation Myocardial Infarction. So in this hospital prescription for CAD were according to the guideline.

Enteric coated HPMC capsules plugged with 5-FU loaded microsponges: a potential approach for treatment of colon cancer

O trabalho teve como objetivo o desenvolvimento de novas capsulas com revestimento enterico HPMC (ECHC) conectadas com microesponjas carregadas com fluoruracila (5-FU) em combinacao com grânuos de pectinato de calcio. O metodo de difusao de solvente modificado quasi-emulsao foi usado para formular microesponjas com base no planejamento fatorial 32 e determinaram-se os efeitos das variaveis independentes (volume de solvente orgânico e conteudo Eudragit RS100) sobre as variaveis dependentes (tamanho de particula, EE% e % CDR). As microesponjas otimizadas (F4) foram caracterizadas por SEM, PXRD, TGA e ligadas aos grânulos de pectinato de calcio em capsulas de HPMC e estas foram, ainda, revestidas com polimero enterico Eudragit L 100 (Ed-L100) e/ou Eudrgit S 100 (Ed S 100) em diferentes proporcoes. No estudo de liberacao in vitro de ECHC foi realizada em varios meios de liberacao sequencial SGF durante 2 h, seguido de SIF para as proximas 6 h, e, em seguida, em SCF (na presenca e na ausencia de enzima pectinase por mais 16 h). A liberacao do farmaco foi retardada em revestimento com a EDS-100, em comparacao com mistura de EDS-100: EDL-100, de revestimento. O percentual de 5-FU liberado de ECHC 3 ao final de 24 h foi 97,83 ± 0,12% em presenca de pectinase, enquanto que para o controle foi de 40,08 ± 0,02% do farmaco. A formulacao otimizada foi submetida a estudos Roentgenograficos in vivo, em coelhos brancos Nova Zelândia, para analisar o comportamento das capsulas desenvolvidas direcionadas ao colon. Os estudos de farmacocinetica em coelhos brancos da Nova Zelândia foram conduzidos para determinar a extensao da exposicao sistemica propiciada pela formulacao desenvolvida, em comparacao com solucao aquosa de 5-FU. Assim, capsulas entericas de HPMC revestidas e conectadas com microesponjas carregadas com 5-FU e grânulos de pectinato de calcio se mostraram promissoras como formulacao para liberacao do farmaco no colon no tratamento do câncer colorretal.

Genetic predisposition to oxcarbazepine induced Stevens-Johnson syndrome

Stevens–Johnson syndrome (SJS) is a rare immunologic reaction that may involve skin or various mucosal surfaces. The etiology may range from multiple pharmacologic agents to viral infections. Associated findings can range from minimal skin and mucosal involvement to extensive dermal exfoliation, nephritis, lymphadenopathy, hepatitis, and multiple serologic abnormalities. We report a female patient of 38 years with a history of drug allergy who was administered oxcarbazepine for the management of right partial bronchial seizure due to left parasagittal mass lesion following which she developed papular rashes all over the body and diagnosed as SJS. Although carbamazepine (CBZ) is the most common cause of SJS, a new anticonvulsant, oxcarbazepine, which is structurally related to CBZ, has been shown to induce SJS.