Formulation Optimization And Evaluation Of Drug Loaded Nanosponges For Oral Drug Delivery

Depression is treated with venlafaxine HCL, Additionally, it is used to treat panic disorder, social anxiety disorder, and generalised anxiety disorder. The main goal of this study was to prepare venlafaxine HCL loaded nanosponges into tablets for an oral purpose by using Box-Behnken design to increase the bio availability. The drug was placed into nanosponges utilising the hot-melt compression technique, three-dimensional colloidal nanosponges were prepared by using β-cyclodextrin and dimethyl carbonate as a cross-linker. The effect of three Independent variables such as β cyclodextrin, dimethyl carbonate and response on two dependent variables  vesicle size and entrapment efficiency were investigated.  With the help of box behnken design 15 formulations were prepared out of which formulation 10 was considered as optimized based on the drug EE. The nanosponge formulations were evaluated for particle size, percent drug entrapment, shape and surface morphology, drug content, and in vivo drug release studies. The prepared nanosponge had a particle size of 257.6 nm, a drug entrapment percentage of 97.42 percent, and was almost spherical in shape. Utilizing HPMC K4M, the formulations NA1 through NA15 matrix tablets were crushed into drug-loaded nanosponges for 24 hours

DEVELOPMENT OF A PROLONGD RELEASE GASTRORETENTIVE TABLET FORMULATION OF LEVOFLOXACIN

Objective: The present investigation concerns the design and evaluation of floating tablets of Levofloxacin, which after oral administration prolong the gastric residence time and increased drug bioavailability. Methods: Levofloxacin is a synthetic chemotherapeutic agent used to treat severe or life-threatening bacterial infections. The present work was designed to formulate floating tablet of Levofloxacin with various swelling agents. Formulations were prepared using various concentrations of Guar gum, Carbopol, hydroxy propyl methyl cellulose and Ethyl Cellulose by direct compression technique. The selected batches were evaluated for various parameters like weight variation, thickness, diameter, friability, floating lag time, duration of floating, swelling index, content uniformity and in-vitro drug release. The data obtained from the in-vitro dissolution studies of optimized batch F7 were fitted in different models. Results: The optimized formulation F7 showed 99.25% drug content, floating lag time of 10 min and swelling index of 40%. Drug release mechanism was found to be zero order along with higuchi release kinetics exhibiting diffusion along with dissolution of the drug from the tablet by non fickian mechanism. Conclusion: Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug. Keywords: Levofloxacin, Gastro retentive, Guar gum, Hydroxy propyl methyl cellulose, Ethyl Cellulose, Carbopol

FORMULATION DEVELOPMENT AND EVALUATION OF ALLOPURINOL SOLID DISPERSIONS BY SOLVENT EVAPORATION TECHNIQUE

Objective: The main objective of the research work is to develop and characterize allopurinol (ALPN) solid dispersions with different polymers to enhance solubility, enrich dissolution profile and improve patient compliance.Methods: ALPN solid dispersions were prepared by solvent evaporation technique using various grades of polyethelene glycol (PEG) such as PEG 4000 and PEG 6000 with different ratios like 1:0.5, 1:1, 1:1.5 and 1:2 and after formation of solid dispersions all physicochemical properties were examined.Results: All the formulations were found within the permissible pharmacopoeial limits for various physicochemical parameters. The pre-formulation studies, like Fourier, transform infrared spectroscopy (FTIR) showed the absence of drug-excipient interactions. The solubility and dissolution profiles of the sample were increased with increasing the concentration of ALPN solid dispersions. Solvent evaporation was proved to be a successful technique for the development of stable solid dispersion of ALPN. The dissolution amount percentage of ALPN formulations was found between 39.58±2.5 to 94.95±1.8 % within 60 min.Conclusion: Hence, from the all evaluation studies, it was evident that F1 formulation was the better formulation. F1 formulation (ALPN: PEG 4000 in the ratio of 1:0.5), 94.95±1.8 % drug released within 50 min. Â

ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF AMLODIPINE IN HUMAN PLASMA USING LIQUID CHROMATOGRAPHY-MASS SPECTROMETRY/MASS SPECTROMETRY

Objective: The objective of the present investigation was to develop a novel, simple, and economic method for the estimation of amlodipine in positive ion mode in human plasma using amlodipine maleate d4 as an internal standard.Methods: The chromatographic separation was performed on Zorbax SB, C18, 50 mm*4.6 mm, and 3.5 mm. The mobile phase was prepared with a mixture of 5 mm ammonium acetate in 0.1% formic acid: High performance liquid chromatographic (HPLC) grade methanol:HPLC grade acetonitrile (40:30:30) that run isocratically at the flow rate of 0.700 ml/min and run time at 2.50 min.Results: The analytical method is valid for the estimation of amlodipine, in human plasma over a range of 0.100 ng/ml–9.990 ng/ml with the detection of amlodipine m/z - 409.10 (parent) and 238.00 (product), and internal standard Amlodipine Maleate d4 m/z - 413.20 (parent), and 238.00 (product) in positive ion mode. The results of carryover test, matrix effect, linearity, precision and accuracy, stabilities, dilution integrity, and run size evaluation test presented in this report are within the acceptance range.Conclusion: A sensitive method for the separation and determination of amlodipine in plasma has been developed based on solid-phase extraction with disposable extraction cartridges in combination with LC and mass spectrophotometers (MS/MS)

Phytopharmacology of Chloroxylon swietenia: a review

The nature has provided a complete store house of remedies to use for all ailments for mankind. The knowledge on drugs has accumulated over thousands of years as a result of mans inquisitive nature. Phytomedicines or natural prescriptions, have assumed a basic part in World wellbeing for a large number of years. As per the World Health Organization (WHO), "natural medications incorporate herbs, home grown materials, home grown arrangements and completed home grown items, that contain as dynamic fixings parts of plants, or other plant materials, or blends. Chloroxylon swietenia DC. (Family: Rutaceae) is an important traditional medicinal plant used in the treatment of various ailments like fungal infection of skin, rheumatism, common cold, cough, ophthalmic infection and cataract, wounds and as an astringent. It is a tropical aromatic tree of dry deciduous forests popularly known as East Indian Satin Wood. The findings of this study will facilitate pharmacognostic standardization of the plant material and aid in the preparation of an herbal monograph for the species. Further studies on this plant must be carried out to explore some other important, necessary and unknown benefits. As the plant has multifunctional properties, this review is worthwhile and therefore it presents comprehensive analysed information on the phytochemical and pharmacological aspects of the botanical. Keywords: Chloroxylon swietenia, phytomedicines, pharmacological aspects, anti-feedant, anti-bacterial activity, IUCN, vulnerable species

Rosmarinus officinalis L.: an update review of its phytochemistry and biological activity

Herbal medicine is one of the oldest valuable bestowals that were given to mankind. Many plants and herbs hold their prestigious position in the field of medicine. The worldwide interest in the use of medicinal plants has been growing, and its beneficial effects being rediscovered for the development of new drugs. Based on their vast ethnopharmacological applications, which inspired current research in drug discovery, natural products can provide new and important leads against various pharmacological targets. This work pioneers an extensive and an updated literature review on the current state of research on Rosmarinus officinalis L., elucidating which compounds and biological activities are the most relevant. According to these references, there has been an increasing interest in the therapeutic properties of this plant, regarding carnosic acid, carnosol, rosmarinic acid and the essential oil. The present manuscript provides an updated review upon the most reported activities on R. officinalis and its active constituents. This knowledge about the medicinal plants usage can also be extended to other fields like field of pharmacology. In view of the nature of the plant, more research work can be done on humans so that a drug with multifarious effects will be available in the future market. Keywords: Rosmarinus officinalis, phytochemicals, carnosic acid, rosmarinic acid, neuroprotective activity, anti-diabetic activity

ASSESSMENT OF PREVALENCE OF DEPRESSION IN CARDIAC PATIENTS AND ITS ASSOCIATION WITH THE USE OF BETA-BLOCKERS AND STATINS

Objective: The objective of the study is to assess the prevalence of depression among patients with cardiovascular disease and its association with the use of β-blockers and statins.Methods: This is a prospective observational study conducted at a corporate hospital, Hyderabad, Telangana, India, for a period of 6 months. 250 cardiac patients above 16 years are included in the study. The required data are collected from the patients through direct interview using standard questionnaires and also from patients' respective case sheets. The acquired data are evaluated based on the standard questionnaires Patient Health Questionnaire-9 (PHQ-9) and Beck Depression Inventory-II (BDI-II) scales; used to diagnose the severity of depression in cardiac patients.Results: Prevalence of minor to major depressive symptoms according to BDI-II was found to be 17.2%. Prevalence of minor to major depressive symptoms according to PHQ-9 was found to be 19.2%. Among male patients, 13% showed depressive symptoms, whereas among female patients 25% showed depressive symptoms. Among the patients coadministering beta-blockers and statins, 15% were depressed according to BDI-II, and 16% were depressed according to PHQ-9 at visit. After 1 month (first follow-up), the percentage increased by 8% (for BDI-II)-12% (for PHQ-9) and remains almost the same at the second follow-up. As per BDI-II and PHQ-9 scores, the percentage of patients with minor to major depression among the patients using only beta-blockers decreased significantly from the time of visit to the second follow-up. The percentage of patients with minor to major depression among the patients using only statins increased significantly from the time of visit to second follow-up.Conclusion: Prevalence of minor to major depression according to BDI-II was found to be 17%, whereas according to PHQ-9, it was found to be 20% in patients with cardiovascular disease. Cardiovascular diseases have been more prevalent in men than in women, whereas depressive symptoms have been more prevalent in women than in men. Patients using only β-blockers showed a decrease in symptoms of depression. Whereas statins have shown to increase the chances of depression slightly which is often negligible, atorvastatin was associated with a higher level of depression when compared to rosuvastatin. Controversies still exist that statins decrease risk of depression.Â

Non-steroidal anti-inflammatory drugs: an overview

Non-steroidal anti-inflammatory drugs (NSAIDs) including both traditional non-selective NSAIDs and the selective cyclooxygenase (COX)-2 inhibitors, are widely used for their anti-inflammatory and analgesic effects. NSAIDs are a necessary choice in pain management because of the integrated role of the COX path way in the generation of inflammation and in the biochemical recognition of pain. NSAIDs are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs). Their use is associated with the side effects such as gastrointestinal and renal toxicity. They are the most commonly employed first line drugs for all these conditions and many others-like musculoskeletal trauma, minor aches and pains, and dysmenorrhoea. The therapeutic anti-inflammatory action of NSAIDs is produced by the inhibition of COX-2, while the undesired side effects arise from inhibition of COX-1 activity. Thus, it was though those more selective COX-2 inhibitors would have reduced side effects. Based upon a number of selective COX-2 inhibitors (Rofecoxib, Celecoxib etc.) were developed as safer NSAIDs with improved gastric safety profile. Several newer applications like prophylaxis of stroke with aspirin are now common place. Use of these drugs for the prophylaxis of conditions like Alzheimer’s disease and colorectal cancer is being evaluated. Unfortunately, they have several toxicities ranging from minor heartburn to severe gastrointestinal haemorrhage and perforation. Therefore, newer NSAIDs have been introduced in recent years to circumvent this problem. In preliminary studies, these have shown better safety, efficacy, and tolerability but the full spectrum of adverse reactions of these drugs is yet to be fully known. This review can be used for further research as well as clinical purpose. Keywords: Non-steroidal anti-inflammatory drugs (NSAIDs), cyclooxygenase inhibitors, prostaglandins, aspirin

Assessment of anti bacterial screening of Pongamia pinnata stem against bacterial species: An In-vitro approach

Numerous studies have shown that aromatic and medicinal plants are sources of diverse nutrient and non-nutrient molecules which protect the human body against various pathogens. Nature has been a source of medicinal agents for thousands of years and a large number of modern drugs have been isolated from natural sources. Herbal medicine is the oldest known healthcare system known to mankind. India has rich medicinal plants of nearly 7500 species. Many medicinal plants were with a long history of use in folk medicine against a variety of diseases. Recently, many researchers have taken a great interest on medicinal plants for their phytochemical constituents and biological activities including anti microbial activity. The anti bacterial activity of the ethanolic crude stem extract of Pongamia pinnata against four bacterial species (Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Escherichia coli) was investigated, using agar diffusion technique. At concentrations ranging from 10-40 mg/mL, the ethanolic crude extract showed activity against the four bacteria (Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and E. coli) from 2 mm-20 mm, after 24 hours incubation. The present study showed the effectiveness of the crude plant extract against the tested bacterial strains and indicates the potential use of the extract as anti bacterial agent for the control of infectious diseases. Keywords:  Pongamia pinnata, anti bacterial activity, agar diffusion technique, bacterial strains, chloramphenicol

IN SITU GEL POLYMERS: A REVIEW

In situ gels have become one of the most prominent and accessible systems. These systems have several advantages like simple manufacturing, easy to use, improved adherence, and patient comfort by minimizing drug administration frequency by its unique characteristic features of sol to gel transition. In the 'sol-gel' method, the precursor goes through hydrolysis and polymerization or condensation to produce a colloidal suspension or solution. As they can administer in solution form, these in situ gelling systems undergo gelation at the achievement site. Some researchers recently developed in situ gelling systems of liposomes, microspheres, nanoemulsions, nanospheres, etc. This review mainly focused on the introduction, advantages, disadvantages, types of polymers, and suitable characteristics for preparing in situ gels