Preparation of Tamsulosin Hydrochloride-Loaded Mucoadhesive In Situ Gelling Polymeric Formulation for Nasal Delivery in Geriatrics.

This study aimed to prepare tamsulosin hydrochloride (HCl)-loaded in situ gelling formulation by using hydroxypropyl methylcellulose (HPMC), gellan gum, poloxamer 188, and benzalkonium chloride. Physicochemical evaluation of formulations included determination of pH, viscosity, gelation time, gel strength, drug content, and sterility. In silico study was performed to analyze interactions between polymers, drug, and mucin glycoprotein. In vitro degradation time, drug release, ex vivo mucoadhesion time, permeation, in vivo pharmacokinetics, and stability studies were performed to assess the formulation. Formulations were transparent and displayed acceptable physicochemical attributes. Tamsulosin HCl and polymers interacted via non-covalent interactions. HPMC formed hydrogen bonds, hydrophobic and van der Waals interactions with mucin protein while the drug formed hydrogen bonds only. Gel formulation degraded in simulated nasal fluid within 24 h. In situ gelling formulation showed 83.8 ± 1.7% drug release and remained adhered to the mucosa for 24.5 ± 1 h. A higher (~ 1.85 times) drug permeation was recorded through mucosa within 6 h by in situ gelling formulation when compared to control counterparts (aqueous solution of drug and in situ gelling formulation without poloxamer 188). Nasal administration of tamsulosin HCl by using in situ gelling formulation led to a ~ 3.3 and ~ 3.5 times, respectively, higher Cmax (maximum plasma concentration) and AUCtotal (total area under the curve) than the orally administered aqueous solution. Relative bioavailability of drug delivered by nasal in situ gelling formulation was 3.5 times the oral counterpart. These results indicated that the prepared in situ gelling formulation can act as a promising candidate for systemic administration of tamsulosin HCl.

Preparation and characterization of indomethacin loaded films by piezoelectric inkjet printing: a personalized medication approach.

The purpose of this study was to investigate the application of piezoelectric inkjet technology in the preparation of custom-made indomethacin (IMC) films. Indomethacin solutions with and without PVP were printed onto polymeric sheets using a commercial inkjet printer. Drug loading was varied by selecting a machine parameter different dots per inches (DPIs). The printed patches were evaluated for particulate morphologies, drug loading, in vitro release and ex vivo skin permeation and anti-inflammatory effects using hind paw inflammation model. Calculated drug loaded in 2 × 2 cm2 patches of IMC of 96, 300, and 600 DPIs were in the range of 40, 60, and 65 µg, respectively. Patches loaded with IMC alcoholic solution showed crystalline structures observed by scanning electron microscopy and the addition of PVP in solution turned it to amorphous form. The drug release profile showed 60-70% of total drug released in 3 h. Permeation studies showed 40-50% of total drug loaded permeated through rat skin using Franz cells. Patches with higher printing density 600 DPI showed anti-inflammatory effect in hind paw inflammation model studies. This study has shown the potential of personalized medicine in which a calculated amount of drug can be delivered to patients by piezoelectric technology.

RP-HPLC based method for the determination of Tamsulosin HCl in API, Prepared dosage form and spiked plasma.

An analytical method for measurement of tamsulosin HCl from its different life cycle stages was developed using RP-HPLC technique. The elution of tamsulsoin was studied using MediterraneaTM Sea 18 column (dimesions 250 × 4.6 mm and pore size 5µm) and mobile phase comprising of buffer (pH 5.4): Acetonitrile (ACN) at ratio 60:40. The tamsolusin HCl elution was also studied by varying the operating conditions including the composition and flow rate of mobile phase, stationary phase temperature and scanning wavelength. The optimal elution conditions include; a) mobile phase flow rate; 1ml/min, b) wavelength; 224nm and stationary phase temperature 30°C. Linearity was recorded in the absorption data over tamsulosin concentration range of 0.007 to 40µg/ml. The values of paramters LOD and LOQ noted for tamsulosin dissolved in mobile phase were 0.0014 and 0.042µg/ml respectively, while for the counterpart in spiked plasma were 0.0017 and 0.051µg/ml respectively. The analytical method was prompt, accurate, reproducible and suitable for analysis of tamsulosin HCl in different samples of interest at formulation, regulation and clinical evaluations.

Development and Validation of Facile RP-HPLC Method for Simultaneous Determination of Timolol Maleate, Moxifloxacin Hydrochloride, Diclofenac Sodium and Dexamethasone in Plasma, Aqueous Humor and Pharmaceutical Products.

The present study aimed to develop a validated RP-HPLC method for the simultaneous determination of timolol maleate (TM), moxifloxacin hydrochloride (MOXI), diclofenac sodium (DS) and dexamethasone (DEXA) in human plasma, bovine aqueous humor and pharmaceutical preparations. The chromatographic separation was studied using the C18 column. The chromatographic conditions, such as composition, pH, the flow rate of mobile phase, the temperature of column, wavelength of absorption and injection volume of the sample, were studied. The method was validated to confirm specificity, linearity and accuracy in accordance with an International Conference on Harmonization guidelines. The optimum conditions for separation included mobile phase 0.05 M monobasic phosphate buffer: acetonitrile (65:35 v/v), pH of buffer adjusted to 6.2 and the flow rate of 1 mL/minute. The optimum temperature of the column was found to be 35°C, absorption wavelength 265 nm and injection volume 50 µL. The baseline separation of all four drugs with good sensitivity, resolution, and a less than 15 min run time was achieved. The retention time of TM, MOXI, DS and DEXA were 4.3,5.7,9.9 and 13.5 minutes respectively. The limit of detection (LOD) values were 6.2, 4.8, 0.8 and 1.2 ng/mL for TM, MOXI, DS and DEXA, respectively, whereas their respective limit of quantification (LOQ) values was: were 42.6, 26.8, 5.6 and 6.2 ng/mL. The coefficient of variation for intra-day and inter-day were in the range of 0.32-1.57 and 1.29-3.07%, respectively. The method was found to be sensitive, precise and accurate in human plasma and bovine aqueous humor and can be applied for the quantification of these compounds in plasma, aqueous humor and pharmaceuticals.

Nexus on climate change: agriculture and possible solution to cope future climate change stresses.

The changing climate scenarios harshen the biotic stresses including boosting up the population of insect/pest and disease, uplifting weed growth, declining soil beneficial microbes, threaten pollinator, and boosting up abiotic stresses including harsh drought/waterlogging, extremisms in temperature, salinity/alkalinity, abrupt rainfall pattern)) and ulitamtely  affect the plant in multiple ways. This nexus review paper will cover four significant points viz (1) the possible impacts of climate change; as the world already facing the problem of food security, in such crucial period, climatic change severely affects all four dimensions of food security (from production to consumption) and will lead to malnutrition/malnourishment faced by low-income peoples. (2) How some major crops (wheat, cotton, rice, maize, and sugarcane) are affected by stress and their consequent loss. (3) How to develop a strategic work to limit crucial factors, like their significant role in climate-smart breeding, developing resilience to stresses, and idiotypic breeding. Additionally, there is an essence of improving food security, as much of our food is wasted before consumption for instance post-harvest losses. (4) Role of biotechnology and genetic engineering in adaptive introgression of the gene or developing plant transgenic against pests. As millions of dollars are invested in innovation and research to cope with future climate change stresses on a plant, hence community base adaptation of innovation is also considered an important factor in crop improvements. Because of such crucial predictions about the future impacts of climate change on agriculture, we must adopt measures to evolve crop.

Identification of novel in vitro antibacterial action of cloprostenol and evaluation of other non-antibiotics against multi-drug resistant A. baumannii.

A total of 24 non-antibiotic compounds were tested for their antimicrobial activity against Escherichia coli, Klebsiella pneumoniae (ATCC) and an MDR strain of Acinetobacter baumannii using an agar well diffusion assay. To study additive effects, 100 µl of each antibiotic and 50 µl of each non-antibiotic were used. Cloprostenol was the only non-antibiotic that showed antibacterial activity against all bacterial strains. Cloprostenol had an additive antimicrobial effect with the tested antibiotics against the MDR A. baumannii strain.

Evaluation of synergistic antimicrobial effect of vitamins (A, B1, B2, B6, B12, C, D, E and K) with antibiotics against resistant bacterial strains.

OBJECTIVES: Multidrug-resistant (MDR) superbugs, including Acinetobacter baumannii and methicillin-resistant Staphylococcus aureus (MRSA), are a challenge for healthcare professionals. In this study, the synergistic activity of vitamins with antibiotics against resistant bacterial strains was evaluated. METHODS: Synergistic effects between antibiotics and stock solutions of vitamins were evaluated by the Kirby-Bauer disk diffusion assay. Distilled water and propylene glycol were used as solvent for water-soluble and fat-soluble vitamins, respectively. Final concentrations of 10mg/mL for each water-soluble vitamin [B1 (thiamine), B2 (riboflavin), B6 (pyridoxine), B12 (methylcobalamin) and C (ascorbic acid)] and 0.1mg/mL for each fat-soluble vitamin [A (retinol), D (cholecalciferol), E (α-tocopherol) and K (menadione)] were used in combination with the antibiotics. RESULTS: The results demonstrated that vitamins K and E had good synergistic activity with piperacillin/tazobactam, imipenem and doripenem against A. baumannii, whilst vitamins B1, B2 and B12 showed remarkable synergistic activity with linezolid against MRSA. Vitamin B1 was further shown to have better synergism with oxacillin, tetracycline, rifampicin and linezolid against MRSA. The fat-soluble vitamins E and K showed good synergism against Gram-negative A. baumannii, whilst the water-soluble vitamins B1, B2 and B12 were effective against MRSA but not against A. baumannii. CONCLUSIONS: This synergistic action of vitamins with antibiotics may be used as a tool to treat MDR superbugs, with further evaluation required at a molecular level.