Formulation and Characterization of Sustained Release Floating Microballoons of Metformin Hydrochloride

Purpose: To formulate sustained release gastroretentive microballoons of metformin hydrochloride with the objective of improving its bioavailability.Methods: Microballoons of metformin hydrochloride were formulated by solvent evaporation and diffusion method using varying mixtures of hydroxypropyl methylcellulose (HPMC) and ethyl cellulose (EC) polymers. The balloons were characterized for particle size, surface morphology, incorporation efficiency, floating behavior and in vitro drug release.Results: The mean particle size of the formulated microballoons was in the range of 34.2 ± 4.7 to 95.7 ± 2.2 μm. Incorporation efficiencies of over 83.8 ± 0.9 % were achieved for the optimized formulations. Most of the formulations were buoyant with maximum buoyancy of 81.4 ± 2.0 % for > 12 h, showing good floating behavior of microballoons. Release kinetic data showed best fit to the Higuchi model, indicating that diffusion was the predominant mechanism of drug release.Conclusion: Microballoons is a potential suitable delivery system for sustained release of metformin hydrochloride with improved bioavailability when compared with conventional dosage forms of the drug.Keywords: Gastroretentive drug delivery system (GDDS), Solvent evaporation and diffusion method, Higuchi, Microballoons, Metformin hydrochlorid

INFANT'S SKIN AND CARE NEEDS WITH SPECIAL CONSIDERATION TO FORMULATION ADDITIVES

Infancy is the time of adaptation from intrauterine life to the rather dry and cold, environment. Infant skin is more sensitive due to the immature immune system, hence, effortlessly prone to complications. Children from different age groups face diverse skin problems such as cradle cap, infant eczema, diaper rash, prickly heat, and many more. During early infancy, the products such as mild cleansers and lotions are used, and later, massage oils, creams, lotions, soaps, bubble bath, and other products are utilized for another few years, as a part of routine care. The preterm infants are more prone to skin damage and percutaneous toxicity from topically applied products. The ingredients incorporated in infant care products require special attention while choosing a product for them. Topical application of any such product requires thorough screening for potentially harmful ingredients before its exposure to the infant's skin. Products used for infants should be safe and restricted of fragrance, coloring agents, parabens, plant oils, extracts, and other obnoxious ingredients. The literature is flooded with the list of safer excipients that can be utilized for the development of skin care products for infants and children

Flurbiprofen- and Suprofen-Dextran Conjugates: Synthesis, Characterization and Biological Evaluation

Purpose: To synthesize and characterize the dextran conjugates of suprofen and flurbiprofen, and also evaluate their biological activities.Methods: Suprofen and flurbiprofen were individually reacted with carbonyldiimidazole to form acylimidazole, which, in turn, was reacted with the dextran of varying molecular weight (40 000, 60 000, and 110 000) to form drug-dextran conjugates. The structures of the synthesized dextran conjugates were confirmed by IR and NMR spectroscopy. In vitro hydrolysis of the conjugates were studied in buffer solutions (pH 7.4 and 9.0) and 80% human plasma (pH 7.4). The analgesic and antipyretic activities, aswell as the ulcerogenic index of the conjugates were also evaluated in albino rats.Results: The mean degree of substitution of flurbiprofen and suprofen was between 8.0 to 9.5 % and 7.5 to 9.0 %, respectively. In vitro hydrolysis studies on the conjugates indicate faster hydrolysis at pH9.0 than in pH 7.4 buffer solution and 80% human plasma (pH 7.4) with the process following First order kinetics. The analgesic activity of flurbiprofen-dextran conjugate (FD-110) suprofen-dextran conjugate(SD-110) was 64.23 and 41.50% which compare well with those of their parent drugs - flurbiprofen (72.60%) and suprofen (44.30%). Similar findings were made in respect of the antipyretic activity. Bothflurbiprofen and suprofen showed deep ulceration, swelling and high intensity perforation in the gastric mucosa after seven days administration of flurbiprofen and suprofen with the ulcerogenic indices of29.69 and 31.0 respectively, cpmpare with 5.88 and 6.06 for FD-110 and SD-110, respectively.Conclusion: Dextran can be employed as a pro-moiety or carrier for the delivery of flurbiprofen and suprofen and showed comparable analgesic and antipyretic activities with the parent drugs but with lower ulcerogenic indices

In Vitro and In Vivo Evaluation of Diclofenac Sodium Gel Prepared with Cellulose Ether and Carbopol 934P

Purpose: To develop diclofenac sodium gel using high molecular weight hydroxypropyl methylcellulose (HPMC) and Carbopol 934P for topical and systemic delivery.Methods: Diclofenac sodium gel was prepared with HPMC K100M and Carbopol 934P as gelling agents. The formulations were examined for pH, spreadability, consistency, viscosity, homogeneity, drug content and stability. In vitro drug release was evaluated using Franz diffusion cell. Carrageenaninduced rat paw oedema model was used for the evaluation of the anti-inflammatory activity of the gels. A commercial diclofenac sodium gel product was used as the reference drug.Results: Formulations containing glycerin as permeation enhancer gave drug release patterns comparable to that of the reference product. The drug content of F2, F5 and F9 was 99.81, 99.75 and 99.96 %, respectively. Accelerated stability results showed no significant variation in the appearance and drug release after storage for 3 months.Conclusion: Diclofenac sodium gel containing HPMC K100M and Carbopol 934P exhibited pronounced anti-inflammatory activity and could be further developed for topical and systemic delivery..Keywords: Diclofenac sodium, Anti-inflammatory, Hydroxypropyl methylcellulose, Carbopol, Drug release, Glyceri

Allele mining in β-lactoglobulin gene of Capra hircus

β-Lactoglobulin (β-LG) genetic polymorphisms are important and well known due to their effects on quantitative traits and technological properties of milk. At the DNA level, polymerase chain reaction (PCR)-single-strand conformation polymorphism (SSCP) allows for the detection of unknown polymorphisms at β-LG loci. Here we describe the usefulness of the PCR-SSCP technique for β-LG typing. In the present study, we amplified and sequenced the part of promoter region and all the seven exons containing the entire coding and untranslated region for the β-lactoglobulin gene in best dairy goat breeds of India namely: Jamunapari and Jakhrana. Nine polymorphisms were detected, one in the l promoter region, four in the introns and four in the exons of the β-lactoglobulin gene. All polymorphisms were single nucleotide substitutions. The polymorphisms in the coding region did not produce any amino acid change.Key words: β-Lactoglobulin gene, dairy goats, polymorphism, single nucleotide polymorphism (SNP), single strand conformational polymorphism (SSCP)

Unique contributions to the scalar bispectrum in `just enough inflation'

A scalar field rolling down a potential with a large initial velocity results in inflation of a finite duration. Such a scenario suppresses the scalar power on large scales improving the fit to the cosmological data. We find that the scenario leads to a hitherto unexplored situation wherein the boundary terms dominate the contributions to the scalar bispectrum over the bulk terms. We show that the consistency relation governing the non-Gaussianity parameter $f_{_{\rm NL}}$ is violated on large scales and that the contributions at the initial time can substantially enhance the value of $f_{_{\rm NL}}$.Comment: v1: 5 pages, 4 figure

An early flame detection system based on image block threshold selection using knowledge of local and global feature analysis

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. Fire is one of the mutable hazards that damage properties and destroy forests. Many researchers are involved in early warning systems, which considerably minimize the consequences of fire damage. However, many existing image-based fire detection systems can perform well in a particular field. A general framework is proposed in this paper which works on realistic conditions. This approach filters out image blocks based on thresholds of different temporal and spatial features, starting with dividing the image into blocks and extraction of flames blocks from image foreground and background, and candidates blocks are analyzed to identify local features of color, source immobility, and flame flickering. Each local feature filter resolves different false-positive fire cases. Filtered blocks are further analyzed by global analysis to extract flame texture and flame reflection in surrounding blocks. Sequences of successful detections are buffered by a decision alarm system to reduce errors due to external camera influences. Research algorithms have low computation time. Through a sequence of experiments, the result is consistent with the empirical evidence and shows that the detection rate of the proposed system exceeds previous studies and reduces false alarm rates under various environments

FindFoci: a focus detection algorithm with automated parameter training that closely matches human assignments, reduces human inconsistencies and increases speed of analysis

Accurate and reproducible quantification of the accumulation of proteins into foci in cells is essential for data interpretation and for biological inferences. To improve reproducibility, much emphasis has been placed on the preparation of samples, but less attention has been given to reporting and standardizing the quantification of foci. The current standard to quantitate foci in open-source software is to manually determine a range of parameters based on the outcome of one or a few representative images and then apply the parameter combination to the analysis of a larger dataset. Here, we demonstrate the power and utility of using machine learning to train a new algorithm (FindFoci) to determine optimal parameters. FindFoci closely matches human assignments and allows rapid automated exploration of parameter space. Thus, individuals can train the algorithm to mirror their own assignments and then automate focus counting using the same parameters across a large number of images. Using the training algorithm to match human assignments of foci, we demonstrate that applying an optimal parameter combination from a single image is not broadly applicable to analysis of other images scored by the same experimenter or by other experimenters. Our analysis thus reveals wide variation in human assignment of foci and their quantification. To overcome this, we developed training on multiple images, which reduces the inconsistency of using a single or a few images to set parameters for focus detection. FindFoci is provided as an open-source plugin for ImageJ

High-Resolution Sonography: A New Technique to Detect Nerve Damage in Leprosy

Mycobacterium leprae, which causes leprosy, infects peripheral nerves resulting in functional impairment, ulcer formation and stigmatizing deformities. Early diagnosis of nerve involvement is important to avoid nerve related complications. We used non-invasive, high-resolution sonography (US) and color Doppler (CD) imaging to study the ulnar (UN), median (MN), lateral popliteal (LP) and posterior tibial (PT) nerves in 20 leprosy patients and compared 30 healthy Indian controls. The nerves were significantly thicker in the patients (p<0.0001 for each nerve). One of the key signs of leprosy is the presence of enlarged nerves. The kappa for clinical palpation and nerve enlargement by sonography was 0.30 for all examined nerves. Increased neural vascularity, the sign of inflammation was observed in 26% (39/152) of nerves by CD imaging. Increased CD was observed in multiple nerves in 3 of 4 patients with type 2 reaction. Significant correlation was observed between clinical parameters of grade of thickening, sensory loss and muscle weakness and US abnormalities of nerve echotexture, endoneural flow and cross-sectional area (p<0.001). We conclude that sonography is a better diagnostic tool to predict nerve damage as compared to clinical assessment. Nerve damage was sonographically more extensive and was observed in nerves considered clinically normal