Design and Evaluation of Chitosan films for Transdermal delivery of Glimepiride

Glimepiride is a third generation oral antidiabetic sulphonylurea drug frequently prescribed to patients of type 2 diabetes. However, its oral therapy is encountered with bioavailability problems due to its poor solubility leading to irreproducible clinical response, in addition to adverse effects like dizziness and gastric disturbances. As a potential for convenient, safe and effective antidiabetic therapy, the rationale of this study was to develop a transdermal delivery system for glimepiride. Chitosan polymer was utilized in developing transdermal films for glimepiride. Chitosan has film forming ability, bioadhesive and absorption enhancing properties. Aiming at optimizing the drug delivery and circumventing the skin barrier function, inclusion complexation of glimepiride with beta-cyclodextrin (β-CyD) as well as the use of several conventional penetration enhancers were monitored for augmenting the drug flux. The physical and mechanical properties of the prepared films were investigated using tensile testing, IR spectroscopy and X-ray diffractometry. Release studies revealed adequate release rates from chitosan films. Permeation studies through full thickness rat abdominal skin were conducted. High flux values were obtained from films comprising a combination of the drug with limonene and ethanol as well as from films containing glimepiride-β-CyD complex. In vivo studies on diabetic rats for selected formulae revealed a marked therapeutic efficacy sustained for about 48 hours. The above-mentioned results shed light on feasibility of utilizing chitosan as an effective, safe transdermal delivery system for glimepiride characterized by increased patient compliance and better control of the disease

Twin load of hypertension and diabetes amongst adults: community based study from Jammu and Kashmir, India

Background: Data regarding the occurrence of hypertension and diabetes in the community are crucial for optimum allocation and utilization of health resources. Objective was to assess the efficacy of such field based exercise in detection of new undiagnosed cases and calculation of the consequent prevalence.Methods: A cross sectional community based study was carried out to find out prevalence of hypertension and diabetes amongst adults (35-64 years) in Chatergam, Budgam (Jammu and Kashmir) during Oct 2011 to Feb 2012 on a pre-tested structured questionnaire. Blood pressure was measured in 2077 adults and random blood sugar (RBS) was measured in 1732 subjects to detect diabetes. Data was analyzed to find out the distribution of systolic (SBP) and diastolic (DBP) and the prevalence of hypertension and diabetes along with 95 percent confidence intervals.Results: Mean SBP and DBP of 2077 subjects were 130.7 ± 40.3 and 83.1 ± 11.4 mm of mercury respectively. Values were the highest for both SBP and DBP amongst women of urban areas and in the 55 – 64 years of age. Quarter of studied persons (24.4%) had the family history of hypertension or diabetes or both. Based on the criteria of JNC 7, 41.1% subjects (95 % CI 38.9 – 43.2) were found hypertensive including 593 known cases (496 alone & 97 in combinations with diabetes). Prevalence of new cases of hypertension was 17.5 percent; it significantly increased with increasing age and was high amongst males and those residing in urban areas. 4.6% subjects (95% CI 3.6-5.7) were positive for diabetes based on RBS. Conclusions: Considering high load of twin diseases and their impact on coronary vascular diseases (CVD), study emphasizes the need to implement an integrated population-based cost-effective control program with a focus on primordial and primary prevention.

FORMULATION AND EVALUATION OF MATRIX TRANSDERMAL PATCHES OF GLIBENCLAMIDE

The present study deals with the formulation and evaluation of transdermal patches of Glibenclamide towards enhance its permeation through the skin and maintain the plasma level concentration. Transdermal patches were prepared by using polymers like Chitosan, HPMC 15cps and EC 20cpsat various concentrations by solvent casting technique employing dibutyl phthalate as plasticizer and iso-propylmyristate as permeation enhancer. The transdermal patches were evaluated for their physico-chemical properties and in-vitro drug release. The transdermal patches were found to be transparent and smooth in texture. Among the formulations studied, at the end of 12th hour, the minimum and maximum in-vitro drug release was observed for the formulations F12 and F4 i.e. 80.012 ± 2.012 % and 98.365±3.012% respectively. The mechanism of drug release was found to be Non-Fickian diffusion controlled. FT-IR studies revealed the integrity of the drug in the formulations. Keywords: Transdermal Patches, Glibenclamide, Chitosan, HPMC 15cps, EC 20 cps, in-vitro diffusion studies

Development and characterization of Glibenclamide containing Transdermal Patches

Transdermal drug delivery has had a rich past and is now emerging as a major alternative to other delivery systems. As this technique has matured and new fundamentals have been integrated into its development, new products and applications have shown new ways in which skin can play a larger part in healthcare and quality of life. Improved delivery has been shown for drugs of differing. The cumulative percentage of drug released in 12 h was found to be minimum and maximum for the formulations F4 and F10 i.e. 81.023 ± 3.013 % and 98.564 ±3.005%.The results of the drug content in all the formulations were found to be in the range of 96 to 98 %. The maximum moisture loss was 4.3300 ± 0.0360 %. The prepared film had tendency to absorb moisture effectively. Glibenclamide is a third generation oral anti-diabetic sulphonylurea drug frequently prescribed to patients of type 2 diabetes. Glibenclamide therapy improves postprandial insulin/C-peptide response, and overall glycaemia control. The development of Glibenclamide transdermal patch for anti-diabetic will be an excellent dosage form for market strategy due to its very fast action and better patient compliance. Keywords: Transdermal, cyclodextrin, formulation, releas

SARS-CoV-2 emerging Omicron subvariants with a special focus on BF.7 and XBB.1.5 recently posing fears of rising cases amid ongoing COVID-19 pandemic

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) Omicron versions have been the sole one circulating for quite some time. Subvariants BA.1, BA.2, BA.3, BA.4, and BA.5 of the Omicron emerged over time and through mutation, with BA.1 responsible for the most severe global pandemic between December 2021 and January 2022. Other Omicron subvariants such as BQ.1, BQ.1.1, BA.4.6, BF.7, BA.2.75.2, XBB.1 appeared recently and could cause a new wave of increased cases amid the ongoing COVID-19 pandemic. There is evidence that certain Omicron subvariants have increased transmissibility, extra spike mutations, and ability to overcome protective effects of COVID-19 neutralizing antibodies through immunological evasion. In recent months, the Omicron BF.7 subvariant has been in the news due to its spread in China and a small number of other countries, raising concerns about a possible rebound in COVID-19 cases. More recently, the Omicron XBB.1.5 subvariant has captured international attention due to an increase in cases in the United States. As a highly transmissible sublineage of Omicron BA.5, as well as having a shorter incubation time and the potential to reinfect or infect immune population, BF.7 has stronger infection ability. It appears that the regional immunological landscape is affected by the amount and timing of previous Omicron waves, as well as the COVID-19 vaccination coverage, which in turn determines whether the increased immune escape of BF.7 and XBB.1.5 subvariants is sufficient to drive new infection waves. Expanding our understanding of the transmission and efficacy of vaccines, immunotherapeutics, and antiviral drugs against newly emerging Omicron subvariants and lineages, as well as bolstering genomic facilities for tracking their spread and maintaining a constant vigilance, and shedding more light on their evolution and mutational events, would help in the development of effective mitigation strategies. Importantly, reducing the occurrence of mutations and recombination in the virus can be aided by bolstering One health approach and emphasizing its significance in combating zoonosis and reversal zoonosis linked with COVID-19. This article provides a brief overview on Omicron variant, its recently emerging lineages and subvairants with a special focus on BF.7 and XBB.1.5 as much more infectious and highly transmissible variations that may once again threaten a sharp increase in COVID-19 cases globally amid the currently ongoing pandemic, along with presenting salient mitigation measures

Synthesis of SAPO-34 nanoplates with high Si/Al ratio and improved acid site density

Two-dimensional SAPO-34 molecular sieves were synthesized by microwave hydrothermal process. The concentrations of structure directing agent (SDA), phosphoric acid, and silicon in the gel solution were varied and their effect on phase, shape, and composition of synthesized particles was studied. The synthesized particles were characterized by various techniques using SEM, XRD, BET, EDX, and NH3-TPD. Various morphologies of particles including isotropic, hyper rectangle, and nanoplates were obtained. It was found that the Si/Al ratio of the SAPO-34 particles was in a direct relationship with the density of acid sites. Moreover, the gel composition and preparation affected the chemistry of the synthesized particles. The slow addition of phosphoric acid improved the homogeneity of synthesis gel and resulted in SAPO-34 nanoplates with high density of acid sites, 3.482 mmol/g. The SAPO-34 nanoplates are expected to serve as a high performance catalyst due to the low mass transfer resistance and the high density of active sites

Protein tyrosine phosphatase 1B inhibitors isolated from Artemisia roxburghiana

Artemisia roxburghiana is used in traditional medicine for treating various diseases including diabetes. The present study was designed to evaluate the antidiabetic potential of active constituents by using protein tyrosine phosphatase 1B (PTP1B) as a validated target for management of diabetes. Various compounds were isolated as active principles from the crude methanolic extract of aerial parts of A. roxburghiana. All compounds were screened for PTP1B inhibitory activity. Molecular docking simulations were performed to investigate the mechanism behind PTP1B inhibition of the isolated compound and positive control, ursolic acid. Betulinic acid, betulin and taraxeryl acetate were the active PTP1B principles with IC50 values 3.49 ± 0.02, 4.17 ± 0.03 and 87.52 ± 0.03 µM, respectively. Molecular docking studies showed significant molecular interactions of the triterpene inhibitors with Gly220, Cys215, Gly218 and Asp48 inside the active site of PTP1B. The antidiabetic activity of A. roxburghiana could be attributed due to PTP1B inhibition by its triterpene constituents, betulin, betulinic acid and taraxeryl acetate. Computational insights of this study revealed that the C-3 and C-17 positions of the compounds needs extensive optimization for the development of new lead compounds

Synthesis of Boron-Doped Zinc Oxide Nanosheets by Using Phyllanthus Emblica Leaf Extract: A Sustainable Environmental Applications

The use of Phyllanthus emblica (gooseberry) leaf extract to synthesize Boron-doped zinc oxide nanosheets (B-doped ZnO-NSs) is deliberated in this article. Scanning electron microscopy (SEM) shows a network of synthesized nanosheets randomly aligned side by side in a B-doped ZnO (15 wt% B) sample. The thickness of B-doped ZnO-NSs is in the range of 20–80 nm. B-doped ZnO-NSs were tested against both gram-positive and gram-negative bacterial strains including Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumonia, and Escherichia coli. Against gram-negative bacterium (K. pneumonia and E. coli), B-doped ZnO displays enhanced antibacterial activity with 26 and 24 mm of inhibition zone, respectively. The mass attenuation coefficient (MAC), linear attenuation coefficient (LAC), mean free path (MFP), half-value layer (HVL), and tenth value layer (TVL) of B-doped ZnO were investigated as aspects linked to radiation shielding. These observations were carried out by using a PTW® electron detector and VARIAN® irradiation with 6 MeV electrons. The results of these experiments can be used to learn more about the radiation shielding properties of B-doped ZnO nanostructures

Recent Synthetic Studies Leading to Structural Revisions of Marine Natural Products

Because of the highly unique structures of marine natural products, there are many examples of structures that were originally proposed based on spectral analyses but later proven incorrect. In many cases, the total syntheses of the originally proposed structures of marine natural products has confirmed their incorrectness and the subsequent total syntheses of the newly proposed structures proved the revised structures. This review will show such cases appearing after 2005 and demonstrate how the true structures were elucidated