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

The work was aimed at developing novel enteric coated HPMC capsules (ECHC) plugged with 5 Florouracil (5-FU) loaded Microsponges in combination with calcium pectinate beads. Modified quasi-emulsion solvent diffusion method was used to formulate microsponges based on 32 factorial design and the effects of independent variables (volume of organic solvent and Eudragit RS100 content) on the dependent variables (Particle size, %EE & % CDR) were determined. The optimized microsponges (F4) were characterized by SEM, PXRD, TGA and were plugged along with calcium pectinate beads in HPMC capsules and the HPMC capsules were further coated with enteric polymer Eudragit L 100 (Ed-L100) and/ or Eudrgit S 100 (Ed-S 100) in different proportions. In vitro release study of ECHC was performed in various release media sequentially SGF for 2 h, followed by SIF for the next 6 h and then in SCF (in the presence and absence of pectinase enzyme for further 16 h). Drug release was retarded on coating with EdS-100 in comparison to blend of EdS-100: EdL-100 coating. The percentage of 5-FU released at the end of 24 h from ECHC 3 was 97.83 ± 0.12% in the presence of pectinase whereas in control study it was 40.08 ± 0.02% drug. The optimized formulation was subjected to in vivo Roentgenographic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon targeted capsules. Pharmacokinetic studies in New Zealand white rabbits were conducted to determine the extent of systemic exposure provided by the developed formulation in comparison to 5-FU aqueous solutions. Thus, enteric coated HPMC capsules plugged with 5-FU loaded microsponges and calcium pectinate beads proved to be promising dosage form for colon targeted drug delivery to treat colorectal cancer.O trabalho teve como objetivo o desenvolvimento de novas cápsulas com revestimento entérico HPMC (ECHC) conectadas com microesponjas carregadas com fluoruracila (5-FU) em combinação com grânuos de pectinato de cálcio. O método de difusão de solvente modificado quasi-emulsão foi usado para formular microesponjas com base no planejamento fatorial 32 e determinaram-se os efeitos das variáveis independentes (volume de solvente orgânico e conteúdo Eudragit RS100) sobre as variáveis dependentes (tamanho de partícula, EE% e % CDR). As microesponjas otimizadas (F4) foram caracterizadas por SEM, PXRD, TGA e ligadas aos grânulos de pectinato de cálcio em cápsulas de HPMC e estas foram, ainda, revestidas com polímero entérico Eudragit L 100 (Ed-L100) e/ou Eudrgit S 100 (Ed S 100) em diferentes proporções. No estudo de liberação in vitro de ECHC foi realizada em vários meios de liberação sequencial SGF durante 2 h, seguido de SIF para as próximas 6 h, e, em seguida, em SCF (na presença e na ausência de enzima pectinase por mais 16 h). A liberação do fármaco foi retardada em revestimento com a EDS-100, em comparação 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 presença de pectinase, enquanto que para o controle foi de 40,08 ± 0,02% do fármaco. A formulação otimizada foi submetida a estudos Roentgenográficos in vivo, em coelhos brancos Nova Zelândia, para analisar o comportamento das cápsulas desenvolvidas direcionadas ao cólon. Os estudos de farmacocinética em coelhos brancos da Nova Zelândia foram conduzidos para determinar a extensão da exposição sistêmica propiciada pela formulação desenvolvida, em comparação com solução aquosa de 5-FU. Assim, cápsulas entéricas de HPMC revestidas e conectadas com microesponjas carregadas com 5-FU e grânulos de pectinato de cálcio se mostraram promissoras como formulação para liberação do fármaco no cólon no tratamento do câncer colorretal

Interactive Concept Bottleneck Models

Concept bottleneck models (CBMs) (Koh et al. 2020) are interpretable neural networks that first predict labels for human-interpretable concepts relevant to the prediction task, and then predict the final label based on the concept label predictions.We extend CBMs to interactive prediction settings where the model can query a human collaborator for the label to some concepts. We develop an interaction policy that, at prediction time, chooses which concepts to request a label for so as to maximally improve the final prediction. We demonstrate thata simple policy combining concept prediction uncertainty and influence of the concept on the final prediction achieves strong performance and outperforms a static approach proposed in Koh et al. (2020) as well as active feature acquisition methods proposed in the literature. We show that the interactiveCBM can achieve accuracy gains of 5-10% with only 5 interactions over competitive baselines on the Caltech-UCSDBirds, CheXpert and OAI datasets.Comment: To appear at AAAI 202

FORMULATION AND CHARACTERIZATION OF FLOATING TABLET DOSAGE FORM OF DUAL DELIVERY OF DRUG CURCUMIN AND BERBERINE HYDROCHLORIDE USING SIMULTANEOUS ESTIMATION BY UV SPECTROSCOPY

Objective: The present study was aimed to develop a combinational floating tablet of curcumin and berberine HCl utilizing synthetic polymers synthetic HPMC K-15M and evaluate its various characteristics. Methods: The formulations were developed by the process of wet granulation and evaluated for drug content, content uniformity, floating lag time, total floating time, in vitro buoyancy studies, and in vitro drug release profile. A simultaneous estimation method for curcumin and berberine was developed using U. V spectroscopy. Results: The results clearly indicated that the tablets produced were having acceptable physical parameters. The absence of any drug/polymer/excipient interactions was confirmed using infrared spectroscopy. It was found that the drug content of was in between 96.22 to 99.45 % in all the formulations. Because of their low densities, in vitro floatability tests showed that most of the tablets floated for more than 8 h. The in vitro release studies confirmed the sustained release of more than 80 percent of drug contained within a period of 8 h. In vitro buoyancy was good in all three batches (F1-F3). The overall floating time for the F2 formulation was 24 h. After one month of storage at 40 °C and 75 percent RH, the F2 formulation showed no noticeable change in physical as well as pharmaceutical performance characteristics. Conclusion: Floating tablets of curcumin and berberine was successfully developed and had passed on various pharmaceutical parameters

Exploring the trends of breathlessness and mortality in conjunction with AQI in India’s coal capital, Dhanbad

Background: Air Quality Index (AQI) has been evidenced to be linked with various health problems including NCDs. Globally, the combined effect of ambient air and household air pollution causes 6.7 million premature deaths. Objective: A study was undertaken to understand various associations of AQI and morbidity data, indigenous to the coal capital region of India. Methodology: This was a cross-sectional study where district AQI data was obtained from the state of Jharkhand while mortality and morbidity data were collected from our medical college. MS Excel and SPSS were used to analyse the data. Results: During the study period, the AQI of Dhanbad has been moderate to poor. The lowest AQI was noted in May 2020 at 105 while the highest in June 2019 at 217. The highest admission, due to respiratory illness, was noted in May 2020 with AQI of 105. Using univariate analysis age categorisation was statistically significant, as the respiratory illness was highest in >85 years age group. In logistic regression, it has the highest odds of 2.9 (1.5-5.5). Conclusion: This region-specific indigenous information is expected to provide a valuable tool for Air quality managers for more focused action. It also highlights the health impacts of the worsening air quality

On designing light-weight object trackers through network pruning: Use CNNs or transformers?

Object trackers deployed on low-power devices need to be light-weight, however, most of the current state-of-the-art (SOTA) methods rely on using compute-heavy backbones built using CNNs or transformers. Large sizes of such models do not allow their deployment in low-power conditions and designing compressed variants of large tracking models is of great importance. This paper demonstrates how highly compressed light-weight object trackers can be designed using neural architectural pruning of large CNN and transformer based trackers. Further, a comparative study on architectural choices best suited to design light-weight trackers is provided. A comparison between SOTA trackers using CNNs, transformers as well as the combination of the two is presented to study their stability at various compression ratios. Finally results for extreme pruning scenarios going as low as 1% in some cases are shown to study the limits of network pruning in object tracking. This work provides deeper insights into designing highly efficient trackers from existing SOTA methods.Comment: Submitted at IEEE ICASSP 202