In vivo evaluation of a mucoadhesive polymeric caplet for intravaginal anti-HIV-1 delivery and development of a molecular mechanistic model for thermochemical characterization

Context and objective: The aim of this study was to develop, characterize and evaluate a mucoadhesive caplet resulting from a polymeric blend (polymeric caplet) for intravaginal anti-HIV-1 delivery.

Materials and methods: Poly(lactic-co-glycolic) acid, ethylcellulose, poly(vinylalcohol), polyacrylic acid and modified polyamide 6, 10 polymers were blended and compressed to a caplet-shaped device, with and without two model drugs 3′-azido-3′-deoxythymidine (AZT) and polystyrene sulfonate (PSS). Thermal analysis, infrared spectroscopy and microscopic analysis were carried out on the caplets employing temperature-modulated DSC (TMDSC), Fourier transform infra-red (FTIR) spectrometer and scanning electron microscope, respectively. In vitro and in vivo drug release analyses as well as the histopathological toxicity studies were carried out on the drug-loaded caplets. Furthermore, molecular mechanics (MM) simulations were carried out on the drug-loaded caplets to corroborate the experimental findings.

Results and discussion: There was a big deviation between the T_g of the polymeric caplet from the T_g's of the constituent polymers indicating a strong interaction between constituent polymers. FTIR spectroscopy confirmed the presence of specific ionic and non-ionic interactions within the caplet. A controlled near zero-order drug release was obtained for AZT (20 d) and PSS (28 d). In vivo results, i.e. the drug concentration in plasma ranged between 0.012–0.332?mg/mL and 0.009–0.256?mg/mL for AZT and PSS over 1–28 d.

Conclusion: The obtained results, which were corroborated by MM simulations, attested that the developed system has the potential for effective delivery of anti-HIV-agents.     

The Spatial LASSO With Applications to Unmixing Hyperspectral Biomedical Images

Hyperspectral imaging (HSI) is a spectroscopic method that uses densely sampled measurements along the electromagnetic spectrum to identify the unique molecular composition of an object. Traditionally HSI has been associated with remote sensing-type applications, but recently has found increased use in biomedicine, from investigations at the cellular to the tissue level. One of the main challenges in the analysis of HSI is estimating the proportions, also called abundance fractions of each of the molecular signatures. While there is great promise for HSI in the area of biomedicine, large variability in the measurements and artifacts related to the instrumentation has slow adoption into more widespread practice. In this article, we propose a novel regularization and variable selection method called the spatial LASSO (SPLASSO). The SPLASSO incorporates spatial information via a graph Laplacian-based penalty to help improve the model estimation process for multivariate response data. We show the strong performance of this approach on a benchmark HSI dataset with considerable improvement in predictive accuracy over the standard LASSO. Supplementary materials for this article are available online.     

Phase-Structural and Electrochemical Properties of La2MgNi9 Alloys

Powder Metallurgy and Metal Ceramics - Multiphase La 2 MgNi 9 alloys are synthesized by induction melting. The crystalline structures of all phases in the alloys are determined with X-ray...