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.     

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...     

Linear friction welding of Ti6Al4V: experiments and modelling

Linear friction welding of the Ti6Al4V alloy is studied. A new definition of the energy input rate is proposed, based on an integration over time of the in-plane force and velocity; a strong correlation with the upset rate is then found. The effective friction coefficient is estimated to be 0·5±0·1 for varying frequencies and amplitudes, with only a weak dependence on the processing conditions displayed. A model is proposed that accounts for both the conditioning and equilibrium stages of the process, which is shown to be in good agreement with the experimental data. The model is used to study the mechanism by which the flash is formed. A criterion is proposed by which the rippled nature of its morphology can be predicted.     

Temperature cycling and its effect on mechanical behaviours of highporosity chalks

Temperature history can have a significant effect on the strength of water-saturated chalk.In this study,hydrostatic stress cycles are applied to understand the mechanical response of chalk samples exposed to temperature cycling between each stress cycle,compared to the samples tested at a constant temperature.The total accumulated strain during a stress cycle and the irreversible strain are reported.Chalk samples from Kansas(USA)and Mons(Belgium),with different degrees of induration(i.e.amount of contact cementation),were used.The samples were saturated with equilibrated water(polar)and nonpolar Isopar H oil to quantify water weakening.All samples tested during 10 stress cycles with varying temperature(i.e.temperature cycled in between each stress cycle)accumulated more strain than those tested at constant temperatures.All the stress cycles were performed at 30℃.The two chalk types behaved similarly when saturated with Isopar H oil,but differently when saturated with water.When saturated with water,the stronger Kansas chalk accumulated more total strain and more irreversible strain within each stress cycle than the weaker Mons chalk.