exhibits extensive first pass metabolism with poor oral bioavailability (27%–50%) limiting its therapeutic efficiency. The present study involved an attempt to enhance its aqueous solubility by formulating as solid dispersions (SDs) using sodium starch glycollate (SSG) as a carrier. The dispersions were formulated by dispersion method and evaluated by phase solubility, drug content, in vitro release and mathematical modelling. Solid state characterisation of samples was carried out by X-ray diffraction (XRD), differential scanning calorimetric (DSC), Fourier transform infrared spectrophotometry (FTIR), near infrared (NIR), Raman analysis and wettability studies. The phase solubility and thermodynamic parameters indicated the spontaneity and solubilisation effect of carrier. The release rate from the dispersions was higher than pure drug and found to increase with an increase in carrier content. The optimised dispersions were selected based on release studies, profiles and dissolution parameters. XRD, DSC, FTIR, NIR and Raman analysis proved the crystallinity reduction, changes in crystal quality and compatibility between drug and carriers. Wettability studies proved the increased wettability in selected dispersions. Based on the findings, possible mechanisms that would have contributed to dissolution enhancement of CLZ were suggested. Such findings could be extrapolated to enhance the aqueous solubility of other poorly water-soluble drugs.
About 95% of earth living space lies deep below the ocean's surface and it harbors extraordinary diversity of marine organisms. Marine biodiversity is an exceptional reservoir of natural products, bioactive compounds, nutraceuticals and other potential compounds of commercial value. Timeline for the development of the drug from a plant, synthetic and other alternative sources is too lengthy. Exploration of the marine environment for potential bioactive compounds has gained focus and huge opportunity lies ahead for the exploration of such vast resources in the ocean. Further, the evolution of superbugs with increasing resistance to the currently available drugs is alarming and it needs coordinated efforts to resolve them. World Health Organization recommends the need and necessity to develop effective bioactive compounds to combat problems associated with antimicrobial resistance. Based on these factors, it is imperative to shift the focus towards the marine environment for potential bioactive compounds that could be utilized to tackle antimicrobial resistance. Current research trends also indicate the huge strides in research involving marine environment for drug discovery. The objective of this review article is to provide an overview of marine resources, recently reported research from marine resources, challenges, future research prospects in the marine environment.
The objective of this study is to provide a mechanistic insight into solubility enhancement and dissolution of acyclovir (ACY) by polyethylene glycol20000 (PEG20000).
The dissolution and subsequent oral bioavailability of acyclovir (ACY) is limited by its poor aqueous solubility. An attempt has been made in this work to provide mechanistic insights into the solubility enhancement and dissolution of ACY by using the water-soluble carrier polyethylene glycol 6000 (PEG6000). Solid dispersions with varying ratios of the drug (ACY) and carrier (PEG6000) were prepared and evaluated by phase solubility, in vitro release studies, kinetic analysis, in situ perfusion, and in vitro permeation studies. Solid state characterization was done by powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared (FTIR) analysis, and surface morphology was assessed by polarizing microscopic image analysis, scanning electron microscopy, atomic force microscopy, and nuclear magnetic resonance analysis. Thermodynamic parameters indicated the solubilization effect of the carrier. The aqueous solubility and dissolution of ACY was found to be higher in all samples. The findings of XRD, DSC, FTIR and NMR analysis confirmed the formation of solid solution, crystallinity reduction, and the absence of interaction between the drug and carrier. SEM and AFM analysis reports ratified the particle size reduction and change in the surface morphology in samples. The permeation coefficient and amount of ACY diffused were higher in samples in comparison to pure ACY. Stability was found to be higher in dispersions. The results suggest that the study findings provided clear mechanical insights into the solubility and dissolution enhancement of ACY in PEG6000, and such findings could lay the platform for resolving the poor aqueous solubility issues in formulation development.