Rosuvastatin (RVT) is a BCS class II antilipidemic crystalline drug, which exhibits low bioavailability due to its very poor aqueous solubility; therefore, it is challenging to develop a proper formulation of RVT. To enhance solubility and bioavailability of this API, an attempt has been made by implementing solid dispersion technique. Solid dispersion (SD) technique is a solubility enhancing technique where one or more active entities are dispersed in an inert medium (matrix or carrier) at solid state. In this study, different ratios of Kollicoat® IR (KIR) and Kollidon® 90F (KF90) polymers were used with API to prepare various formulations by physical mixing (PM) and SD approaches; here solvent evaporation technique was used whereas methanol was used as solvent which was completely evaporated from the homogenously dispersed system by placing in a water-bath at 60-65°C and then in oven for 30 minutes at 50 °C. Among the formulations, RVT-KF90 SD formulations showed the most promising result in in-vitro study in terms of drug release profile (78.04 – 99.21%) in comparison to pure RVT (63.1%) and physical mixing of RVT with those polymers. USP dissolution apparatus type II was used at 37°C ± 0.5°C with 50 rpm to conduct the in-vitro experiment. The experiment also unraveled that the dissolution of RVT improved with increasing the amounts of polymers. Subsequently, stability of the developed formulations was conducted by Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) as well as scanning electron microscopy (SEM). The results obtained from FTIR ensured no involvement of any significant drug-excipient interaction. Moreover, the DSC study signified thermal stability at high temperature. Besides, the SEM micrograph illustrated homogenous distribution of RVT in the polymer and transformation of crystal-like RVT into amorphous formulations.
Dhaka Univ. J. Pharm. Sci. 20(2): 199-211, 2021 (December)
Without adaptive immunity, invertebrates have evolved innate immune systems that react to antigens on the surfaces of pathogens. These defense mechanisms are included in horseshoe crab hemocytes’ cellular responses to pathogens. Secretory granules, large (L) and small (S), are found on hemocytes. Once the invasion of pathogens is present, these granules release their contents through exocytosis. Recent data in biochemistry and immunology on the granular constituents of granule-specific proteins are stored in large and small granules which are involved in the cell-mediated immune response. L-granules contain most clotting proteins, which are necessary for hemolymph coagulation. They also include tachylectins; protease inhibitors, such as cystatin and serpins; and anti-lipopolysaccharide (LPS) factors, which bind to LPS and agglutinate bacteria. Big defensin, tachycitin, tachystatin, and tachyplesins are some of the essential cysteine-rich proteins in S-granules. These granules also contain tachycitin and tachystatins, which can agglutinate bacteria. These proteins in granules and hemolymph act synergistically to fight infections. These biomolecules are antimicrobial and antibacterial, enabling them to be drug resistant. This review is aimed at explaining the biomolecules identified in the horseshoe crab’s hemolymph and their application scopes in the pharmaceutical and biotechnology sectors.
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