The aim of this study was to investigate the potential application of thermosensitive gels formed by a xyloglucan polysaccharide derived from tamarind seed for nasal drug delivery. Xyloglucan that had been partially degraded by β-galactosidase to eliminate 45% of galactose residues formed gels at concentrations of 2.5% w/w at gelation temperatures decreasing over the range 27-28°C. The in vitro release of ondansetron hydrochloride from the enzyme-degraded xyloglucan gels followed higuchi kinetics over a period of 5 h at 34°C by anomalous transport mechanism. The ex vivo permeation of ondansetron hydrochloride from the gels was sustained. Histological examination of nasal mucosa following a single administration of the gels showed no evidence of mucosal damage. Finally, the bioavailability study in rabbits revealed that the absolute bioavailability of ondansetron hydrochloride was significantly increased from 28.64% in the case of the oral drug solution to 52.79% in the case of the nasal in situ gel. The results of this study suggest the potential of the enzyme-degraded xyloglucan gels as vehicles for nasal delivery of drugs.
Certain problems regarding the drugs like high first pass metabolism, also the bioavailability of the certain drugs varies due to instability in acidic environment of stomach. Hence, to resolve such problems the drug should be incorporated in the microspheres for sustained release using a suitable polymer. Natural polymer like chitosan gained great interest in pharmaceutical sector because of its advantages like biodegradability, biocompatibility, non-toxicity, non-immunogenicity and low cost. In the present study, formulation and evaluation of polymeric microspheres of Atorvastatin Calcium was carried out and the release profile of such drug using the alginate and chitosan was studied. Microspheres were prepared for sustained release of drug using chitosan and alginate polymers by ionotropic gelation method. Microspheres were spherical in shape, having good flow properties and further its encapsulation efficiency, swelling index, micromeritic study, invitro drug release study and stability studies were performed in order to characterize microspheres. Three different concentrations of sodium alginate (1%, 2% and 3%) were used. The higher encapsulation efficiency was observed as the concentration of alginate increased. This is due to the greater availability of active calcium binding sites in the polymeric chains and consequently the greater degree of cross linking. The highest encapsulation efficiency (88.36) was achieved with 2% w/v sodium alginate in combination with 3% chitosan (F6). Among the prepared formulations with respect to the entrapment efficiency, swelling studies and in vitro drug release, the alginate-chitosan microspheres prepared by ionotropic gelation using calcium chloride found to be better than ionically cross linked alginate spheres alone. Therefore, dual cross-linked, microspheres are promising carrier for sustained release of drug.
Cannabis sativa L. is a significant herbaceous species native to Central Asia that has been utilised for folk medicine and other industrial applications. It is a rich source of cellulosic and woody fibres as well as a treasure trove of phytochemicals. The pharmaceutical and construction industries are both very interested in this plant since its metabolites have powerful bioactivities on humans. Cannabinoids are the most researched class of chemicals, primarily because of the vast range of pharmacological effects they have on humans, including psychoactive effects. The phytoconstituents Apigenin and Alpha-bisabolol were synthesised in the current study, and Cannabis sativa L. phytoconstituent was further studied through in silico screening utilising (PDB ID: 6FYZ) along with spectral characterization NMR (1H and 13C) to confirm the presence of saturated and unsaturated moiety in Cannabis sativa L. phytoconstituents. Apigenin and Alpha-bisabolol, two phytoconstituents found in leaves and flower of Cannabis sativa L., were found to have higher docking scores and glide energies when comapred with the standard drugs like Levetiracetam. Cannabis sativa's phytoconstituent has been shown in in-silico studies to have high anti-epileptic potency, making it a crucial source for novel anti-epileptic/anti-convulsant/anti-seizure medications that in the future will focus on a variety of neurological diseaeses and disorders.
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